微乳法与溶剂蒸发法提高苯磺酸氨氯地平溶解度的比较

JULY ISSUE Pub Date : 2022-07-02 DOI:10.47836//mjmhs18.4.19
Raja Nurul Batrisyia Hamzah, Long Chiau Ming, A. H. Helal Uddin, Z. Sarker, Kai Bin Liew, Yik Ling Chew
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引用次数: 1

摘要

苯磺酸氨氯地平是一种钙通道阻滞剂,适用于高血压和心绞痛。它被描述为微溶于水,由于其溶解度有限,可能导致生物利用度差。本研究的目的是利用溶剂蒸发法和微乳液法提高苯磺酸氨氯地平的溶解度,并对两种方法进行比较。方法:采用溶剂蒸发法制备苯磺酸氨氯地平固体分散体。PEG6000为首选聚合物,采用不同的药聚合物比。评价制备的SDs包括溶解度研究,溶解研究和扫描电子显微镜(SEM)。微乳技术方面,采用相滴定法制备微乳,并对优化后的微乳配方进行了溶解度和溶出度的表征。结果:药聚合物比为1:4的SD3溶解度最高,为96.97 mg/ml±0.92;优化后的微乳溶解度为112.54 mg/ml±0.92。在溶剂蒸发法中,随着药物与聚合物比的增加,SDs的溶解度和溶出率增加。结论:两种方法均能显著提高苯磺酸氨氯地平的溶解度,但微乳法具有更好的溶解度。
本文章由计算机程序翻译,如有差异,请以英文原文为准。
Comparison of Microemulsion and Solvent Evaporation Technique for Solubility Enhancement of Amlodipine Besylate
Introduction: Amlodipine besylate is a calcium channel blocker indicated for hypertension and angina. It is described as slightly soluble in water and due to its limited solubility, it may result in poor bioavailability. The aim of this study is to enhance the solubility of amlodipine besylate using solvent evaporation method and microemulsion technique and to compare the two methods. Method: Solid dispersions (SD) of amlodipine besylate were developed by employing solvent evaporation method. PEG6000 was the polymer of choice and different drug:polymer ratios were used. Evaluation of the prepared SDs include solubility studies, dissolution studies and scanning electron microscopy (SEM). As for the microemulsion technique, microemulsions were prepared by phase titration method and the optimized microemulsion formulation was then characterized for solubility studies and dissolution studies. Results: SD3 with drug:polymer ratio of 1:4 achieved the highest solubility which was 96.97 mg/ml ± 0.92 whereas the solubility of the optimized microemulsion was found to be 112.54 mg/ml ± 0.92. In solvent evaporation method, as the drug:polymer ratio increases, the solubility and dissolution rate of SDs increases. Conclusion: The two methods had significantly enhance the solubility of amlodipine besylate however the microemulsion technique showed better solubility profile.
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