Independent University,
Bangladesh
Dept. of Pharmacy
Course Code: PHA302L
Page i
TABLE OF CONTENTS
Sl.
No.
01.
Name of the experiment
Page
No.
Formulation and preparation of pediatric paracetamol oral solution.
(Each 5 mL contains Paracetamol BP 120 mg)
01 – 05
Date
02.
Formulation and preparation of Ferrous Sulphate oral solution.
(Each 5 mL contains Ferrous Sulphate BP 200 mg)
06 – 10
03.
Formulation and preparation of Chlorpheniramine oral solution.
(Each 5 mL contains Chlorpheniramine Maleate BP 2 mg)
11 – 15
04.
Formulation and preparation of Antacid Suspension.
(Each 5 mL contains Aluminum Hydroxide 200 mg and Magnesium Hydroxide 400 mg)
16 – 20
05.
Formulation and preparation of Metronidazole oral Suspension.
(Each 5 mL contains Benzoyl Metronidazole BP 320 equivalent to Metronidazole BP 200 mg)
21 – 26
Formulation and preparation of Preparation of oil in water (O/W)
emulsion.
(Each 5 mL contains 0.5 mL castor oil)
27 – 31
06.
Bibliography.
31
Page ii
Experiment No. 01
Name of the Experiment: Formulation and preparation of pediatric paracetamol oral
solution. (Each 5 mL contains Paracetamol BP 120 mg)
Introduction
In pharmaceutical terms, solutions are “liquid preparations that contain one or more chemical
substances dissolved in a suitable solvent or mixture of mutually miscible solvents”. Generally
solution is a homogeneous mixture, prepared by dissolving a solid, liquid, or gas in another liquid,
in which the solute molecules or dissolved substance are dispersed among those of the solvent.
Based on use, the pharmaceutical solution’s may be classified as oral, otic, ophthalmic, or topical.
For example, aqueous solutions containing a sugar are classified as syrups; sweetened hydroalcoholic (combinations of water and ethanol) solutions are termed elixirs etc.
Oral solutions such as syrups, elixirs, spirits, and tinctures are prepared & used for the specific
effects of the medicinal agents they carry. Solutes other than the medicinal agent are usually
present in orally administered solutions. These additional agents are frequently included to
provide colour, flavour, sweetness, or stability. In formulating or compounding a pharmaceutical
solution, the solubility and stability of each solute with regard to the solvent or solvent system
must be considered.
Advantages and disadvantages of pharmaceutical solutions for oral administration
Advantages
Therapeutic agents can easily be administered orally to individuals who have difficulty in
swallowing, e.g. elderly patients, infants.
The therapeutic agent is dissolved in the formulation and is therefore immediately available
for absorption.
The bioavailability of pharmaceutical solutions is greater than that of oral solid-dosage forms.
Taste-masking of bitter therapeutic agents can be readily achieved.
Disadvantages
⦿ Pharmaceutical solutions for oral administration are unsuitable for therapeutic agents that are
chemically unstable in the presence of water.
⦿The poor solubility of certain therapeutic agents may prohibit their formulation as
pharmaceutical solutions.
⦿ Pharmaceutical solutions are expensive to ship and are bulky for the patient to carry due to
the associated mass of the product.
Syrups: Syrups are sweet, viscous, concentrated aqueous preparations of sugar or sugar
substitute with or without flavours and medicinal substances. The concentration of sugar in
syrup should be 66.7% (w/w) according to BP. (85%w/v in USP)
Types of Syrups:
Non-medicated syrup: Syrups containing various aromatic or pleasantly flavored
substances and are intended to be used as a vehicle or flavor for prescriptions are called non
medicated or flavoured syrups. For example Acacia, Cherry, Cocoa, Orange, and Raspberry USP.
Medicated syrup: Syrups containing a therapeutic agent are called medicated syrups.
Medicated syrup is formulated by the components; API along with the sucrose, purified water,
flavouring agent & other excipients.
Page 1
Components of Syrup: Most syrups contain the following components in addition to the
purified water or Distilled Water (DW) and any medicinal agents present.
 The sugar, usually Sucrose or Sucrose substitutes: Which provides sweetness and viscosity.
 Antimicrobial preservatives.
 Flavorants.
 Colorants.
 Commercial syrups contain special solvents, solubilizing agents, thickeners or stabilizers.
Advantages of Syrup: Syrups have the following advantages;
i. Syrups can retard oxidation by partly hydrolysing into reducing sugar such as laevulose and
dextrose.
ii. It prevents decomposition of many vegetable substances; syrups have high osmotic pressure
which prevents microbial growth.
iii. They are palatable due to the presence of sugar, thus provides suitable vehicle for the
administration of bitter and bad odorous substances.
iv. They are more quickly effective than solid dosages forms like tablet, capsule etc.
v. They are homogenous formulation so the active ingredients are also homogenously distributed.
vi. Syrups are suitable formulation for the paediatric and geriatric patients.
Disadvantages of Syrup: Some disadvantages of Syrups are as follows;
i. In a closed container of syrup, surface dilution is possible due to solvent evaporation.
ii. Solvent evaporation condenses in the upper internal surface of the container and then flows
back on to the surface of the product which provides an ideal medium for the growth of certain
microorganisms.
iii. During storage and use of syrup, crystallization of the sugar within the screw cap may occur.
This problem is solved by the addition of polyhydric alcohols.
Preparation of 66.7% Sucrose syrup BP
🞛 Take 66.7 gram sucrose B.P.
🞛 Add purified water B.P with continuous trituration to mix the sugar.
🞛 Heat together until dissolved and add sufficient boiling Purified Water to produce 100 g.
Paediatric Paracetamol Oral Solution is a solution containing 2.4% w/v of Paracetamol in a suitable flavoured vehicle.
Formula:[60 mL]
Name of the ingredients
Paracetamol BP
Propylene glycol BP
Sucrose Syrup (66.7%)BP
Theoretical amount
1.44 gm
5 mL
20 mL
Sorbitol Solution (70%) BP
10 mL
Glycerin BP
5 mL
Methyl 4-Hydroxybenzoate BP
Propyl 4-Hydroxybenzoate BP
Flavor
Color
Purified water
50 mg / 0.05 gm
5 mg / 0.005 gm
Q.S.
Q.S.
Q.S. up to 60 mL
Purpose
API. Analgesic, Antipyretic.
Co-solvent, Preservative.
Increase viscosity, Sweeting agent.
Sweeting agent, Retard crystallization of
sucrose around the cap of the bottles. Stabilizing agent.
Increase viscosity, Sweeting agent.
Solvent. Increase the solubility of added ingredients.
Antimicrobial preservative.
Antimicrobial preservative.
Improving organoleptic Property.
Solvent/Vehicle.
A non-sugar based product can be prepared by omitting Syrup and adding non-sugar sweeting
agents (e.g. Saccharine, Aspartame, Sucralose) for diabetes patients.
Page 2
Apparatus:
1. Beaker
2. Stirrer/Glass rod
4. Measuring cylinder
3. Electric balance
5. Bottle
Calculation:
60 mL syrup contain
Thus , 1 mL ”
So, 5 mL
”
=1.44 gm or 1440 mg of paracetamol
1440
mg of
60
1440  5
=
mg of
60
=
”
”
’’
’’
= 120 mg of paracetamol
Recipe: For 60 mL paracetamol syrup where each 5 mL contains 120 mg of paracetamol BP
Since 5 mL contains 120 mg, thus 60 mL would contain 1440 mg or 1.44 gm paracetamol BP
Method of preparation:
1. Take 1.44 gm Paracetamol in a beaker.
2. Dissolve it by adding 5 mL propylene glycol.
3. Subsequently add 20 mL sucrose syrup & 5 mL glycerin. Mix them properly.
4. Afterwards add 10 mL sorbitol solution.
5. Now add the preservatives; namely 50 mg Methyl Hydroxybenzoate, 5 mg Propyl
Hydroxybenzoate (Better to dissolve in propylene glycol/Glycerin, with some DW).
6. After complete mixing of all the portions, add the flavor& color (e.g. Orange/Raspberry)
7. Later transfer the syrup to a measuring cylinder adjusts the volume to 60 mL by adding
purified water.
8. Finally transfer the preparation into a bottle, close properly & label it.
Function of each ingredient:
1. Paracetamol:( para-acetyl-amino-phenol ,N-acetyl-para-aminophenol)
Acetaminophen is an odorless, slightly bitter taste white or almost
white, crystalline powder. It is freely soluble in alcohol; soluble in
methanol but very slightly soluble in cold water, soluble in boiling water.
Propylene glycol may be used for good solubility. It is the active ingredient of the preparation
acting as antipyretic & analgesic.
2. Propylene Glycol
Propylene glycol is a useful solvent with a wide range of applications and is frequently
substituted for glycerin in modern pharmaceutical formulations.
Properties:
i. Clear, colorless, practically odorless
ii. Hygroscopic in nature
iii. Viscous
iv. Usually tasteless (/faintly sweet)
Functions:
♦ Solvent or co-solvent (Oral , Parenterals, Topical, Aerosol)
♦ Antimicrobial preservative (Solutions, Semisolids)
♦ Disinfectant
♦ Humectant (Topical)
Page 3
3. Sucrose syrup
It is used in the preparation as sweetening agent to mask the bitter taste of preparation.
Sucrose: (β-D-Fructofuranosyl α-D-glucopyranoside.)
Properties:
♦ Colorless or Brown, Odorless, Crystalline Powder.
♦ Viscous in nature.
♦ It has a sweet taste.
♦ Free flowing (crystalline sucrose).
Sucrose:C12H22O11
♦ Cohesive solid (Powder Sucrose).
♦ Melting Point: 160°C –186°C (with decomposition)
♦ Good stability at room temperature and at moderate relative humidity.
♦ Dilute sucrose solutions are liable to fermentation by microorganisms.
♦ Sucrose is also considered to be more cariogenic than other carbohydrates since it is
more easily converted to dental plaque. For this reason, its use in oral pharmaceutical
formulations is declining.
Functions:
♦ Sweetening Agent: Used to enhance palatability.
♦ Viscosity imparting agent: Used to increase viscosity.
4. Sorbitol Solution
Sorbitol is D-glucitol. It is a hexahydric alcohol related to mannose and is isomeric with mannitol.
Sorbitol: Sorbitol is widely used as an excipient in pharmaceutical formulations.
Properties:
i. Odorless, white or almost colorless
iii. Crystalline
ii. Hygroscopic powder
iv. Sweet in taste
Functions:
♦ Prevent crystallization of sugar around the cap of bottles
♦ Vehicle in sugar-free formulations
(♦ Stabilizing agent)
♦ Sweetener
♦ Humectant
5. Glycerin:( Glycerol; Glycerine)
Glycerin is used in a wide variety of pharmaceutical formulations including
oral, otic, ophthalmic, topical, and parenteral preparations. Glycerin has preservative
qualities and is often used as a stabilizer and as an auxiliary solvent in conýunction with water or alcohol.
Properties:
i. Clear, colorless, odorless
ii. Hygroscopic liquid
iii. Viscous
iv. Sweet in taste (App. 0.6 times as sweet as sucrose)
Functions:
♦ Solvent, Co-solvent
♦ Humectant
♦ Antimicrobial preservative
♦ Viscosity increasing agent
♦ Sweetening agent
6. Methyl & Propylparaben: (parabens : Alkyl esters of p-hydroxybenzoic acid )
Methylparaben is widely used as an antimicrobial preservative in cosmetics, food products, and
pharmaceutical formulations.
Methylparaben
Properties:
i. Colorless crystals or a white crystalline powder
ii. Odorless or almost odorless .Slight burning taste.
Page 4
Propylparaben
Properties:
i. White
ii. Crystalline powder
iii. Odorless
iv. Tasteless
Function:
i. Methylparaben & Propylparaben (10:1) exhibit antimicrobial activity over the pH range 4–8.
ii. They are also more active against Gram-positive than against Gram-negative bacteria.
Activity may be improved by using combinations of parabens, as synergistic effects occur.
Other ingredients that can be used:
√ Vehicle: Macrogols (PEG) (Dissolution enhancer, Solubilizing agent)
√ Sweetening agent(Other than sugar): Sorbitol, Glycerol and Propylene glycol.
√ Preservatives: Na-benzoate, Benzoic acid and salts, Sorbic acid and its salts.
√ Coloring agent: Amaranth, Apple green.
√ Flavoring agent: Peppermint oil, clove oil, vanilla, lemon oil etc.
√ Buffer: Na-citrate, potassium bisulfite.
Indications: Paediatric paracetamol oral solution is indicated to be used🞛 As antipyretic & analgesic agent. ( temporarily relieve fever)
🞛 In mild to moderate pain myalgia, headache, toothache, arthritis and backache.
Contraindications: Severe hepatic impairment & renal impairment; Allergy
Dose: The dose of syrup is as follows
Children under 3 months: 10 mg/kg body weight (reduce to 5 mg/ kg if jaundiced 3–4 times/day
Children (below 1yr) : ½ -1 teaspoonful syrup 3–4 times/day
Children (6-12yrs) : 2–4 teaspoonful syrup 3–4 times/day
Or, as per the recommendation of the physician.( Maximum 4 doses in 24 hours.)
Paracetamol BP Oral solution
Indication
Palatable 60 mL Solution, Sugar Free
Each 5 mL Contains Paracetamol BP 120mg
: Antipyretic , Analgesic, Fever,
Common cold, Influenza, Headache.
Dose
: As Directed By The Physician
0171740
Storage condition:
: Apr 2018
: Mar 2020
✯ Should be protected from light.
✯ Should not be refrigerated.
: 23 (Including all taxes.)
: 12 & 80
Precaution: Keep every medicine out of reach of children.
: 025-0144-088
Manufactured by: Department of Pharmacy, Independent University, Bangladesh
Batch No.
Mfg. Date
Exp. Date
M.R.P. Tk.
Mfg. Lic. No.
DAR No.
Market preparation: Paediatric paracetamol oral solution.
SL.
01
02
03
04
05
Trade/Brand Name
Manufacturer
Dosage form
Page 5
Experiment No. 02
Name of the Experiment: Formulation and preparation of Ferrous Sulphate oral
solution. (Each 5 mL contains Ferrous Sulphate BP 200 mg)
Introduction:
Pharmaceutical syrup is concentrated, aqueous preparation of sugar or sugar substitute
with or without added flavoring agents and medicinal substances.
Ferrous Sulphate oral solution belongs to a group of medicines called iron supplements.
These medicines work by replacing body iron. Iron is a key component which is required for
the production of red blood cells (a process known as haematopoiesis), but it's also part of
haemoglobin (that is the pigment of the red blood cells) binding to the oxygen and thus
facilitating its transport from the lungs via the arteries to all cells throughout the body..
When the body does not get enough iron, it cannot produce the number of normal red blood cells
needed to keep good health. This condition is called iron-deficiency anaemia.
Ferrous sulphate is an iron salt which contains elemental iron or ferrous iron and used for
the prevention and treatment of iron deficiency anemia before, during and after pregnancy as
well as during lactation.
Anemia
Anemia is a decrease in the total amount of red blood cells (RBCs) or hemoglobin in the
blood, or a lowered ability of the blood to carry oxygen. The oxygen carrying capacity is
determined by hemoglobin content of the erythrocytes. Hence a reduction in the blood
hemoglobin level & the number of circulating erythrocytes is the characterization of anemia.
Classification
According to the etiology, anaemia may be classified as follows:
Anaemia due to blood loss by hemorrhage.
Anaemia due to dietary deficiency of factors essential for
normal blood production.
e.g. Iron, Folic Acid.
Anaemia due to excessive blood cell destruction in comparison to the production .
Anaemia due to aplasia (Failure of an organ or tissue to develop normally),
hypoplasia Underdevelopment of a tissue organ or body), or destruction of bone marrow.
Anaemia due to infection, rheumatic arthritis etc.
Anaemia due to defective formation of R.B.C.
Iron deficiency anemia is caused by the deficient synthesis of hemoglobin in which iron is an
important constituent. Males of average height have about 4 grams of iron in their body; females
about 3.5 grams and children will usually have 3 grams or less. These 3-4 grams
are distributed throughout the body in haemoglobin, tissues, muscles, bone
marrow, blood proteins, enzymes, ferritin, hemosiderin, and transport in plasma.
Apparatus:
1. Beaker
4. Pipette
7. Glass rod
2. Stirrer
5. Bottle
8. Mortar and pestle
3. Measuring cylinder
6. Funnel
9. Electric balance.
Page 6
Recipe: For 60 mL Iron Syrup
Each 5 mL contains 200 mg of FeSO4
Then 60 mL contains = 200  60 mg of FeSO4
5
=2400 mg of FeSO4
=2.4 gm of FeSO4
Formula: For 60 mL Iron syrup
Each 5 mL contains 200 mg of FeSO4
Name of the ingredient
Theoretical weight
Ferrous Sulphate BP
Citric acid BP
Ascorbic acid BP
Sorbitol Solution (70%) BP
Sucrose Syrup BP
Methyl 4-Hydroxybenzoate BP
Propyl 4-Hydroxybenzoate BP
Glycerin BP
Flavor Pharma Grade
Color FDC
Purified Water BP
2.4 gm
200 mg / 0.2 gm
100 mg / 0.1 gm
5 mL
20 mL
50 mg/ 0.05 gm
5 mg/ 0.005 gm
5 mL
Q.S.
Q.S.
Q.S. to 60 mL
Purpose
API. For the treatment of iron deficiency
anemia and anemia due to pregnancy.
Buffering agent; Acidifying agent.
Antioxidant.
Retard crystallization of sucrose;
Sweetener, Humectant.
Viscosity imparting &sweetening agent.
Antimicrobial preservative.
Antimicrobial preservative.
Viscosity imparting agent; Humectant.
Improve organoleptic property.
Solvent/ Vehicle.
Method of preparation:
1. Take 2.4 gm ferrous sulphate in a mortar & crush it properly with pestle.
2. Now take 10 mL DW in a 250 mL beaker. Add ascorbic acid and citric acid into it, mix them
properly.
3. Afterwards add the ferrous sulphate (previously crushed in step 1) and dissolve in this beaker.
Later add 20 mL sucrose syrup to it.
4. Take 5 mL DW in a 50 mL beaker and add 0.05 gm Methyl Hydroxybenzoate, 0.005 gm Propyl
Hydroxybenzoate and dissolve in it (Better to dissolve in Propylene glycol/Glycerin. Add some
DW & then add to the syrup). Later add 5 mL Sorbitol & 5 mL Glycerin to it and blend them
properly.
5. Add this new solution (made in the step 4) to the 250 mL beaker containing ferrous sulphate
solution (obtained in step 3). Blend them appropriately to get a uniform mixture.
6. After homogenous mixing of all the portions, add the flavor & color.
7. Now transfer the syrup in a measuring cylinder, adjust the volume to 60 mL by adding purified
water Q.S.
8. Finally transfer the preparation in a bottle, close the bottle properly & label it.
Page 7
Function of the ingredients:
1. Ferrous Sulphate (FeSO4.7H2O):
It is the active ingredient of the hematinic preparation. Ferrous Sulfate is used for the prevention
and treatment of iron-deficiency anaemia.
Properties:
√ Physical form
√ Color
√ Odor
√ Taste
√ Nature
√ pH
√ Solubility
: Crystal or crystalline powder, Efflorescent in air.
: Light green, Bluish-green (Oxidized to brown in moist air).
: Odorless.
: Metallic in taste.
: Acidic in nature.
: Is about 3.7. (3.0 ― 4.0)
: Freely soluble in water, very soluble in boiling water.
2. Citric acid :( Citric acid monohydrate) 2-Hydroxypropane-1,2,3-tricarboxylic acid monohydrate.
Properties:
i . Colorless or translucent crystals or granules, /or as a white crystalline powder.
ii. Odorless.
iii. Strong acidic taste.
iv. Efflorescent.
v. It is slightly deliquescent in moist air.
vi. Melting point 100°C (Monohydrate), 153°C (anhydrous).
Functions:
♦ Buffering agent (adjust the pH of solutions)
♦ Acidifying agent
♦ Flavor enhancer
♦ Sequestering agent
♦ Sialogogue An agent increasing the flow of saliva.
♦ Antioxidant synergist.
3. Ascorbic acid:
Properties:
√ Physical form
√ Color
√ Odor
√ Taste
√ Nature
√ PH
√ Melting point
: White or almost white, crystalline powder or colorless crystals.
: Light Yellow. Gradually darkens in color upon exposure to light.
: Odorless.
: Sharp, acidic taste.
: Non-hygroscopic.
: Between 2.1–2.6
: 190°C (with decomposition).
Functions:
🞛 Antioxidant (0.01-0.1% w/v).
🞛 pH adjusting agent (for injection).
🞛 Stabilizing agent.
🞛 Adjunct for oral liquids
4. Sorbitol Solution
Sorbitol is D-glucitol. It is a hexahydric alcohol related to mannose and is isomeric with mannitol.
Sorbitol (D-Glucitol): Sorbitol is widely used as an excipient in pharmaceutical formulations.
Page 8
Properties:
i. Odorless, white or almost colorless
ii. Hygroscopic powder
iii. Crystalline
iv. Sweet in taste
Functions:
🞛 Prevent crystallization of sugar around the cap of bottles
🞛 Vehicle in sugar-free formulations
🞛 Stabilizing agent
🞛 Sweetener
🞛 Humectant
5. Sucrose syrup
It is used in the preparation as sweetening agent to mask the bitter taste of preparation.
Sucrose: (β-D-Fructofuranosyl α-D-glucopyranoside.)
Properties:
🞛 Colorless or Brown, Odorless, Crystalline Powder.
🞛 Viscous in nature.
🞛 It has a sweet taste.
🞛 Free flowing (crystalline sucrose).
🞛 Cohesive solid (Powder Sucrose).
🞛 Melting Point: 160°C –186°C (with decomposition)
🞛 Good stability at room temperature and at moderate relative
humidity.
Sucrose:C12H22O11
🞛 Dilute sucrose solutions are liable to fermentation by microorganisms.
🞛 Sucrose is also considered to be more cariogenic than other carbohydrates since it is
more easily converted to dental plaque. For this reason, its use in oral pharmaceutical
formulations is declining.
Functions:
♦ Sweetening Agent: Used to enhance palatability.
♦ Viscosity imparting agent: Used to increase viscosity.
6.
Methyl & Propylparaben: (Parabens : Alkyl esters of
p-hydroxybenzoic acid ) Methylparaben is widely used as an antimicrobial
preservative in cosmetics, food products, and pharmaceutical formulations.
Methylparaben
Properties:
i. Colorless crystals or a white crystalline powder
ii. Odorless or almost odorless .Slight burning taste.
Propylparaben
Properties:
i. White
iii. Odorless
ii. Crystalline powder
iv. Tasteless
Function:
i. Methylparaben & Propylparaben exhibit antimicrobial activity over the pH range 4–8.
ii. They are also more active against Gram-positive than against Gram-negative bacteria.
Activity may be improved by using combinations of parabens, as synergistic effects occur.
7. Glycerin:( Glycerol; Glycerine)
Glycerin is used in a wide variety of pharmaceutical formulations including
oral, otic, ophthalmic, topical, and parenteral preparations.
Glycerin has preservative qualities and is often used as a stabilizer and as an auxiliary solvent in conýunction with water or
alcohol.
Page 9
Properties:
i. Clear, colorless, odorless
ii. Hygroscopic liquid
iii. Viscous
iv. Sweet in taste (App. 0.6 times as sweet as sucrose)
Functions:
♦ Solvent, Co-solvent
♦ Antimicrobial preservative
♦ Humectant
♦ Sweetening agent
♦ Viscosity increasing agent
Other ingredients used:
√ Coloring agent: Amaranth, Apple green.
√ Flavoring agent: Raspberry/Orange flavor.
FD&C yellow No. 6 (sunset yellow FCF)
Guarana flavor 12144–33
Indications: Iron preparations are used in Iron deficiency anemia.
Pregnancy and lactation induced iron deficiency.
Dosage and Administration:
Adult: Initial therapeutic dose: 3–4½ teaspoonful daily in divided doses or as prescribed by the physician.
Maintenance dose: 1½ teaspoonful daily, but if needed up to 1.8 gm (9 teaspoonful) daily can be given.
Children : Under 1 year
: ¼ teaspoonful thrice daily or as directed by physician.
1-5 years
: 1 teaspoonful thrice daily.
6-12 years
: 1½ teaspoonful twice daily.
Contraindications: Iron therapy is contraindicated in hemachromatosis and hemosiderosis.
Side effects: Some general & common side effects are as follows:General:
1. Constipation.
3. Temporary staining of teeth.
Severe:
2. Black discoloration of faeces.
4. Nausea, Vomiting, Diarrhoea.
 Gastro-intestinal erosion (with high doses).
Ferrous Sulphate Syrup BP
Each 5 mL contains Ferrous Sulphate
Heptahydrtate BP 200mg
 Blood in stool.
Indications
: Iron deficiency syndrome and Anaemia.
Dose
: To be written from- Dosage and Administration
Storage condition: Keep in cool and dry place.
0171740
Precaution
: Keep every medicine out of reach of children.
: Oct 2017
DAR
No.
: 025-0144-088
: Oct 2019
Mfg. Lic. No. :12 & 80
: 67 (Including VAT)
Manufactured by: Department of Pharmacy, Independent University, Bangladesh
Batch No.
Mfg. Date
Exp Date
M.R.P. Tk.
Market preparation: Ferrous Sulphate Syrup BP
SL.
01
02
03
04
05
Trade/Brand Name
Manufacturer
Dosage form
Page 10
Experiment No. 03
Name of the Experiment: Formulation and preparation of Chlorpheniramine oral
solution. (Each 5 mL contains Chlorpheniramine Maleate BP 2 mg)
Introduction:
Syrup is a viscous concentrated solution of a sugar, such as sucrose, in water or other aqueous
liquid; combined with other ingredients.
Chlorpheniramine maleate is an antihistamine which reduces allergic vasodilatation
and mucosal congestion. It is a first-generation alkyl amine antihistamine used in the
prevention of the symptoms of allergic conditions such as rhinitis and urticaria.
It works by blocking the action of histamine, which helps reduce symptoms such as
watery eyes and sneezing. Its sedative effects are relatively weak compared to other firstgeneration antihistamines. Although not generally approved as an antidepressant or
anti-anxiety medication, chlorphenamine appears to have these properties as well.
Apparatus:
1. Beaker
2. Funnel
3. Measuring cylinder
4. Pipette
5. Electric balance
6. Bottle
7. Glass rod
Recipe: For 60 mL Chlorphenamine maleate Syrup:
Each 5 mL contains 2 mg Chlorphenamine maleate
For 60 mL syrup it requires =
2  60
5
mg of Chlorphenamine maleate
= 24 mg of Chlorphenamine maleate
= 0.024 gm of Chlorphenamine maleate
Formula: For 60 mL Chlorpheniramine Maleate solution
Each 5 mL contains 2 mg Chlorphenamine maleate
Name of Ingredient
Theoretical weight
Purpose
24 mg / 0.024 gm
API. (H1 histamine receptor antagonist).
Sucrose Syrup BP
20 mL
Glycerin BP
5 mL
Sorbitol Solution (70%) BP
6 mL
Viscosity imparting &Sweetening agent.
Retard
crystallization
of sucrose;
Sweetener, Humectant.
Viscosity imparting agent; Humectant,
Sweetener; Anti-crystallization Agent
Antimicrobial Preservative.
Antimicrobial Preservative.
Antioxidant; Buffer; Acidifying agent.
Alkalizing agent; Buffering agent.
Chlorpheniramine Maleate BP
Methyl 4-Hydroxybenzoate BP
Propyl 4-Hydroxybenzoate BP
Citric Acid BP
Sodium Citrate BP
Flavor
Color
Distilled water
80 mg / 0.08 gm
8 mg / 0.008 gm
80 mg / 0.08 gm
60 mg / 0.06 gm
Q.S.
Q.S.
Q.S. up to 60 mL
Improve organoleptic property.
Solvent / Vehicle.
Page 11
Method of preparation:
1. At first take 0.024 gm Chlorpheniramine maleate in a 250 mL beaker and dissolve it in
10 mL DW.
2. Afterwards add 20 mL sugar syrup, 6 mL sorbitol solution, 5 mL glycerol, 0.06 gm
Na- citrate, 0.08 gm citric acid, 0.08 gm Methylparaben, 0.008 gm Propylparaben step by
step in the Chlorpheniramine maleate solution. Carefully mix all the ingredients with
proper stirring.
3. After uniform blending of all the portions, add the organic flavor and color and mix them
appropriately.
4. Later transfer the whole content of the beaker in a 100 mL measuring cylinder and adjust
the volume to 60 mL by the addition of purified water.
5. Finally transfer the preparation in a bottle. Close & label the bottle properly.
Functions of each ingredient:
1. Chlorpheniramine Maleate: It is the active ingredient of
the preparation. It acts as Histamine H1 receptor antagonist;
commonly known as antihistamines.
Properties:
√ Physical form
√ Color
√ Odor
√ Solubility
: Crystalline powder.
: White.
: Odorless.
: Soluble in 4 parts of water, 10% ethanol (96%) 10 parts of
chloroform, slightly soluble in ether.
2. Sucrose syrup:
It is used in the preparation as sweetening agent to mask the bitter taste of preparation.
Sucrose: (β-D-Fructofuranosyl α-D-glucopyranoside.)
Properties:
🞛 Colorless or Brown, Odorless, Crystalline Powder.
🞛 Viscous in nature.
🞛 It has a sweet taste.
🞛 Free flowing (crystalline sucrose).
🞛 Cohesive solid (Powder Sucrose).
🞛 Melting Point: 160°C –186°C (with decomposition)
🞛 Good stability at room temperature and at moderate relative humidity.
Sucrose:C12H22O11
🞛 Dilute sucrose solutions are liable to fermentation by microorganisms.
🞛 Sucrose is also considered to be more cariogenic than other carbohydrates since it is
more easily converted to dental plaque. For this reason, its use in oral pharmaceutical
formulations is declining.
Functions:
♦ Sweetening Agent: Used to enhance palatability.
♦ Viscosity imparting agent: Used to increase viscosity.
Page 12
3. Glycerin:( Glycerol; Glycerine)
Glycerin is used in a wide variety of pharmaceutical formulations including
oral, otic, ophthalmic, topical, and parenteral preparations.
Glycerin has preservative qualities and is often used as a stabilizer and as an auxiliary solvent in conýunction with
water or alcohol.
Properties:
i. Clear, colorless, odorless
ii. Hygroscopic liquid
Functions:
♦ Solvent
♦ Humectant
♦ Antimicrobial preservative
iii. Viscous
iv. Sweet in taste (App. 0.6 times as sweet as sucrose)
♦ Co-solvent
♦ Sweetening agent
♦ Viscosity increasing agent
4. Sorbitol Solution
Sorbitol is D-glucitol. It is a hexahydric alcohol related to mannose and is isomeric with mannitol.
Sorbitol (D-Glucitol): Sorbitol is widely used as an excipient in pharmaceutical formulations.
Properties:
i. Odorless, white or almost colorless
ii. Hygroscopic powder
iii. Crystalline
iv. Sweet in taste
Functions:
🞛 Prevent crystallization of sugar around the cap of bottles
🞛 Sweetener
🞛 Vehicle in sugar-free formulations
🞛 Stabilizing agent
🞛 Humectant
5. Methyl & Propylparaben: (Parabens : Alkyl esters of p-hydroxybenzoic acid )
Methylparaben is widely used as an antimicrobial preservative in cosmetics, food products, and pharmaceutical
formulations.
Methylparaben
Properties:
i. Colorless crystals or a white crystalline powder
ii. Odorless or almost odorless.
iii. Slight burning taste.
Propylparaben
Properties:
i. White
ii. Crystalline powder
iii. Odorless
iv. Tasteless
Function:
i. Methylparaben & Propylparaben exhibit antimicrobial activity over the pH range 4–8.
ii. They are also more active against Gram-positive than against Gram-negative bacteria.
Activity may be improved by using combinations of parabens, as synergistic effects occur.
Page 13
6. Citric acid :( Citric acid monohydrate) 2-Hydroxypropane-1,2,3-tricarboxylic acid monohydrate.
Properties:
i. Colorless or translucent crystals or granules, /or as a white crystalline powder.
ii. Odorless.
iii. Strong acidic taste.
iv. Efflorescent.
v. It is slightly deliquescent in moist air.
vi. Melting point 100°C (Monohydrate), 153°C (anhydrous).
Functions:
♦ Buffering agent (adjust the pH of solutions)
♦ Acidifying agent
♦ Flavor enhancer
♦ Sequestering agent
♦ Sialogogue An agent increasing the flow of saliva.
♦ Antioxidant synergist.
7. Sodium Citrate (dihydrate) Trisodium citrate; C6H5Na3O7.2H2O
Properties:
i. Monoclinic crystals or a white crystalline powder.
ii. Odorless, colorless.
iii. Cooling, saline (sour) taste.
iv. It is slightly deliquescent in moist air and efflorescent in warm dry air.
Functions:
♦ Buffering agent
♦ Alkalizing agent
♦ Sequestering agent
♦ Emulsifying agent
♦ Preservatives and Antioxidants
♦ Processing Aids and Additives
Other ingredients used:
Organic flavour
Organic colour
Distilled water
: It is used as flavouring agent. Green banana flavour
: It is used as colouring agent.
: Used as vehicle.
Indications: Chlorpheniramine relieves Urticarial rashes, Red, itchy, watery eyes;
 Pruritus, Sneezing; insect bites and stings
 Itchy nose or throat; and
 Runny nose caused by allergies, hay fever, and the common cold.
Side-effects
♦ Drowsiness
♦ Headache,
♦ Psychomotor impairment,
♦ Urinary retention
♦ Dry mouth,
♦ Blurred vision,
♦ Gastro-intestinal disturbances. ♦ Hypotension,
♦ Palpitation,
♦ Arrhythmias,
♦ Extrapyramidal effects,
♦ Dizziness,
♦ Confusion,
♦ Depression,
♦ Sleep disturbances,
♦ Tremor,
♦ Convulsions,
♦ Blood disorders,
♦ Liver dysfunction
♦ Angle-closure glaucoma
and ♦ Hypersensitivity reactions (including bronchospasm,
angioedema, and anaphylaxis, rashes, and photosensitivity reactions).
Page 14
Cautions and contra-indications
Must be used with caution in-



Prostatic hypertrophy,
Angle-closure glaucoma
Hepatic disease
 Urinary retention,
 Pyloroduodenal obstruction
 Eepilepsy.
Dose:
Adults and children 12 years and over:
10 mL (4 mg) every 4 to 6 hourly. Maximum daily dose: 60 mL (24 mg) in any 24 hours.
Children
6 - 12 years: 5 mL (2 mg) every 4 to 6 hourly. Maximum daily dose: 30 mL (12 mg) in any 24 hours.
2 - 6 years: 2.5 mL (1mg) every 4 to 6 hourly. Maximum daily dose: 15 mL (6 mg) in any 24 hours.
1 - 2 years: 2.5 mL (1 mg) twice daily. The minimum interval between the doses should be 4
hours. Maximum daily dose: 5 mL (2 mg) in any 24 hours.
 Not recommended for children below 1 year
Chlorpheniramine Syrup
Each 5 mL contains
Chlorpheniramine Maleate BP 2 mg
Batch No.
0171740
Mfg. Date
: Oct 2017
Exp Date
: Oct 2019
M.R.P. Tk.
67
Mfg. Lic. No. :12 & 80
Indication: Allergic
conditions
and urticaria.
such
as
rhinitis
Dose: As directed by Physician
Storage condition: Keep in cool and dry place
Precaution:
Keep every medicine out of reach of children.
Oral administration only
DAR No.
: 025-0144-088
Manufactured by: Department of Pharmacy, Independent University, Bangladesh
Market preparation: Chlorpheniramine Maleate Syrup
SL.
01
02
03
04
05
Trade/Brand Name
Manufacturer
Dosage form
Page 15
Experiment No. 04
Name of the Experiment: Formulation and preparation of Antacid Suspension.
(Each 5 mL contains Aluminum Hydroxide 200 mg and Magnesium Hydroxide 400 mg)
Introduction:
Suspensions may be defined as a coarse dispersion in which finely divided insoluble drug
particles (the suspensoid) generally greater than 1µm in diameter are dispersed uniformly
throughout a liquid medium in which the drug exhibits a minimum degree of solubility.
A coarse suspension is a dispersion of finely divided, insoluble solid particles (the disperse phase)
in a fluid (the dispersion medium or continuous phase). Most pharmaceutical suspensions consist of
an aqueous dispersion medium, although in some instances it may be an organic or oily liquid.
A gastric antacid is a chemical substance introduced into the stomach for the purpose of
lowering the hydrogen ion concentration, or acidity, of the gastric contents; resulting in an
increase in the pH of stomach and duodenum. Gastric acidity occurs due to excessive secretion of
HCl in stomach due to various reasons. The suspension form of antacids is given for faster
absorption, because the rate of dissolution is higher than tablets. It is because of resulting from
higher surface area provided by smaller fine particles.
Such antacids are in common use in medical practice, mostly in the treatment of peptic ulcer.
They react with gastric HCl and neutralize the acids as follows:
Al (OH) 3+3HCl⭢AlCl3+3H2O
Mg(OH)2+2HCl→MgCl2+2H2O
Classification:
a. Systemic Antacid:
Systemic antacids are antacids which get systemically absorbed. They are capable of producing
metabolic alkalosis because the certain moiety does not form insoluble basic compound in the
intestine e.g. NaHCO3, KHCO3, Na-citrate etc.
b. Non Systemic Antacid:
A non- insoluble basic systemic antacid is one which forms insoluble basic compound in the
intestine and is not subsequently absorbed. So these antacids do not produce systemic alkalosis.
e.g. Al(OH)3,Ca(OH)2 Mg(OH)2, Ca3(PO4)2,Mg-trisilicate.
Apparatus:
1. Beaker
3.Stirrer
5. Measuring cylinder
7. Droppers
2. Mortar
4.Pestle
6. Funnel
8.
Electric
balance
Recipe:
Note: Actual 5 mL formulation contains dried Al (OH) 3 Gel USP equivalent to 200 mg Al2O3,
400mg Mg(OH)2 BP and 30 mg Simethicone USP (which is omitted here).
For 60 mL Antacid Suspension (Calculation is only for Al(OH)3):
Each 5 mL contains 200 mg Al(OH)3
Then 60 mL contains = 200  60 mg of Al(OH)3
5
=2400 mg of Al(OH)3
=2.4 gm of Al(OH)3
Page 16
Formula:
Each 5 mL suspension contains 200 mg of Al(OH)3 & 400 mg of Mg(OH)2
Name of the ingredient
Dried Aluminium Hydroxide
Magnesium hydroxide
Na-CMC BP
Weight
2.4 gm
4.8 gm
0.4 gm
Glycerin BP
3 mL
Sorbitol Solution (70%) BP
10 mL
Methyl 4-Hydroxybenzoate BP
Propyl 4-Hydroxybenzoate BP
Saccharine Sodium BP
Sodium Citrate BP
Flavour
Colour
Purified Water BP
100 mg / 0.1 gm
10 mg / 0.01 gm
15 mg / 0.015 gm
50 mg / 0.05 gm
Q.S.
Q.S
Q.S. to 60 mL
Purpose/Justification
API. Gastric antacid.
API. Gastric antacid.
Suspending agent
Retard crystallization of sucrose;
Sweetener, Humectant.
Viscosity imparting agent; Humectant,
Sweetener; Anti-crystallization Agent
Antimicrobial Preservative.
Antimicrobial Preservative.
Sweetening agent. 500 × more sweet than sucrose
Flocculating agent.
Improving organoleptic properties.
Solvent/Vehicle.
Method of Preparation:
1. Take 2.4 gm Al (OH) 3 & 4.8 gm Mg(OH)2 in a mortar. Crush them properly and then dissolve
them in 10 mL DW with continuous trituration by pestle in order to get a uniform mixture.
2. Then take 0.4 gm Na-CMC along with 10 mL DW in a 50 mL beaker. Mix it slowly to make
uniform mucilage.
3. Now mix the Al(OH)3 & Mg(OH)2 solution (previously made in the step one) and NaCMC mucilage (from the step two) in a 250 mL beaker. Appropriately blend these two solutions to
get a homogenous mixture.
4. Afterwards add 10 mL Sorbitol solution, 3 mL Glycerine, 0.1 gm Methyl Hydroxybenzoate,
0.01 gm Propyl Hydroxybenzoate, 0.015 gm Saccharine sodium and 0.05 gm Na-Citrate. Mix them
thoroughly with continuous stirring.
5. Finally add organic oil (Flavor) with triturate to mix it with the preparation properly.
6. Take the final solution in a measuring cylinder and adjust the volume to 60 mL by adding
sufficient quantity of purified water.
7. From the cylinder, transfer the final preparation in a well-polished bottle. Finally cork & label
the bottle.
Function of ingredients:
1. Al(OH)3 and Mg(OH)2: Al(OH)3 and Mg(OH)2 are the active part of the preparation. They
act as antacid and serve to reduce acidity.
Page 17
Properties: Al(OH)3
√ Physical form
√ Color
√ Odor
√ Solubility
Properties: Mg (OH)2
√ Physical form
√ Color
√ Odor
√ Solubility
: Amorphous powder
: White
: Odorless
: Soluble in dilute mineral acids and aqueous solutions of Alkali
hydroxides. Insoluble in water.
: Fine amorphous powder
: White
: Odorless
: Soluble in dilute acids. Insoluble in water.
2. Na-CMC: Carmellose sodium
Carboxymethylcellulose Sodium is widely used in oral and topical pharmaceutical formulations,
primarily for its viscosity-increasing properties.
Properties:
i.
ii.
iii.
iv.
v.
It occurs as a white to almost white
Odourless and tasteless
Granular powder
It is hygroscopic after drying
Easily dispersed in water at all temperatures, forming clear, colloidal solutions.
The aqueous solubility varies with the degree of substitution.
Function:
🞛 Suspending agent
🞛 Viscosity-increasing agent
🞛 Stabilizing agent
🞛 Water-absorbing agent
3. Glycerin:( Glycerol; Glycerine)
Glycerin is used in a wide variety of pharmaceutical formulations including
oral, otic, ophthalmic, topical, and parenteral preparations.
Glycerin has preservative qualities and is often used as a stabilizer and as an auxiliary solvent in conýunction with water or
alcohol.
Properties:
i. Clear, colorless, odorless
ii. Hygroscopic liquid
iii. Viscous
iv. Sweet in taste (App. 0.6 times as sweet as sucrose)
Functions:
🞛 Solvent, Co-solvent
🞛 Humectant
🞛 Antimicrobial preservative
🞛Viscosity increasing agent
🞛 Sweetening agent
🞛 Retard crystallization of sucrose
4. Sorbitol Solution
Sorbitol is D-glucitol. It is a hexahydric alcohol related to mannose and is isomeric with mannitol.
Sorbitol: Sorbitol is widely used as an excipient in pharmaceutical formulations.
Page 18
Properties:
i. Odorless, white or almost colorless
ii. Hygroscopic powder
iii. Crystalline
iv. Sweet in taste
Functions:
🞛 Prevent crystallization of sugar around the cap of bottles
🞛 Vehicle in sugar-free formulations
🞛 Stabilizing agent
🞛Sweetener
🞛 Humectant
5. Methyl & Propylparaben: (parabens : Alkyl esters of p-hydroxybenzoic acid )
Methylparaben is widely used as an antimicrobial preservative in cosmetics, food products, and pharmaceutical formulations.
Methylparaben
Properties:
i. Colorless crystals or a white crystalline powder
ii. Odorless or almost odorless .
iii. Slight burning taste.
Propylparaben
Properties:
i. White
ii. Crystalline powder
iii. Odorless
iv. Tasteless
Function
i. Methylparaben & Propylparaben (10:1) exhibit antimicrobial activity over the pH range 4–8.
ii. They are also more active against Gram-positive than against Gram-negative bacteria.
Activity may be improved by using combinations of parabens, as synergistic effects occur.
6. Saccharine Sodium
Saccharinum
Properties:
i . White crystalline powder.
ii. Odorless or faintly aromatic.
iii. Efflorescent.
SACCHARIN-Na
SACCHARIN
iv. It has an intensely sweet taste, with a metallic or bitter aftertaste.
Functions:
♦ Sweetening agent (approximately 300–600 times sweet than sucrose).
♦ Saccharin sodium enhances flavor systems and may be used to mask some unpleasant
taste characteristics.
7. Sodium Citrate (dihydrate) Trisodium citrate; C6H5Na3O7.2H2O
Properties:
i. Monoclinic crystals or a white crystalline powder.
ii. Odorless, colorless.
iii. Cooling, saline (sour) taste.
iv. It is slightly deliquescent in moist air and efflorescent in warm dry air.
Functions:
♦ Buffering agent
♦ Alkalizing agent
♦ Sequestering agent
♦ Emulsifying agent
♦ Preservatives and Antioxidants
♦ Processing Aids and Additives
Page 19
Other ingredient(s) used:
Peppermint Oil
: It is used as flavouring agent. Green banana flavour
Indications: Antacid Suspension is indicated for🞛 Dyspepsia,
🞛 Gastritis;
🞛 Windy colic.
🞛 Hyperacidity,
🞛 Relief of flatulence,
🞛 Gastric and duodenal ulcer,
🞛 Abdominal distention and
Dosage & Administration:
1-2 teaspoonfuls one hour after meals and at bed time or as directed by the physician.
Warning & Precautions:
Drugs containing Al(OH)3 shouldn’t be taken concomitantly with any form of Tetracycline, as the
absorption of the later may be affected. Al(OH)3 may also reduce the absorption of Digoxin.
Side effects:
1. Theoretically, if the gastric pH is raised too much, acid rebound may occur, since an effort to
maintain a lower pH, the stomach secretes additional HCl acid which consumes the antacid.
2. A second potential problem is systemic alkalosis. If the antacid is sufficiently water soluble
and is composed of readily absorbable ions, the antacid may be absorbed and exert its alkaline
effort on the body’s buffer system.
3. Another problem is sodium content of antacid. Those patients who are sodium restricted, diet
should be advised of this when antacid is recommended.
4. The 4th side effect is the local effect is the GIT. Antacid containing calcium and aluminum salts,
after being converted to soluble salt by gastric acid, tend to constipating, while containing
magnesium salts tend to have a laxative effect.
Antacid Suspension
Each 5 mL contains
200 mg Aluminium Hydroxide &
200 mg Magnesium Hydroxide Gel
Batch No.
Mfg. Date
Exp. Date
M.R.P. Tk.
0171740
: Oct 2017
: Oct 2019
67
Indication: Peptic Ulcer, Gastric Ulcer, Gastric acidity.
Dose
: As directed by Physician
Storage condition: Keep in cool and dry place
Precaution
: Shake before use.
Keep every medicine out of reach of children.
Store in cool and dry place.
DAR No.
: 025-0144-088
Mfg. Lic. No. :12 & 80
Manufactured by: Department of Pharmacy, Independent University, Bangladesh
Market preparation: Antacid Suspension
SL.
01
02
03
04
05
Trade/Brand Name
Manufacturer
Dosage form
Page 20
Experiment No. 05
Name of the Experiment: Formulation and preparation of Metronidazole oral
Suspension. (Each 5 ml contains Metronidazole Benzoate BP 320 mg equivalent to
200 mg Metronidazole.)
Introduction:
Suspensions are biphasic liquid dosage form of medicament in which the finely divided solid
particles ranging from 0.5 to 5 micron are suspended or dispersed in a liquid or semisolid vehicle.
The vehicle may be aqueous or oily.
Suspensions represent a useful method of preparing drugs that are poorly soluble in acceptable
solvents. They are formulated for all the major routes of administration, in particular the oral,
parenteral and topical routes, with specific requirements for each route and desired response.
Metronidazole oral suspension is a suspension of Metronidazole Benzoate in a
flavoured vehicle.
suitable
Metronidazole is a nitroimidazole, has an extremely broad spectrum
antiprotozoal and antimicrobial activities, with high activity against
anaerobic bacteria and protozoa. It is used either alone or with other
antibiotics to treat pelvic inflammatory disease, endocarditis, and
bacterial vaginosis.
Metronidazole benzoate
Some physical properties of a well formulated suspension
1. The suspension must remain sufficiently homogenous for at least the period between shaking
the container and removing the required dose.
2. The sediment produced on storage must be easily re-suspended by the use of moderate
agitation.
3. The suspension may be required to be thickened in order to reduce the rate of settling of the
particles. The viscosity must not be so high that the removal of the product from the container
and transfer to the site of application becomes difficult.
4. The suspended particles should be small and uniformly sized in order to give a smooth, elegant
product free from a gritty texture.
Recipe:
For 60 mL Metronidazole Suspension:
Each 5 mL contains 320 mg Benzoyl Metronidazole (Metronidazole benzoate~Metronidazole 200 mg BP)
320  60
Then 60 mL contains =
mg of Benzoyl Metronidazole
5
= 3840 mg ~3.84 gm of Benzoyl Metronidazole
Apparatus:
1. Beakers
2. Master & pestle
3. Funnel
4. Bottle
5. Measuring cylinder
6. Electric balance
7. Pipette
Page 21
Formula
For 60 mL Metronidazole suspension:
Each 5 mL contain 320 mg of benzoyl metronidazole. (Metronidazole benzoate)
Name of Ingredient
Theoretical weight
Purpose
Benzoyl Metronidazole BP
3.84 gm
API. Imidazole antibacterial.
Na-CMC BP
0.5 gm
Suspending agent.
Sucrose syrup BP
20 mL
Sweetening agent.
Sorbitol Solution (70%) BP
5 mL
Glycerin/Glycerol BP
5 mL
Methyl 4-Hydroxylbenzoate BP
100 mg / 0.1 gm
Viscosity imparting agent; Humectant,
Sweetener; Anti-crystallization agent.
Sweetener, Humectant,
Retard crystallization of sucrose.
Antimicrobial Preservative.
Propyl 4-Hydroxbenzoate BP
10 mg / 0.01 gm
Antimicrobial Preservative.
Saccharine –Na BP
0.1 mg / 0.0001 gm
Sweetening agent. 500 × more sweet than sucrose
Citric acid BP
100 mg / 0.1 gm
Acidifying & buffering agent.
Na-Citrate BP
60 mg / 0.06 gm
Flocculating & sequestering agent.
3 drops
Wetting agent; Solvent; Humectant.
Propylene glycol
Organic flavor
Q.S.
Organic color
Q.S.
Distilled water
Q.S. up to 60 mL
Improving organoleptic property.
Solvent/Vehicle.
Method of preparation:
1. Take 0.5 gm of Na-CMC in a clean & dry 50 mL beaker and add 15 mL DW. Carefully stir and
allow for proper swelling to form a homogenous mucilage.
2. Take 3.84 gm Benzoyl Metronidazole in a 250 mL beaker and dissolve it in 5 mL propylene
glycol with proper stirring. Then add the previously made Na-CMC mucilage (Step-1) in it.
3. Afterwards add 0.1 mg (0.0001 gm) Na-saccharine, 0.1 gm Methylparaben and 0.01 gm
Propylparaben, 0.1 gm Citric acid & 0.06 gm Na- Citrate to this solution with proper trituration.
4. Later add 20 mL sucrose syrup, 5 mL sorbitol solution and 5 mL glycerin with continuous
stirring to obtain proper homogeneous product.
5. Now add the organic flavor and color and mix them appropriately.
6. Transfer the whole content of beaker in a measuring cylinder and adjust the volume to
60 mL by the addition of purified water.
7. Finally transfer the preparation in an amber colored glass bottle since the metronidazole is
light sensitive. Close & label the bottle properly.
Page 22
Functions of each ingredient:
1. Bezoyl Metronidazole: It is the active ingredient of the preparation. It is used in the
treatment of infection caused by protozoa & flagella.
Properties:
√ Physical form
√ Color
√ Odor
√ Nature
√ pH
√ Solubility
: Crystalline powder or Flakes
: White, Slightly yellowish
: Odorless
: Acidic in nature
: 5.6―6.5
: Freely soluble in methylene chloride, soluble in acetone, Slightly
soluble in alcohol. Practically insoluble in water.
Function:
Metronidazole is also used in the treatment of infections caused by―
👉 Giardia lamblia,
👉 Trichomonas vaginalis,
👉 anaerobic cocci, and anaerobic gram-negative bacilli (for example, Bacteroides species)
It is the drug of choice for the treatment of pseudomembranous colitis caused by the
anaerobic, gram-positive bacillus Clostridium difficile.
2. Na-CMC: (Carmellose sodium)
Carboxymethylcellulose Sodium is widely used in oral and topical pharmaceutical formulations,
primarily for its viscosity-increasing properties.
Properties:
i.
ii.
iii.
iv.
v.
vi.
It occurs as a white to almost white
Odourless
Tasteless
Granular powder
It is hygroscopic after drying
Easily dispersed in water at all temperatures, forming clear, colloidal solutions.
The aqueous solubility varies with the degree of substitution.
Function:
🞛 Suspending agent
🞛 Viscosity-increasing agent
🞛 Stabilizing agent
🞛 Water-absorbing agent
3. Sucrose syrup:
It is used in the preparation as sweetening agent to mask the bitter taste of
preparation.
Sucrose: (β-D-Fructofuranosyl α-D-glucopyranoside.)
Page 23
Properties:
🞛 Colorless or Brown, Odorless, Crystalline Powder.
🞛 Viscous in nature.
🞛 It has a sweet taste.
🞛 Free flowing (crystalline sucrose).
🞛 Cohesive solid (Powder Sucrose).
🞛 Melting Point: 160°C –186°C (with decomposition)
🞛 Good stability at room temperature and at moderate relative humidity.
🞛 Dilute sucrose solutions are liable to fermentation by microorganisms.
🞛 Sucrose is also considered to be more cariogenic than other carbohydrates since it is
more easily converted to dental plaque. For this reason, its use in oral pharmaceutical
formulations is declining.
Functions:
♦ Sweetening Agent: Used to enhance palatability.
♦ Viscosity imparting agent: Used to increase viscosity.
4. Sorbitol Solution
Sorbitol is D-glucitol. It is a hexahydric alcohol related to mannose and is isomeric with mannitol.
Sorbitol: Sorbitol is widely used as an excipient in pharmaceutical formulations.
Properties:
i. Odorless, white or almost colorless
iii. Crystalline
ii. Hygroscopic powder
iv. Sweet in taste
Functions:
🞛 Prevent crystallization of sugar around the cap of bottles
🞛 Vehicle in sugar-free formulations
🞛 Stabilizing agent
🞛Sweetener
🞛 Humectant
5. Glycerin:( Glycerol; Glycerin)
Glycerin is used in a wide variety of pharmaceutical formulations including
oral, otic, ophthalmic, topical, and parenteral preparations.
Glycerin has preservative qualities and is often used as a stabilizer and as an auxiliary solvent in conýunction with water or
alcohol.
Properties:
i. Clear, colorless, odorless
ii. Hygroscopic liquid
Functions:
🞛 Solvent, Co-solvent
🞛 Antimicrobial preservative
🞛 Sweetening agent
iii. Viscous
iv. Sweet in taste (App. 0.6 times as sweet as sucrose)
🞛 Humectant
🞛Viscosity increasing agent
🞛 Retard crystallization of sucrose
6. Methyl & Propylparaben: (parabens : Alkyl esters of p-hydroxybenzoic acid )
Methylparaben is widely used as an antimicrobial preservative in cosmetics, food products, and pharmaceutical formulations.
Methylparaben
Properties:
i. Colorless crystals or a white crystalline powder
ii. Odorless or almost odorless .
iii. Slight burning taste.
Page 24
Propylparaben
Properties:
i. White
ii. Crystalline powder
iii. Odorless
iv. Tasteless
Function:
i. Methylparaben & Propylparaben (10:1) exhibit antimicrobial activity over the pH range 4–8.
ii. They are also more active against Gram-positive than against Gram-negative bacteria.
Activity may be improved by using combinations of parabens, as synergistic effects occur.
7. Saccharine Sodium
Saccharinum
Properties:
i . White crystalline powder.
ii. Odorless or faintly aromatic.
iii. Efflorescent.
SACCHARIN-Na SACCHARIN
iv. It has an intensely sweet taste, with a metallic or bitter aftertaste.
Functions:
♦ Sweetening agent (approximately 300–600 times sweet than sucrose).
♦ Saccharin sodium enhances flavor systems and may be used to mask some unpleasant
taste characteristics.
8. Citric acid :( Citric acid monohydrate) 2-Hydroxypropane-1,2,3-tricarboxylic acid monohydrate.
Properties:
i. Colorless or translucent crystals or granules, /or as a white crystalline powder.
ii. Odorless.
iii. Strong acidic taste.
iv. Efflorescent.
v. It is slightly deliquescent in moist air.
vi. Melting point 100°C (Monohydrate), 153°C (anhydrous).
Functions:
♦ Buffering agent (adjust the pH of solutions)
♦ Acidifying agent
♦ Flavor enhancer
♦ Sequestering agent
♦ Sialogogue An agent increasing the flow of saliva.
♦ Antioxidant synergist.
9. Sodium Citrate (dihydrate) Trisodium citrate; C6H5Na3O7.2H2O
Properties:
i. Monoclinic crystals or a white crystalline powder.
ii. Odorless, colorless.
iii. Cooling, saline (sour) taste.
iv. It is slightly deliquescent in moist air and efflorescent in warm dry air.
Functions:
♦ Buffering agent
♦ Alkalizing agent
♦ Sequestering agent
♦ Emulsifying agent
♦ Preservatives and Antioxidants
♦ Processing Aids and Additives
Page 25
10. Propylene Glycol
Propylene glycol is a useful solvent with a wide range of applications and is frequently
substituted for glycerin in modern pharmaceutical formulations.
Properties:
i. Clear, colorless, practically odorless
ii. Hygroscopic in nature
iii. Viscous
iv. Usually tasteless (/faintly sweet)
Functions:
♦ Solvent or co-solvent (Oral , Parenterals, Topical, Aerosol)
♦ Antimicrobial preservative (Solutions, Semisolids)
♦ Disinfectant
♦ Humectant (Topical)
11. Flavouring agent: Lemon flavour & Bergamot flavor
Indications: It is also used to treat🞛 Urogenital trichomoniasis in the female and male, 🞛 Giardiasis, (amebiasis SYN: Amebic dysentery)
🞛 Anerobic bacterial infections, 🞛 Intestinal and extra-intestinal amebiasis
🞛 Metronidazole is an alternative to penicillin for the treatment of many oral infections.
Cautions & Side-effects of Metronidazole: Some side effects of Metronidazole include –
Gastrointestinal discomfort,
Nausea, Coated tongue,
headache
Dryness of mouth and unpleasant metallic or bitter taste.
It should not be used- during pregnancy, breast-feeding, in patients with blood dyscrasia.
Dose: For amebic dysenteryAdult & Children over 10 years: 800mg tid (2g once daily)
Children 7-10 years:400mg tid
Children 3-7 years:200mg qid
Metronidazol Suspension
Each 5 mL contains Metronidazole BP 200mg
Batch No.
Mfg. Date
Exp Date
M.R.P. Tk.
DAR No.
0171740
: Oct 2017
: Oct 2019
67
: 025-0144-088
Children 1-3 years:200mg tid
Indication
Dose
Storage
Precaution
: Antiprotozoal, Antibacterial
: As directed by Physician
: Keep in cool and dry place
: Suspension should be taken at least
one hour before a meal.
Shake before use.
Keep every medicine out of reach of children.
Mfg. Lic. No. :12 & 80
Manufactured by: Department of Pharmacy, Independent University, Bangladesh
Market preparation: Metronidazole Suspension
SL.
01
02
03
04
05
Trade/Brand Name
Manufacturer
Dosage form
Page 26
Experiment No. 06
Name of the Experiment: Formulation and preparation of Preparation of oil in water
(O/W) emulsion. (Each 5 mL contains 0.5 mL castor oil)
Introduction
An emulsion may be defined as a dispersion of two immiscible liquids, in which the dispersed
phase is finely subdivided and uniformLy distributed as droplets throughout the dispersion
medium with the aid of an emulsifying agent that achieves emulsification and maintains stability.
The liquid dispersed into small droplets is called the dispersed, internal, or discontinuous phase.
The other liquid is the dispersion medium, external phase, or continuous phase.
Emulsion is widely used in pharmacy and medicine. Emulsions may be employed orally,
topically, or parenterally, depending on the formulation ingredients and the intended application.
They are made internally as well as externally, certain medicinal agent having an unpleasant
taste & odour can be made more palatable for oral administration in the form of emulsion.
The activity of certain drugs can be increased & action can be prolonged by emulsifying the drug
in a suitable vehicle.
Castor oil has been used as a stimulant laxative to relieve occasional constipation. However,
castor oil usually is avoided for simple constipation because it produces violent purgation.
Classification of Emulsion:
There are two types of emulsion
a) Oil in water (o/w) type emulsion and
b) Water in oil (w/o) type emulsion
Oil in water (O/W) type emulsion:
In oil in emulsion, the oil is the dispersed phase and water is the dispersion medium. This type
of emulsion is preferable or preferred for internal use because the unpleasant taste & odour is
masked by emulsification. The aqueous phase constitutes> 45% of the total weight.
Water in oil (W/O) type emulsion:
In water in oil emulsion, the water is the dispersed phase and oil is the dispersion medium.
This type of emulsion is mainly used externally. The aqueous phase constitutes < 45% of the
total weight.
According to the consistence:
a) Liquid emulsion: They are generally oil in water emulsion and they are used orally,
parentally and externally. e.g. lotion, ointment.
b) Semi-solid emulsion: They are both o/w and w/o type of emulsion. They are used as
internally and externally. e.g. cream.
According to the route of administration:
a) Emulsion for internal use.
According to the particle size:
a) Coarse emulsion
b) Fine emulsion
&
b) Emulsion for external use.
c) Micro emulsion
Page 27
Preparation of Emulsion:
For small scale preparation, emulsion can be prepared by the following method:
a) Dry gum method
b) Wet gum method
c) Bottle method
The proportion of oil, water and gum acacia required for fixed oil and volatile oil for the
preparation of primary emulsion areName of the oil
Fixed oils
Volatile oils
–
–
–
Rose oil
4
4
:
:
:
Water
2
4
:
:
:
Gum
1
2
Formula or Recipe:
For 100 mL Castor oil Emulsion
Each 5 mL emulsion contains 0.5 mL of castor oil
Name of ingredient
Theoretical weight
Purpose
Castor oil
10 mL
API . Cathartics and Laxatives
Acacia
2.5 gm
Emulsifying agent.
Sugar syrup
10 mL
Sweeting agent.
Methylparaben
0.2 gm
Preservative.
Sorbitol solution
10 mL
Sweetening agent.
Raspberry oil
1-2 drops or Q.S.
Flavouring agent.
Distilled water
Q.S. to 100 mL
Vehicle.
Apparatus:
1. Mortar and pestle
2. Beakers
7. Droppers
3. Bottle
5. Filter papers
8. Stirrers
4. Measuring cylinders
6. Funnel
Method of preparation:
1. Take thoroughly cleaned and completely dried mortar and pestle. Transfer accurately
weighed 2.5 mg acacia in the mortar.
2. Slowly triturate the acacia by adding small quantity of purified water to obtain uniform
mucilage.
3. Now add 10 mL castor oil in small portions with rapid trituration in one direction until a
clicking sound is produced and the product become white or nearly white. At this stage, the
emulsion is known as primary emulsion. Later add Methylparaben to the emulsion.
4. Afterwards add 10 mL sugar syrup and 10 mL sorbitol in small quantities at a time with
constant unidirectional trituration so as to get homogeneous product.
5. Transfer the emulsion in a measuring cylinder and add more vehicles with gentle stirring to
produce the final volume 100 mL.
6. After the formation of a uniform emulsion, transfer the preparation in a bottle, close and label
the bottle properly.
Page 28
Functions of ingredient:
1. Castor oil : It is the active ingredient of the preparation. It acts as a laxative.
2. Acacia:
Properties:
i. Acacia is available as white or yellowish-white thin flakes, spheroidal tears, granules,
powder, or spray-dried powder.
ii. Odorless.
iii. Bland taste.
Functions:
♦ Emulsifying agent
♦ Suspending agent
♦ Stabilizing agent
♦ Viscosity-increasing agent.
3. Sucrose syrup:
It is used in the preparation as sweetening agent to mask the bitter taste of preparation.
Sucrose: (β-D-Fructofuranosyl α-D-glucopyranoside.)
Properties:
🞛 Colorless or Brown, Odorless, Crystalline Powder.
🞛 Viscous in nature.
🞛 It has a sweet taste.
🞛 Free flowing (crystalline sucrose).
🞛 Cohesive solid (Powder Sucrose).
🞛 Melting Point: 160°C –186°C (with decomposition)
🞛 Good stability at room temperature and at moderate relative humidity.
🞛 Dilute sucrose solutions are liable to fermentation by microorganisms.
🞛 Sucrose is also considered to be more cariogenic than other carbohydrates since it is
more easily converted to dental plaque. For this reason, its use in oral pharmaceutical
formulations is declining.
Functions:
♦ Sweetening Agent: Used to enhance palatability.
♦ Viscosity imparting agent: Used to increase viscosity.
imparting agent: Used to increase viscosity.
4. Methylparaben:
Methylparaben
Properties:
i. Colorless crystals or a white crystalline powder
ii. Odorless or almost odorless.
iii. Slight burning taste.
Functions:
i. Methylparaben exhibits antimicrobial activity of pH 4–8.
ii. More active against Gram-positive than against Gram-negative bacteria.
iii. Activity may be improved by using combinations of parabens, as additive effects occur.
Page 29
5. Sorbitol Solution
Sorbitol is D-glucitol. It is a hexahydric alcohol related to mannose and is isomeric with mannitol.
Sorbitol: Sorbitol is widely used as an excipient in pharmaceutical formulations.
Properties:
i. Odorless, white or almost colorless
iii. Crystalline
ii. Hygroscopic powder
iv. Sweet in taste
Functions:
🞛 Prevent crystallization of sugar around the cap of bottles
🞛 Vehicle in sugar-free formulations
🞛 Stabilizing agent
6. Raspberry oil
7. Distilled water
🞛Sweetener
🞛 Humectant
: As a flavoring agent.
: It is used as a vehicle.
Other ingredients that can be used:
♦ Active ingredients
♦ Emulsifying agent
♦ Sweetening agent
♦ Preservative
♦ Flavouring agent
: Arachid oil can be used.
: Agar, tragacanth, and starch
: Sucrose can be used.
: Na-benzoate and Propylparaben.
: Peppermint oil, lemon oil and clove oil can be used.
Importance of emulsion in pharmacy and medicine:
1. The activity of certain drugs can be increased and action can be prolonged by emulsifying the
drug in a suitable vehicle.
2. Certain medicinal agent having the unpleasant odour and taste can be more palatable for oral
administration in the form of emulsion.
Dose
Pediatric Patients:
Constipation- Use in children for occasional constipation generally is avoided.
Adults:
Constipation (Oral)~ 15 mL, but rarely indicated for occasional constipation.
Colonic Evacuation (Oral)~ 15–60 mL about 16 hours before the surgery or procedure.
Contraindications It should not be usedIn acute abdominal pain, nausea, vomiting, or other symptoms of appendicitis or undiagnosed
abdominal pain or rectal bleeding.
Intestinal obstruction.
Pregnancy or menstruation.
Warnings/Precautions
Potentially serious toxicity with chronic use.
Page 30
Common Adverse Effects
Abdominal discomfort,
Griping, and/or Faintness,
Nausea,
Cramps,
Excessive irritation of the colon and violent purgation,
Diarrhoea,
Fluid and Electrolyte depletion and
Castor oil emulsion 100 mL
Each 5 mL contains 0.5 mL of castor oil
Batch No.
Mfg. Date
Exp Date
M.R.P. Tk.
DAR No.
Mfg. Lic. No.
0171740
: Oct 2017
: Oct 2019
67
: 025-0144-088
: 12 & 80
GI irritation.
Indication: Cathartic.
Dose: As directed by Physician.
Storage condition: Keep in cool and dry place.
Precaution: Shake before use.
The emulsion may be mixed with 120–240 mL of water,
milk, fruit juice, or soft drink before administration
Administer orally.
Keep every medicine out of reach of children.
Manufactured by: Department of Pharmacy, Independent University, Bangladesh
Bibliography:
1) Rowe RC et al. eds (2009). Handbook of Pharmaceutical Excipients, 6th edn. Washington
DC: American Pharmaceutical Association.
2) Linda A. Felton. eds (2013).
Remington: Essentials of Pharmaceutics 1st edn.
Pharmaceutical Press, Lambeth High Street, London SE1 7JN, UK.
3) British Pharmacopoeia eds (2013). 151 Buckingham Palace Road ; London SW1W 9SZ.
4) British National Formulary eds (2013) 58th edn. BMJ Group and RPS Publishing; Tavistock
Square, London WC1H 9JP, UK and 1 Lambeth High Street, London, SE1 7JN, UK.
5) Lachman L et al. eds (1986). The Theory and Practice of Industrial Pharmacy, 3rd edn.
Philadelphia: Lea & Febiger.
6) Loyd V., Nicholas G. and Howard C. Ansel. eds (2011). Ansel’s Pharmaceutical Dosage
Forms and Drug Delivery Systems., 9th edn. Philadelphia PA/ Baltimore, MD: Wolters
Kluwer Health/Lippincott Williams & Wilkins.
7) David S. Jones. eds (2008). FASTtrack: Pharmaceutics – Dosage Form and Design.
1st edn. Pharmaceutical Press, Lambeth High Street, London SE1 7JN, UK.
8) ACETAMINOPHEN-http://www.chemicalland21.com/lifescience/phar/ACETAMINOPHEN.htm
Page 31
Appendix- Brief description
LAB-01: Acetaminophen is known as a non-aspirin pain reliever. Acetaminophen is a
nonprescription analgesic and antipyretic drug similar to aspirin. But acetaminophen is not an
NSAID (Nonsteroidal Antiinflammatory Drug) as it doesn't participate in the inflammatory response
as it can not inhibit cyclooxygenases in the presence of peroxides.
LAB-01: Sucrose syrup s.g. 1.31g/mL (85% w/V ) 100 mL = 131 gm which contains 85 gm
sucrose USP is denser than bp. Syrup has a specific gravity of about 1.313, which means that each
100 mL of syrup weighs 131.3 g. Because 85 g of sucrose is present, the difference between 85
and 131.3 g, or 46.3 g, represents the weight of the purified water.
LAB-01: Methylparaben is the least active of the parabens; antimicro-bial activity increases with
increasing chain length of the alkyl moiety. Activity may be improved by using combinations of
parabens as synergistic effects occur. Therefore, combinations of methyl-, ethyl-, propyl-, and
butylparaben are often used together. Activity has also been reported to be enhanced by the addition
of other excipients such as: propylene glycol (2–5%); phenylethyl alcohol; and edetic acid.
Solubility 25°C
Meth-P is less lipophilic more hydrophilic (Water :1 in 400 & Mineral oil: Practically insoluble &
Ether 1 in 10). Thus suitable for preventing the Gr+ve bacteria.
Pro-P is more lipophilic less hydrophilic (Water:1 in 4350 & Mineral oil 1 in 3330 Ether: Freely
soluble).
Thus, suitable for preventing the Gr-ve bacteria (Gr-ve bacteria contains
lipopolysaccharide in outer membrane). Thus combination encompasses a broad
spectrum of bacteria.
Urticaria (u˘ r-tı˘-ka￣ _re￣-a˘ ) [L. urtica, nettle] An allergic reaction marked
by multiple discrete swellings on the skin (wheals) that are intensely itchy and last
up to 24 hr. The wheals appear primarily on the chest, back, extremities, face, or
scalp. SYN: hives.
Pruritus (proo-rı¯tu˘ s ) [L., itching] Itch; a tingling or faintly burning skin sensation
that prompts a person to rub or scratch. It may be a symptom of a disease process, such as an allergic
response or hyperbilirubinemia, or it may be due to emotional factors.
Page 32