Ointments, Creams, Transdermal, Gels

OINTMENTS, CREAMS, PASTE, GELS, TRANSDERMALS PATCHES

OINTMENTS

-          Semisolid

-          Medicated or unmedicated

-          Unmedicated: PROTECTANTS, EMOLLIENTS, LUBRICANTS

-           

OINTMENT BASES

1.       Oleaginous Base

“Hydrocarbon base”

 

-          Emollient effect

-          Occlusive

-          Long periods without drying out

-          Hard to incorporate with aqueous preparations (water)

*Powdered substances:

Liquid petrolatum (mineral oil)- use as levigating agent

Petrolatum, USP –purified mix, yellowish, light-amber

Yellow petrolatum, jelly

 

 

White petrolatum- purified, DECOLORIZED

WHITE petrolatum

PETROLEUM JELLY

…Vaseline

 

Yellow ointment-

Simple Ointment

Yellow wax (50 g) + Petrolatum (950 g)

*yellow wax: Apis mellifera

 

White Ointment

Uses  WHITE WAX

2.       ABSORPTION BASE

a.        W/O (e.g Lanolin)

b.      O/W (e.g Hydrophilic petrolatum)

 

-Not easily removed because of external phase oil

- USEFUL AS ADJUNCTS TO INCORPORATE small vols of aqueous into HYDROCARBON BASE

 

AQUAPHOR à

 Hydrophilic Petrolatum

(melt- stearyl alc + whitewax + cholesterol + white petrolatum)

 

 

Lanolin, USP

-obtain from SHEEP Ovis aries

purified waxlike; cleaned, deodorized, decolorized (less 0.25% water)

 

 

3.       WATER-REMOVABLE BASE

       Water- washable

Oil in WATER

O/W

-          Easily washed out from skin

-          Absorb serous discharges

Hydrophilic OINTMENT

( + parabens, Na lauryl sulphate, water)

4.       WATER-SOLUBLE Bases

Greaseless

NO OLEAGINOUS

Mostly used for incorporation Of SOLID SUBSTANCES

Polyethylene Glycol Ointment (PEG)

-          Polymer of ethylene oxide and water

MW less 600- clear

600-1000 - semisolid

MW above 1000- white

 

PREPARATION OF OINTMENTS

1.       INCORPORATION

Mixed until uniform preparation achieved

By mortar pestle

Unguator-mixing device

INCORPORATION OF SOLIDS

-          Geometric dilution- small portion of powder is added with a portion of base until uniform

-          Levigating- mixing solid in avehicle to make smooth dispersion (e.g mineral oil)

-          Pulverization by Intervention- for gummy materials( camphor)

INCORPORATION OF LIQUIDS

 

-          HYDROPHILIC+ enough Hydrophobic= blend; then add to rest HYDROPHOBIC

 

2.       FUSION

All or some of the components of an ointment are combined by being MELTED together and COOLED with CONSTANT STIRRING until CONGEALED

-          Heat labile or volatile: ADDED LAST

-          Substance with highest melting point- are heated to their lowest temp they can melt

 

COMPENDIAL REQUIREMENTS

1.       Absence of

Staphylococcus aureus

Pseudomonas aeruginosa

 

 

CREAMS

-          Semi-solid

-          One or more medicinal agents dissolved or dispersed in either W/O or O/W emulsions containing large amounts of WATER, STEARIC ACID, or other oleaginous substances

-          After application, water EVAPORATES, leaving thin film of stearic acid

-          VS OINTMENTS: EASIER TO SPREAD OR REMOVE

GELS

-          Semi-solid systems consisting of dispersion of small or large molecules in an aqueous liquid vehicle rendered jelly like

-           

Gelling agents

 

Carbomers :

Tragacanths, -methycellulose

 

Single Phase Gel

Uniformly dispersed throughout the liquid

No boundaries between macromolecules and liquid

Two phase system

“Magma”

Gel mas  consisting of floccules of small distinct particles

Ex: MILK OF MAGNESIA, thixotrope

PASTE

-          CONTAIN LARGER AMOUNT OF SOLID (SUCH AS 25%)

-          STIFFER THAN OINTMENT

-           Ex: Zinc Oxide Paste (LASSAR’s Plain Zinc Paste)

 

PLASTER

-          Solid or semisolid adhesive masses spread on backing paper, fabric moleskin, plastic

-          EX: Salicylic Acid plaster (remove corns)

GLYCEROGELATINS

-          Plastic masses containing: gelatin (15%); glycerine (40%), water (35%), medicinal substance (10%)

-          Ex: Zinc Gelatin (varicose)

TYPES OF PLASTICS

HDPE

Superior moisture barrier, less resilient

LDPE

Soft, resilient, good moisture barrier

Polypropylene (PP)

High level of heat resistance

PET (polyethylene terephthalate)

Transparency; high degree of product compatibility

 

TRANSDERMAL DRUG DELIVERY SYSTEMS

-          Facilitate passage of therapeutic quantities of drug substances through the skin and general circulation for their systemic effects

-          STRATUM CORNEUM; MAJOR RATE LIMITING BARRIER TO TRANSERMAL DRUG TRANSPORT

-          MW 100 TO 800

-          Ideal MW: MW 400 or less

Enhance drug delivery by:

-          Iontophoresis: delivery of  a charged chemical compound across skin membrane using electric field

-          Sonophoresis: High frequency ultrasound

-          Ex: Transdermal Scopolamine: for motion sickness

-          Nitroglycerin transdermal: Nitro-dur, Nitrodisc, Minitran

-                   To avoid tolerance: 12-14 hr patch on; 12 to 14 hrs patch off

 

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