Stability behaviour of antiretroviral drugs and their combinations. 9: Identification of incompatible excipients.
Incompatibility studies of antiretroviral drugs, viz., lamivudine (3TC), emtricitabine (FTC), abacavir sulfate (ABC), tenofovir disoproxil fumarate (TDF), zidovudine (ZDV), efavirenz (EFV) and nevirapine (NVP) were carried out in the presence of ten selected excipients, i.e., microcrystalline cellulose, lactose monohydrate, starch, magnesium stearate, sodium lauryl sulfate, sodium starch glycolate, croscarmellose sodium, colloidal silica, povidone K-30 and hydroxypropyl cellulose. Among all, ABC showed reaction with lactose monohydrate, resulting in the formation of two interaction products, while sodium lauryl sulphate enhanced the degradation of TDF. The interaction products of ABC-Lactose were separated by high performance liquid chromatography (HPLC) and subjected to liquid chromatography-high resolution mass spectrometry (LC-HRMS) studies for their characterization. One of the products was also isolated and subjected to 1D and 2D nuclear magnetic resonance (NMR) studies for structural confirmation. The toxicity of both was predicted using TOPKAT and ADMET™ software and compared to the drug.
['Kurmi|Moolchand|M|', 'Sahu|Archana|A|', 'Ladumor|Mayurbhai Kathadbhai|MK|', 'Kumar Bansal|Arvind|A|', 'Singh|Saranjit|S|']
D000818:Animals D044966:Anti-Retroviral Agents D002851:Chromatography, High Pressure Liquid D003198:Computer Simulation D004347:Drug Interactions D004355:Drug Stability D005079:Excipients D006801:Humans D009682:Magnetic Resonance Spectroscopy D008954:Models, Biological D015394:Molecular Structure D011237:Predictive Value of Tests D053719:Tandem Mass Spectrometry
Incompatibility Lactose monohydrate Interaction products Characterization Toxicity Abacavir sulphate