Ointments, Creams, and Gels

Topicals•Preparations applied to the skin either for their physical effects or for the specific effect of a medicinal agent•Protectants, lubricants, emollients, drying agents, astringents

Transdermals•Designed to support the passage of drug substances from the surface of the skin, through its various layers, and even into the systemic circulation

INTRODUCTION

Functions of Dermatologicals•Protect injured areas from the environment•Provide for skin hydration (emollient)•Vehicle for medication transport

Drug Penetration Is Dependent Upon:•Amount of pressure and vigor of rubbing•Surface area covered•Condition of the skin•Base used•Occlusive dressing use

Application Areas for DermatologicalsLOTIONS

CREAMS

OINTMENTS

Intertriginous areas

Moist, weeping lesions

Dry, scaly lesions

INTRODUCTION

Ointments

•Semisolid preparations intended for external

application to the skin or mucous membranes.

•Semisolid plastic flow characteristics

•Definite yield value

•Resistance to flow drops as application continues

Compendial Requirements for Ointments•Microbial Content•Minimum Fill•Packaging, Storage, and Labeling•Additional Standards

• Oleaginous Bases• Absorption Bases• Water-Removable Bases• Water-Soluble Bases

Ointment Bases Preparation of Ointments• Incorporation• Fusion

Ointments

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

Examples:•Hydrocarbons (mineral oils, petrolatums, paraffins, waxes)•Animal fats/vegetable oils (castor oil, cottonseed oil, olive oil)•Synthetic esters (glyceryl monostearate, butyl stearate, isopropyl lanolate, stearyl alcohol)•WHITE PETROLATUM•WHITE OINTMENT

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

Examples:•Hydrophilic petrolatum•Aquaphor•Aquabase

Ointments

Emulsion BaseWater-in-Oil•Water insoluble•Not water washable•Can absorb water•Contains water

Examples:•Cold Cream (Petrolatum-Rose Water Ointment)•Lanolin•Nivea•Eucerin

Emulsion BasesOil-in-Water•Water insoluble•Water washable•Can absorb water•Contains water

Examples:•Hydrophilic Ointment•Velvachol•Unibase•Dermabase•Vanicream•Acid Mantle

Ointments

Humectants•Glycerin•Propylene glycol•Sorbitol 70%

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, Whitfields Ointment•Veegum 10% Dermatological base•Veegum 5% Thixotropic lotion

Ointments

Selection of the Appropriate Base•Release rate•Topical or percutaneous drug absorption•Occlusion•Stability of drug•Effect of drug on ointment base•Easily removable?•Characteristics of surface for application

Incorporation•Mortar and pestle•Pill tile and spatula•Ointment mill•Unguator•Incorporation of solids•Incorporation of liquid

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

Heat highest melting point material first

Water phase a few degrees higherW/O: add water slowlyO/W: add oil slowly

Ointments

Ointment 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

Labeling and Storage•Labeling

Protect with tapeDual labelsCreativity often required

•StorageStore in a cool place

Ointments

Creams

•Opaque, soft solids, or thick liquids intended for external application.•Semisolid, pseudoplastic flow•Very little yield value•Won’t flow under force of gravity but small force will initiate flow•Viscous liquids or semisolid emulsions of either the O/W type or the W/O type•Term “cream” is most frequently applied to soft, cosmetically acceptable types of preparations.

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•A semirigid system in which the movement of the dispersing medium is restricted by an interlacing network of particles or solvated macromolecules of the dispersed phase

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

Gel Composition•Gelling agent•Water•Cosolvents•Preservatives•Stabilizers

Kinds of Gels•Hydrogels

Silica, bentonite, pectin, sodium alginate, methylcellulose, alumina

•Organic GelsContain an organic liquid (e.g., Plastibase)

•Carbomer GelsAqueous dispersion neutralized with sodium

hydroxide or triethanolamine•Methylcellulose Gels•Starch Glycerite•Aluminum Hydroxide Gel

Gelation•As a hot, colloidal dispersion of gelatin cools, the gelatin macromolecules lose kinetic energy.•With a reduction of kinetic energy or thermal agitation.•Gelatin, agar, pectin, Irish moss, pectin, tragacanth form gels by this mechanism.

Gels

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

Gels

Applications•Oral•Topical•Intranasal•Vaginal•Rectal

Gelling Agents•Alginic acid•Bentonite•Carbomer•CMC•CMC Sod•Colloidal Silicon Dioxide•Veegum

•Methylcellulose•Plastibase/Jelene•Poloxamer/Pluronic•Povidone•Propylene Glycol Alginate•Sodium Alginate•Tragacanth

Gels

Quality Control•Appearance•Uniformity•Weight/Volume•Viscosity•Clarity•pH•Others

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

Stability•Physical Stability

- Shrinkage- Separation of liquid from the gel- Discoloration

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

Patient Counseling•Proper application•Proper storage•Keep tightly closed

Transdermal Preparations•Pastes•Plasters•Glycerogelatins•Packaging Semisolid Preparations

- Filling Ointment Jars- Filling Ointment Tubes

Features and Use of Dermatologic Preparations•Ointments•Creams•Gels•Pastes•Plasters•Topical or systemic effect

Gels

Features and Use of Ophthalmic Ointments and Gels•Relative short residence time after application•Sterile•Nonirritating•Softening point close to body temperature•Application technique

Features and Use of Nasal Ointments and Gels•Primarily local effects but some systemic also•Rich blood supply in nasal lining

Gels

Features and Use of Rectal Preparations•Ointments, creams, gels•Perianal area and anal canal•Anorectal pruritus, inflammation, hemorrhoids•Proper instruction for use to patient

Features and Use of Vaginal Preparations•Ointments, creams, foams, and gels•Anti-infectives, hormones, pH modifiers, spermicides

Gels

Pastes•Thick, stiff ointments that do not ordinarily flow at body temperature, and therefore serve as protective coatings over the areas to which they are applied. Usually >20% solids.•Semisolid, dilatant flow•Definite yield value•Resistance to flow increased with increased force of application

Lotions•Aqueous preparations with insoluble material for external application without friction•Fluid preparations, Newtonian flow•No yield value•Flow under gravity•“Lotions” actually also refers to fluid oil-in-water and water-in-oil emulsions.

Others

Cerates•Semisolid preparations containing a relatively high wax content•Semisolid•High yield point•Not to be directly rubbed onto skin

Plasters•Solid or semisolid preparations that cannot be spread at room temperature

Cataplasms or Poultices•Wet masses of solid matter applied to the skin to reduce inflammation and act as counterirritants

Others

Prepared By:

Cerna, DivinaDipus, SheenaraRabara, Starette