检索结果-南通市图书馆

An Improved Synthetic Method of saquinavir

Chemical Research in Chinese Universities 2006年第1期22卷 51-55页

作者： YANG Qin-gang HE Xu-chang LEI Li-jun ZHOU Qi-ting BAI Dong-lu Shanghai Institute of Materia Medica Shanghai Institutes of Biological Sciences Chinese Academy of Sciences Shanghai 201203 P. R. China

An improved synthetic method of saquinavir, an HIV protease inhibitor, is described. In comparison with the methods in the reported works, the improved procedures had several advantages, such as less expensive agents, shorter reaction time, and a smaller amount of the solvent needed. To measure the optical purities of the products, the intermediates were determined by means of chiral HPLC. Some of the intermediates can also be used for the preparation of new protease inhibitors.

关键词： HIV Protease inhibitor saquinavir Synthesis

来源：

维普期刊数据库

同方期刊数据库评论

在线全文

学校读者我要写书评

暂无评论

Enhanced intestinal lymphatic absorption of saquinavir through supersaturated self-microemulsifying drug delivery systems

引用

Asian Journal of Pharmaceutical Sciences 2020年第3期15卷 336-346页

作者： Kanghee Jo Hyeongmin Kim Prakash Khadka Taejun Jang Soo Jin Kim Seong-Ha Hwang Jaehwi Lee College of Pharmacy Chung-Ang UniversitySeoul 06974Republic of Korea

The therapeutic potential of saquinavir, a specific inhibitor of human immunodeficiency virus(HIV)-1 and HIV-2 protease enzymes, has been largely limited because of a low solubility and consequnt low bioavailability. Thus, we aimed to design a supersaturated selfmicroemulsifying drug delivery system(S-SMEDDS) that can maintain a high concentration of saquinavir in gastro-intestinal fluid thorugh inhibiting the drug precipitation to enhance the lymphatic transport of saquinavir and to increase the bioavailability of saquinavir considerably. Solubilizing capacity of different oils, surfactants, and cosurfactants for saquinavir was evaluated to select optimal ingredients for preparation of *** the construction of pseudo-ternary phase diagram, SMEDDS formulations were established. A polymer as a precipitation inhibitor was selected based on its viscosity and drug precipitation inhibiting capacity. The S-SMEDDS and SMEDDS designed were administered at an equal dose to rats. At predetermined time points, levels of saquinavir in lymph collected from the rats were assessed. SMEDDS prepared presented a proper selfmicroemulsification efficiency and dispersion stability. The S-SMEDDS fabricated using the SMEDDS and hydroxypropyl methyl cellulose 2910 as a precipitation inhibitor exhibited a signficantly enhanced solubilizing capacity for saquinavir. The drug concentration in a simulated intestinal fluid evaluated with the S-SMEDDS was also maintained at higher levels for prolonged time than that examined with the SMEDDS. The S-SMEDDS showed a considerably enhanced lymphatic absoprtion of saquinavir in rats compared to the ***, the S-SMEDDS would be usefully exploited to enhance the lymphatic absorption of hydrophobic drugs that need to be targeted to the lymphatic system.

关键词： Lymphatic drug delivery Self-microemulsifying drug delivery system saquinavir Precipitation inhibitor Supersaturation Lipid-based formulation

来源：

维普期刊数据库

同方期刊数据库评论