Amari J V, Brown P R, Pivarnik P E, Sehgal R K, Turcotte J G
Department of Chemistry, University of Rhode Island, Kingston 02881.
J Chromatogr. 1992 Jan 24;590(1):153-61. doi: 10.1016/0021-9673(92)87017-3.
The experimental anti-AIDS glycerophosphatidic acid: nucleoside (sn-1/sn-2 diacylglycerol:dideoxynucleotide) drugs 3'-azido-3'-deoxythymidine monophosphate diglyceride (AZT-MP-DG) and 2',3'-dideoxycytidine monophosphate diglyceride (ddC-MP-DG) were isolated and purified by reversed-phase high-performance liquid chromatography (HPLC). The chromatographic separation was based on the glycerophospholipid moiety of the drugs and detection of the nucleoside component. The separations were optimized on method development columns packed with the stationary phase to be used in the micro-preparative column and monitored by a UV detector. Fractions were collected and analyzed for purity by analytical-scale HPLC and by thin-layer chromatography (TLC). The purity of the recovered drugs based on UV and light-scattering detection and on TLC was greater than 99%. The purified compounds were isolated for studies on structure confirmation, physical, biophysical and formulation properties and anti-HIV efficacy in culture.
核苷（sn-1/sn-2二酰基甘油：双脱氧核苷酸）药物3'-叠氮基-3'-脱氧胸苷单磷酸二甘油酯（AZT-MP-DG）和2'，3'-双脱氧胞苷单磷酸二甘油酯（ddC-MP-DG）通过反相高效液相色谱法（HPLC）进行分离和纯化。色谱分离基于药物的甘油磷脂部分并检测核苷成分。在装有将用于微型制备柱的固定相的方法开发柱上对分离进行优化，并通过紫外检测器进行监测。收集馏分，并通过分析规模的HPLC和薄层色谱法（TLC）分析纯度。基于紫外和光散射检测以及TLC，回收药物的纯度大于99%。分离出纯化的化合物用于结构确证、物理、生物物理和制剂性质以及在培养物中的抗HIV功效研究。
