方法通过提高溶解度和生物利用度来开发盐酸氯吡格雷的技术

Deevan Paul A., A. Neelima, Chitra Prasanthi, N. Kota
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摘要

盐酸氯吡格雷(CB)是一种结晶性、水溶性差的药物,生物利用度低于50%。该药物是血小板细胞膜上发现的P2Y12二磷酸腺苷受体的不可逆抑制剂。本研究使用不同的聚合物如聚乙烯吡咯烷酮(PVP) K-30和聚乙烯醇与不同的表面活性剂如Tween 80进行比较,并使用超崩解剂如淀粉乙醇酸钠(SSG)和微晶纤维素(MCC)。通过对粒径分布的分析,纳米颗粒的粒径范围为232.6 ~ 995.6 nm,多分散性指数范围为0.11 ~ 0.96,表明纳米颗粒具有良好的物理性质。硫酸氯吡格雷纳米颗粒的药物包封效率(DEE)在30.10% ~ 94.4%之间。研究发现,含PVP K-30和l -精氨酸的F2制剂与其他制剂相比,80min内释药最佳,最大累积释药量为96.8%,并对制备的硫酸氯吡格雷颗粒剂的7种制剂进行了溶出度研究,其中含氯旋维酮的F5制剂在80min内释药最大为91.6%。在这里,我们陈述了方法开发技术通过生产纳米颗粒来提高溶解度和生物利用度的研究。
本文章由计算机程序翻译,如有差异,请以英文原文为准。
Method Development Technologies for Clopidogrel Bisulphate by Improving Solubility and Bioavailability
Clopidogrel bisulphate (CB) is a crystalline, poorly water-soluble drug of bioavailability less than 50%. The drug is an irreversible inhibitor of the P2Y12 adenosine diphosphate receptor found on the membranes of platelet cells. The present work was performed using different polymers such as Polyvinylpyrrolidone (PVP) K-30 and polyvinyl alcohol with varied surfactants such as Tween 80 in comparison by using superdisintegrants like Sodium Starch Glycolate (SSG) and Microcrystalline Cellulose (MCC). By performing the particle size distribution, the size ranges from 232.6 nm to 995.6 nm and the polydispersity index ranges from 0.11 to 0.96, these ranges indicating the good physical nature of nanoparticles. The drug entrapment efficiency (DEE) of clopidogrel bisulphate nanoparticles was found to be in the range of 30.10% to 94.4%. From the study, it was found that F2 formulation containing PVP K-30 and L-arginine has given the best release in 80mins and the maximum cumulative drug release was 96.8% in comparison with other formulation, and the dissolution studies were performed for the seven formulations of prepared clopidogrel bisulphate granules among which F5 formulation containing crospovidone has given maximum drug release of 91.6% within 80mins. Here we state that the method development technologies improve the solubility and bioavailability studies by producing the nanoparticles.
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