دورية أكاديمية
Mechanistic Framework to Predict Maternal-Placental-Fetal Pharmacokinetics of Nifedipine Employing Physiologically Based Pharmacokinetic Modeling Approach.
| العنوان: | Mechanistic Framework to Predict Maternal-Placental-Fetal Pharmacokinetics of Nifedipine Employing Physiologically Based Pharmacokinetic Modeling Approach. |
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| المؤلفون: | Werdan Romão MA; Laboratório de Farmacometria (LabFarma), Faculdade de Farmácia, Universidade Federal do Rio de Janeiro, Rio de Janeiro, RJ, Brazil., Pinto L; Universidade Federal de Ouro Preto, Ouro Preto, MG, Brazil., Cavalli RC; Departamento de Obstetrícia e Ginecologia, Faculdade de Medicina de Ribeirão Preto, Universidade de São Paulo, Ribeirão Preto, SP, Brazil., Duarte G; Departamento de Obstetrícia e Ginecologia, Faculdade de Medicina de Ribeirão Preto, Universidade de São Paulo, Ribeirão Preto, SP, Brazil., de Moraes NV; Center for Pharmacometrics and Systems Pharmacology, Department of Pharmaceutics, College of Pharmacy, University of Florida, Orlando, FL, USA., Abduljalil K; Simcyp Division, Certara UK Limited, Sheffield, UK., Moreira FL; Laboratório de Farmacometria (LabFarma), Faculdade de Farmácia, Universidade Federal do Rio de Janeiro, Rio de Janeiro, RJ, Brazil. |
| المصدر: | Journal of clinical pharmacology [J Clin Pharmacol] 2024 May; Vol. 64 (5), pp. 568-577. Date of Electronic Publication: 2024 Feb 02. |
| نوع المنشور: | Journal Article; Research Support, Non-U.S. Gov't |
| اللغة: | English |
| بيانات الدورية: | Publisher: Wiley Country of Publication: England NLM ID: 0366372 Publication Model: Print-Electronic Cited Medium: Internet ISSN: 1552-4604 (Electronic) Linking ISSN: 00912700 NLM ISO Abbreviation: J Clin Pharmacol Subsets: MEDLINE |
| أسماء مطبوعة: | Publication: 2013- : Oxford : Wiley Original Publication: Stamford, Conn., Hall Associates. |
| مواضيع طبية MeSH: | Nifedipine*/pharmacokinetics , Nifedipine*/administration & dosage , Maternal-Fetal Exchange* , Models, Biological* , Placenta*/metabolism, Humans ; Pregnancy ; Female ; Caco-2 Cells ; Fetus/metabolism ; Adult ; Cytochrome P-450 CYP3A/metabolism |
| مستخلص: | Nifedipine is used for treating mild to severe hypertension and preventing preterm labor in pregnant women. Nevertheless, concerns about nifedipine fetal exposure and safety are always raised. The aim of this study was to develop and validate a maternal-placental-fetal nifedipine physiologically based pharmacokinetic (PBPK) model and apply the model to predict maternal, placental, and fetal exposure to nifedipine at different pregnancy stages. A nifedipine PBPK model was verified with nonpregnant data and extended to the pregnant population after the inclusion of the fetoplacental multicompartment model that accounts for the placental tissue and different fetal organs within the Simcyp Simulator version 22. Model parametrization involved scaling nifedipine transplacental clearance based on Caco-2 permeability, and fetal hepatic clearance was obtained from in vitro to in vivo extrapolation encompassing cytochrome P450 3A7 and 3A4 activities. Predicted concentration profiles were compared with in vivo observations and the transplacental transfer results were evaluated using 2-fold criteria. The PBPK model predicted a mean cord-to-maternal plasma ratio of 0.98 (range, 0.86-1.06) at term, which agrees with experimental observations of 0.78 (range, 0.59-0.93). Predicted nifedipine exposure was 1.4-, 2.0-, and 3.0-fold lower at 15, 27, and 39 weeks of gestation when compared with nonpregnant exposure, respectively. This innovative PBPK model can be applied to support maternal and fetal safety assessment for nifedipine at various stages of pregnancy. (© 2024, The American College of Clinical Pharmacology.) |
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| معلومات مُعتمدة: | E-26/204.526/2022 Fundação Carlos Chagas Filho de Amparo à Pesquisa do Estado do Rio de Janeiro |
| فهرسة مساهمة: | Keywords: PBPK; fetus; nifedipine; placenta; pregnancy |
| المشرفين على المادة: | I9ZF7L6G2L (Nifedipine) EC 1.14.14.1 (Cytochrome P-450 CYP3A) |
| تواريخ الأحداث: | Date Created: 20240202 Date Completed: 20240424 Latest Revision: 20240424 |
| رمز التحديث: | 20240425 |
| DOI: | 10.1002/jcph.2404 |
| PMID: | 38305718 |
| قاعدة البيانات: | MEDLINE |
Full Text Finder | تدمد: | 1552-4604 |
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| DOI: | 10.1002/jcph.2404 |