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Cream Formulation

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

Requirement of formulation efficacy, safety, and quality

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

Factors to be considered in formulation

Physicochemical properties

Choice of vehicle Waxes and oils or emulsions

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

Bases for Creams


Bases from mixtures of low and high MW PEG Liposomes Microemulsions Multiple emulsions

Fluorocarbon emulsions ultra low

Functions of excipients
Aid processing during manufacturing Protect, support, or enhance stability and bioavailability

Assist product identification colour

Improve effectiveness and safety of product during storage or use

Choice of excipients
physiological inertness physical and chemical stability conformance to regulatory agency requirements no interference with drug bioavailability absence of pathogenic microbial organisms

commercially available at low cost

Limitation in choice of excipients


no single excipient would satisfy all the criteria; therefore, a compromise of the different requirements has to be made.

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..

Microstructural properties of creams


texture and consistency is determined by the phase behaviour of the component emulsifiers. Rheological, thermal and microscopical means characterise the physico-chemical properties X-ray diffraction data

Effect of carrier on drug delivery


Must not interact with active substance Control rate of release from vehicle What are the delivery systems? Alter stratum corneum resistance Physical? Chemical? Enhance stratum corneum hydration..

Delivery systems (in cosmetics)


Vesicular liposomes & niosomes Molecular cyclodextrin Particulate Microcapsules, matrix particles

Excipients as Penetration enhancers


Increase delivery of active substance
1.

Disturb packing of SC lipid bilayers..

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

Effect of type of preparation Absorption of retinyl palmitate


18% absorbed from acetone vehicle compared to only 4% absorbed from o/w emulsion Q What is the mechanism of absorption?

Excipients for hydration


Hygroscopic effect of NaCl, sorbitol, polypropylene glycol, glycerol Low MW glycerols alter water-binding capacity of corneocytes Urea not for < 5 years old Gives moisturising effect

Types

Physical and chemical properties of excipients


solubility hygroscopicity swelling hydration capacity

particle size distribution

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)

Physical Immiscibility insolubility

Drug type and pH of medium


Drug
Promethazine Chlorhexidine Ibuprofen Fentiazac Piroxicam Fluorouracil Crotamiton

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

Hinder release of cationic medicaments

Lower the antimicrobial activity of a cationic medicament or preservative.

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

Exercise: Determine functions of excipients


Nizoral cream Ketoconazole PPG Steary alcohol Cetyl alcohol Sorbitan stearate Polysorbate Isopropyl myristate Sodium sulfite Purified water Elomet cream 0.1% Mometasone furoate White petrolatum White wax PPG stearate Stearyl alcohol Ceteareth-20 Hexylene glycol Titanium dioxide Al starch octenylsuccinate

Purified water Phosphoric acid - pH

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