Stability behaviour of antiretroviral drugs and their combinations. 4: Characterization of degradation products of tenofovir alafenamide fumarate and comparison of its degradation and stability behaviour with tenofovir disoproxil fumarate
| Autor: | Karimullah Shaik, Moolchand Kurmi, Saranjit Singh, Vijaya Madhyanapu Golla |
|---|---|
| Rok vydání: | 2016 |
| Předmět: |
0301 basic medicine
Drug Tenofovir Anti-HIV Agents media_common.quotation_subject 030106 microbiology Clinical Biochemistry Pharmaceutical Science 02 engineering and technology High-performance liquid chromatography Tenofovir alafenamide Analytical Chemistry 03 medical and health sciences Drug Stability Drug Discovery medicine Humans Prodrugs Spectroscopy media_common Chromatography Gastric fluid Chemistry Prodrug 021001 nanoscience & nanotechnology Anti-Retroviral Agents Degradation (geology) 0210 nano-technology Multistage mass spectrometry medicine.drug |
| Zdroj: | Journal of pharmaceutical and biomedical analysis. 131 |
| ISSN: | 1873-264X 6117-9612 |
| Popis: | In this study, stress degradation behaviour of tenofovir alafenamide fumarate (TAF), a novel prodrug of tenofovir, was investigated and compared with currently used prodrug congener, tenofovir disoproxil fumarate (TDF), whose intrinsic stability was reported by us earlier [14]. Also, pH stability and gastrointestinal stability studies were conducted on both the drugs. High performance liquid chromatography (HPLC) analysis of stressed samples of TAF revealed formation of six degradation products (DPs) against twelve characterized earlier in the case of TDF (RSC Adv. 5(2015) 96117-96129). Like TDF, characterization of DPs of TAF was done by using sophisticated hyphenated liquid chromatography-high resolution mass spectrometry (LC-HRMS) and multistage mass spectrometry (MSn) tools. pH-stability studies between pH 1.2-10 revealed greater stability of TAF, except in acidic conditions, where TAF was degraded extensively. Investigation of gastrointestinal stability in simulated gastric fluid (SGF), simulated intestinal fluid (SIF) and fed state simulated gastric fluid (FeSSGF) suggested that TAF must be administered in fed state, as the drug was practically stable in FeSSGF as compared to extensive loss at acidic pH and in SGF. |
| Databáze: | OpenAIRE |
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