固体分散技术增强西尼地平的溶解度及评价

S. Mankar, Arpita Tupe
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摘要

西尼地平溶解度差,生物利用度低,限制了其治疗效果。研制稳定、有效、生物利用度高的剂型。有必要增加这类药物的溶解度。本研究旨在利用固体分散技术提高西尼地平的溶解度。采用溶剂蒸发法和熔体熔合法制备了不同聚合物的西尼地平固体分散体。用FT-IR光谱、差示扫描比色法和x射线衍射法对所制备的固体分散体的溶解度进行了评价。用西尼地平和波洛沙姆188以1:9的比例组成的溶剂蒸发技术制备的固体分散体溶解度最高,为21.07µg/mL。目前的研究表明,使用poloxam188进行固体分散是一种提高西尼地平溶解度和溶出速度的潜在有效方法。
本文章由计算机程序翻译,如有差异,请以英文原文为准。
Solubility enhancement and evaluation of Cilnidipine using solid Dispersion techniques
The poor solubility of Cilnidipine leads to low bioavailability and limits its therapeutic efficacy. To develop a dosage form that is stable, effective and has a higher bioavailability. It is necessary to increase the solubility of such medications. The present study aimed to improve the solubility by solid dispersion technique of Cilnidipine by solid dispersion techniques. Solvent evaporation and melt fusion methods were used to prepare solid dispersions of the drug cilnidipine with various polymers. The solubility of these prepared solid dispersions was evaluated by FT-IR spectroscopy, Differential Scanning Colorimetry and X-ray diffraction. The greatest solubility, of 21.07 µg/mL, was found in the solid dispersion that was developed by solvent evaporation technique employing a combination of Cilnidipine and Poloxamer 188 in a 1:9 ratio. The current investigation showed that solid dispersion using Poloxamer 188 can be a potentially effective method to increase the solubility and rate of dissolution of cilnidipine.
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