SEMISOLIDS Flashcards

1
Q

Emollient

A

softens the skin

soothes irritation in skin or mucous membrane

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2
Q

Protective

A

protects injured skin

protects exposed skin surfaces from harmful or annoying stimuli

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3
Q

Occlusive

A

promotes retention of water in the skin by forming a hydrophobic barrier that prevents moisture in the skin from evaporating

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4
Q

Humectant

A

a substance that causes water to be retained because of its hygroscopic properties

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5
Q

Uses of Dermatologicals

A

To protect skin or mucous membranes from chemical or physical irritants in the environment
To permit rejuvenation of the skin
To provide hydration of the skin or an emollient effect
To provide a vehicle for applying a medication either for local or systemic effects

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6
Q

Ointments features

A

1) Semisolid preparations intended for the external application to the skin or mucous membranes
2) Soften or melt at body temperature
3) Should spread easily and be non-gritty
4) Semisolid plastic flow characteristics
5) Definite yield value
6) Resistance to flow drops as application continues

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7
Q

Desirable Properties of Bases

A

1) Chemically and physically stable under normal conditions of use and storage
2) Nonreactive and compatible with a wide variety of drugs and auxiliary agents (such as emulsifier, preservatives)
3) Free from objectionable odor
4) Nontoxic, nonsensitizing and nonirritating
5) Aesthetically appealing
6) easy to apply and nongreasy
7) Remains in contact with the skin until removal is desired, then is easily removed

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8
Q

Ointment Bases types

A

Oleaginous
Absorption
Water-removable
Water-soluble

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9
Q

Oleaginous Bases properties

A

1) Also called hydrocarbon bases; water insoluble
2) Emollient effect; prevent escape of moisture
3) Can remain on skin for prolonged periods without drying out; difficult to wash off
4) Not water washable
5) Can only incorporate small amounts of water
5) Oily, occlusive, lack cosmetic appeal

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10
Q

Advantages of Oleaginous Bases

A

Inexpensive, Nonreactive, Nonirritating,
Good emollient, protective and occlusive properties,
Not water-washable, so they stay on the skin and keep incorporated medications in contact with the skin

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11
Q

Disadvantages of Oleaginous Bases

A

1) Poor patient acceptance because of their greasy nature
2) Not removed easily with washing
3) Can only incorporate limited amounts of water and aqueous preparations and then with great difficulty

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12
Q

Oleaginous Bases types

A

Petrolatum, USP
White Petrolatum, USP
Yellow Ointment, USP
White Ointment, USP

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13
Q

Petrolatum, USP

A

1) Yellow petrolatum and petroleum jelly
2) Purified mixture of semisolid hydrocarbons obtained from petroleum
3) Unctuous mass, varying in color from yellowish to light amber
4) Melts at 38° to 60°C
5) May be used alone or in combination with other agents as an ointment base

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14
Q

White Petrolatum, USP

A

1) Purified mixture of semisolid hydrocarbons that has been decolorized
2) More esthetically appealing than petrolatum, but used for same purposes

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15
Q

Yellow Ointment, USP

A

1) Simple ointment
2) Slightly more viscous than plain petrolatum
3) Petrolatum 95% w/w and Yellow wax 5% w/w
Yellow wax is obtained from honeycomb

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16
Q

White Ointment, USP

A

Same as yellow ointment, but is made with white wax (bleached and purified yellow wax) instead of yellow wax

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17
Q

Absorption Bases properties

A

1) May be used as emollients, but don’t provide the degree of occlusion of oleaginous bases
2) Not easily removed from the skin with water washing
3) Useful as adjuncts to incorporate small volumes of aqueous solutions into hydrocarbon bases
4) Oily, occlusive, lacks cosmetic appeal

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18
Q

Absorption Bases: Two basic types:

A

1) Those that permit the incorporation of aqueous solutions resulting in the formation of water-in-oil emulsions (e.g., hydrophilic petrolatum)
2) Those that are water-in-oil emulsions that permit the incorporation of additional quantities of aqueous solutions (e.g., lanolin)

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19
Q

Advantages of Absorption Bases

A

1) Moderately good protective, occlusive and emollient properties
2) Do not wash off easily, so they hold incorporated medications in contact with the skin
3) Can absorb liquids

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20
Q

Disadvantages of Absorption Bases

A

1 Some bases in this class have poor patient acceptance

2) Not easily removed with washing
3) May be sensitizing
4) Can have compatibility issues related to the emulsifying agent
5) May be chemical stability issues with bases that contain water and ingredients sensitive to hydrolysis
6) Those that contain water may be subject to microbial growth ( adding preservative can reduce microbial growth but sensitive to skin)

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21
Q

Absorption Bases

Examples

A

Hydrophilic Petrolatum, USP
Aquaphor and Aquabase
Lanolin, USP
Modified Lanolin, USP

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22
Q

Lanolin, USP

A

1) Obtained from the wool of sheep
2) Purified wax-like substance that has been cleaned, deodorized and decolorized
3) Contains not more than 0.25% water
4) Modified Lanolin, USP has been processed to reduce the contents of free lanolin alcohols and any detergent and pesticide residues

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23
Q

Water-Removable Bases

A

1) Water-washable bases
2) Oil-in-water emulsions also called creams
3) Easily washed from the skin
4) May be diluted with water or aqueous solutions
5) Can absorb serous discharges

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24
Q

Advantages of Water-Removable Bases

A

1) Nongreasy
2) Can be removed from the skin by washing
3) Can absorb some water or alcohol
4) Will allow dissipation of fluids from injured skin

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25
Q

Disadvantages of Water-Removable Bases

A

1) Less protective, less emollient, a less occlusive than hydrocarbon or absorption bases
2) Can have compatibility issues with certain emulsifying agents
3) May be chemical stability issues with bases that contain water and ingredients sensitive to hydrolysis
4) Those that contain water may be subject to microbial growth
5) May dry out due to evaporation of water

26
Q

Water-Removable Bases

Examples

A

Hydrophilic ointment
Vanishing cream
Dermabase®

27
Q

Water-Soluble Bases

A

1) Contain no oleaginous components
2) Completely water washable, greaseless
3) Soften greatly with addition of water so not able to incorporate large amount of aqueous solutions effectively
4) Mostly used to incorporate solids

28
Q

Advantages of Water-Soluble Bases

A

1) Soluble in water, so easily removed by washing
2) Leaves no oil residue
3) Can absorb limited amounts of water or aqueous solutions

29
Q

Disadvantages of Water-Soluble Bases

A

1) Irritating
2) Little to no emollient properties
3) PEG-type bases may have compatibility problems with drugs that are sensitive to oxidation
4) Those that contain water may have the compatibility and stability problems associated with water and require a preservative

30
Q

Selection of the Appropriate Base

A

1) Desired release rate of the drug substance from the ointment base
2) Desirability of topical or percutaneous drug absorption
3) Desirability of occlusion of moisture from the skin
4) Stability of the drug in the ointment base
5) Effect of the drug on the consistency of the ointment base
6) Desire for a base that is easily removed from the skin
7) Characteristics of the surface to which it is applied

31
Q

Preparation of Ointments

A

Incorporation

Fusion

32
Q

Preparation of Ointments: Compounding:

Equipments:

A

1) Ointment Slabs or Pads
2) Spatulas
3) Small-scale ointment mills

33
Q

Preparation of Ointments: Compounding

A

Allow excess to compensate for loss during compounding

Either % (e.g., 10%) or stated amount (e.g., 3 g)

34
Q

Preparation of Ointments: Compounding:

Incorporation of Solids

A

1) Should be solubilized or the particle size should be reduced as far as possible
2) Auxiliary agents, levigating agents and solvents, can be added to facilitate making a smooth, elegant product

35
Q

Preparation of Ointments: Compounding:

Choice of drug form

A

If possible, select fine powder

36
Q

Preparation of Ointments: Compounding:

Levigation

A

Levigating agents are usually chosen to be similar to the ointment base
Melted ointment base may be used

37
Q

Common levigating agents

A

1) Mineral oil – oleaginous, absorption, W/O emulsion bases

2) Glycerin/propylene glycol/water - O/W Emulsion bases, water-soluble bases

38
Q

Preparation of Ointments: Compounding

Fusion

A

1) Heat highest melting point material first
2) Water phase a few degrees higher
3) W/O: add water slowly
4) O/W: add oil slowly

39
Q

Beyond-Use Dates – Compounded Preparations

For Nonaqueous Formulations

A

The BUD is not later than the time remaining until the earliest expiration date of any API or 6 months, whichever is earlier.

40
Q

Beyond-Use Dates – Compounded Preparations

For Water-Containing Topical/Dermal and Mucosal Liquid and Semisolid Formulations—

A

The BUD is not later than 30 days

41
Q

Creams

A

Semisolid preparations containing one or more medicinal agents dissolved or dispersed in either a water-in-oil emulsion or an oil-in-water emulsion base or in another type of water-washable base

42
Q

Creams:

Preparation usually involves

A

separating and heating lipid and aqueous components separately and then combining the phases

43
Q

Creams primarily used in

A

topical skin products and rectally and vaginally and Often preferred to ointments because they are easier to spread and remove

44
Q

Gels

A

1) Semisolid systems consisting of dispersions of small or large molecules in a liquid vehicle rendered jellylike by the addition of a gelling agent
2) May also contain drug substances, solvents, preservatives and/or stabilizers

45
Q

Gels route of administration

A

skin, the eye, the nose, the vagina and the rectum

46
Q

Gelling Agents:

Synthetic Macromolecules

A

Carbomer 934

47
Q

Gelling Agents: Cellulose Derivatives

A

Carboxymethylcellulose

Hydroxypropyl methylcellulose

48
Q

Gels: gelling agents: Natural gums

A

Tragacanth

49
Q

Types of Gels

Single-phase gels

A

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

50
Q

Two-phase gels

A

magmas; gel mass consisting of floccules of small distinct particles

51
Q

Hydrogels

A

include ingredients that are dispersible as colloidals or soluble in water

52
Q

Organogels

A

include ingredients such as hydrocarbons, animal and vegetable fats, etc

53
Q

Syneresis

A

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

54
Q

Swelling

A

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

55
Q

Imbibition

A

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

56
Q

Thixotropy

A

A reversible gel-sol transition with no change in volume or temperature

57
Q

Xerogel

A

Formed when the liquid is removed from a gel and only the framework remains

58
Q

Transdermal Preparations

A

Topical ointments, creams and gels can be designed to deliver a drug systemically by the addition of penetration enhancers to the vehicle

59
Q

transdermal preparations: Penetration enhancers

A

dimethyl sulfoxide (DMSO), ethanol, propylene glycol, glycerin, polyethylene glycol, urea, dimethyl acaetamide, sodium lauryl sulfate , the poloxamers, Spans, Tweens, lecithin, terpenes and others

60
Q

Pluronic Lecithin Organogel (PLO)

A

Commonly compounded transdermal preparation which aids in the rapid penetration of many active drugs through the skin

61
Q

Pluronic Lecithin Organogel (PLO) consists of

A

Pluronic (Poloxamer) F127 gel (usually 20% or 30% concentration) mixed at a ratio of approximately 1:5 with a mixture of equal parts of isopropyl palmitate and lecithin