含阿托伐他汀钙的固体分散体在人体志愿者体内吸收研究

Kholoud Ali, Khaled Abozeid, M. Nasr
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摘要

目的:固体分散体是改善难水溶性药物的口服吸收和口服生物利用度的一种独特而有前途的方法。阿托伐他汀钙(ATV)是一种抗高血脂药物,根据生物制药分类系统(BCS),它属于II类药物,口服吸收后进行广泛的一过代谢,生物利用度为12%。本研究的目的是探讨以固体分散形式配制疏水药物(ATV)对其生物利用度的影响。方法:以poloxamer188为亲水性载体,采用微波诱导融合法制备ATV固体分散体(ATV- sd)。将合成的ATV- sd与其他成分一起压缩成片剂,并与ATV纯片剂进行对比,进行体外溶出度研究,比较制备的ATV- sd与ATV纯片的溶出度。采用健康男性志愿者(n = 6)进行体内研究,采用高效液相色谱法测定人血浆中药物水平。结果:体外溶出研究显示ATV-SD的溶出谱增强。药代动力学参数研究也显示口服ATV- sd片较纯ATV片增强,其中口服ATV- sd片AUC0-60h和Cmax较纯ATV片增加。结论:ATV- sd可作为提高ATV口服生物利用度的有效手段。
本文章由计算机程序翻译,如有差异,请以英文原文为准。
In vivo Absorption Study of Solid Dispersion Containing Atorvastatin Calcium in Human Volunteers
Objectives: Solid dispersion is a unique and promising approach for improving the oral absorption and oral bioavailability of the poorly water soluble drugs. Atorvastatin Calcium (ATV) is an anti-hyper lipidemic agent, It belongs to class II drugs according to the biopharmaceutical classification system (BCS), and undergoes extensive first-pass metabolism after oral absorption exhibiting 12% bioavailability. The Objective of the present study is to investigate the effect of formulating the hydrophobic drug (ATV) in a solid dispersion form on its bioavailability. Methods: ATV solid dispersion (ATV-SD) was prepared by microwave induced fusion method, containing poloxamer188 as a hydrophillic carrier. The resultant ATV-SD was compressed into tablets with other ingredients and was evaluated against pure ATV tablets, in vitro dissolution study was carried out to compare the dissolution profiles of the prepared ATV-SD against the pure form of ATV.  In vivo study was conducted using healthy male volunteers (n = 6). A high performance liquid chromatography method was employed to determine the level of drug in human plasma. Results: In vitro dissolution study revealed an enhancement in the dissolution profile of ATV-SD. The study of pharmacokinetics parameters also showed an enhancement after oral administration of ATV-SD tablet when compared with pure ATV tablets, where , the AUC0–60h and Cmax were increased after intake of ATV-SD tablets orally compared with that of pure ATV tablets. Conclusion: All these could be demonstrated that ATV-SD would be prospective means for enhancing higher oral bioavailability of ATV.
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