Pharmacokinetics and pharmacodynamics of Tongshuan Jiuxin pH-Dependent Delayed-release Capsula in dogs in vivo
- VernacularTitle:通栓救心pH依赖型缓释胶囊在犬体内的药动学和药效学研究
- Author:
Yeling YU
;
Xin ZHENG
;
Xing TANG
- Publication Type:Journal Article
- Keywords:
Tongshuan Jiuxin pH-Dependent Delayed-release Capsula;
Tongshuan Jiuxin Tablet;
pharmacokinetics;
pharmacodynamics;
paeonol
- From:
Chinese Traditional and Herbal Drugs
1994;0(05):-
- CountryChina
- Language:Chinese
-
Abstract:
Objective To prepare Tongshuan Jiuxin pH-Dependent Delayed-release Capsula and study its pharmacokinetics and pharmacodynamics in dogs in vivo. Methods Borneol and the extracts of Cortex Moutan, Rhizoma Chuanxiong, and Rhizoma Cyperi prepared by CO2 supercritical fluid extraction method were solidified or included with ?-cyclodextrin. Pellets were prepared by means of powder layering with the solidified extracts and borneol. The pH-dependent delayed-release pellet system was prepared by coating with HPMC, Eudragit L-30D-55, and Eudragit L100-S100 (1∶5) combinations, respectively. Tongshuan Jiuxin pH-Dependent Delayed-release Capsula was prepared by mixing the three kind of pellets at the ratio of 1∶1∶1. The concentration of paeonol in plasma was determined by HPLC and the pharmacodynamic parameters were evaluated by serum pharmacology method. Results The results from the paeonal concentration in plasma showed that the mean residence time (MRT) in vivo were 8.04 h for Tongshuan Jiuxin pH-Dependent Delayed-release Capsula and 2.89 h for Tongshuan Jiuxin Tablet, and the relative bioavailability was 126.3%. Meanwhile, the results from the pharmcodynamic parameters evaluated by serum pharmacology method showed that the MRT were 11.27 h for Tongshuan Jiuxin pH-Dependent Delayed-release Capsula and 5.94 h for Tongshuan Jiuxin Tablet, and the relative bioavailability was 129.1%. Conclusion Tongshuan Jiuxin Tablet has the characteristics of rapid absorption, qucik elimination, and shorter action-maintaining time. Whereas Tongshuan Jiuxin pH-Dependent Delayed-release Capsula has the characteristics of rapid absorption, prolonged and relaxed effective action compared with Tongshuan Jiuxin Tablet.