Name: Pharmaceutical Dosage Chapter 10: Ointments, Creams, and Gels Ointments, Creams, and Gels

y y y y

Semisolid dosage forms for topical application Applied to the: skin, surface of the eye, nasally, vaginally or rectally Used for therapeutic effects of the agents they contain (emollients, protective barriers , and vehicles)

Topical Dermatological Products

y y y

Drugs delivered into the skin for treatment of dermal disorder For local effects Skin as the target organ

Transdermal Products
y y y

Drugs delivered through the skin absorption) to the general circulation For systemic effects Skin not the target organ

(percutaneous

Do not permit the escape of moisture of the skin to the atmosphere  Difficult to wash: act as occlusive dressing  They do not change noticeably upon aging Levigating agent: liquid petrolatum when powdered substance is incorporated into HC bases  Petrolatum, USP (yellow petrolatum and petroleum jelly)  Purified mixture of semisolid HCs obtained from petroleum  Product: Vaseline (ChesebroughPonds)  White Petrolatum, USP (white petrolatum jelly)  Wholly or nearly decolorized purified mixture of semisolid HCs from petrolatum  Uses: diaper rash, dry skin  Commercial product: White Vaseline (Chesebrough-Ponds)  Yellow Ointment, USP (simple ointment)  Purified wax obtained from the honeycomb of the bee Apis mellifera  Has slightly greater viscosity than plain petrolatum  White Ointment  Consists of white wax and white petrolatum


Ointments
y

Absorption Bases
y

Semisolid preparations for external application to the skin or mucous membranes

Types of Ointments
y

Medicated  For treatments of cutaneous ( skin disease)  For both local and systemic effects  Systemic drug absorption considered since drugs:  Enter the fetal blood supply  Breast milk can be transferred to the fetus or nursing mother  Examples: Sulfur Ointment, Zinc Oxide Ointment and Compound Resorcinol Non-medicated  Referred to as ointment bases  Use as for their physical effects: protectant, emollient or lubricating effect or use as vehicles in medicated ointments  Example: White Ointment

Ointment Bases
y

Used for medicated ointments:  Physical effects  Vehicles Four general groups:  Oleaginous bases  Absorption bases  Water-removable bases  Water-soluble bases

2 types those that:  Permit the incorporation of aqueous solutions resulting in the formation of water in oil emulsions  Examples: hydrophilic petrolatum and anhydrous lanolin  Water in oil emulsions that permit the incorporation of additional quantities of aqueous solutions  Examples: lanolin (as emollient) and cold cream Characteristics  Not easily removed from the skin with water washing  May possess some power of penetration into the deepest layers of the skin  Therefore are used for endodermic ointment Uses  As emollient but do not provide the degree of occlusion  Incorporates aqueous solutions into oleaginous bases

Types of Absorption Bases

y

Oleaginous or Hydrocarbon Bases

y y y y

Uses: emollient effect  Effective as occlusive dressing Remain on the skin for long periods without drying out Immiscibility with water (difficult to wash off) Characteristics  Retained on the skin for prolong period of time

Hydrophilic petrolatum  Composed of stearyl alcohol, white wax, cholesterol, and white petrolatum  Characteristics: ability to absorb water with the formation of water in oil emulsion  Commercial product: aquaphor (variation of hydrophillic petrolatum) Anhydrous lanolin, USP  May contain no more than 0.25% water  Characteristics:  Insoluble in water but mixes without separation with about two times its weight in water

incorporation of water results in the formation of a water in oil emulsion  Synonym: refined wool fat Lanolin, USP  Obtained from wool of sheep (Ovis aries)  Purified wax-like substance: cleaned, deodorized, and decolorized  Processed to reduce contents of free lanolin alcohols, any detergent and pesticide residues  Characteristics: o Water in oil emulsion that contains between 25% to 30% water o Additional water may be incorporated by mixing  Synonym: hydrous wool fat Cold cream, USP  Semisolid white water in oil emulsion prepared with cetyl esters wax, white wax, mineral oil, sodium borate, and purified water  Uses: emollient and base  Examples: Eucerin cream: a water in oil emulsion of petrolatum, mineral oil, mineral wax, wool wax, alcohol and bronopol o

     

Desirability of occlusion of moisture from the skin Stability of the drug in the ointment base Effect if any of the drug on the consistency or other features of the ointment base Desire for a base that is easily removed by washing off water Characteristic of the surface to which it is applied Selected: base that provides the best combination of the most desired attributes

Preparation of Ointments: y Incorporation y Fusion Incorporation

y y

Components mixed until a uniform preparation is attained On a small scale (extemporaneous compounding): components mixed using a mortar and pestle or spatula to rub the ingredients together on an ointment slab Non-absorbent parchment paper used to cover the working surface

Water-Removable Bases (Water Washable Bases) Oil in water emulsion resembling creams Aqueous external phase Easily washed from skin Can absorb serous discharges Characteristics:  Resemble creams in their appearance  May be diluted with water or with aqueous solution  Can absorb serous discharges  Certain medicinal agents may be better absorbed in the skin Types of Water-Removable Bases (Water Washable Bases)
y y y y y y

Incorporation of Solid y The particle size of a powder or crystalline material is reduced before incorporation into the ointment base for the final product not to be gritty y Done by levigating (mineral oil) or mixing the solid material in a vehicle in which it is insoluble to make a smooth dispersion Incorporation of Liquids y Small amounts of an aqueous solution may be incorporated into an oleaginous ointment y Bases, even if hydrophilic have limits to retain liqu ids, beyond: become too soft and semiliquid y Alcohol solution (small volume) ma y be added easily to oleaginous vehicle or emulsion bases y Large scale: roller mills force coarsely formed ointments through stainless steel rollers to produce ointments that are uniform in composition and smooth in texture y Small ointment mills: used also in product development laboratories and in small batch manufacture Ointment Roller Mill y Suitable for grinding ointment, paste, paints, printers ink, etc. in the pharmaceutical p lastic industry y The machine is conducted on a closed sheet iron base, with in-built foot mounting, for floor positioning Fusion Method y All or some of the components of an ointment are combined by being meted together and cooled with constant stirring until congealed y The heat labile substances and volatile constituents are added last when temperature is low enough not to cause decomposition y Carried out:  Small scale: porcelain dish or glass beaker  Large scale: large steam-jacketed kettle y Prepared by fusion:  Medicated ointments and ointment bases (with beeswax, paraffin, stearyl alcohol, and high molecular weight PEG)  Preparation of ointments with an emulsion base: manufacturing involves melting and emulsification

Hydrophilic ointment  Sodium lauryl sulfate (emulsifying agent)  Stearyl alcohol and white petrolatum (oleaginous phase of the emulsion)  Methylparaben and propylparaben (antimicrobial preservatives)  USE: employed as water removable vehicle for medicinal substances

Water-Soluble Bases y Do not contain oleaginous components y Water washable, referred to as greaseless y Soften greatly with water, large amount of aqueous solutions not effectively incorporated y Used for incorporation of solid substances y Polyethylene Glycol Ointment  Polymer of ethylene oxide and water  Combining PEG 3350 (solid) with PEG 400 (liquid), results in a very pliable semisolid ointment Selection of the Appropriate Base y Selection for use in the formulation of an ointment depends on a number of factors:  Desired released rate of the drug substance from the ointment base  Desirability of topical or percut aneous drug absorption

Stainless Steel Tank y Creams and ointments in batch sizes up t o 1500 kilos are manufactured in stainless steel tanks. Compendial Requirements (USP Tests) for Ointments
y

Microbial content  Topical applications are not required to be sterile (except ophthalmic preparations)  Strict adherence to environment control and application of good manufacturing practices: to minimize the microorganisms in unstrerilized pharmaceutical products  Antimicrobial preservatives in topical preparations: methylparaben, propylparaben, phenols, benzoic acid, sorbic acid amd quarternary ammonium salts  Must meet the requirements of the test for absence of Stap. Aureus and Pseudomonas aeruginosa  For rectal, urethral, vaginal use: tested for yeast and molds Minimum fill  Determination of the net weight or volume of the contents of containers: to ensure proper contents compared with labeled amount Packaging, storage and labeling  Packaging:  Ointments and other semisolid preparation: large-mouth ointment jars, metal or plastic tubes  Light-sensitive preparations: opaque of lightresistant containers  Storage  Well-closed containers to product contamination  Labeling (USP):  Include the type of base used

y y

Semisolid system consisting of small or large molecules in an aqueous liquid vehicle rendered jelly like by the addition of a gelling agent. Gelling agent used:  Synthetic  Macromolecules Sometimes called jellies Gelling agents: carbomer 934, cellulose derivat ives (carboxymethyl-cellulose) and natural gums (tragacanth)

Single-Phase Gels y Macromolecules uniformly distributed throughout a liquid y Example: Na CMC and tragacanth gel Two-Phase Systems y Gel mask consists of floccules of small distinct particles y Example: Milk of Magnesia (often referred as magma) Characteristics of Gels y Thickens on standing, forming a thixotrope, shaken before use to liquefy the gel and enable pouring y Remain fairly uniform upon standing and does not readily settle because of high degree of attraction between the dispersed phase and water medium y Aluminum hydroxide gel y Formulated to contain drug substance:  Solvents (alcohol and/or propylene)  Antimicrobial preservatives (methylparaben or chlorhexidine gluconate)  Stabilizers (edentate disodium) Uses of Gels y Lubricant for catheters y Bases for patch testing y Examples:  NaCl gel for electrocardiography  Floucinonide Gel for anti-inflammatory corticosteroid  Na Fluoride & Phosphoric acid gel dental care prophylactic  Tretionoin Gel for treatment of acne Gels and Magmas y Considered colloidal dispersion since they contain particles of colloidal dimensions Approriate Names (Colloidal Dispersion) y SOLS: term to designate a dispersion of solid in either a liquid, solid or gas dispersion medium  Prefix hydro: water as dispersion medium so called hydrosol  Prefix alco: alcohol as the dispersion medium so called alcosol  Aerosol: dispersion of solid or liquid in gaseous phase Preparation of Gels y By freshly precipitating the disperse phase upon reaching an inorganic agent, a gelatinous precipitate results y Example: Preparation of Al(OH)3 gel AlCl3 + Na2CO3 p NaHCO3  By direct hydrating the inorganic material in water Al2O3 + H2O p Al(OH) 3 y Examples: Aluminum Hydroxide Gel, Alugel, Amphogel, Ce-lu-gel, Cremalin, Hydroxal, Vanogel, Aluminum Phosphate Gel (Phosphagel): antacid Examples of Topical Gels y Erythromycin and Benzamycin

Additional Standards y USP requires manufacturer: examine semisolid preparation for viscosity and for in vitro drug release Creams y Semisolid preparations containing one or more medicinal agents dissolved y Dispersed either in W/O emulsion or O/W emulsion or in another type of water-washable base  Vanishing cream: O/W emulsions containing large percentages of water and stearic acid or other oleaginous components  Primary application:  Topical skin products used rectally and vaginally  Easier to spread and remove, preferred than ointments Examples of Ointments and Creams y Anesthetics  Benzocain: various  Dibucaine: Nupercainal cream and ointment y Astringent or protectant  Zinc oxide: various y Depigmenting agents  Hydroquinone cream: Eldoopaque cream y Scabicides  Lindane: Kweel cream y Sunscreen agent  Dioxybenzone: Solvar cream and oxybenzone Gels

benzoyl peroxide

topical

gel:

y y y y y

Clindamycin topical gel: Cleocin T Topical Gel Benzoyl peroxide gel: Desquam-X 10 Gel-acne vulgaris Hydroquinone gel: Solaquin Forte Gel: bleach for hyperpigmented skin Salicylic acid gel: Compound W Gel: keratolytic Desoximetasone gel: Topicort: anti-Inflammatory, antipruritic agent

Examples: Cantharides cerates, rosin cerate, camphor cerate, cerate of lead acetate, compound rosin cerate

Miscellaneous Semi-solid Preparation y Pastes y Plasters y Glycerogelatins Pastes y

y y y

Cataplasm y Viscous preparation intended for warm, external application to a body for purpose of reducing inflammation y Soft semisolid, external applications which either stimulate a body surface or alleviate an inflamed area by supplying medication substance in the presence of heat and mixture. y Example: numotizine Cements y Dental preparation employed primarily as temporary coverings for exposed pulps and also for holding medicinal agents in tooth cavities and rebasing of dentures Glycerogelatins y Plastic masses containing 15% gelatin, 40% glycerin, 35% water and 10% added medicinal substance (zinc oxide) y For the long term application y For treatment of varicose ulcers y Official: zinc gelatin or zinc gelatin boot-form pressure bandage (treatment of varicose ulcers) Dressings y External application resembling ointments in consistency, but remaining semisolid at body temperature, they liquefy at 50C and remain pliable in thin films below 28C Classes of Dressing y Primary wound dressing or now as wet dressing y Absorbents: surgical cotton and gauze y Bandages y Adhesive tapes Examples of Dressings y Paraffin Dressing: formerly official in the NF VI and employed as an air-excluding, soft, pliable, analgesic, splint-like covering for surface denuded by burns y Petrolatum Gauze, USP: absorbent gauzr saturated with white petrolatum y Fruazone Gauza Pads-sterile: antibacterial dressings containing nitrofurazone y Surgical dressing: any material used as covering, protective, or support for a diseased part: (1) Adhesive bandages, USP; (2) Gauze bandage Other Examples of Dressings y Bandages y Paper tapes y Surgical tapes Packaging Semisolid Preparation y Topical dermatologic products  Packaged in either jars or tubes  Ophthalmic y Nasal, vaginal, and rectal semisolids products  Packaged in tubes  Aluminum or plastic y Ophthalmic ointments  Packaged in small aluminum or collapsible plastic tubes holding 3.5g y Tubes: sterilizes before aseptically filled, fitted with narrow-gauge

Semisolid preparation for application to the skin, for its stiffness and impenetrability Remain in place after application and effectively employed to absorb serous secretions Not suited for application to hairy parts of the body Example: zinc oxide paste (Lassars Plain Zinc Paste)

Types of Paste y Dermatologic paste y Paste for injection Examples of Paste 1. Zinc oxide paste with acid: Lassars Paste: Salicylic acid 20g and ZnO paste q.s. to make 1000g 2. Zinc oxide paste: ZnO 250g, starch 250g, white petrolatum 500g to make 1000g 3. Triamicinolone acetonide dental p aste Plasters y Solid or semisolid adhesive masses spread on a backing of paper, fabric, moleskin, or plastic  Nonmedicated plaster: for protection and mechanical support (Adhesive Plaster)  Medicated plaster: provide effects at the site of application (Salicylic acid plaster removal of corns on toes by the keratolytic action) Purposes of Plasters y To afford protection and mechanical support y To furnish an occlusive macerating action y To bring medication into close contact with surface of skin Example of Plaster y Modern plasters are practically all machine made and are available in colors such as flesh, striped, and others. Examples of Medicated Plasters y Salicylic acid plaster y Salonpas Back Plasters y Made of heavy cotton or wool and cotton backing to provide warmth and support y Used to backache, sore shoulder, sore arms, and other muscular aches y Active constituents of back plasters is oleoresins of capsicum y Examples: Chili Plaster, Hot Salonpas Cerates y Unctouse preparations of such consistency that may be easily spread at ordinary temperature upon muslin cloth or similar material with spatula yet not soft to liquefy and run when applied to the skin y Contents: oil, hard, petrolatum and beeswax

Plastic Tubes are made of: y High or low-density polyethylene (HDPE or LDPE) or a blend of each y Polypropylene (PP) y Polyethylene terephthalate (PET) y Various plastic, foil, and/paper laminates Special features and Advantages of Plastic y LPDE: soft and resilient with good moisture barrier y HPDE: with superior moisture barrier but less resilient y PP: has high level of heat resistance y PET: offers transparency and high degree of product chemical compatibility Laminates y With excellent moisture barrier because of the foil content, high durability, and product compatibility Ointment jars y Clear or opaque glass or plastics y Amber-colored, some are porcelain Filling Ointment Jars y Small scale pharmacy: weighted amount of ointment transferred into the jar with a spatula Filling and Crimping Machine y A small-scale fully automatic filling and crimping machine for collapsible metal tubes Tube-filling Machine y This machine automatically fills 125 tubes a minute with proper amount, tightens cap, and orients each tube by electric eye so that label faces forward then closes and crimps the end. Filling Ointment Tubes y Tubes filled from the open back end of the tube opposite from the cap end y Manual filling of ointment t ube requires:  Prepare ointment on a wax or parchment: paper rolled into a cylindrical shape, inserted into the open end of the tube, pushed forward  The spatula pressing against the lower portion of the tube and making a crease below the ointment full, the paper is slowly remove leaving the ointment in the tube  The bottom of the tube is flattened, folded and sealed with a crimping tool or clip Features and Use Dermatologic Preparations y Drug penetration into the skin depends on a number of factors:  Physiochemical properties of the medicinal substance  Characteristics of the pharmaceutical vehicle  Condition of the skin itself  Oleaginous bases  Greater occlusion and emollient effects than hydrophilic or water-washable bases  Pastes  Greater occlusion and more effective than ointments at absorbing serous discharge  Creams  O/W emulsions, spread more easily than ointments and are easier to remove  Water-soluble bases  Non-greasy and are easily removed Features and Uses of Ophthalmic Ointments and Gels

y y y

Ophthalmic ointments must meet the:  USP sterility tests  Test for metal particles in ophthalmic ointments Steam sterilization or ethylene oxide methods: not capable of penetrating the ointment Dry heat sterilization: can penetrate the ointment base, the high heat may pose a threat to the stability of the drug Antimicrobial preservatives: methylparaben, prophylparaben, combination of phenylmercuric acetate, chlorobutanol, benzalkonium chloride Strict methods of aseptic processing: drug and non-drug component is rendered sterile, aseptically weighed and incorporated in a final product

Features and Use of Nasal Ointment and Gels y Introduce into the nasal passage for local effects on the mucous membrane and underlying tissues y Nasal route of administration: also for the systemic absorption of the numbers of drugs:  Butorphanol tartrate (Stadol NS, Bristol Myers, Squibb)  An analgesic  Cyanocobalamine (Nascobat gel, Schwartz)  A hematopoietic  Narfaralin acetate (Synarel, Searle)  For txt of endometriosis  Nicotine (Nicotrol NS, McNeil)  As an adjunct in smoking sensation Features and Use of Rectal Preparation y For anorectal conditions: ointments, gels, creams, and creamlike aerosol foams, solutions (for enema and irrigation) and suppositories y Local condition of anorectal pruritus: inflammation, pain and discomfort associated with hemorrhoids y Example:  Prochlorperazine as suppositories  Zinc oxide y Bases used in anorectal ointments and creams  Combinations of polyethylene glycol 300 and 3350  Emulsion cream bases using cetyl esters wax, and butylated hydroxyanisole (BHA) Features and Use of Vaginal Preparations y Treatment of Conditons and Disease of the vulvovaginal area: ointments, creams, cream-like foams, and gels  Topical product to treat:  Vulvovaginal infection, vaginitis, conditions of endometrial atrophy and for contraception with spermatocidal agents.  Pathogenic organisms: o Trichomonas vaginalis o Candida (Monilia) albicans o Hemophilus vaginalis  Anti-infective agents are: nystatin, chlotrimazole, miconazole, clindamycin, and sulfonamides  Endometrial atrophy treated locally with: hormones dienestrol and progesterone  Contraceptive preparations contained spermicidal agents such as: nonoxynol-9 and octoxynol with cervical diaphragm  Vaginal gels are preserved with antimicrobial agents: E.g. Vulva (Mycelex-7 Vaginal Cream, Bayer)

Table 10.1: Dermatologic Ointments and Creams by Therapeutic Category y Preparation  Adrenocortical steroids  Aclometasone dipropionate cream and ointment o Corresponding commercial product: Aclovate Cream and Ointment (GlaxoSmithKline) o Usual strength of active ingred ient: 0.05% cream and ointment o Use: relief of inflammatory dermatoses  Fluocinolone acetonide cream and ointment o Corresponding commercial product: Synalar Cream and Ointment (Roche) o Usual strength of active ingredient: 0.025% cream and ointment o Use: relief of inflammatory dermatoses  Hydrocortisone acetate cream and ointment o Corresponding commercial product: Cortaid Cream and Ointment (Pharmacia & Upjohn) o Usual strength of active ingredient: 0.5% and 1% o Use: relief of inflammatory dermatoses  Triamcinolone acetonide cream and ointment o Corresponding commercial product: Aristocort A Cream and Ointment (Fujisawa) o Usual strength of active: 0.01% ointment; 0.1%, 0.025%, 0.5% cream o Use: relief of inflammatory dermatoses  Adrenocorticoid - antifungal combination  Betamethasone, clotrimazole cream o Corresponding commercial product: Lotrisone Cream (Schering-Plough) o Usual strength of active ingredient: 1% betamethasone, 0.05% clotrimazole o Use: relief, treatment of inflammatory pruritic manifestations that may be complicated by fungal overgrowth  Analgesic  Capsaicin cream o Corresponding commercial product: Zostrix Cream (Medicis) o Usual strength of active ingredient: 0.025% o Use: relief of arthritic pain  Antiacne  Tretinoin cream o Corresponding commercial product: Retin-A (Ortho McNeil) o Strength: 0.025%, 0.05%, 0.1% o Usual strength of active ingredient: derivative of Vitamin A for topical treatment of acne vulgaris  Antianginal  Nitroglycerin ointment o Corresponding commercial product: Nitro-Bid Ointment (Hoechst Marion Roussel)

Usual strength of active ingredient: 2% o Use: reduces workload of heart by smooth muscle relaxation of peripheral arteries and veins Antibacterial or anti-infectives  Gentamicin sulfate cream, ointment o Corresponding commercial product: Garamycin Cream and Ointment (Schering-Plough) o Usual strength of active ingredient: 0.1% o Use: local treatment of skin infections by susceptible microorganisms  Nystatin cream o Corresponding commercial product: Mycostatin Cream (Apothecon) o Usual strength of active ingredient: 0.5% 100,000 U/g o Use: local treatment of skin infections by susceptible microorganisms  Polymyxin B sulfate, bacitracin zinc, neomycin ointment o Corresponding commercial product: Neosporin Ointment (GlaxoSmithKline) o Usual strength of active ingredient: 5,000 U/g polymyxin B, 400 U/g bacitracin zinc; 3.5 mg/g neomycin o Use: treatment of minor cuts, scrapes Antifungals  Miconazole nitrate cream o Corresponding commercial product: Monistat-Derm Cream (Ortho McNeil) o Usual strength of active ingredient: 2% o Use: cutaneous candidiasis, tinea infections of Trichophyton spp.  Tolnaftate cream o Corresponding commercial product: Tinactin Cream (Schering-Plough) o Usual strength of active ingredient: 1% o Use: topical treatment of tinea pedis, tinea corporis, tinea manuum Antineoplastic  Fluorouracil cream o Corresponding commercial product: Efudex Cream (Roche) o Usual strength of active ingredient: 5% o Use: treatment of multiple actinic, solar keratoses Antipruritic, analgesic  Lidocaine ointment o Corresponding commercial product: Xylocaine Ointment (Astra) o Strength: 2.5% o Use: relief of pain, itching of minor skin irritation, insect bites Astringent, protectant  Zinc oxide ointment o Corresponding commercial product: Desitin Ointment (Pfizer) o Usual strength of active ingredient: 40% o Use: topical astringent, protective in skin conditions such as diaper rash o

Depigmenting agents  Hydroquinone cream o Corresponding commercial product: Eldopaque Cream (ICN) o Usual strength of active ingredient: 4% o Use: temporary bleaching of skin with freckles, old age spots, chloasma

Scabicide  Crotamiton cream o Corresponding commercial product: Eurax Cream (Westwood-Squibb) o Usual strength of active ingredient: 10% o Use: eradication of scabies, symptomatic treatment of pruritus

Table 10.2: Examples of Topical Gels Active Ingredient Acetic acid Becaplermin

Proprietary Product Aci-Jel (Ortho McNeil) Regranex Gel (Ortho McNeil)

Gelling Agent Tragacanth, acacia Sodium, CMC

Benzoyl peroxide Clindamycin

Desquam-X Gel (WestwoodSquibb) Cleocin T Topical Gel (Pharmacia & Upjohn) Temovate Gel (GlaxoSmithKline) Nascobal (Schwartz Pharma) Topicort Gel (Medicis Dermatologics) Metro-Gel Vaginal (Galderma) Condylox Gel (Oclassen) Crinone Gel (Serono)

Carbomer 940 Carbomer 934P

Route and Use Vaginal; restoration and maintenance of acidity Dermatologic; recombinant human platelet-derived growth factor; promotes healing of diabetic ulcers of lower extremity Dermatologic; acne vulgaris Dermatologic; acne vulgaris

Clobetasol propionate Cyanocobalamin Desoximetasone Metronidazole Podofilox Progesterone

Carbomer 934P Methylcellulose Carbomer 940 Carbomer 934P Hydroxypropyl cellulose Carbomer 934P

Dermatologic; antipruritic Nasal; hematologic Dermatologic; anti-inflammatory, antipruritic Vaginal; bacterial vaginosis Rectal; anogenital warts Vaginal; bioadhesive gel for progesterone supplementation and replacement Opthalmic gel-forming solution used in treatment of elevated intraocular pressure Dermatologic; acne vulgaris

Timolol maleate

Timoptic-XE (Merck)

Gelrite gellan gum

Tretinoin o o

Retin-A Gel (Ortho McNeil)

Hydroxypropyl cellulose

Table 10.3: Examples of Ophthalmic Ointments Commercial Product Chloramphenicol ophthalmic Chloromycetin Opthalmic Ointment (Parke-Davis) Dexamethasone sodium phosphate ophthalmic Gentamicin sulfate ophthalmic Decadron Phosphate Opthalmic Ointment (Merck) Garamycin Opthalmic Ointment (Schering-Plough) Floropryl Sterile Opthalmic Ointment (Merck) Polysporin Opthalmic Ointment (Monarch) Neosporin Opthalmic Ointment (Monarch)

Active Ingredient 1%

Category Antibacterial, antibiotic

0.05%

Anti-inflammatory, adrenocortical steroid Antibacterial, antibiotic

0.3%

Isoflurophate ophthalmic

0.025%

Cholinesterase inhibitor

Polymyxin B-bacitracin ophthalmic Polymyxin B-bacitracinneomycin ophthalmic

Per gram: polymyxin B sulfate, 10,000 U; bacitracin zinc, 500 U Per gram: polymyxin B sulfate, 5,000 U; bacitracin zinc, 400 U; neomycin sulfate, 5 mg 10%, 30%

Antimicrobial

Antimicrobial

Sulfacetamide sodium ophthalmic

Sodium Sulamyd Opthalmic Ointment (Schering-Plough) Tobrex Opthalmic Ointment (Alcon) Vira-A Opthalmic Ointment

Antibacterial

Tobramycin ophthalmic

0.3%

Antibacterial, antibiotic

Vidarabine ophthalmic

3%

Antiviral

(Monarch) o o

Table 10.4: Examples of Rectal and Vaginal Creams and Ointments Active Ingredient Product Type Starch Pramoxine HCl Ointment Cream

Primary Use Hemorrhoid treatment Hemorrhoidal, analgesic, antipruritic Antifungal Vulvovaginitis (Candida albicans) Bacterial vaginosis Antifungal (Candida albicans) Estrogenic for vulvar, vaginal atrophy Atrophic vaginitis, kraurosis vulvae

Rectal Anusol (GlaxoSmithKline) Tronolane (Ross) Vaginal Mycelex-7 (Bayer) AVC (Novavax)

Clotrimazole Sulfanilamide

Cream Cream

Cleocin (Pharmacia & Upjohn) Terazol 7 (Ortho McNeil) Ogen (Pharmacia & Upjohn) Premarin (Wyeth-Ayerst)

Clindamycin PO4 Terconazole Estropipate Conjugated estrogens

Cream Cream Cream Cream