‫به نام آنکه هستی نام از او‬
‫یافت‬
‫فلک جنبش زمین آرام از او‬
‫یافت‬
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‫فارما ‪3‬‬
‫دکتر عباسی‬
‫دکتر عباسی‬
‫دکتر عباسی‬
‫دکتر عباسی‬
‫دکتر عباسی‬
‫دکتر عباسی‬
‫دکتر مسجدی‬
‫دکتر مسجدی‬
‫دکتر مسجدی‬
‫دکتر مسجدی‬
‫دکتر مسجدی‬
‫دکتر مسجدی‬
‫دکتر نیکوفال‬
‫دکتر نیکوفال‬
‫دکتر نیکوفال‬
‫دکتر نیکوفال‬
‫دکتر نیکوفال‬
‫دکتر فرهنگی‬
‫دکتر فرهنگی‬
‫دکتر فرهنگی‬
‫دکتر فرهنگی‬
‫دکتر فرهنگی‬
‫دکتر فرهنگی‬
‫‪4‬‬
‫آشنایی با محلولیت و انحالل‬
‫عوامل موثر بر محلولیت‬
‫اکسپیان ها‬
‫اکسپیان ها‬
‫محلول های خوراکی‬
‫محلول های خوراکی‬
‫محلول های غیرخوراکی‬
‫تزریقی‬
‫تزریقی‬
‫فرموالسیون داروهای تزریقی‬
‫دارورسانی چشمی‬
‫دارورسانی چشمی‬
‫بسته بندی‬
‫بسته بندی‬
‫کلین روم‬
‫کلین روم‬
‫روش های استریلیزاسیون‬
‫میان ترم‬
‫سوسپانسیون‬
‫سوسپانسیون‬
‫سوسپانسیون‬
‫دارورسانی گوشی‬
‫دارورسانی بینی‬
‫دارورسانی بینی‬
‫جلسه‬
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Liquid preparations:
dispersing drug substance in the appropriate solvents for
internal or external applications.
8
Classification of liquid preparations
1. Based on the homogeneity of the system
2. Base on the route of administration
9
Homogeneous system: thermodynamically stable:
 Low molecular solutions: solute < 1 nm
 High molecular solutions: solute 1~100 nm
Non-homogeneous system: thermodynamically unstable:
 Emulsion: > 100 nm
 Suspensions: > 500 nm
emulsion
colloid solution
suspension
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2. Classification based on route of administration:
ORAL: drops, syrups, elixirs, tincture, mouth washes, emulsion,
suspensions, and etc.
 Parentral
 Dermal: lotion, liniment
 For ENT (ears, nose, throat): nasal drops (auristillae).
 For ophthalmic administration: eye drops (collyria).
 For rectal, vaginal and urethral administration: enema, irrigations.
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Advantages of liquid formulations
Easy to swallow.
Easy to adjust required dose.
Immediate availability for absorption.
Reduced irritation.
Suitable for formulation of hydrophobic drugs (emulsion,
suspension).
USP teaspoon: 4.93 ± 0.24 mL
Broad route of administration.
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Disadvantages of liquid preparations
 Reduced chemical stability: hydrolysis, oxidation…
 Reduced physical stability: emulsion, suspension
 Reduced microbial stability.
 Inconvenient for transportation and storage.
 Needs proper volumetric tool for dosing.
 Needs taste masking.
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Characteristics:
• homogenous
• one-phase system
• consisting of two or more components.
Solute: component which is dispersed as small molecules or ions in the solvent.
Solvent: the phase in which the dispersion occurs.
15
Solid dispersions
• solute and solvent are solids,
• improved bioavailability of poorly soluble drugs.
Gas-in liquid solutions: Aerosols
• Gas (propellant is dissolved in solvent
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Pharmaceutical solutions are extensively used as dosage forms for the oral
administration of therapeutic agents.
Pharmaceutical solutions are homogeneous, i.e. the therapeutic agent(s) and
excipients are dissolved in the vehicle.
Pharmaceutical solutions for oral administration are non-sterile dosage
forms.
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Dissolution:
o transfer of molecules or ions from a solid state into solution
o How fast we reach the solubility
Solubility:
• Maximum concentration of a solute in a specific solvent and at a particular
temperature.
• The extent to which the dissolution proceeds under a given set of
experimental conditions .
• amount of solute that passes into solution when equilibrium is
established between the solute in solution and the excess
(undissolved) substance.
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Saturation
Equilibrium between solid and dissolved solute.
Depends on pH and temperature.
Super saturated: Solutions with a concentration greater than equilibrium
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Drug solubility: empirical
• High aqueous solubility of the therapeutic agent at the selected pH of the
formulation.
• Moderate aqueous solubility (application of co-solvents)
• Low aqueous solubility (alternative formulations like suspension)
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Key molecular steps in dissolution of a
therapeutic agent in water
1) Removal of a molecule of the drug from the solid state
2) Formation of a cavity within the solvent
3) Accommodation of drug molecule into the formed cavity.
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Energy/work changes during dissolution
Step 1 & 2: Endothermic processes: breakage of solute–solute and solvent–
solvent bonds.
Step 3: Exothermic: formation of a bond between the solute and solvent.
• Dissolution occurs whenever Gibb’s free energy (G) is negative.
Usually dissolution is an endothermic process. However,
where marked affinity between solute and solvent occurs, the process is exothermic.
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