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| 利用计算机模拟技术对头孢克肟口服固体制剂有效性的研究与评价 |
| Research and Assessment of the Efficacy of Cefixime Oral Solid Preparations Using Computer Simulation Techniques |
| 投稿时间：2019-07-09 修订日期：2019-10-25 |
| DOI： |
| 中文关键词: 头孢克肟，生理药代动力学，有效性，药物动力学（吸收、分布、代谢、排泄） |
| 英文关键词: cefixime,physiologically based pharmacokinetic（PBPK）,efficacy,ADME |
| 基金项目:国家科技重大专项课题-药物一致性评价关键技术与标准研究(2017ZX09101001-007) |
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| 中文摘要: |
| 本研究建立了一种头孢克肟口服固体制剂通用型有效性评价方法。通过对品种结构、理化性质、药代动力学特征和生物药剂学参数的研究和确证，结合静脉注射、口服等不同给药途径在比格犬及人类等不同种属中的药时曲线数据，建立并验证人口服头孢克肟的生理药代动力学模型，以此模拟口服头孢克肟在人体内的吸收、分布、代谢、消除过程，拟合药物在的累计吸收曲线，作为品种口服固体制剂溶出曲线的评价依据。通过对不同规格片剂、分散片、胶囊、颗粒剂和混悬剂的体内数据的验证比较，证实该模型应用的适用性和准确性。 |
| 英文摘要: |
| We constructed a method to assess the efficacy of cefixime oral-solid preparations. We carried out research and validation of the structural, physiochemical, pharmacokinetic, and biopharmaceutic characteristics of cefixime oral-solid preparations. These characterizations were combined with concentration-time-curve data, including when cefixime was administered orally or via intravenous injection to beagles and humans, to establish and validate a physiologically based pharmacokinetic model for oral cefixime in humans. This model was used to simulate the absorption, distribution, metabolism, and elimination of oral cefixime in humans. Additionally, the model was fitted to the cumulative-absorption curve of cefixime, and can therefore serve as a basis for assessing the dissolution curves of oral-solid preparations of different moieties. We verified the applicability and accuracy of this model through validation and comparison with in vivo data of different strengths of tablets, dispersible tablets, capsules, granules, and suspensions. |
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