A New, Rapid and Simple RP-HPLC Method for Stability Quantification of a Protease Inhibitor in Tablets

Abstract

Fosamprenavir calcium is a protease inhibitor widely used in the treatment and prevention of human immunodeficiency virus and acquired immunodeficiency syndrome. This protease inhibitor serves as a prodrug of amprenavir, offering better oral bioavailability. Although this drug was approved by the FDA in 2003, there are few methods established for quantifying the stability for quality control analysis of fosamprenavir-coated tablets. The purpose of the study was to develop and validate a method for determining the stability of fosamprenavir-coated tablets (Telzir®) that may be applied by any quality control laboratory. Chromatographic separation was performed using a Vertical RP-18 column programmed to run a gradient elution with sodium acetate buffer and acetonitrile. Flow rate was 1.2 mL min−1 for a total run time of 15 min. Ultraviolet detection was set at 264 nm and the use of a photodiode array detector in scan mode allowed selectivity confirmation by peak purity evaluation. The analyte peak was found to be adequately separated from degradation products generated during forced degradation studies. Thus, the proposed method was found to accurately indicate stability and was sufficient for routine quantitative analysis of fosamprenavir in coated tablets without interference from major degradation products and excipients.

Overview of Forced Degradation Analysis for FDA Approved Antiretroviral agents: A Review

“…Antiviral medicines have been quantified using a variety of methods, including UV, capillary electrophoresis, and chromatographic methods such as GC and HPLC, LC-MS, and GC-MS. The authors of this review focus on stability, recommending HPLC/RP-HPLC technologies for the precise and effective development and validation of antiviral medicines such as Zidovudine, [15][16][17][18][19][20] Lamivudine, [20][21][22][23] Nevirapine, [24][25][26][27] Ritonavir, [28][29][30][31] Abacavir, [32][33][34] Efavirenz, [35][36][37][38] Tenofovir, [39][40][41] Fosamprenavir, [42][43][44][45][46] Atazanavir, [47][48] Emtricitabine, 35,35,39,49 Fosamprenavir, [42][43][44][45][46] Tipranavir, [50][51] Darunavir, [52]…”