中国临床药理学与治疗学2025，Vol.30Issue(4)：493-500,8.DOI:10.12092/j.issn.1009-2501.2025.04.007
基于群体药动学模型的阿立哌唑微球给药方案研究
Optimizing the dosing regimen of aripiprazole microspheres by popu-lation pharmacokinetic modeling and simulation
摘要
Abstract
AIM:To optimize the clinical dosage and administration regimen of a novel long-acting injectable aripiprazole microsphere(LZMT05)using plasma concentration data from two clinical trials.METHODS:Plasma concentrations were collected from 196 schizophrenia patients administered LZMT05,and a population pharmacokinetic(Pop-PK)model was developed.The therapeutic window was defined as the steady-state trough-to-peak concentration range(94.0-534 ng/mL)of oral ar-ipiprazole.Multiple clinical scenarios were simulat-ed to identify the optimal regimen.RESULTS:A one-compartment model with dual first-order ab-sorption and first-order elimination characterized LZMT05 pharmacokinetics.Covariates like sex and CYP2D6 genotype were integrated into the final model.Simulations demonstrated that switching from 10 mg oral aripiprazole to 350 mg LZMT05 ev-ery 4 weeks sustained concentrations within the therapeutic window with minimal peak-to-trough fluctuations.CONCLUSION:The PopPK-guided opti-mized LZMT05 regimen maintained drug exposure within the therapeutic window,suggesting favor-able efficacy and safety.关键词
阿立哌唑/微球/群体药动学/建模模拟Key words
aripiprazole/microspheres/popula-tion pharmacokinetics/modeling and simulation分类
临床医学引用本文复制引用
孟庆恒,黄钦,韩智慧,雷琦,陈斌,尹霞,胡海棠,刘红霞,郑青山,许羚..基于群体药动学模型的阿立哌唑微球给药方案研究[J].中国临床药理学与治疗学,2025,30(4):493-500,8.基金项目
上海市2017年度"科技创新行动计划"项目(17401970900) （17401970900）
