Exam 2 - Powerpoint 3 (Ointments) Flashcards
Transdermal
deliver drug to skin for entry into systemic circulation
Transdermal not same as topical
Topical
Local effect on skin, not systemic like transdermal
Humectants
Draw moisture
Emollients
Exfoliate skin
Topical Dermatological’s
Pro vs Con
Pro:
Drug goes to site of action
Minimal amount of drug needed
Low risk systemic adverse events
Con
Absorption of drug
Skin irritation
Application process
Ointment
Semisolid preparation intended for external application to skin or mucous membranes that soften or melt at body temp
Oleaginous Bases (Hydrocarbon Base)
Emollient, protective and Occlusive effects (prevents moisture from escaping, keeping it moist)
Immiscible with water
Levigating agents (like mineral oil) can be used if drug being incorporated is a powder
Absorption bases
Anhydrous Absorption bases
Emulsion bases
occlusive but not as much as oleaginous bases, not easily removed…..external phase is oil
Anhydrous absorption bases
permit incorporation of aqueous solutions resulting in Water in Oil (W/O) emulsions
Emulsion bases
permit incorporation of additional quantities of aqueous solutions
Emulsion
Dispersed phase - Oil and Water separate
Continuous phase - All mixed together
Sulfectants used to prevent emulsion going back to dispersed phase
emulsifiers
used to prepare emulsions such as cream and lotions
Water-Removable bases
Oil in water (O/W) emulsions resembling creams
External phase of emulsion is water, easily removed from skin
absorbs serous discharges
Water-soluble bases
Do not contain oleaginous components
Can contain and absorb water
water washable, greaseless
used in incorporation of solid drug substance
PEG 1-1000+ (M/w)
PEG 1 - 600 = Liquid
PEG 600 - 1000 = semi solid
PEG 1000+ = solid
Table: Oleaginous or Hydrocarbon
Water soluble? N Water washable? N water absorption capability? N contain water? N contain emulsifiers? N occlusibe/greasy? Y Easy spread? N
Table: Anhydrous
Water soluble? N Water washable? MOD water absorption capability? Y contain water? N contain emulsifiers? Y W/O occlusibe/greasy? Y Easy spread? N
Table: Emulsion:
Water soluble? N Water washable? MOD water absorption capability? Y contain water? Y contain emulsifiers? Y W/O occlusibe/greasy? MOD Easy spread? MOD
Table: Water removable
Water soluble? Water washable? Y water absorption capability? Y contain water? Y contain emulsifiers? Y O/W occlusibe/greasy? MOD Easy spread? Y
Table: Water soluble
Water soluble? Y Water washable? Y water absorption capability? Y contain water? Y AND N contain emulsifiers? N occlusibe/greasy? N Easy spread? MOD
Selection of appropriate base
release rate of drug form ointment (strong affinity = no good)
occlusion of moisture from skin
stability of drug
removal by washing with water
topical percutaneous drug absorption
Incorporation method
Used to prepare ointments
Ingredients are mixed until uniform mixture is attained
Fusion Method
Melt and mix
Components are melted and allowed to congeal under constant stirring.
W/O - add water slowly to oil phase
O/W - add oil slowly to aqueous phase
Add drug while congealing when its cooler due to heat
Ointment Compendia Requirements
Microbial Content <1111>
USP Minium Fill Test <755> (Have amount says it has)
Stability <795> (BUD)
Nonsterile BUD
BUD of 30 days, or intended duration, whiter is shorter
Creams
soft solids or thick liquids for external application
Semisolid, pseudoplastic flow
recently term restricted to products consisting of Oil-in-water emulsions…used to be either or
Pseudoplastic flow
Think ketchup, need to apply pressure/shake for it to get moving…same concept creams
Gels
Semisolid systems consisting of dispersion of small or large molecules in an aqueous liquid vehicle
Single Phase Gel
Gels in which macromolecules are uniformly distributed through liquid, usually involves organics
Two Phase Gel
When gel consists of floccules of small distinct particles, usually inorganic
Milk of magnesia
Gel Composition
Gelling agent Water Cosolvents Preservatives Stabilizers
Gelling agent
Synthetic Macromolecules
Natural gums
Alginic Acid
Pastes
Thick, stiff ointments that don’t flow at body temp
Usually >20% solids
Semisolid, dilatant flow
Plasters
Solid or semisolid preparations that cannot be spread at room temp
Ie. Wart remover, 40% salicylic acid plaster
Lotion
Not semisolid, Free flowing (flow under gravity)
Term being phased out, it can be a suspension, solution or emulsion currently
Application Areas Dermatologicals
Lotions:
Intertriginous areas, place where skin rubs together
Creams:
Moist, weeping lesions
Ointments:
Dry, scaly lesions
Other routes of Admin
Ophthalmic
Nasal
Rectal
Vaginal