阿托伐他汀分散自微乳化片的研制

K. Midha, M. Nagpal, G. Aggarwal, T. G. Singh
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引用次数: 6

摘要

目的:为提高阿托伐他汀的溶解度和口服生物利用度,研制阿托伐他汀分散自微乳化(SMEDDS)片。材料与方法:以油、表面活性剂和助表面活性剂为原料,采用水滴定法制备液体SMEDDS,经固体载体(Neusilin US2)吸附转化为固体SMEDDS (S-SMEDDS)。将S-SMEDDS与乙醇酸淀粉钠(崩解剂)和片剂赋形剂混合,压缩成具有分散性和自微乳化性质的片剂。对各配方进行了重量变化、硬度、脆性、崩解试验等理化指标的评定。进行了纯药、SMEDDS、S-SMEDDS及分散片的体外研究。结果:60 min内药物纯释药率仅为29.84±0.16%,所有SMEDDS制剂(即SMEDDS;S-SMEDDS和分散的sme片)在相对较短的时间内释放100%的药物。在体外研究中,含有阿托伐他汀、30%油酸、65%吐温80和5%共表面活性剂的配方显示出最好的效果。但是,FB1(片剂)被认为是最好的,因为它在35分钟内释放100%的药物,并且在稳定性和患者依从性方面也优于SMEDDS和S-SMEDDS。结论:本研究揭示了SMEDDS分散片用于阿托伐他汀等疏水药物口服给药的潜在应用前景。关键词:阿托伐他汀;生物利用度;相图;
本文章由计算机程序翻译,如有差异,请以英文原文为准。
Development of Dispersible Self-microemulsifying Tablet of Atorvastatin
Aim: The aim of this study was to develop dispersible self-microemulsifying (SMEDDS) tablet of atorvastatin for promoting its solubility and thus its oral bioavailability. Materials and Methods: The liquid SMEDDS were prepared by water titration method using oil, surfactant and co-surfactant and converted into solid- SMEDDS (S-SMEDDS) by adsorption on solid carriers (Neusilin US2). The S-SMEDDS were blended with sodium starch glycolate (disintegrant) and tablet excipients and compressed into tablets that were dispersible and self-microemulsifying in nature. All these formulations were assessed for various physicochemical parameters viz. weight variation, hardness, friability, disintegration test. In vitro studies of pure drug, SMEDDS, S-SMEDDS and dispersible SME-tablets were carried out. Results: Pure drug released only 29.84 ± 0.16% upto 60 minutes and all the SMEDDS formulations (i.e. SMEDDS. S-SMEDDS and dispersible SME-tablets) released 100% of drug in comparatively lesser time. Formulations containing atorvastatin, 30% oleic acid, 65% tween 80 and 5% co-surfactant came out to show the best results in in vitro studies. But, FB1 (tablet) was considered to be the best since it released 100% drug in 35 min and also has advantages over SMEDDS and S-SMEDDS in terms of stability and patient compliance. Conclusion: The study revealed the potential use of dispersible SMEDDS tablet for the oral delivery of hydrophobic drugs, such as atorvastatin. Key words: Atorvastatin, Bioavailability, Phase diagram, SMEDDS.
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