Formulation of Cream and Ointment

Formulation of Cream and Ointment

Cream Formulation 1 KA U S A R A H M A D KU L L I Y YA H O F P H A R M A C Y http://staff.iium.edu.my/akausar PHM4153 Dosage Design 2 2011/12 Contents 2 Ideal formulati on PHM4153 Dosage Design 2 2011/12

Types of excipient s Propertie s Examples of Creams 3 Whitenin g Benzophenone, hydroquinone Fruit extracts

Antiageing Collagen, seaweed extract Liposome Virility Fish Herbs PHM4153 Dosage Design 2 2011/12 Formulation 4 Process whereby drugs are combined

with other substances (excipients) e.g. preservative to produce dosage forms e.g. cream suitable for administration to or by patients. PHM4153 Dosage Design 2 2011/12 Ideal formulation 5 Non-irritant Nonallergenic

Non-staining Easy to apply Pleasant feeling to the skin Non-toxic Non-harmful Incapable of microorganis m growth Free from

side-effects PHM4153 Dosage Design 2 2011/12 Formulation requirement: efficacy, safety, and quality 6 Contain accurate dose Convenient to take or administer Retain quality throughout

shelf life & usage period PHM4153 Dosage Design 2 2011/12 Provide drug in a form for absorption or other delivery to the target Manufactured by a process that does not compromise performance and that is reproducible and economical

Factors to be considered in formulation 7 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 PHM4153 Dosage Design 2 2011/12 Choice of vehicle 8

Bases from mixtures of low and high MW PEG Liposomes Multiple emulsions PHM4153 Dosage Design 2 2011/12 Microemulsio ns Fluorocarbon emulsions

ultra low i Examples of Oils & Fats 9 Silicones Triglyceride s/ vege oils Simple esters PHM4153 Dosage Design 2 2011/12 Cyclomethicones Dimethicones Castor oil Glyceryl tricaprylate Octyl stearate

Isopropyl palmitate Advantages of Silicones 10 Chemical and physical stable, colourless, odourless Cosmetic Skin-feel, gloss/matte Dermo-toxicology Not sensitizing, non-comedogenic, PHM4153 Dosage Design 2 2011/12 Examples of Lipids 11

Hydrocarbon Mineral oil s Wax Ether Alcohols Acids PHM4153 Dosage Design 2 2011/12 Beeswax Dicaprilyl ether Cetyl alcohol Stearic acid Choosing Oils

12 Properties Limitation Emollient effect Shine Odour Lubricity Viscosity Spreadability

Miscibility with Solvency other oils Toxicity Impurities Cost Drying PHM4153 Dosage Design 2 2011/12 Colour Polarity of oils 13

Non-polar Polar Lasting emollient Varying emollient effect Barrier effect Inert Stable against oxidation Shine Spreadability cheap

PHM4153 Dosage Design 2 2011/12 effect Little barrier effect Varying stability against oxidation Good absorption Good delivery expensive Excipients 14 Other components other than API added to formulation PHM4153 Dosage Design 2 2011/12

Categories of excipients 15 Provide essential parts of dosage form & enhance bioavailability Emulsifiers Viscosity modifier Prevent degradation of the formulation: protect, improve safety & enhance stability Anti-oxidants Anti-bacterials Preservatives UV absorbers Aid processing during manufacturing Assist product identification colour PHM4153 Dosage Design 2 2011/12

Choosing excipients 16 physiological inertness commercially available at low cost physical and chemical stability absence of pathogenic microbial organisms

conformance to regulatory agency requirements no interference with drug bioavailability PHM4153 Dosage Design 2 2011/12 Emulsifiers 17 w/o o/w PHM4153 Dosage Design 2 2011/12

Penetration enhancers 18 Increase delivery of active substance by: Disturb packing of SC lipid bilayer Examples: surfactants Disruption of skin barrier Extraction of skin lipids with apolar solvents e.g. acetone Physical stripping Physically or chemically induced irritation PHM4153 Dosage Design 2 2011/12 Hydration

19 Hygroscopic effect NaCl Sorbitol PPG glycerol PHM4153 Dosage Design 2 2011/12 Alter waterbinding capacity of corneocytes Low MW glycerol s

Q. How does urea moisturise the skin? 20 PHM4153 Dosage Design 2 2011/12 21 PHM4153 Dosage Design 2 2011/12 pH adjustment 22 Triethanolamine NaoH PHM4153 Dosage Design 2 2011/12

Preservatives 23 Sodium methyl/butyl/propyl paraben Imidazolidinyl urea PHM4153 Dosage Design 2 2011/12 Anti-oxidant 24 Butyl hydroxy toluene Butyl hydroxy anisole

PHM4153 Dosage Design 2 2011/12 UV filters 25 Zinc oxide Titanium dioxide Benzophenone PHM4153 Dosage Design 2 2011/12 Other types of excipients 26 Soothing Allantoin Anti-free radicals

Polyphenols PHM4153 Dosage Design 2 2011/12 Effects of excipients 27 texture and consistency phase behaviour of the component emulsifiers. PHM4153 Dosage Design 2 2011/12 physicochemical properties

rheological, thermal and microscopical Physicochemical properties 28 Oils susceptible to oxidation Add antioxidants E.g. BHT, BHA PHM4153 Dosage Design 2 2011/12 Aqueous solutions support microbial

growth Add preservatives E.g. methyl and propyl paraben BUT these may affect the endocrine.. Physical and chemical properties of excipients 29 solubility hygroscopici

ty swelling hydration capacity particle size distribution bulk & tap density specific surface area complexatio

n infrared spectrum microbes PHM4153 Dosage Design 2 2011/12 Polyamide: Carrier for insoluble ingredients; Protector for sensitive ingredients; Slow delivery & long lasting effect 30 7 m, empty spheres 10 m, porous

PHM4153 Dosage Design 2 2011/12 Excipient: Particle size distribution 31 PHM4153 Dosage Design 2 2011/12 Excipient: Pore volume & pore diameter 32 PHM4153 Dosage Design 2 2011/12 Incompatibility 33 Chemical

Physical pH/ dissociation Immiscibility pH/disperse systems Insolubility polyvalent cations complexation cationic and anionic compounds of high MW reducing agents (cause

fading of dyes) PHM4153 Dosage Design 2 2011/12 Packaging Formulation and packaging materials Detection of Incompatibility 34 PHM4153 Dosage Design 2 2011/12 Cracked cream Hydrolysis

or oxidation Discolorati on Precipitati on Effect of type of preparation: Absorption of retinyl palmitate 35 Exercise: 18% absorbed from acetone vehicle compared to only 4% absorbed from o/w emulsion

Q WHY? PHM4153 Dosage Design 2 2011/12 Exercise: Determine functions of excipients 36 Nizoral cream Ketoconazole PPG Stearyl alcohol Cetyl alcohol Sorbitan stearate Polysorbate Isopropyl myristate Sodium sulfite Purified water

PHM4153 Dosage Design 2 2011/12 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

References 37 Bugay, D. E. (1999). Pharmaceutical excipients : characterization by IR, Raman, and NMR spectroscopy. RS201E87B931P Kibbe, A. H. (2000). Handbook of pharmaceutical excipients. RS201E87H236K Rowe, R. C., Sheskey, P. J. & Owen, S. C. (2006). Handbook of pharmaceutical excipients RS201E87H236K Rowe, R. C. (2009). Handbook of pharmaceutical excipients. RS201E87H236K PHM4153 Dosage Design 2 2011/12 38

Some materials sourced from the following: http://www.eastman.com/Markets/Pharmaceutical/Excipients/Excipients_in tro.asp http://www.pharmaceutical-technology.com/contractors/materials/uniqema/ http://www.pformulate.com/ http://images.vertmarkets.com/CRLive/files/Downloads/89FB7970-7376-44 A0-B6B6-4B171E4B978B/InsolubleKollidon.pdf Thank you to contributors. PHM4153 Dosage Design 2 2011/12

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