A Validated Stability Indicating RP-HPLC Method for the Determination of Emtricitabine, Tenofovir Disoproxil Fumarate, Elvitegravir and Cobicistat in Pharmaceutical Dosage Form

Abstract

A new simple, rapid stability indicating assay method has been developed and validated for the determination of emtricitabine, tenofovir disoproxil fumarate, elvitegravir and cobicistat using reverse-phase high-performance liquid chromatography in their pharmaceutical dosage form. The chromatographic separation was performed on an ODS column (250 × 4.6 mm, 5 µm) using mobile phase A (potassium dihydrogen orthophosphate, pH adjusted to 2.5) and mobile phase B (acetonitrile) in the ratio of 55:45% v/v at a flow rate of 1 mL/min. The analytes were detected at 250 nm. The method was found to be linear in the concentration range of 2-12 µg/mL for EMT, 3-18 µg/mL for TNDF, 1.5-9 µg/mL for ELV and COB, with the coefficient value (R(2)) of >0.9990. The accuracy was measured via recovery studies and found to be acceptable, and the percentage recoveries were found in the range of 99.93-100.08 ± 0.5%. Forced degradation studies were also conducted, and the drugs were subjected to various stress conditions such as acid hydrolysis, base hydrolysis, oxidative, photolytic and thermal degradation. The proposed method was successfully validated and applied for the quantitative estimation of these drugs in both bulk and tablet dosage forms.

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]…”

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“…Various HPLC and HPTLC methods were reported in the literature for the estimation of cobicistat and elvitegravir individually [6][7][8] , simultaneously [9][10] and other antiretroviral drugs [10][11][12][13][14][15][16][17][18][19][20] . The present method is novel and was successfully validated in accordance with ICH guidelines 21 .…”

RP-HPLC Method for Quantification of Emtricitabine and Tenofovir Alafenamide Fumarate Drug Substance and Tablet Dosage Form

“…The antiviral activity of Emtricitabine is due to its metabolite Emtricitabine 5'-triphosphate, which effectively inhibits the reverse transcriptase enzyme blocks replication of the HIV [1,2]. Tenofovir alafenamide fumarate is a prodrug of Tenofovir prepared by reacting one mole of fumaric acid with two moles of tenofovir alafenamide.…”

“…Tenofovir alafenamide fumarate is a prodrug of Tenofovir prepared by reacting one mole of fumaric acid with two moles of tenofovir alafenamide. The IUPAC name of TAF is [2][3][4][5][6][7][8]. Along with the individual methods, analytical and bio analytical methods were available in simultaneous estimation in combination with other antiviral drugs [9,10].…”