Term
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Definition
| Attribute of a material characterized by a reduced ability to flow or conform to its container at room temperature. |
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Term
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Definition
Topical: deliver active pharmaceutical ingredients INTO the skin to treat disorders of the dermis.
Transdermal: deliver active pharmaceetuical ingredients through the skin to create a systemic effect |
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Term
| Benefits of Semisolid Dosages |
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Definition
Easy application.
Good ability to incorporate hydrophobic and hydrophilic ingredients.
Retention
Maintain consistent drug levels.
Ability to reduce systemic metabolism |
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Term
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Definition
A semisolid dosage form, usually containing <20% water and volatiles, and >50% hydrocarbons, waxes, or polyols as the vehicle. and "a viscous oleaginous or polymeric semisolid dosage form"
- Typical bases used: hydrocarbon, anhydrous absorption, PEG
- External applicaiton to the skin or mucous membranes
- Systemic absorption or local action
- Soften or melt at body temperatures
- Long duration of action |
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Term
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Definition
FDA: an emulsion, semisolid dosage form, usually containing > 20% water and volatiles and/or <50% hydrocarbons, waxes or polyols as the vehicle.
- Semisolid emulsion dosage form, water in oil or oil in water
- Used for topical, rectal or vaginal use
- Soft, spreadable consistency
- Increased patient acceptance |
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Term
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Definition
A semisolid dosage form, containing a large proportion (20-50%) of solids finely dispersed in a fatty vehicle.
- Typical base: hydrocarbon base
- Stiff consistency
- Do not flow at body temperature
- Use on skin, oral cavity, or mucous membranes
- Not appropriate for hairy parts of the body.
- Systemic delivery for veterinary medicine via the oral route
- Ex: broken skin b/c absorptive qualities, occlusive or protective coating |
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Term
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Definition
| A semisolid dosage form that contains a gelling agent to provide stiffness to a solution or a colloidal dispersion. A gel may contain suspended particles. |
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Term
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Definition
| Adhesive semisolid spread on a backing, prolonged contact to API after skin application, protective qualities |
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Term
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Definition
Semisolid gelatinous masses
Vehicle for drug delivery
Protective qualities
Long duration of action = remain on skin for weeks
Melted prior and applied with a brush to appropriate site
Covered after hardening |
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Term
Preparation of Semi-Solids
Fusion |
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Definition
Used for bases with high content of stiff materials
Heating during the preparation of the semisolid (highest mp first)
Homogenization
Controlled rate of cooling
Avoid stratification and settling
Mfg may use this method for emulsion bases as well |
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Term
Preparation of Semi-Solids
Compounding |
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Definition
Spatulation
Geometric dilution; ensures uniform mixing, use when small amounts of API are added to large amounts of base, mix equal amounts of base and API together |
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Term
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Definition
| Using a solvent or oil to dissolve the solid prior to incorporation into the base. Used for larger particle size or crystalline ingredients. Choose an appropraite solvent based on solubility of API. |
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Definition
Not needed?: Solid has fine particles, quantity of solid to be incorporated is small, semisolid base is soft, final preparation is intended to be a stiff paste
What qualities should a good levigating agent possess?
- Viscous, low surface tension
How to choose a levigating agent?
- Choose something chemically similar to your semisolid base
- Check for compatability issues
- No volatile solvents |
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Term
Levigating Agents
- Hydrocarbon and absorption bases |
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Definition
| Mineral oil, castor oil, olive oil, Tween 80 |
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Term
Levigating Agents
- Water washable and water soluble bases |
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Definition
| Glycerin, propylene glycol, PEG |
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Term
Levigating Agents
- Emulsion |
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Definition
Hydrophobic API in the Oil phase = mineral oil.
Hydrophilic API in the water phase = glycerin, alcohol or propylene glycol |
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Term
| How much levigating agent to use? |
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Definition
| 4-6% w/w ; use specific gravity |
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Term
| Desirable properties of Semisolid Bases |
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Definition
Chemically and physically stable
Nonreactive and compatible with most active ingredients
Aesthetically appealing
Appropriate contact time
Good absorptive properties
Good release properties of drug from base
Does no harm |
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Term
Hydrocarbon aka Oleaginous bases
Disadvantages |
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Definition
| Greasy, incorporates small amounts of water, poor solvents for most API, difficult to spread, cannot incorporate large amounts of aqueous components, but maybe some alcohol components |
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Term
Hydrocarbon aka Oleaginous bases
Advantages |
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Definition
Inexpensive, non-irritating, prolonged contact, emollient, occlusive, protectant.
Both adv/dis: insoluble in water, not water washable |
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Term
Hydrocarbon aka Oleaginous bases
Uses |
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Definition
Emollients, occlusive dressings, protectants.
- Vehicle for drugs prone to hydrolysis, not a good vehicle for deep penetration into and through the skin
- Humectant: promotes retention for moisture
- Provide a good vehicle for active ingredients that are prone to hydrolysis |
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Term
| Hydrocarbon bases - examples |
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Definition
| Petrolatum (jelly, vaseline), white petrolatum, white ointment, yellow ointment, paraffin |
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Term
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Definition
Dis: Greasy, difficult to spread
Adv: Anhydrous, can absorb water, emollient, occlusive
Both: Insoluble in water, less occlusive than hydrocarbon bases |
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Term
Anhydrous Base
uses/examples |
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Definition
Skin perfusion into the dermis; better release for hydrophobic API's Ability to absorb water
Uses: emollients, protectants, occlusive barrier, vehicle for aqueous solutions, vehicle for solids and API's
Ex: hydrophilic petrolatum, aquabase, aquaphor, lanolin |
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Term
Water in oil emulsion
Adv/Dis |
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Definition
Dis: greasy
Adv: Can absorb water, emollient
- Essentially hydrocarbon bases with an emulsifying agent
- Still greasy and hard to wash off (oil is external phase)
- Can absorb water, but not as much as anhydrous |
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Term
Water-in-oil emulsion
Uses/examples |
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Definition
Skin permeability into and through the skin, cleansing creams, make-up is mostly lipophilic, contain water and require preservative
Uses: emollient, cleansing cream, vehicle for liquids, vehicle for solids and API's
Ex: cold cream, lanolin, hydrocream, eucerin, nivea |
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Term
Oil-in-water emulsion
Adv/Dis |
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Definition
Adv: non-greasy, water washable, easy to spread, will absorb water
Both: Contains water, insoluble in water, non-occlusive |
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Term
Oil-in-water emulsion
Uses/examples |
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Definition
Skin permeability into and through the skin, less emollient/protective/occlusive
- Absorption of serious drainage; help with weeping wounds that have drainage
- Requires tight container closure systems
-Uses: emollient, vehicle for liquids, vehicle for solids and API's
-Examples: Hydrophilic ointment, dermabase, velvachol, unibase |
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Term
Water soluble bases
Adv/Dis |
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Definition
Dis: will dissolve if too much water is added
Adv: No oleaginous components, greaseless, anhydrous or hydrous, water washable, will absorb some water, moderate spreadability
Both: Non-occlusive, Non-emollient |
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Term
Water soluble bases
Uses/examples |
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Definition
Skin permeability into and through the skin, not generally used for wounds or sensitive skin; may be irritating
Uses: emollient, vehicles for liquids, vehicle for solids and drugs, local anesthetic
Ex: PEG; PEG <600 are liquid, 600-1000 semisolid, >1000 is more solid/wax-like |
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