Synthesis Of M-Nifedipine Analogues And Its Intestinal Absorption Prediction

Aim: To investigate the intestinal absorption kinetics of m-Nifedipine and its analogues by Caco-2 cell lines to give more evidences on the research and development of DHPs.Methods: 1. The m-nifedipine and its analogues were synthesized by reformative line. In the synthetic procedures of m-Nif, strong aqua ammonia was used to take place of NH₄HCO₃. In the synthesis of MN9202, m-Nif was hydrolysized to produce intermediate in alkaline condition at first, then the intermediate was esterificated with n-butanol. The compounds were analyzed by RT-HPLC and were determined. 2. The method used for analyzing the m-Nifedipine and its analogues in bio-medium samples by RT-HPLC was founded. 3. Matured Caco-2 cells were incubated with 100uM m-Nif, MN9201, MN9202 and MN9203 for 5, 10, 20, 30, 40, 60 min respectively, then the drugs absorbed by cells were determined by RT-HPLC to investigate the relationship between time and the uptake of drugs. 4. m-Nif, MN9201,...