Compounding Powders (Pulvis et Pulveres) Dr. Muslim Suardi, MSi., Apt. Faculty of Pharmacy University of Andalas Pharmaceutical Powder “a mixture of finely divided drugs or chemicals in a dry form meant for internal or external use” Powder The word "powder" refers to a chemical or mixture that is solid in physical state. In compounding, "powder" refers to a dosage formulation that is solid in physical state. But the formulation may be composed of only the active drug or may be a mixture of the active drug & other ingredients. Powder Frequently prescribed by physician Divided powders Bulk powders Dusting powder Capsules Granules Types of Pharmaceutical Powders Oral powders Topical powders, Dusting powders Powders for inhalation Insufflations powders as a starting material Caps, Tab Dispersions, Injections Suspensions reconstituted Advantages Wide choice of ingredients & varying doses can be prescribed to fulfill the individual patient needed It is convenient for the physician to prescribe a specific amount of powder Each dose can contain a different amount of active drug Easy to carry Advantages Fewer incompatibility than in liquids Since small particle size & no desintegration step look like tablets, dispersion of ingredients will be rapid A greater & more rapid dissolution in the stomach On set of action is faster as compared to tablet, capsules, because it is easily in dissolved in body fluids Advantages Advantages When it is not possible to dispense a drug as a solution or a suspension, because of its insolubility or because it is susceptible to microbial contamination if it is wetted, then it is a good idea to dispense it as a powder. Easy administration to the patient orally by dissolving in suitable liquids Advantages When the patient has to mix the ingredients before administration, dispensing in separate divided powders is a convenient way. Bulky doses or large volume can be more easily taken by the patient, it mean a powder is a good way of administering it. Advantages It can be administered easily to infants, young children, geriatry or other patients who cannot swallow tablets or capsules. In such situations powders are a good option. Flexibility of compounding. Advantages Good chemical stability related with moisture, oxidized, & interaction. Drugs tend to most stable as a solid It is more stable than liquid dosage form. Advantages It is used both internally & externally Can be applied to many body cavities: ears, nose, tooth socket, throat Can be made into many different dosage formulations: capsules, tablets, powders for reconstitution, dusting powders, bulk powders, powders for inhalation, etc. DISADVANTAGES Time-consuming preparation Quantity <100 mg cannot be weighed conveniently Inaccuracy of dose (size of measuring spoon, density of powder, humidity, degree of settling, fluffiness). Unsuitability for many unpleasant tasting, hygroscopic & deliquescent drugs. DISADVANTAGES Bitter taste, nausea & unpleasant taste drugs can’t be administered in powder form. Deliquescent & hygroscopic drugs can’t be dispensed in powder form they are packed in double wrapping. Drugs which get affected by atmospheric condition aren’t suitable for dispense. List of Mesh Sizes Mesh Size Number Mesh Opening Size Mesh Opening Size Millimeters Microns 2 9.52 9520 10 2.00 2000 20 0.84 840 40 0.42 420 60 0.250 250 80 0.177 177 100 0.149 149 200 0.074 74 Usage Based Classification Divided Powders (Pulveres) Bulk Powders (Pulvis for internal used) Dusting Powders (Pulvis adspersorius) Douche Powders Insufflations Powder Sprays Dental Powder (Pulvis dentrificius) Size Based Classification Description Term Mesh Opening Size (microns) Mesh Size Number > 1000 2 - 10 Coarse 355 -1000 20 - 40 Moderately Coarse 180 - 355 40 - 80 Fine 125 - 180 80 - 120 Very Fine 90 - 125 120 - 200 Very Coarse Reducing Particle Size Objectives: Uniform & finely divided mixture. Methods: Trituration Spatulation Sifting Tumbling Trituration Mortar methods, (mortar & pestles, or mortir & stamfer) Most frequently Used for both pulverization & mixing Glass mortars are preferred for dyes & highly colored materials Spatulation Used to mix small quantities of powders & combination of powders having the same densities. A powder spatula is used as the mixing instrument, & the powders are stirred on a pill tile or piece of clean paper. Sifting Sifting is an excellent way to mix powders that resist mixing by trituration. Exceedingly light powders such as MgO & charcoal can be rapidly & completely mixed by shaking them through a sieve. Any large particles which do not pass through the sieve should be powdered by trituration & then re-sieved. Tumbling Mixing powders together by shaking or rotating them in a closed container. This is a simple mixing process & does not effect any reduction in particle size. Mixing Crystalline salts, even if already powdered, are mixed best by trituration. Chlorobutanol & phenyl salicylate electrify & stick or fly when rubbed Salts with contain much water of crystallization , such as alum, sodium phosphate, etc., may need to be dried before mixing, to prevent reactions. Powerful Remedies Mixing An equal bulk of diluent with the potent drug is first placed in the mortar & triturated until well mixed, then a double volume more of added & mixed before a further quantity is added. Incompatible Salts Mixing Should be mixed lightly, as pressure may start a reaction. Rolling on a sheet of paper is a convenient method for avoiding pressure. Eutectic Mixtures When phenols or phenolic compounds, aldehyde compounds & ketonic bodies are mixed, the mixture may have a melting point considerably below that of any of the individual ingredients A suitable remedy for most eutetic mixtures is the addition of an inert powder to separate the offending powder. Bulk Powders Nonpotent & can be dosed with acceptable accuracy & safety using measuring devices such as the teaspoon, cup, or insufflator This practically limits the use of orally administered bulk powders to antacids, dietary supplements, laxatives, & a few analgesics. Many bulk powders are used topically. Dispensed in Bulk Powder Powders which are applied externally as antiseptic or dusting powders In relatively large doses such as a teaspoonful at a time Some powders used to make solutions. Dosage Bulk Powder Usually measured out by the patient All other forms of powder the dosage is measured & package by the pharmacist. Bulk Powder Dispense in either cardboard glass containers. Topically powders: special shaker-top boxes are used Drug to be taken u.i, glass wide-mouth bottles of appropriate size are the containers of choice. Bulk Powder When volatile oils or aromatic substance are contained in the prescription, air-tight containers should be used. Appropriate auxiliary labels should be used on bulk powders for u.e. Dusting Powders Dusting powders are fine medicinal (bulk) powders intended to be dusted on the skin by means of sifter-top containers. A single medicinal agent may be used as a dusting powder; however, a base is frequently used to apply a medicinal agent and to protect the skin from irritation and friction. Dusting Powders Bentonite, kaolin, kieselguhr, MgCO3, starch, & talc are used as inert bases for dusting powders. Powder bases absorb secretions & exert a drying effect, which relieves congestion & imparts a cooling sensation. Dusting Powders All extemporaneous dusting powders should be passed through a 100-200 mesh sieve to ensure that they are grit free and will not further mechanically irritate traumatized areas Douche Powders Used to prepare solutions that cleanse the vagina. Most of them are used for their hygienic effects, but a few contain antibiotics. Prescribed as a matter of convenience for the patient, since a powder is more portable than a bulky solution. Douche Powders The formula is developed so that a teaspoonful or tablespoonful of powder dissolved in a specified volume of water provides the desired concentration. The pH usually ranges from 3.5 to 5 when the solution is prepared. Feminine bulb syringes or fountain syringes are used for vaginal irrigation. Douche Powders Since many of the ingredients are volatile (e.g., menthol, thymol, & volatile oils), douche powders should be packaged in glass jars with a wide mouth. Some commercial are available in metal foil packets, which contain the proper amount of powder for a single douche. Insufflations Extremely fine powders to be introduced into body cavities. To administer an insufflation, the powder is placed in the insufflator, and when the bulb is squeezed, the air current carries the fine particles through the nozzle to the region for which the medication is intended. Insufflations All extemporaneously compounded insufflations must be passed through a 100 mesh sieve. Pressurized packages provide an elegant approach to the administration of insufflations. Powder Sprays In contrast to dusting powders, powders dispensed under pressure will deliver targeted and uniform application at the desired site. Also, in an aerosol container medicated powders may be maintained in a sterile condition. Powder Sprays The powder particles must be a definite size range to prevent clogging of the valve orifice and to provide uniformity of application. In general, powders that are to be packaged as powder sprays must not contain particles greater than 50 microns if they are to be sprayed successfully. Divided Powders (Pulveres) Divided powders or charts are single doses of powdered medicinals individually wrapped in cellophane, metallic foil, or paper. The divided powder is a more accurate dosage form than bulk powder because the patient is not involved in measurement of the dose. Divided Powders (Pulveres) Cellophane and foil-enclosed powders are better protected from the external environment until the time of administration than paper-enclosed powders. Divided powders are commercially available in foil, cellophane or paper packs. Granulations Particles ranging in size from about 410 mesh. Generally made by first blending the powders together & then moistening the mixture to form a pasty mass. The mass is passed through a sieve & then dried in air or in an oven. Granulations They are prepared as a convenience for packaging, as a more stable product due to less surface exposure, & as a popular dosage form. Granulations are also used as intermediates in the preparation of capsules & tablets, since they flow more smoothly & predictably than do small powder particles. Granulations The most popular compounded granulation is the effervescent powder (sometimes called effervescent salts). They are popular due to their taste & psychological impression. When added to water, the granulation effervesces ("fizzes") as CO2 is liberated. Preparation of Effervescent Granulation It has been found that citric acid monohydrate & tartaric acid used in the certain ratio, produces a powder with good effervescent properties. Citric acid monohydrate is not used alone because it results in a sticky mixture that will not easily granulate. Effervescent Granulation Tartaric acid is not used alone because the granules are too friable & crumble The amount of NaHCO3 to be used may be calculated from the reaction which occur when the granules come in contact with water.