Prediction of the bioequivalence of different crystal forms of rifampicin based on physiologically based pharmacokinetic model

CAI Qilin; LI Wenxing; YAN Zhen; YIN Lifang

doi:10.11665/j.issn.1000-5048.20220211

Journal of China Pharmaceutical University > 2022 > 53(2): 207-214. > DOI: 10.11665/j.issn.1000-5048.20220211

CAI Qilin, LI Wenxing, YAN Zhen, YIN Lifang. Prediction of the bioequivalence of different crystal forms of rifampicin based on physiologically based pharmacokinetic model[J]. Journal of China Pharmaceutical University, 2022, 53(2): 207-214. DOI: 10.11665/j.issn.1000-5048.20220211

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Prediction of the bioequivalence of different crystal forms of rifampicin based on physiologically based pharmacokinetic model

1.
Department of Pharmaceutics,School of Pharmacy, China Pharmaceutical University,Nanjing 210009
2.
Engineering Ｒesearch Center for Development and Evaluation of Sustained-Ｒelease Intelligent Preparations and Key Functional Excipients of Jiangsu Province,Nanjing 210009, China

Funds: This study was supported by the Advantage Discipline Project of Jiangsu (III)—The Disruptive Theory and Technology Innovative Research Team Project; and the China Pharmaceutical University "Major Scientific and Technological Achievements Transformation" Project (Research on the Industrialization of High-end Slow and Controlled Release Preparations)

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Received Date: September 13, 2021
Revised Date: March 29, 2022

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Abstract

The physiologically based pharmacokinetic (PBPK) modeling strategy was adopted to predict the pharmacokinetic behavior of crystal forms I and II of rifampicin in humans, which was used to determine whether the two were bioequivalent.After conducting studies in vitro of the two crystal forms, a rat PBPK model was established based on the pharmacokinetic data of intravenous administration in rats.The model was optimized by the pharmacokinetic data of oral administration in rats.Species were extrapolated to healthy humans, and the extrapolation model was used to predict such pharmacokinetic behaviors as the drug-time curve, absorption site, and absorption amount of the two crystal forms of rifampicin in healthy humans.The prediction results of the healthy human model showed that the c_max of form I and form II rifampicin were 8.42 and 10.35 μg/mL, t_max were 0.40 and 0.32 h,and AUC_0-_t were both 62.90 μg·h/mL.According to the prediction results of absorption, neither crystal form I nor crystal form II rifampicin was absorbed in the stomach, yet both were completely absorbed in the intestinal tract, with both the absorption site and the absorption amount were basically the same.The pharmacokinetic parameters of both crystal forms I and II of rifampicin were very close, which could indicate bioequivalence.
- rifampicin,
- crystal form,
- GastroPlus^TM,
- PBPK model,
- species extrapolation

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