US Pharm. 2018;43(11):47-48.
Method of Preparation: Calculate the quantity of each ingredient for the amount to be prepared. Accurately weigh or measure each ingredient. Add the sertraline hydrochloride to the isopropyl palmitate and mix to form a smooth paste. Geometrically, add the Lipoderm base and mix until uniform. Package and label.
Use: This preparation has been used in the treatment of anxiety disorder.
Packaging: Package in a tight, light-resistant container. A syringe (without needle) that has 0.1-mL graduations works well for administration, as does a click-type dispenser.
Labeling: Keep out of reach of children. Discard after ____ [time period]. Protect from light. For external use only. Use only as directed. May cause drowsiness.
Stability: A beyond-use date of up to 30 days when stored at room temperature may be used for this preparation.1
Quality Control: Quality-control assessment can include theoretical weight compared with actual weight, specific gravity, active drug assay, color, texture–surface, texture–spatula spread, appearance, feel, rheologic properties, and physical observations.2
Discussion: By bypassing first-pass metabolism, transdermal administration of sertraline may provide greater activity within the central nervous system, as the drug is known to undergo extensive first-pass metabolism following oral administration. The major metabolite N-desmethylsertraline has a 10- to 20-fold reduction in its potential to block serotonin reuptake transporters compared with sertraline. A case report of the successful use of this compounded preparation in a 6-year-old female patient has been published.3
Sertraline hydrochloride (Zoloft, Lustral, C17H17Cl2N.HCL, MW 342.69) is an antidepressant of the selective serotonin reuptake inhibitor class that is prescribed primarily for major depressive disorder in adult outpatients, as well as obsessive-compulsive disorder, panic disorder, and social anxiety disorder in both adults and children.1,4 It occurs as a white or off-white, crystalline powder that is slightly soluble in water (3.8 mg/mL) and sparingly soluble or slightly soluble in absolute alcohol (15.7 mg/mL). Sertraline hydrochloride melts at 243°C to 245°C.
Isopropyl palmitate (C19H38O2, MW 298.51) is a colorless, mobile liquid with a very slight odor; it is used as an emollient, oleaginous vehicle, and solvent, and it has good spreading characteristics. Isopropyl palmitate is soluble in acetone, castor oil, cottonseed oil, alcohol, and mineral oil, and it is insoluble in water, glycerin, and propylene glycol. Isopropyl palmitate is resistant to oxidation and hydrolysis, and it does not become rancid. It has a specific gravity ranging from 0.8500 to 0.8550 and a viscosity of 5 to 10 mPa·s at 25°C. Isopropyl palmitate has a freezing point of 13.0°C to 15.0°C and a boiling point of 160°C. It should be stored in well-closed containers and should be protected from light.5
Lipoderm transdermal cream, an alternative to traditional Pluronic Lecithin Organogel (PLO), is a gel or cream with a smooth and creamy feel, in contrast to the tacky feel of PLOs, and it is less greasy than PLO. Lipoderm transdermal cream contains a proprietary liposomal component that may increase the permeation of a variety of actives.6 Lipoderm base allows the medication to reach the system’s circulation and local areas efficiently. It can be refrigerated, and because it is a stable system, it does not separate upon refrigeration or in the presence of ionic substances. Lipoderm transdermal cream is listed as containing water, glycerin, C12-15 alkyl benzoate, glyceryl stearate, dimethicone, cetearyl alcohol, cetearyl glucoside, polyacrylamide, cetyl alcohol, magnesium aluminum silicate, xanthan gum, aloe vera, tocopheryl acetate, bitter almond oil, grapeseed extract, wheat germ oil, vitamin A palmitate, ascorbyl palmitate, pro-lipo multiemulsion liposomic system, tetrasodium ethylenediaminetetraacetic acid, phenoxyethanol, and sodium hydroxymethylglycinate.
REFERENCES
1. U.S. Pharmacopeia/National Formulary [current revision]. Rockville, MD: U.S. Pharmacopeial Convention, Inc; October 2018.
2. Allen LV Jr. Standard operating procedure for performing physical quality assessment of ointments/creams/gels. IJPC. 1998;2:308-309.
3. Wynn T, Goetsch D. Extemporaneous preparation of sertraline cream for transdermal administration. IJPC. 2011;15(3):200-203.
4. Sertraline hydrochloride. http://compoundingtoday.com/index.cfm. Accessed October 2, 2018.
5. Quinn ME. Isopropyl palmitate. In: Sheskey PJ, Cook WG, Cable CG, eds. Handbook of Pharmaceutical Excipients. 8th ed. London, England: Pharmaceutical Press; 2017:497-498.
6. Lipoderm transdermal. www.pccarx.com/lipoderm-base. Accessed October 2, 2018.
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