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ZHANG Ruiqing, YANG Wenqian, YU Yubing, TU Jiasheng, SUN Yixin. Pharmacokinetics of nifedipine matrix sustained-release pellets in rats and the relationship with CYP3A4[J]. Journal of China Pharmaceutical University, 2018, 49(4): 427-432. DOI: 10.11665/j.issn.1000-5048.20180407
Citation: ZHANG Ruiqing, YANG Wenqian, YU Yubing, TU Jiasheng, SUN Yixin. Pharmacokinetics of nifedipine matrix sustained-release pellets in rats and the relationship with CYP3A4[J]. Journal of China Pharmaceutical University, 2018, 49(4): 427-432. DOI: 10.11665/j.issn.1000-5048.20180407
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Pharmacokinetics of nifedipine matrix sustained-release pellets in rats and the relationship with CYP3A4

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  • 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.
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