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Contents
Ideal formulation Types of excipients Functions Factors for consideration
Every medicinal product is a combination of the drug substance and excipients. Knowledge of the composition, function, and behavior of excipients is a prerequisite to the successful design, development and manufacture of pharmaceutical dosage forms.
Formulation
Process whereby drugs are combined with other substances (excipients) Binders Fillers Preservatives etc.
to produce dosage forms Oral (liquid, solid) Parenteral (IV, aqueous or oily injections) Rectal (suppositories, aerosols) Topical (cream, ointment, lotion) suitable for administration to or by patients.
Excipients
Other components other than ACTIVE ingredient/s intentionally added to.formulation
Ideal formulation
Non-irritant Non-allergenic Non-staining Easy to apply Pleasant feeling to the skin Non-toxic Non-harmful Incapable of microorganism growth Free from side-effects
Contain an accurate dose Be convenient to take or administer Provide the drug in a form for absorption or other delivery to the target Retain quality throughout the shelf life and usage period
Be manufactured by a process that does not compromise performance and that is reproducible and economical
Physicochemical properties
Categories of excipients Provide essential part of the dosage form Prevent degradation of the formulation
Stability
Physicochemical Properties
Oils susceptible to oxidation Incorporate antioxidants E.g. BHT, BHA Aqueous solutions support microbial growth Incorporate water-soluble preservatives E.g. methyl and propyl paraben BUT these may affect the endocrine..
Examples of Creams
Whitening Benzophenone, Hydroquinone Herbal-based (fair & lovely) Pearl Fruit extracts (olay, estee) Anti-ageing Collagen, seaweed extract (Imedeen) liposome Virility Active: fish & herbs (2 types) Excipients: aromatic emollient, Vitamin E, D-panthenol
Functions of excipients
Aid processing during manufacturing Protect, support, or enhance stability and bioavailability
Choice of excipients
physiological inertness physical and chemical stability conformance to regulatory agency requirements no interference with drug bioavailability absence of pathogenic microbial organisms
For example, although widely used in pharmaceutical tablet and capsule formulations as a diluent, lactose may not be suitable for patients who lack the intestinal enzyme lactase to break down the sugar, thus leading to the gastrointestinal tract symptoms such as cramps and diarrhea.
Categories of excipients
Provide essential parts of dosage form Emulsifiers Suspending agents Gelling agents Binders Prevent degradation of the formulation Anti-oxidants Anti-bacterials Preservatives UV absorbers
Excipients in CREAMS
Bases.. SAA Anionic - SDS Non-ionic Span, Tween Anti-oxidants BHA, BHT Preservatives: methyl and propyl paraben (potency, integrity, prevent microbial growth) Stearic acid
Stearyl alcohol, cetyl alcohol Glycerol monostearate Lanolin Glycerin Zinc stearate opacifying agent, dusting powder..
Examples: Sulfoxides, alcohols, polyols, alkanes, esters, amines/amides of fatty acids, terpenes, surfactants, cyclodextrins
2. disruption of skin barrier Extraction of skin lipids with apolar solvents e.g. acetone Physical stripping Physically or chemically induced irritation
Types
bulk density, tap density specific surface area complexation infrared spectrum microbes
Polyamide an excipient
20 m
Carrier for insoluble ingredients Protector for sensitive ingredients Slow delivery & long lasting effect
Incompatibility
Chemical pH effects dissociation? pH and disperse systems Soap emulsions and polyvalent cations Complexation Cationic and anionic compounds of high MW Reducing agents (cause fading of dyes)
Hydrocortisone acetate
pH
Basic acidic Neutral
Incompatibility
Formulation and packaging materials E.g. softening of plastic containers by methyl salicylate ointment.
Detection of Incompatibility
Cracked cream Hydrolysis or oxidation Discoloration Precipitation .visual..?
Emulsifying Wax BP
Incorporation of anionic emulgent resulted in the following: Crack
Cationic compounds
1. Tertiary ammonium compounds Cetrimide Cetylpyridinium chloride Benzalkonium salts Domiphen bromide 2. Chlorhexidine salts 3. Dequalinium salts 4. Acridines 5. Triphenylmethane dyes 6. Neomycin sulphate