Topical medications

Creams, Ointments, Pastes And Gels

Presented by: Faryal Alam

Introduction To Topical Medications

Topical preparations:

1. Preparations applied to the skin either for their physical effects or for the specific effect of a medicinal agent.

2. They maybe applied to skin, placed on surface of eye, or used nasally, vaginally or rectally.

3. They can be medicated or non medicated.

4. Used as Protectants, lubricants, emollients, drying agents, astringents.

Topical medications include

1. Ointment

2. Cream

3. Gels

4. pastes

ointment

• Semi-solid dosage forms

• Applied to skin or mucous membrane

• Medicated or non medicated

• Un-medicated are used for physical effects such as emollient, protectant, lubricants.

• Oleaginous Bases

• Absorption Bases

• Water-Removable Bases

• Water-Soluble Bases

Ointment bases

Oleaginous bases

• Water insoluble• Not water washable• Can’t absorb water• Oily, occlusive, lack cosmetic

appeal

Examples:1. Hydrocarbons (mineral oils,

petrolatums, paraffins, waxes)2. Animal fats/vegetable oils (castor

oil, cottonseed oil, olive oil)3. Synthetic esters (glyceryl

monostearate, butyl stearate, isopropyl lanolate, stearyl alcohol)

4. WHITE PETROLATUM5. WHITE OINTMENT

absorption bases

•Water insoluble•Not water washable•Can absorb water•Anhydrous•Oily, occlusive, lacks cosmetic appeal

Examples:1. Hydrophilic petrolatum2. Bees wax 3. lanolin

water-removable bases

• Water Washable• Can Absorb Water• External Phase Contains

Water

Examples:•Hydrophilic Ointment

water-soluble bases

• Water soluble• Water washable• Can absorb water• Anhydrous or hydrous• All water soluble, no oil phase

Example:•Polyethylene Glycol Ointment•Biozyme Ointment, Desenex Ointment

selection of ointment bases

Depends upon

• Release rate• Topical or percutaneous drug

absorption• Occlusion• Stability of drug• Effect of drug on ointment

base• Easily removable• Characteristics of surface for

application

preparation of ointment

•Ointment Slab/Pill Tile•Mortar/Pestle•Ointment Mill•Fusion

Heat highest melting point material first

Water phase a few degrees higher

W/O: add water slowly O/W: add oil slowly

• Incorporation Mortar and pestle or spatula is

used Materials are rubbed on a slab Material of spatula is stainless steel

or rubber Ointment is prepared by thoroughly

rubbing solid material in base

packaging

• Jars: Glass, Plastic Do not pour in while hot!

• Disp. Jars: Plastic

• Tubes: Plastic, tin, aluminum

• Syringes: Individually dosed, good protection of the product

creams

creams

•Opaque, soft solids, or thick liquids intended for external application

•Can be of two types

o/w

w/o

manufacturing area

1.Wax melting device

2.Water heating device

3.Manufacturing vessel

4.Storage vessels

5.Automated panel

manufacturing of creams

Wax melting vessel

Water heating vessel

Mfg vessel

Silverson mixerPaddle mixerWater and steam jacketed

Wat

er

Wax

Wax, water, antioxidants, emulsifying agents, preservatives

60-80 0C

SS316

Muslin cloth

SS316

Temp gauge

gels

gels

•Semisolid systems consisting of dispersions of small or large molecules in an aqueous liquid vehicle rendered jelly-like through the addition of a gelling agent.

Types of gels

•Single Phase

• Gels in which the macromolecules are uniformly distributed throughout a liquid with no apparent boundaries between the dispersed macromolecules and the liquid

• Usually involve organics

•Two Phase

• When the gel mass consists of floccules of small distinct particles

• Usually involve inorganics

gels

Composition of gels

• Gelling agent• Water• Cosolvents• Preservatives• Stabilizers

Kinds of Gels

1. Hydrogels• Silica, bentonite, pectin, sodium

alginate, methylcellulose, alumina

2. Organic Gels• Contain an organic liquid (e.g.,

Plastibase)

3. Carbomer Gels• Aqueous dispersion neutralized with

sodium hydroxide or triethanolamine

4. Methylcellulose Gels5. Starch Glycerite6. Aluminum Hydroxide Gel

Phenomena Associated with Gels

•Syneresis- When the interaction between particles of the dispersed phase becomes so great that on standing, the dispersing medium is squeezed out in droplets and the gel shrinks

•Swelling- The taking up of liquid by a gel with an increase in volume

•Imbibition- The taking up of a certain amount of liquid without a measurable increase in volume

•Thixotropy- A reversible gel-sol formation with no change in volume or

temperature•Jelene/Plastibase

- A combination of mineral oils and heavy hydrocarbon waxes with a MW of about 1300

•Carbomer 934- A polymer of acrylic acid cross-linked with a polyfunctional agent; recognized as an official emulsifying and suspending agent

phenomenon associated with gels

Applications of gels•Oral•Topical•Intranasal•Vaginal•Rectal

Gelling agents

1. Carbomer2. Cmc3. Tragacanth4. Gelatin5. Aerosil

applications and gelling agents

gelling agents

Carbomers:1. Acrylic based2. Sustain release in stomach3. Thickening agent4. Used in conc of 0.5-1%

Carboxy methyl cellulose:

5. Used in conc of 4-6%6. Viscosity enhancer7. Insoluble in water but salts

are soluble in water such as sodium CMC

Tragacanth• Soaked overnight• Used with glycerine and

propylene glycol as wetting agent

Gelatin• Obtained from bone

collagen• Bio-compatible• cosmotological• Contains human serum

albumin

Ehtyl cellulose• 5% conc

Aerosil• Inorganic• No microbial growth

•Physical Stability- Shrinkage- Separation of liquid from the gel- Discoloration

•Microbial Stability•BUD: Unless otherwise documented, 14 days when stored in a refrigerator (USP)

Stability

Packaging/Storage/Labeling

•Tight containers•Room or refrigerated temperatures, as appropriate•Prior to use, store in tight containers.

pastes

• Thick, stiff ointments that do not ordinarily flow at body temperature.

• Serve as protective coatings over the areas to which they are applied.

• Usually >20% solids

• Medicated (zinc oxide)

• Un-medicated (toothpaste)

• Bulking agent calcium carbonate, starch.