二元和三元固体分散技术增强难溶性阿托伐他汀钙的溶解谱

Sarkar, A. Hossin, Asm Monjur Al Hossain, K. Sikdar, SZ Raihan, M. Hossain
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引用次数: 0

摘要

阿托伐他汀钙(ATV)是一种HMG-CoA(3-羟基-3-甲基戊二酰辅酶A)还原酶抑制剂,通常被称为胆固醇降低剂。作为一种水溶性差的药物,其绝对生物利用度非常低。为了提高水溶性和口服生物利用度,以不同的比例(1:0.5、1:1和1:2)使用不同的亲水性载体,通过简单的物理混合(PM)和融合或熔融技术制备可重复的ATV二元和三元固体分散体制剂。体外溶出度研究结果显示,在所有情况下,ATV三元SD制剂的累积药物释放百分比均大于二元制剂、一些上市产品和纯ATV粉末。对于三元SD制剂,载体在增强药物释放方面的顺序为kollidon 90F>预凝胶化淀粉>lutrol>kollidon 12F(分别为99.1%、98.8%、96%和95%),而纯ATV粉末和上市产品的累积释放百分比分别为70.8%、68.9%(B1)和73.1%(B2)。使用FT-IR和SEM进一步表征了表现最好的三元SD制剂ATV:Kollidon 90F(1:2)。SEM分析表明晶体药物转化为无定形形式,FT-IR数据表明药物与聚合物之间几乎没有或根本没有相互作用。孟加拉国科学杂志。Ind.Res.56(3),165-1762021
本文章由计算机程序翻译,如有差异,请以英文原文为准。
Enhancement of dissolution profile of poorly aqueous soluble atorvastatin calcium by binary and ternary solid dispersion techniques
Atorvastatin calcium (ATV) is an HMG-CoA (3-hydroxy-3-methylglutaryl coenzyme A) reductase inhibitor commonly known as a cholesterol-lowering agent. As a poorly water-soluble drug its absolute bioavailability is very low. To increase the water solubility as well as oral bioavailability, different hydrophilic carriers were used in different ratios (1:0.5, 1:1 and 1:2) to prepare reproducible binary and ternary solid dispersion formulations of ATV by simple physical mixing (PM) and fusion or melting technique. In vitro dissolution studies results revealed that in all cases, the cumulative percent drug release from ATV ternary SD formulations were greater than binary formulations, some marketed products and pure ATV powder. The order of the carriers in enhancing the drug release was found as kollidon 90F > pregelatinized starch > lutrol> kollidon 12F (99.1%, 98.8%, 96% and 95% respectively) for ternary SD formulations whereas pure ATV powder and marketed products showed cumulative percentage release 70.8%, 68.9% (B1) and 73.1% (B2), respectively. The best-out performed ternary SD formulation ATV:Kollidon 90 F (1:2) were further characterized using FT-IR and SEM. SEM analyses indicated conversion of crystal drug to amorphous form and FT-IR data suggested that little or no interaction between the drug and polymer. Bangladesh J. Sci. Ind. Res.56(3), 165-176, 2021
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