科研之友
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摘要
The aim of the present study was to design a new pH-enzyme double-dependent mesalamine colon-specific delivery system. The drug release behaviors in vitro and pharmacokinetics and biodistribution in vivo were further evaluated. The mean particle diameters of mesalamine-coated microparticles were 312.2 mu m. In vitro, a small amount of mesalamine was released in HCl at a pH of 1.2 and PBS medium at a pH of 7.4 for 5 hours, and 71% of the entrapped mesalamine was further released during the subsequent 20 hours of incubation. A greater area under the plasma concentration-time curve (AUC)(0-t) was obtained for the coated microparticles (1.9-fold) compared to the suspensions group, which indicated that the encapsulated mesalamine had mostly been absorbed in rats over the period of 12 hours. The AUC(0-t) of the coated microparticles in colon was 2.63-fold higher compared to the suspensions (P < 0.05). Hence, mesalamine-coated microparticles are considered to maintain the drug concentration within target ranges for a long period of time.
- 出版日期2016
- 单位上海中医药大学
