Drug Formulation Science Intro

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Drug

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Chemical substance intended for use in the diagnosis, mitigation, treatment, cure or prevention of disease, in humans or other animals.

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Excipient

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Substance without any pharmaceutical effect (inert material). They are used together with the active ingredient to facilitate the preparation of the dosage form.

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Dosage form

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A finished product that an active drug and inactive ingredients.

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Active ingredients are transformed into a dosage form

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to facilitate delivery of the active ingredient to the biological target.

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drug absorption

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usually involves passive diffusion of drug down a concentration gradient between the fluids in the gastrointestinal lumen and the portal bloodstream.

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bioavailability

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rate and extent of drug absorption into the systemic circulation

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rate of drug absorption into the systemic circulation

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most important with acute single dose therapy eg analgesia, sedation

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Extent of drug absorption into the systemic circulation

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major determinant of plasma levels of drug with chronic therapy.

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bioequivalence

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comparable bioavailability

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therapeutic equivalence

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comparable therapeutic efficacy

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drug administered in solid dosage form then:-

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disintegration

dissolution

absorption

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considerations in dosage form design

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physicochemical consideration

biopharmaceutical consideration

therapeutic consideration

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physicochemical considerations

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pre-formulation

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biopharmaceutical formulations

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influence of administration route

drug disposition (ADME)

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therapeutic considerations

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implications of disease state

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What is a pharmaceutical powder?

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a mixture of finely divided drugs or chemicals in a dry form meant for internal or external use

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advantages of powders

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flexibility of compounding

good chemical stability

rapid dispersion of ingredients because of particle size.

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Types of medicated powders?

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Aerosol

Bulk and divided

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disadvantage of powders

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time consuming preparation

inaccuracy of dose

unsuitability for many unpleasant tasting, hygroscopic and deliquescent drugs

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what does hygroscopic mean?

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absorbing or attracting moisture from the air

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what does deliquescent mean?

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tendency to become liquid

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Very Coarse

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#8 Sieve 2,360 μm 2.36 mm

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Coarse

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#20 Sieve 850 μm 0.85mm

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Mod. Coarse

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#40 Sieve 425 μm

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Fine

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#60 Sieve 250 μm

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Very Fine

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#80 Sieve 180 μm

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Bulk Powders

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Pharmaceutical powders dispensed as a whole in one container

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Oral Powders definition

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Oral - These generally are supplied as finely divided powders or effervescent granules.

The finely divided powders are intended to be suspended or dissolved in water or mixed with soft foods, e.g., apple sauce, prior to administration.

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Examples of oral powders

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Antacids and laxative powders frequently are administered in this form Examples: Antacid powder, Oral antibiotic powder

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Bulk powders for external use

Examples:

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• Douche powders

• Dentifrice powders

• Insufflations

• Dusting powders

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Dentifrices

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These may be prepared in the form of a bulk powder, generally containing a soap or detergent, mild abrasive and an anticariogenic agent.

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Douche Powders - definition

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These products are completely soluble and are intended to be dissolved in water prior to use as antiseptics or cleansing agents for a body cavity.

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most common uses for douche powders

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They most commonly are intended for vaginal use, although they may be formulated for nasal, otic or ophthalmic use.

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How are douche powders stored?

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Generally, since aromatic oils are included in these powders dispensing in wide-mouth glass jars serves to protect against loss of volatile materials and permits easy access by the patient

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What are insufflations?

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These are finely divided powders introduced into body cavities such as the ears, nose, throat, tooth sockets and vagina. An insufflator (powder blower) usually is employed to administer these products.

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What are dusting powders?

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These are applied to various parts of the body as lubricants, protectives, absorbents, antiseptics, antipruritics, anti-bromhidrosis agents, astringents and antiperspirants.

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How are divided powders dispensed?

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In the form of individual doses and generally are dispensed in papers, properly folded (chartulae). They also may be dispensed in metal foil, small heat-sealed plastic bags or other containers

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Re. divided powders, how can hygroscopic and volatile drugs be protected?

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By using a wax paper.

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Applications of divided powders

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Easily alter dose

• Clinical studies, easy to prepare and alter

• Infants/young children (“sprinkles”)

• Rapid onset of action, good bioavailability

• Stable

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Advantages of Divided Powders

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1. Allows physicians to prescribe a precise amount of the drug.

2. More stable than the liquid form of many drugs.

3. Dissolve more rapidly than compressed solid dosage forms.

4. Rapid dissolution leads to faster blood levels and possibly less GI irritation.

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Stages of powder preparation are:-

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Spatulation • Trituration • Sifting • Tumbling

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What is trituration?

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This term refers to the process of reducing substances to fine particles by rubbing them in a mortar with a pestle. This results in blending powders and breaking up soft aggregates of powders.

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When granular or crystalline materials are to be incorporated into a powdered product

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these materials are triturated individually and then blended together in the mortar

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What is Pulverization by Intervention

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This is the process of reducing the state of solids with the additional material as volatile solvents which evaporates off fairly quickly leaving the residue as a powder.

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Why can't camphor be easily pulverised by trituration

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Because of its gummy properties

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How can camphor be pulverised?

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It can be reduced to a fine powder by the addition of a small amount of alcohol or other volatile solvent.

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How can Iodine crystals be triturated?

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With a small amount of ether.

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What is Levigation?

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this technique is used to incorporate solids into ointments and suspensions.

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How is Levigation achieved?

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In this process a paste is first formed by the addition of a suitable non-solvent to the solid material.

Particle-size reduction then is accomplished by robbing the paste in a mortar with a pestle.

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When is geometric dilution used?

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When potent substances are to be mixed with a large amount of diluent, this method is employed to ensure the uniform distribution of the potent drug.

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By this method, the potent drug placed upon an equal volume the diluent in a mortar and the mixture is mixed by trituration. Then a second portion of diluent equal in volume to the powder mixture in the mortar is added, and the trituration is repeated. • This process is continued by adding equal volumes of diluent to that powder present in the mortar and repeating the mixing until all of the diluent is incorporated.

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Geometric dilution

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What is blending?

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Blending is used when two or more substances are to be combined to form a uniform powder mixture.

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When blending, depending upon the nature of the ingredients and the amount of powder to be prepared...

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mixing may be by spatulation, trituration, sifting, tumbling or by mechanical mixers.

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When is spatulation used?

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This method is used when small amounts of powders are to be blended by the movement of a spatula through the powders on a sheet of paper or an ointment slab

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When is sifting not acceptable?

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This process is not acceptable for the incorporation of potent drugs into a diluent base

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Tumbling

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The powder enclosed in a large container which rotates generally by a motorized process.

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Volatile substances

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The loss of camphor, menthol and essential oils by volatilization when incorporated into powders may be prevented or retarded by use of heat-sealed plastic bags or by double wrapping with a waxed or glassine paper inside a bond paper.

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What does eutectic mean?

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A mixture of substances having a melting point lower than that of any of its components;

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Liquids result from the combination of:-

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phenol,

camphor,

menthol,

thymol,

antipyrne, phenacetin, acetanilide, aspirin, salol at ordinary temperatures.

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Liquids may be incorporated into divided powders.

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Magnesium carbonate, starch or lactose may be added to increase the absorbability of the powders

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When the liquid is a solvent for a nonvolatile heat-stable compound,

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it may be evaporated gently on a water bath

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DELIQUESCENT

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Substances that absorb moisture from the air to the extent that they liquefy by partially or wholly forming a solution

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Examples: Hygroscopic and Deliquescent Powders

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Ammonium Bromide/Chloride/Iodide • Calcium Bromide/Chloride • Ephedrine Sulfate • Hyoscyamine HBr/Sulfate • Lithium Bromide • Phenobarbital Sodium • Potassium Acetate/Citrate • Sodium Bromide/Iodide/Nitrate • Physostigmine Sulfate/HCl/HBr

pilocarpine

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Substances that become moist because of affinity for moisture in the air may be prepared as divided powders by doing what?

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adding inert diluents.

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Granules

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• Particles ranging from 4 to 10 mesh in size

• Not intended for use with potent drugs because of inherent error when a patient measures the dose with a teaspoon, scoop, etc.

• Good for unstable drugs

• Example: antibiotics for reconstitution

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How are granules prepared?

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Prepared by moistening blended powders and by passing this mass through a screen or a granulator • Granules are then air or oven dried. • Flavors can be sprayed on the granules and then dried.

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What do effervescent granules contain?

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mixtures of citric acid, tartaric acid, with sodium or potassium bicarbonate and a medicinal agent

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What is the advantage of an effervescent solution?

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The carbonated solution is a pleasant vehicle and lessens the bitter and salty taste of salts (e.g., magnesium sulfate).

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Examples of effervescet granules?

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Lactinex, Bassoran, Zantac

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How should powders be stored?

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In tightly closed containers for protection against humidity, air oxidation and loss of volatile ingredients.

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Hygroscopic and volatile drugs can be protected by using what?

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Waxed paper.

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Storage/Labeling of powders

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Store in dry places. • Protect from light in some cases. • Keep out of reach of children.

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Patient Counseling

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Dose measuring technique? • Mix with liquid or food? • Premix and store? • Quantity of powder to apply? • Rub or pat into skin? • Should skin be dry? Sweaty?

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Douche Powder

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Boric acid 80 g • Ammonium aluminum sulfate 15 g • Menthol 500 mg • Sodium lauryl sulfate 500 mg • Thymol 300 mg • Phenol 200 mg • Tannic acid 500 mg