Pharmacokinetics of nifedipine matrix sustained-release pellets in rats and the relationship with CYP3A4
10.11665/j.issn.1000-5048.20180407
- VernacularTitle:硝苯地平骨架型缓释微丸在大鼠体内药代动力学及其与CYP3A4代谢酶活性的关系
- Author:
Ruiqing ZHANG
1
;
Wenqian YANG
;
Yubing YU
;
Jiasheng TU
;
Yixin SUN
Author Information
1. 南京医科大学附属儿童医院
- Publication Type:Journal Article
- Keywords:
nifedipine;
sustained-release pellets;
pharmacobinetics;
CYP3A4;
6β-hydroxycortisol;
hydrocortisone
- From:
Journal of China Pharmaceutical University
2018;49(4):427-432
- CountryChina
- Language:Chinese
-
Abstract:
To conduct the characterization of its pharmacokinetics in rats of nifedipine sustained-release pellets and to study the relationship between the pellets and CYP3A4 activity. A gradient HPLC method was developed to simultaneously determine 6β-hydroxycortisol and hydrocortisone. CYP3A4 activity of rats was quantified by urinary ratio of 6β-hydroxycortisol/hydrocortisone after intravenous injection of hydrocortisone as a biomarker. HPLC method was also developed to quantify the drug concentration in plasma of rats, and the studies of pharmacokinetics were performed after oral administration of single dose of two formulations: Nifedipine matrix sustained-release pellets and nifedipine tablet(using as control). The results showed that the ratio of ten rats was 0. 271±0. 129. cmax of nifedipine sustained-release pellets decreases by nearly 70%, tmax significantly increased by 400% and t1/2 and MRT significantly increased by 230% compared to control. Nifedipine sustained-release pellets had a significant sustained-release property compared to the control and CYP3A4 activity affected its pharmacokinetics behavior.
