• 中国精品科技期刊
  • 中国高校百佳科技期刊
  • 中国中文核心期刊
  • 中国科学引文数据库核心期刊
Advanced Search
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
Citation: 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

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

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)
More Information
  • Received Date: September 13, 2021
  • Revised Date: March 29, 2022
  • 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 cmax of form I and form II rifampicin were 8.42 and 10.35 μg/mL, tmax were 0.40 and 0.32 h,and AUC0-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.
  • [1]
    .J Occup Environ Med,2020,62(7):e355-e369.
    [2]
    Yulug B,Hanoglu L,Ozansoy M,et al.Therapeutic role of rifampicin in Alzheimer''s disease[J].Psychiatry Clin Neurosci,2018,72(3):152-159.
    [3]
    Allen FH.The Cambridge structural database:a quarter of a million crystal structures and rising[J].Acta Crystallogr B,2002,58(Pt3Pt1):380-388.
    [4]
    Censi R, di Martino P.Polymorph impact on the bioavailability and stability of poorly soluble drugs[J].Molecules,2015,20(10):18759-18776.
    [5]
    Guo LL.Investigation on polymorphs and crystallization process of rifampicin(利福平多晶型及其结晶过程研究)[D].Tianjin:Tianjin University,2018.
    [6]
    Zhao P,Zhang L,Grillo JA,et al.Applications of physiologically based pharmacokinetic (PBPK) modeling and simulation during regulatory review[J].Clin Pharmacol Ther,2011,89(2):259-267.
    [7]
    Poggesi I,Snoeys J,van Peer A.The successes and failures of physiologically based pharmacokinetic modeling:there is room for improvement[J].Expert Opin Drug Metab Toxicol,2014,10(5):631-635.
    [8]
    Agoram B,Woltosz WS,Bolger MB.Predicting the impact of physiological and biochemical processes on oral drug bioavailability[J].Adv Drug Deliv Rev,2001,50(Suppl 1):S41-S67.
    [9]
    U.S. Department of Health and Human Services Food and Drug Administration Center for Drug Evaluation and Research (CDER):Clinical drug interaction studies -cytochrome P450 enzyme-and transporter-mediated drug interactions guidance for industry[EB/OL].U.S.Food and Drug Administration,2020[2022-03-09].https://www.fda.gov/media/134581/download.
    [10]
    Amidon GL,Tsume Y.Oral product input to the GI tract: GIS an oral product performance technology[J].Front Chem Sci Eng,2017,11(4):516-520.
    [11]
    de Pinho Pessoa Nogueira L,de Oliveira YS,de C Fonseca J,et al.Crystalline structure of the marketed form of rifampicin:a case of conformational and charge transfer polymorphism[J].J Mol Struct,2018,1155:260-266.
    [12]
    Biganzoli E,Cavenaghi LA,Rossi R,et al.Use of a Caco-2 cell culture model for the characterization of intestinal absorption of antibiotics[J].Farmaco,1999,54(9):594-599.
    [13]
    Toutain PL,Bousquet-Mélou A.Plasma clearance[J].J Vet Pharmacol Ther,2004,27(6):415-425.
    [14]
    U.S.Food and Drug Administration.FDA approves RIFADIN? IV (rifampin for injection USP)[EB/OL].(2019-02-28)[2021-04-15https://www.accessdata.fda.gov/drugsatfda_docs/label/2019/050420s080,050627s023lbl.pdf.
    [15]
    Becker C,Dressman JB,Junginger HE,et al.Biowaiver monographs for immediate release solid oral dosage forms:Rifampicin[J].J Pharm Sci,2009,98(7):2252-2267.
  • Related Articles

    [1]MO Xinhe, WAN Youqiong, WANG Sibu, MA Qin, ZHANG Jun, CHEN Ying. Ameliorative effect of baicalin nanomedicine on hydrogen peroxide-induced senescence of human umbilical vein vascular endothelial cells[J]. Journal of China Pharmaceutical University, 2025, 56(1): 110-118. DOI: 10.11665/j.issn.1000-5048.2024052101
    [2]WANG Sibu, CHEN Ying, DING Yang, XIAO Ting, LIU Wen, SHEN Xiangchun, TAO Ling, LUO Xinghong. Preparation of paeonol nanoemulsion and investigation of vascular endothelial cells uptake[J]. Journal of China Pharmaceutical University, 2022, 53(6): 690-697. DOI: 10.11665/j.issn.1000-5048.20220607
    [3]DUAN Lanlan, DONG Jing, FAN Xiangcheng, ZHU Junyi, ZHANG Yifan, HAN Jichun, SHANG Jing. β-Elemene improves endothelial cells dysfunction, and abnormal proliferation and migration of vascular smooth muscle cells[J]. Journal of China Pharmaceutical University, 2020, 51(3): 333-339. DOI: 10.11665/j.issn.1000-5048.20200311
    [4]ZHU Chengyan, LIU Haochen, HE Hua, LIU Xiaoquan. Evaluating cerebral endothelial dysfunction induced by amyloid based on the time series model[J]. Journal of China Pharmaceutical University, 2018, 49(4): 456-462. DOI: 10.11665/j.issn.1000-5048.20180411
    [5]HE Shuying, XIONG Rui, LIU Kun, XU Yungen. Molecular mechanisms of combretastatin A-4 amino sugar derivative CPU-XT-008 on inhibiting proliferation of vascular endothelial cells[J]. Journal of China Pharmaceutical University, 2015, 46(5): 594-599. DOI: 10.11665/j.issn.1000-5048.20150513
    [6]LIU Yu, GU Yue, YUN Dong-jie, CHEN Jian-quan, LIU Si-guo, ZHANG Ai-min. Generation of fully human anti-vascular endothelial growth factor 165 monoclonal antibody with antitumor efficacy from transgenic five-feature mice[J]. Journal of China Pharmaceutical University, 2009, 40(3): 269-272.
    [7]Effects of Melatonin on the Immune Functions of Diabetic Rats Combined with Injury-induced Stress[J]. Journal of China Pharmaceutical University, 2004, (4): 71-74.
    [8]Effect of Lomerizine on the Activity of P-glycoprotein in Primary Cultured Rat Brain Microvessel Endothelial Cells[J]. Journal of China Pharmaceutical University, 2003, (4): 62-65.
    [9]Protective Effects of Shark Hepatic Stimulator Substance on Alloxan-induced Diabetes in Mice[J]. Journal of China Pharmaceutical University, 2003, (2): 59-63.
    [10]Influences on Serum Insulin and Glucose by Different Fasting Time in Alloxan Diabetic Mice[J]. Journal of China Pharmaceutical University, 2001, (3): 59-62.
  • Cited by

    Periodical cited type(2)

    1. 周德军,王珂洋,郝婷,张钰滢,赵桂琴. 三氮唑香豆素的合成进展. 化学研究与应用. 2024(04): 696-703 .
    2. 李卓远,史佳慧,刘楠,薛玉涛,李婉倩,蒋治坤,周佳雨,刘晖,熊山. 香豆素衍生物的生物活性研究进展. 精细与专用化学品. 2024(06): 23-30 .

    Other cited types(0)

Catalog

    Article views (517) PDF downloads (314) Cited by(2)

    /

    DownLoad:  Full-Size Img  PowerPoint
    Return
    Return