卡比多巴-左旋多巴口服缓释胶囊制剂(IPX066)与速释卡比多巴-左旋多巴(Sinemet(®))、缓释卡比多巴-左旋多巴(Sinemet(®)CR)、卡比多巴-左旋多巴-恩他卡彭(Stalevo(®))的药代动力学比较

IF 2.4 4区医学 Q3 PHARMACOLOGY & PHARMACY

Journal of clinical pharmacology Pub Date : 2015-09-01 Epub Date: 2015-05-20 DOI:10.1002/jcph.514

Ann Hsu, Hsuan-Ming Yao, Suneel Gupta, Nishit B Modi

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引用次数: 60

摘要

IPX066 (carbidopa-左旋多巴缓释[ER CD-LD])是一种卡比多巴和左旋多巴的口服缓释胶囊制剂。ER CD-LD(2胶囊)单剂量药代动力学研究;在健康受试者中评估总剂量，97.5 mg-390 mg CD-LD)与速释(IR) CD-LD (25 mg-100 mg)、缓释(CR) CD-LD (25 mg-100 mg)和CD-LD-恩他卡彭(25 mg-100 mg-200 mg)。IR给药后，LD在1小时达到峰值浓度(Cmax);随后，LD浓度迅速下降，5小时后降至峰值的10%以下。CR CD-LD和CD-LD-entacapone在1.5 h达到最大剂量，6.3 h和7.5 h浓度分别低于峰值的10%。ercd -LD和IR CD-LD的初始浓度增加相似，且比CR CD-LD和CD-LD-entacapone更快。ER CD- LD的LD浓度持续约5小时，直到10.1小时才降至峰值的10%。ER CD-LD的剂量标准化LD Cmax值显著低于其他CD-LD产品(P< 0.05)。相对于IR CD-LD、CR CD-LD和CD-LD-entacapone, ER CD-LD的生物利用度分别为83.5%、78.3%和58.8%。

本文章由计算机程序翻译，如有差异，请以英文原文为准。

Comparison of the pharmacokinetics of an oral extended-release capsule formulation of carbidopa-levodopa (IPX066) with immediate-release carbidopa-levodopa (Sinemet(®)), sustained-release carbidopa-levodopa (Sinemet(®) CR), and carbidopa-levodopa-entacapone (Stalevo(®)).

查看原文本刊更多论文

IPX066 (extended-release carbidopa-levodopa [ER CD-LD]) is an oral extended-release capsule formulation of carbidopa and levodopa. The single-dose pharmacokinetics of ER CD-LD (as 2 capsules; total dose, 97.5 mg-390 mg CD-LD) versus immediate-release (IR) CD-LD (25 mg-100 mg), sustained-release (CR) CD-LD (25 mg-100 mg), and CD-LD-entacapone (25 mg-100 mg-200 mg) was evaluated in healthy subjects. Following IR dosing, LD reached peak concentrations (Cmax ) at 1 hour; LD concentrations then decreased rapidly and were less than 10% of peak by 5 hours. With CR CD-LD and CD-LD-entacapone, LD Cmax occurred at 1.5 hours, and concentrations were less than 10% of peak by 6.3 and 7.5 hours, respectively. The initial increase in LD concentration was similar between ER CD-LD and IR CD-LD and faster than for CR CD-LD and CD-LD-entacapone. LD concentrations from ER CD---LD were sustained for approximately 5 hours and did not decrease to 10% of peak until 10.1 hours. Dose-normalized LD Cmax values for ER CD-LD were significantly lower (P< .05) than for the other CD-LD products. Bioavailability of LD from ER CD-LD was 83.5%, 78.3%, and 58.8% relative to IR CD-LD, CR CD-LD, and CD-LD-entacapone, respectively.

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来源期刊

Journal of clinical pharmacology 医学-药学

CiteScore

5.10

自引率

3.40%

发文量

176

审稿时长

2 months

期刊介绍： The Journal of Clinical Pharmacology (JCP) is a Human Pharmacology journal designed to provide physicians, pharmacists, research scientists, regulatory scientists, drug developers and academic colleagues a forum to present research in all aspects of Clinical Pharmacology. This includes original research in pharmacokinetics, pharmacogenetics/pharmacogenomics, pharmacometrics, physiologic based pharmacokinetic modeling, drug interactions, therapeutic drug monitoring, regulatory sciences (including unique methods of data analysis), special population studies, drug development, pharmacovigilance, womens’ health, pediatric pharmacology, and pharmacodynamics. Additionally, JCP publishes review articles, commentaries and educational manuscripts. The Journal also serves as an instrument to disseminate Public Policy statements from the American College of Clinical Pharmacology.