Abstract
A novel, stability-indicating UHPLC method was developed for the quantitative determination of Abacavir sulfate, its related substances, and forced degradation impurities in bulk drugs. The chromatographic separation was achieved on a Waters Acquity BEH C8, 50 mm × 2.1 mm, 1.7 μm particle size column with a mobile containing a gradient mixture of solution A (0.10 % v/v o-phosphoric acid in water) and solution B (0.10% v/v o-phosphoric acid in methanol). The flow rate was set at 0.40 mL/min and the run time was 6.0 min. The drug substance was subjected to the stress studies of hydrolysis, oxidation, photolysis, and thermal degradation. Abacavir sulfate was found to degrade significantly under acidic hydrolysis and oxidative stress conditions. The formed degradation products were reported and were well-resolved from Abacavir and its related substances. The mass balance was found to be satisfactory in all of the stress conditions, thus proving the stability-indicating capability of the method. The developed UHPLC method was validated to be in agreement with ICH requirements and found to be rapid, accurate, precise, linear, specific, and suitable for the quantitative determination of related substances and degradants in the bulk drug samples of Abacavir sulfate.
Highlights
Abacavir Sulfate, {(1S,4R)-4-[2-amino-6-(cyclopropylamino)-9H-purin-9-yl]cyclopent-2-en1-yl}methanol sulfate (2:1), is a nucleoside reverse transcriptase inhibitor (NRTIs) [1]
When a solution spiked with impurities was injected into the ultra-high performance liquid chromatography (UHPLC) system, the system suitability parameters for the analyte peak were observed to be very poor with very little resolution between the Imp-C and analyte peak
To improve the peak shape, mobile phase A was replaced with a 10 mM ammonium acetate buffer solution and the spiked solution was injected into the UHPLC system
Summary
Abacavir Sulfate, {(1S,4R)-4-[2-amino-6-(cyclopropylamino)-9H-purin-9-yl]cyclopent-2-en1-yl}methanol sulfate (2:1), is a nucleoside reverse transcriptase inhibitor (NRTIs) [1]. It is used either as a 600-mg once-daily or 300-mg twice-daily regimen exclusively in the treatment of human immunodeficiency virus (HIV) infection [2], and mainly helps to halt the inroads of the human immunodeficiency virus (HIV). HIV gradually undermines the body's immune system, encouraging other infections to take hold until the body succumbs to full-blown acquired immune deficiency syndrome (AIDS). Abacavir is phosphorylated to its corresponding monophosphate as an intracellular reaction. Cytosolic enzymes convert Abacavir monophosphate to carbovir monophosphate (CBV-MP), which is phosphorylated to the biologically active moiety, carbovir triphosphate (CBV-TP). CBV-TP inhibits HIV reverse transcriptase by competing with the endogenous substrate dGTP and by chain termination subsequent to incorporation into the growing polynucleotide strand [3]
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