Professional Documents
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Insoluble in water but mixes Desirability of topical or percutaneous drug
without separation with about absorption
two times its weight in water Desirability of occlusion of moisture from the
o incorporation of water results in skin
the formation of a water in oil Stability of the drug in the ointment base
emulsion Effect if any of the drug on the consistency or
Synonym: refined wool fat other features of the ointment base
Lanolin, USP Desire for a base that is easily removed by
Obtained from wool of sheep (Ovis aries) washing off water
Purified wax-like substance: cleaned, Characteristic of the surface to which it is applied
deodorized, and decolorized Selected: base that provides the best combination
Processed to reduce contents of free lanolin of the most desired attributes
alcohols, any detergent and pesticide residues
Characteristics: Preparation of Ointments:
o Water in oil emulsion that Incorporation
contains between 25% to 30% Fusion
water
o Additional water may be Incorporation
incorporated by mixing
Synonym: hydrous wool fat Components mixed until a uniform preparation is
Cold cream, USP attained
Semisolid white water in oil emulsion prepared On a small scale (extemporaneous compounding):
with cetyl esters wax, white wax, mineral oil, components mixed using a mortar and pestle or spatula
sodium borate, and purified water to rub the ingredients together on an ointment slab
Uses: emollient and base Non-absorbent parchment paper used to cover the
Examples: Eucerin cream: a water in oil working surface
emulsion of petrolatum, mineral oil, mineral
wax, wool wax, alcohol and bronopol Incorporation of Solid
The particle size of a powder or crystalline material is
Water-Removable Bases (Water Washable Bases) reduced before incorporation into the ointment base for
the final product not to be gritty
Oil in water emulsion resembling creams Done by levigating (mineral oil) or mixing the solid
Aqueous external phase material in a vehicle in which it is insoluble to make a
Easily washed from skin smooth dispersion
Can absorb serous discharges
Characteristics: Incorporation of Liquids
Resemble creams in their appearance Small amounts of an aqueous solution may be
May be diluted with water or with aqueous incorporated into an oleaginous ointment
solution Bases, even if hydrophilic have limits to retain liquids,
Can absorb serous discharges beyond: become too soft and semiliquid
Certain medicinal agents may be better absorbed Alcohol solution (small volume) may be added easily to
in the skin oleaginous vehicle or emulsion bases
Types of Water-Removable Bases (Water Washable Bases) Large scale: roller mills force coarsely formed ointments
through stainless steel rollers to produce ointments that
Hydrophilic ointment are uniform in composition and smooth in texture
Sodium lauryl sulfate (emulsifying agent) Small ointment mills: used also in product development
Stearyl alcohol and white petrolatum (oleaginous laboratories and in small batch manufacture
phase of the emulsion)
Methylparaben and propylparaben (antimicrobial Ointment Roller Mill
preservatives) Suitable for grinding ointment, paste, paints, printer’s
USE: employed as water removable vehicle for ink, etc. in the pharmaceutical plastic industry
medicinal substances The machine is conducted on a closed sheet iron base,
with in-built foot mounting, for floor positioning
Water-Soluble Bases
Do not contain oleaginous components Fusion Method
Water washable, referred to as greaseless All or some of the components of an ointment are
Soften greatly with water, large amount of aqueous combined by being meted together and cooled with
solutions not effectively incorporated constant stirring until congealed
Used for incorporation of solid substances The heat labile substances and volatile constituents are
Polyethylene Glycol Ointment added last when temperature is low enough not to cause
Polymer of ethylene oxide and water decomposition
Combining PEG 3350 (solid) with PEG 400 Carried out:
(liquid), results in a very pliable semisolid Small scale: porcelain dish or glass beaker
ointment Large scale: large steam-jacketed kettle
Prepared by fusion:
Selection of the Appropriate Base Medicated ointments and ointment bases (with
Selection for use in the beeswax, paraffin, stearyl alcohol, and high
formulation of an ointment depends on a number of factors: molecular weight PEG)
Desired released rate of the drug substance from
the ointment base
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Preparation of ointments with an emulsion Lindane: Kweel cream
base: manufacturing involves melting and Sunscreen agent
emulsification Dioxybenzone: Solvar cream and oxybenzone
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Examples: Aluminum Hydroxide Gel, Alugel, Examples: Chili Plaster, Hot Salonpas
Amphogel, Ce-lu-gel, Cremalin, Hydroxal, Vanogel, Cerates
Aluminum Phosphate Gel (Phosphagel): antacid Unctouse preparations of such consistency that may be
easily spread at ordinary temperature upon muslin cloth
Examples of Topical Gels or similar material with spatula yet not soft to liquefy and
Erythromycin and benzoyl peroxide topical gel: run when applied to the skin
Benzamycin Contents: oil, hard, petrolatum and beeswax
Clindamycin topical gel: Cleocin T Topical Gel Examples: Cantharides cerates, rosin cerate, camphor
Benzoyl peroxide gel: Desquam-X 10 Gel-acne vulgaris cerate, cerate of lead acetate, compound rosin cerate
Hydroquinone gel: Solaquin Forte Gel: bleach for
hyperpigmented skin Cataplasm
Salicylic acid gel: Compound W Gel: keratolytic Viscous preparation intended for warm, external
Desoximetasone gel: Topicort: anti-Inflammatory, application to a body for purpose of reducing
antipruritic agent inflammation
Soft semisolid, external applications which either
Miscellaneous Semi-solid Preparation stimulate a body surface or alleviate an inflamed area by
Pastes supplying medication substance in the presence of heat
Plasters and mixture.
Glycerogelatins Example: numotizine
Pastes Cements
Semisolid preparation for application to the skin, for its Dental preparation employed primarily as temporary
stiffness and impenetrability coverings for exposed pulps and also for holding
Remain in place after application and effectively medicinal agents in tooth cavities and rebasing of
employed to absorb serous secretions dentures
Not suited for application to hairy parts of the body
Example: zinc oxide paste (Lassar’s Plain Zinc Paste) Glycerogelatins
Plastic masses containing 15% gelatin, 40% glycerin,
Types of Paste 35% water and 10% added medicinal substance (zinc
Dermatologic paste oxide)
Paste for injection For the long term application
For treatment of varicose ulcers
Examples of Paste Official: zinc gelatin or zinc gelatin boot-form pressure
1. Zinc oxide paste with acid: Lassar’s Paste: Salicylic acid bandage (treatment of varicose ulcers)
20g and ZnO paste q.s. to make 1000g
2. Zinc oxide paste: ZnO 250g, starch 250g, white Dressings
petrolatum 500g to make 1000g External application resembling ointments in
3. Triamicinolone acetonide dental paste consistency, but remaining semisolid at body
temperature, they liquefy at 50°C and remain pliable in
Plasters thin films below 28°C
Solid or semisolid adhesive masses spread on a backing
of paper, fabric, moleskin, or plastic Classes of Dressing
Nonmedicated plaster: for protection and Primary wound dressing or now as wet dressing
mechanical support (Adhesive Plaster) Absorbents: surgical cotton and gauze
Medicated plaster: provide effects at the site of Bandages
application (Salicylic acid plaster – removal of Adhesive tapes
corns on toes by the keratolytic action)
Examples of Dressings
Purposes of Plasters Paraffin Dressing: formerly official in the NF VI and
To afford protection and mechanical support employed as an air-excluding, soft, pliable, analgesic,
To furnish an occlusive macerating action splint-like covering for surface denuded by burns
To bring medication into close contact with surface of Petrolatum Gauze, USP: absorbent gauzr saturated with
skin white petrolatum
Fruazone Gauza Pads-sterile: antibacterial dressings
Example of Plaster containing nitrofurazone
Modern plasters are practically all machine made and are Surgical dressing: any material used as covering,
available in colors such as flesh, striped, and others. protective, or support for a diseased part: (1) Adhesive
bandages, USP; (2) Gauze bandage
Examples of Medicated Plasters
Salicylic acid plaster Other Examples of Dressings
Salonpas Bandages
Paper tapes
Back Plasters Surgical tapes
Made of heavy cotton or wool and cotton backing to
provide warmth and support Packaging Semisolid Preparation
Used to backache, sore shoulder, sore arms, and other Topical dermatologic products
muscular aches Packaged in either jars or tubes
Active constituents of back plasters is oleoresins of Ophthalmic
capsicum Nasal, vaginal, and rectal semisolids products
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Packaged in tubes Greater occlusion and more effective than
Aluminum or plastic ointments at absorbing serous discharge
Ophthalmic ointments Creams
Packaged in small aluminum or collapsible O/W emulsions, spread more easily than
plastic tubes holding 3.5g ointments and are easier to remove
Tubes: sterilizes before aseptically filled, fitted with Water-soluble bases
narrow-gauge Non-greasy and are easily removed
Plastic Tubes are made of: Features and Uses of Ophthalmic Ointments and Gels
High or low-density polyethylene (HDPE or LDPE) or a Ophthalmic ointments must meet the:
blend of each USP sterility tests
Polypropylene (PP) Test for metal particles in ophthalmic
Polyethylene terephthalate (PET) ointments
Various plastic, foil, and/paper laminates Steam sterilization or ethylene oxide methods: not
capable of penetrating the ointment
Special features and Advantages of Plastic Dry heat sterilization: can penetrate the ointment base,
LPDE: soft and resilient with good moisture barrier the high heat may pose a threat to the stability of the drug
HPDE: with superior moisture barrier but less resilient Antimicrobial preservatives: methylparaben,
PP: has high level of heat resistance prophylparaben, combination of phenylmercuric acetate,
PET: offers transparency and high degree of product chlorobutanol, benzalkonium chloride
chemical compatibility Strict methods of aseptic processing: drug and non-drug
component is rendered sterile, aseptically weighed and
Laminates incorporated in a final product
With excellent moisture barrier because of the foil
content, high durability, and product compatibility Features and Use of Nasal Ointment and Gels
Introduce into the nasal passage for local effects on the
Ointment jars mucous membrane and underlying tissues
Clear or opaque glass or plastics Nasal route of administration: also for the systemic
Amber-colored, some are porcelain absorption of the numbers of drugs:
Butorphanol tartrate (Stadol NS, Bristol Myers,
Filling Ointment Jars Squibb)
An analgesic
Small scale pharmacy: weighted amount of ointment
Cyanocobalamine (Nascobat gel, Schwartz)
transferred into the jar with a spatula
A hematopoietic
Narfaralin acetate (Synarel, Searle)
Filling and Crimping Machine
For txt of endometriosis
A small-scale fully automatic filling and crimping
Nicotine (Nicotrol NS, McNeil)
machine for collapsible metal tubes
As an adjunct in smoking sensation
Tube-filling Machine
Features and Use of Rectal Preparation
This machine automatically fills 125 tubes a minute with
For anorectal conditions: ointments, gels, creams, and
proper amount, tightens cap, and orients each tube by
creamlike aerosol foams, solutions (for enema and
electric eye so that label faces forward then closes and
irrigation) and suppositories
crimps the end.
Local condition of anorectal pruritus: inflammation, pain
and discomfort associated with hemorrhoids
Filling Ointment Tubes
Example:
Tubes filled from the open back end of the tube opposite
Prochlorperazine as suppositories
from the cap end
Zinc oxide
Manual filling of ointment tube requires:
Bases used in anorectal ointments and creams
Prepare ointment on a wax or parchment: paper
Combinations of polyethylene glycol 300 and
rolled into a cylindrical shape, inserted into the open
3350
end of the tube, pushed forward
Emulsion cream bases using cetyl esters wax,
The spatula pressing against the lower portion of the
and butylated hydroxyanisole (BHA)
tube and making a crease below the ointment full,
the paper is slowly remove leaving the ointment in
Features and Use of Vaginal Preparations
the tube
The bottom of the tube is flattened, folded and Treatment of Conditons and Disease of the vulvovaginal
sealed with a crimping tool or clip area: ointments, creams, cream-like foams, and gels
Topical product to treat:
Features and Use Dermatologic Preparations Vulvovaginal infection, vaginitis,
conditions of endometrial atrophy
Drug penetration into the skin depends on a number of
and for contraception with
factors:
spermatocidal agents.
Physiochemical properties of the medicinal
Pathogenic organisms:
substance
o Trichomonas vaginalis
Characteristics of the pharmaceutical vehicle
Condition of the skin itself o Candida (Monilia) albicans
Oleaginous bases o Hemophilus vaginalis
Greater occlusion and emollient effects than Anti-infective agents are: nystatin,
hydrophilic or water-washable bases chlotrimazole, miconazole, clindamycin, and
Pastes sulfonamides
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Endometrial atrophy treated locally with: o Corresponding commercial product:
hormones dienestrol and progesterone Retin-A (Ortho McNeil)
Contraceptive preparations contained o Strength: 0.025%, 0.05%, 0.1%
spermicidal agents such as: nonoxynol-9 and o Usual strength of active ingredient:
octoxynol with cervical diaphragm derivative of Vitamin A for topical
Vaginal gels are preserved with antimicrobial treatment of acne vulgaris
agents: E.g. Vulva (Mycelex-7 Vaginal Cream, Antianginal
Bayer) Nitroglycerin ointment
o Corresponding commercial product:
Table 10.1: Dermatologic Ointments and Creams by Therapeutic Nitro-Bid Ointment (Hoechst Marion
Category Roussel)
Preparation o Usual strength of active ingredient:
Adrenocortical steroids 2%
Aclometasone dipropionate cream and o Use: reduces workload of heart by
ointment smooth muscle relaxation of
o Corresponding commercial product: peripheral arteries and veins
Aclovate Cream and Ointment Antibacterial or anti-infectives
(GlaxoSmithKline) Gentamicin sulfate cream, ointment
o Usual strength of active ingredient: o Corresponding commercial product:
0.05% cream and ointment Garamycin Cream and Ointment
o Use: relief of inflammatory (Schering-Plough)
dermatoses o Usual strength of active ingredient:
Fluocinolone acetonide cream and 0.1%
ointment o Use: local treatment of skin
o Corresponding commercial product: infections by susceptible
Synalar Cream and Ointment microorganisms
(Roche) Nystatin cream
o Usual strength of active ingredient: o Corresponding commercial product:
0.025% cream and ointment Mycostatin Cream (Apothecon)
o Use: relief of inflammatory o Usual strength of active ingredient:
dermatoses 0.5% 100,000 U/g
Hydrocortisone acetate cream and o Use: local treatment of skin
ointment infections by susceptible
o Corresponding commercial product: microorganisms
Cortaid Cream and Ointment Polymyxin B sulfate, bacitracin zinc,
(Pharmacia & Upjohn) neomycin ointment
o Usual strength of active ingredient: o Corresponding commercial product:
0.5% and 1% Neosporin Ointment
o Use: relief of inflammatory (GlaxoSmithKline)
dermatoses o Usual strength of active ingredient:
Triamcinolone acetonide cream and 5,000 U/g polymyxin B, 400 U/g
ointment bacitracin zinc; 3.5 mg/g neomycin
o Corresponding commercial product: o Use: treatment of minor cuts, scrapes
Aristocort A Cream and Ointment Antifungals
(Fujisawa) Miconazole nitrate cream
o Usual strength of active: 0.01% o Corresponding commercial product:
ointment; 0.1%, 0.025%, 0.5% cream Monistat-Derm Cream (Ortho
o Use: relief of inflammatory McNeil)
dermatoses o Usual strength of active ingredient:
Adrenocorticoid - antifungal combination 2%
Betamethasone, clotrimazole cream o Use: cutaneous candidiasis, tinea
o Corresponding commercial product: infections of Trichophyton spp.
Lotrisone Cream (Schering-Plough) Tolnaftate cream
o Usual strength of active ingredient: o Corresponding commercial product:
1% betamethasone, 0.05% Tinactin Cream (Schering-Plough)
clotrimazole o Usual strength of active ingredient:
o Use: relief, treatment of 1%
inflammatory pruritic manifestations o Use: topical treatment of tinea pedis,
that may be complicated by fungal tinea corporis, tinea manuum
overgrowth Antineoplastic
Analgesic Fluorouracil cream
Capsaicin cream o Corresponding commercial product:
o Corresponding commercial product: Efudex Cream (Roche)
Zostrix Cream (Medicis) o Usual strength of active ingredient:
o Usual strength of active ingredient:
5%
0.025% o Use: treatment of multiple actinic,
o Use: relief of arthritic pain solar keratoses
Antiacne Antipruritic, analgesic
Tretinoin cream Lidocaine ointment
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o Corresponding commercial product: o Corresponding commercial product:
Xylocaine Ointment (Astra) Eldopaque Cream (ICN)
o Strength: 2.5% o Usual strength of active ingredient:
o Use: relief of pain, itching of minor 4%
skin irritation, insect bites o Use: temporary bleaching of skin
Astringent, protectant with freckles, old age spots,
Zinc oxide ointment chloasma
o Corresponding commercial product: Scabicide
Desitin Ointment (Pfizer) Crotamiton cream
o Usual strength of active ingredient: o Corresponding commercial product:
40% Eurax Cream (Westwood-Squibb)
o Use: topical astringent, protective in o Usual strength of active ingredient:
skin conditions such as diaper rash 10%
Depigmenting agents o Use: eradication of scabies,
Hydroquinone cream symptomatic treatment of pruritus
Progesterone Crinone Gel (Serono) Carbomer 934P Vaginal; bioadhesive gel for
progesterone supplementation
and replacement
Timolol maleate Timoptic-XE (Merck) Gelrite gellan gum Opthalmic gel-forming solution
used in treatment of elevated
intraocular pressure
Tretinoin Retin-A Gel (Ortho McNeil) Hydroxypropyl cellulose Dermatologic; acne vulgaris
o
oTable 10.3: Examples of Ophthalmic Ointments
Commercial Product Active Ingredient Category
Chloramphenicol ophthalmic Chloromycetin Opthalmic 1% Antibacterial, antibiotic
Ointment (Parke-Davis)
Polymyxin B-bacitracin Polysporin Opthalmic Ointment Per gram: polymyxin B sulfate, Antimicrobial
ophthalmic (Monarch) 10,000 U; bacitracin zinc, 500 U
Polymyxin B-bacitracin- Neosporin Opthalmic Ointment Per gram: polymyxin B sulfate, Antimicrobial
neomycin ophthalmic (Monarch) 5,000 U; bacitracin zinc, 400 U;
neomycin sulfate, 5 mg
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Sulfacetamide sodium ophthalmic Sodium Sulamyd Opthalmic 10%, 30% Antibacterial
Ointment (Schering-Plough)
o
o Table 10.4: Examples of Rectal and Vaginal Creams and Ointments
Active Ingredient Product Type Primary Use
Rectal
Anusol (GlaxoSmithKline) Starch Ointment Hemorrhoid treatment
Ogen (Pharmacia & Upjohn) Estropipate Cream Estrogenic for vulvar, vaginal
Premarin (Wyeth-Ayerst) atrophy
Conjugated estrogens Cream Atrophic vaginitis, kraurosis
vulvae