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Cream Formulation

Cream Formulation

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Published by: dropdeadbeautifull on Dec 20, 2012
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07/04/2013

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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

safety.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. 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 .

methyl and propyl paraben  BUT these may affect the endocrine…. BHT.g. .g. 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.. BHA  Aqueous solutions support microbial growth  Incorporate water-soluble preservatives  E.

Examples of Creams  Whitening  Benzophenone. seaweed extract (Imedeen)  liposome  Virility  Active: fish & herbs (2 types)  Excipients: aromatic emollient. Hydroquinone  Herbal-based (fair & lovely)  Pearl  Fruit extracts (olay. estee)  Anti-ageing  Collagen. D-panthenol Bases for Creams  Bases from mixtures of low and high MW PEG  Liposomes  Microemulsions  Multiple emulsions  Fluorocarbon emulsions – ultra low γ i . Vitamin E.

 For example. . support. thus leading to the gastrointestinal tract symptoms such as cramps and diarrhea.Functions of excipients  Aid processing during manufacturing  Protect. a compromise of the different requirements has to be made. or enhance stability and bioavailability  Assist product identification à 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. lactose may not be suitable for patients who lack the intestinal enzyme lactase to break down the sugar. although widely used in pharmaceutical tablet and capsule formulations as a diluent.

 SAA  Anionic .SDS  Non-ionic – Span. Tween  Anti-oxidants – BHA. BHT  Preservatives: methyl and propyl paraben (potency.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….. integrity. prevent microbial growth)  Stearic acid .

 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…. cetyl alcohol  Glycerol monostearate  Lanolin  Glycerin  Zinc stearate  opacifying agent.. Stearyl alcohol.. Microstructural properties of creams  texture and consistency is determined by the phase behaviour of the component emulsifiers. dusting powder…. .

. terpenes. alcohols. disruption of skin barrier  Extraction of skin lipids with apolar solvents e. polyols. surfactants. esters. acetone  Physical stripping  Physically or chemically induced irritation . alkanes. cyclodextrins 2. amines/amides of fatty acids.g.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.

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

Types .

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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 µ 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 .

. softening of plastic containers by methyl salicylate ointment.? .visual.g.Hydrocortisone acetate pH Basic acidic Neutral Incompatibility  Formulation and packaging materials  E. Detection of Incompatibility  Cracked cream  Hydrolysis or oxidation  Discoloration  Precipitation ….

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. Chlorhexidine salts 3. Cationic compounds 1. Acridines 5. Dequalinium salts 4. Neomycin sulphate . Triphenylmethane dyes 6. Tertiary ammonium compounds  Cetrimide  Cetylpyridinium chloride  Benzalkonium salts  Domiphen bromide 2.

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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