Correlation between integrated pharmacokinetics and pharmacodynamics of bile processed Rhizoma Coptidis in febrile rats
10.16438/j.0513-4870.2015-0553
- VernacularTitle:胆黄连在实热证大鼠体内的整合药代动力学与药效学的相关性
- Author:
Jing WANG
1
;
Yue CHEN
1
;
Zi-min YUAN
1
Author Information
1. School of Pharmacy, Liaoning University of Traditional Chinese Medicine, Dalian 116600, China
- Publication Type:ORIGINAL ARTICLES
- Keywords:
bile processed Rhizoma Coptidis;
alkaloid;
excessive heat syndrome;
integrated pharmacokinetic;
pharmacodynamics
- From:
Acta Pharmaceutica Sinica
2016;51(1):127-
- CountryChina
- Language:Chinese
-
Abstract:
This study was designed to validate the correlation between integrated pharmacokinetic and therapeutic effects of alkaloids using bile processed Rhizoma Coptidis (BRC). Rats were divided into three groups: normal, disease model, model+BRC. Rats were induced to have an excessive heat syndrome. Rectal temperatures were collected at 0, 3, 6 and 9 h after single oral administration of the drugs. The plasma concentrations of three alkaloids were quantified at different times by UPLC-MS/MS after the administration of BRC. An approach of self-defined weighting coefficiency was created to the holistic pharmacokinetic profiles of alkaloids in BRC. The classified and integrated synthetic concentrations were obtained, and then the pharmacokinetic parameters of alkaloids were calculated from non-compartmental model analysis. The potential relationship between the integrated mean concentration of alkaloids and the antifebrile efficacy was investigated. The holistic tmax of alkaloids was 1.11 h, the antifebrile effect of BRC at 3 h was improved over the model group. Double peaking appeared in the integrated blood concentration-time curve, the second tmax of alkaloids was 4.82 h. The antifebrile effects of BRC at 3-6 h were significant, and the antifebrile effects at 6-9 h was decreased significantly. Dynamic variation of alkaloids of BRC in the body exhibited the similarity to the pattern of its antifebrile effect.
