Dissolution enhancement of glimepiride dispersion using glyceryl monostearate and β-cyclodextrin as carrier.

Abu Shuaib Rafshanjani, Mofizur Rahman, S. Parvin, A. Kader
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引用次数: 3

Abstract

Glimepiride is an antidiabetic drug of sulfonylurea group and indicated for the treatment of type 2 diabetes mellitus. The present study was conducted to enhance the dissolution rate of glimepiride solid lipid nano particle dispersions using hot homogenization method and glimepiride solid dispersion by precipitation method. Solid lipid nanoparticles have been used as suitable carriers for delivery of drug with poor solubility. In this investigation glyceryl monostearate and stearic acid were used as solid lipid, Lutrol F-68 as surfactant, Tween 80 as stabilizer and the used polymer were urea crystal and β-cyclodextrin. Three formulations were prepared in different ratios for two methods and were designated as GMLN1 to GMLN3 in case of hot homogenization method and GMP1 to GMP3 for precipitation method. The evaluation of all the dispersions were done by in vitro dissolution studies using US Pharmacopeia type II apparatus (paddle method) in 900ml distilled water at 50 rpm to a temperature of 37°C ± 0.5°C for 45 minutes. In situ and externally sink method revealed the release pattern of drug was found to follow zero order, first order and Korsmeyer-Peppas equations. Improved dissolution profile was observed in all the solid lipid nano particle dispersions as compared to pure drug as well as market preparation. Thus, glyceryl monostearate and β-cyclodextrin can be successfully used as carrier for improvement of dissolution and bioavailability of glimepiride. Rafshanjani et al., International Current Pharmaceutical Journal, September 2015, 4(10): 436-441
单硬脂酸甘油和β-环糊精为载体增强格列美脲分散体的溶出度。
格列美脲是磺脲类抗糖尿病药物,适用于2型糖尿病的治疗。本研究分别采用热均质法和沉淀法提高格列美脲固体脂质纳米颗粒分散体的溶出率。固体脂质纳米颗粒已被用作运载溶解度差的药物的合适载体。本实验以单硬脂酸甘油酯和硬脂酸为固体脂质,Lutrol F-68为表面活性剂,Tween 80为稳定剂,使用的聚合物为尿素晶体和β-环糊精。两种方法按不同比例配制三种配方,热均质法为GMLN1 ~ GMLN3,沉淀法为GMP1 ~ GMP3。使用美国药典II型仪器(桨叶法),在900ml蒸馏水中,以50 rpm的转速,37°C±0.5°C, 45分钟,对所有分散体进行体外溶出研究。体外沉降法和原位沉降法发现药物的释放模式遵循零阶、一阶和Korsmeyer-Peppas方程。与纯药物和市场制剂相比,所有固体脂质纳米颗粒分散体的溶解谱都有所改善。因此,单硬脂酸甘油酯和β-环糊精可以作为改善格列美脲溶出度和生物利用度的载体。Rafshanjani et .,国际现代医药杂志,2015,4(10):436-441
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