利用溶解度增强技术配制和评价水溶性差的药物 "格列美脲 "口服分散片

Nimisha Solanki, Arpit Gawshinde, Komal Tikariya, Dharmendra Solanki, U. Atneriya
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摘要

本研究涉及的格列美脲(GMP)是一种水溶性较差的药物。根据 BCS,格列美脲属于 II 级--高渗透性和低溶解性。本研究项目的目标是利用溶解度增强技术提高格列美脲的溶解度。努力的方向是通过使用超级崩解剂来提高格列美脲的溶解度,从而增强奥罗分散片的崩解能力。为了提高 GMP 的溶解度,我们选择了一种方法,即固体分散技术,因为固体分散技术是提高水溶性差的药物的溶解速率并进而提高其生物利用率的一种有效方法。使用的聚合物是 PEG 4000 和 PEG 6000,通过两种方法(即熔融法和溶剂蒸发法)以不同比例制备固体分散体。溶剂蒸发法能更好地提高药物的溶解度。格列美脲口服分散片采用直接压片法制备。格列美脲口服分散片使用了不同的超级崩解剂,如淀粉乙醇酸钠、交联聚维酮和卡莫司琼糖钠。此外,还对片剂的形状和颜色、厚度、硬度、易碎性、重量变化、药物含量均匀性、体外溶出率研究和体外崩解时间等后评价参数进行了评价和讨论。
本文章由计算机程序翻译,如有差异,请以英文原文为准。
Formulation and Evaluation of Oral Dispersible Tablet of Poorly Water-Soluble Drug ‘Glimepiride’ by Using Solubility Enhancement Technique
The present study is regarding Glimepiride (GMP) is poorly water-soluble drug. According to the BCS, Glimepiride undergoes Class II - High Permeability and Low Solubility. The objective of the research project is to enhance the solubility of Glimepiride by using solubility enhancement techniques. The endeavor is to improve its solubility by using super disintegrating agent to enhance the ability of disintegration of Oro dispersible tablet. To enhance of solubility of GMP, our select the method i.e. solid dispersion technique because Solid dispersion is an effective way of improving the dissolution rate of poorly water-soluble drugs and hence its bioavailability. The polymers used were PEG 4000 and PEG 6000 for prepared solid dispersions in different ratio by two method i.e. Fusion and solvent evaporation method. The solvent evaporation method is better result of drug for enhancement of solubility. Oral dispersible tablet of Glimepiride was prepared by direct compression method. ODTs of glimepiride by using different super disintegrants such as sodium starch glycolate, cross povidone and croscarmellose sodium. Further, post evaluation parameters like Shape and Color of Tablets, Thickness, hardness, friability, weight variation, Uniformity of Drug Content, In vitro Dissolution Rate Studies and In-vitro disintegration time were also evaluated and the results were discussed.
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