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Title: Pharmacokinetics of nifedipine sustained release tablets in healthy subjects after a single oral administration: Bioequivalence study and Food effects
  • +5
  • youxuan Wu,
  • xuefeng zhong,
  • Xiaomin Li,
  • Wanli Liu,
  • Yanxin Zhang,
  • qiuying shen,
  • Sumei Xu,
  • Pingsheng Xu
youxuan Wu
Xiangya Hospital Central South University
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xuefeng zhong
Xiangya Hospital Central South University
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Xiaomin Li
Xiangya Hospital Central South University
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Wanli Liu
Xiangya Hospital Central South University
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Yanxin Zhang
Xiangya Hospital Central South University
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qiuying shen
Xiangya Hospital Central South University
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Sumei Xu
Xiangya Hospital Central South University

Corresponding Author:1107754823@qq.com

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Pingsheng Xu
Xiangya Hospital Central South University
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Abstract

Aim: This study has been designed to assess the bioequivalence of the newly developed delayed-release oral tablets (test) 30 mg nifedipine compared to its marketed counterpart (30 mg; reference) in healthy adult Chinese volunteers. Methods: We conducted randomized, open-label, four-period, crossover trials, including a fasting trial and a fed trial. The subjects were administered the test or reference products in a 1:1 ratio at random throughout each period with 7 days washout period. Then, in the next session, they got the alternate products. Liquid chromatography-tandem mass spectrometry and WinNonlin software were used to evaluate the bioequivalence of nifedipine peak blood concentration (Cmax) and area under the concentration-time curve (AUC). Result: A total of 46 subjects participated in the fasting trial and 48 subjects in the postprandial trial. In both cases, the 90% CI of the geometric mean ratios of Cmax, AUC0-t and AUC0-∞ were in the equivalence range (80-125%). When nifedipine was given concomitantly with a high-fat meal, tmax was approximately twofold earlier, absorption was approximately 4.8% less, and Cmax changed little compared to fasting conditions. In addition, no serious adverse events were observed in the subjects. Conclusion: This study confirms the bioequivalence of the test and reference formulations of nifedipine extended-release tablets under fasting and postprandial conditions. Food giving leads to a much earlier Tmax, which is different from the results of other studies. The effect of food effect on the pharmacokinetics of nifedipine needs to be further explored.