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含格列齐特的亚麻籽壳微粒的胃肠道转运及抗糖尿病作用

Gastrointestinal transition and anti-diabetic effect of Isabgol husk microparticles containing gliclazide.

作者信息

Sharma Vipin Kumar, Mazumder Bhaskar

机构信息

Department of Pharmaceutical Sciences, Faculty of Ayurved and Medical Sciences, Gurukul Kangri University, Haridwar 249404, Uttarakhand, India.

Department of Pharmaceutical Sciences, Dibrugarh University, Dibrugarh 786004, Assam, India.

出版信息

Int J Biol Macromol. 2014 May;66:15-25. doi: 10.1016/j.ijbiomac.2014.02.014. Epub 2014 Feb 14.

DOI:10.1016/j.ijbiomac.2014.02.014
PMID:24530641
Abstract

Isabgol husk with sodium alginate was formulated into gliclazide loaded microparticles which were characterized for particle size, swelling index, entrapment efficiency, in vitro release, release kinetics, stability, hypoglycemic effect, surface morphology, and gastrointestinal transition. The particle size in different formulations varied from 752.83 ± 0.630 to 872.03 ± 0.293 μm. It was analyzed by dissolution study that up to 98% of loaded gliclazide was released in simulated intestinal fluid (SIF, pH 7.4) within 8h. The formulations containing sodium alginate and Isabgol husk-sodium alginate showed bioequivalency with marketed sustained release tablets (Glizid MR 60(®)) in terms of release pattern. The drug maintained its integrity in terms of functional groups after fabrication in formulations as observed by FTIR analysis. The hypoglycemic effect of gliclazide loaded Isabgol husk-sodium alginate microparticles was found to be 37 ± 6.356% in terms of changes of blood glucose level from base glucose level (100%) in diabetic condition after 24h of oral administration and it was more than marketed conventional tablets (95.5 ± 3.286%). The retention of microparticles was observed in small intestine up to 10h during whole body X-ray imaging. The study revealed that microparticles composing of Isabgol husk may have the potential for regulating blood glucose level in diabetic animals with controlled release of gliclazide.

摘要

将洋车前子壳与海藻酸钠制成载有格列齐特的微粒,并对其粒径、溶胀指数、包封率、体外释放、释放动力学、稳定性、降血糖作用、表面形态和胃肠道转运进行了表征。不同制剂的粒径在752.83±0.630至872.03±0.293μm之间。通过溶出度研究分析发现,在模拟肠液(SIF,pH 7.4)中,8小时内高达98%的载药格列齐特被释放。含有海藻酸钠和洋车前子壳-海藻酸钠的制剂在释放模式方面与市售缓释片(Glizid MR 60(®))具有生物等效性。通过傅里叶变换红外光谱(FTIR)分析观察到,药物在制剂制备后其官能团方面保持完整。口服给药24小时后,载有格列齐特的洋车前子壳-海藻酸钠微粒在糖尿病状态下,相对于基础血糖水平(100%)的血糖水平变化而言,其降血糖作用为37±6.356%,高于市售传统片剂(95.5±3.286%)。在全身X射线成像过程中,在小肠中观察到微粒保留长达10小时。该研究表明,由洋车前子壳组成的微粒可能具有通过控制释放格列齐特来调节糖尿病动物血糖水平的潜力。

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