Tretinoin and Dexpanthenol Gel

Abstract

QUALITY CONTROL Quality-control assessment can include theoretical weight compared to actual weight, pH, specific gravity, active drug assay, color, texture-surface, texture-spatula spread, appearance, feel, rheological properties, and physical observations.2 DISCUSSION Tretinoin (C^sub 20^H^sub 28^O^sub 2^, MW 300.44) occurs as a yellow to lightorange crystalline powder that is insoluble in water, slightly soluble in alcohol, and is sensitive to light, heat, and air. It occurs as a white or pale yellow crystalline solid or powder with a faint characteristic odor that is practically insoluble in water, glycerin, propylene glycol, solutions of alkali hydroxides, and dilute aqueous mineral acids.6 Pluronic F-127, generally available in powdered form, is one of the polxamers, which are used as emulsifying, solubilizing, and wetting agents that are available in different grades.

METHOD OF PREPARATION

1. Calculate the required quantity of each ingredient for the total amount to be prepared.

2. Weigh and/or measure each ingredient accurately.

3. Mix the tretinoin, PEG 400, Cremophor RH400, and butylated hydroxytoluene together and heat to about 40°C.

4. Add the dexpanthenol and purified water and mix well and heat to about 50°C.

5. Add about 4 g of the Pluronic F-127 and mix well.

6. Cool to about 5°C to 8°C and dissolve the rest of the Pluronic F-127.

7. Keep cool until all air bubbles have escaped.

8. Package and label.

PACKAGING

Package in tight, light-resistant containers.1

LABELING

Keep out of reach of children. Use only as directed.

STABILITY

A beyond-use date of up 6 months can be used for this preparation.1

USE

Tretinoin and dexpanthenol gel has been used in the treatment of dermatological conditions, including skin neoplasm and actinic keratoses.

QUALITY CONTROL

Quality-control assessment can include theoretical weight compared to actual weight, pH, specific gravity, active drug assay, color, texture-surface, texture-spatula spread, appearance, feel, rheological properties, and physical observations.2

DISCUSSION

Tretinoin (C^sub 20^H^sub 28^O^sub 2^, MW 300.44) occurs as a yellow to lightorange crystalline powder that is insoluble in water, slightly soluble in alcohol, and is sensitive to light, heat, and air. Tretinoin is used primarily in the topical treatment of acne vulgaris and various neoplastic and related skin disorders, to include rosacea.3

Dexpanthenol (C^sub 9^H^sub 19^NO^sub 4^, MW 205.25) occurs as a clear, viscous, somewhat hygroscopic liquid, having a slight characteristic odor. It is freely soluble in water, alcohol, and propylene glycol and slightly soluble in glycerin. Some crystallization may occur upon standing. It should be stored in air-tight containers. It has been used topically in 2% to 5% concentrations in the treatment of various minor skin disordes.3

Polyethylene glycol 400 (Carbowax, PEG) occurs as a clear, colorless, or slightly yellow-colored viscous liquid with a slight, but characteristic odor and a bitter, slightly burning taste. It is soluble in water and miscible with other PEGs.4

Cremophor RH400 (Polyoxyl 40 hydrogenated castor oil) is used as an emulsifying agent, solubilizing agent, and wetting agent. It occurs as a white to yellowish semisolid paste at 20°C that liquifies at 30°C. It has a very faint characteristic odor and is almost tasteless in aqueous solutions.5

Butylated hydroxytoluene (BHT) is an antioxidant used in cosmetics, foods, and pharmaceuticals primarily to delay or prevent oxidative rancidity of fats and oils and to prevent loss of activity of oil-soluble vitamins. It occurs as a white or pale yellow crystalline solid or powder with a faint characteristic odor that is practically insoluble in water, glycerin, propylene glycol, solutions of alkali hydroxides, and dilute aqueous mineral acids.6

Pluronic F-127, generally available in powdered form, is one of the polxamers, which are used as emulsifying, solubilizing, and wetting agents that are available in different grades. They generally are white-colored, waxy, free-flowing granules or as cast solids that are practically odorless and tasteless. It is freely soluble in water, alcohol, and isopropyl alcohol.7

Purified water is water that is obtained by distillation, ion exchange, reverse osmosis, or some other suitable process. It is miscible with most polar solvents and is chemically stable in all physical states (ice, liquid, and steam).8

References

REFERENCES

1. United States Pharmacopeial Convention, Inc. USP Pharmacists' Pharmacopeia. Rockville, MD: US Pharmacopeial Convention, Inc.; 2005: 408-413.

2. Allen LV Jr. Standard operating procedure for performing physical quality assessment of ointments/creams/gels. IJPC 1998; 2(4): 308-309.

3. Sweetman SC, ed. MARTINDALE: The Complete Drug Reference. 35th ed. London, UK: Pharmaceutical Press; 2007:1455-1456, 2142.

4. Price JC. Polyethylene glycol. In: Rowe RC, Sheskey PJ, Owen SC, eds. Handbook of Pharmaceutical Excipients. 5th ed. Washington, DC: American Pharmaceutical Association; 2006: 545-550.

5. Singh KK. Polyoxyethylene castor oil derivatives. In: Rowe RC, Sheskey PJ, Owen SC, eds. Handbook of Pharmaceutical Excipients. 5th ed. Washington, DC: American Pharmaceutical Association; 2006: 572-579.

6. Groves MJ. Butylated hydroxytoluene. In: Guest RT, ed. Handbook of Pharmaceutical Excipients. 5th ed. Washington, DC: American Pharmaceutical Association; 2006: 81-82.

7. Collett JH. Poloxamer. In: Rowe RC, Sheskey PJ, Owen SC, eds. Handbook of Pharmaceutical Excipients. 5th ed. Washington, DC: American Pharmaceutical Association; 2006: 535-538.

8. Galichet LY. Water. In: Rowe RC, Sheskey PJ, Owen SC, eds. Handbook of Pharmaceutical Excipients. 5th ed. Washington, DC: American Pharmaceutical Association; 2006: 802-806.