Solubility Enhancement of Efavirenz by Solid Dispersion Techniques using Soluplus as Hydrophilic Carrier
Author (s): Ajit Nahak1, Ruchita Kumari Patra2, Soudamini Mallick2
Department of Drug Regulatory Affairs Brawn’s Laboratories, Gurugram, 122001, INDIA
Royal College of Pharmacy and Health Sciences, Berhampur-2, Odisha, INDIA
Low water solubility is an industry wide issue. Low bioavailability and irregular oral absorption are common problems in low water-soluble drugs. Efavirenz is an oral non- nucleoside reverse transcriptase inhibitor (NNRTI). It is a synthetic purine derivative and, similar to zidovudine, zalcitabine, and stavudine. Efavirenz was originally approved specifically for the treatment of HIV infections in patients who failed therapy with zidovudine. It comes under BCS class II drugs. Its water Solubility is 0.00855 mg/mL, practically insoluble in water. Although numerous methods are available to improve the solubility and/or dissolution rate of low soluble drugs, the most promising method for promoting dissolution is with preparation of solid dispersions. To enhance the solubility of low soluble drug efavirenz, solvent evaporation and lyophilization technique was followed, which can improve the solubility and dissolution rate of the drug. Among all the formulation soluplus (1:1.5) shows highest % of drug release i.e., 95.11 % in solvent evaporation process.
Keywords: Efavirenz, soluplus, HIV, BCS class II, lyophilization.