Modification in the Approach of Developing Solid Dispersed Particles for Enhanced Dissolution

Rahul Gupta, A. Mishra, A. Pathak
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Abstract

Objective: To use tween 80 with a novel approach of applying a layer over the outer surface of solid dispersion particles for the improvement of the poor results of solubility enhancement by solid dispersion produced by the conventional technique of using surfactant in the matrix form. Methods: The solid dispersed particles of Repaglinide and Polyvinylpyrrolidone K30 were formulated using solvent evaporation method. The surfactant tween 80 was added as matrix forming agent during the solid dispersion and the prepared solid dispersed particles were also allowed to coat with tween 80 just by applying over the surface of container in which solvent was allowed to evaporate. Key findings: It was inferred that tween 80 coated particles were formulated with maximum solubility enhancement of 1982 μg/ml as compared to 103 μg/ml of non coated solid dispersed particles and to 3.82 μg/ml of Repaglinide. The conversion of the crystalline form of drug into an amorphous form was confirmed by DSC, X-RD, FT-IR studies and SEM images. The dissolution study showed that 90% of drug released within 30 min of dissolution. Conclusion: The solubility estimation data confirmed the efficiency of novel approach used for the formulation of particles as the best technique for solubility enhancement over conventional techniques.
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固体分散颗粒增强溶解方法的改进
目的:采用在固体分散颗粒外表面加一层的新方法,改善传统的表面活性剂以基质形式使用固体分散剂提高溶解度的不良效果。方法:采用溶剂蒸发法制备瑞格列奈和聚乙烯吡咯烷酮K30的固体分散颗粒。在固体分散过程中加入表面活性剂吐温80作为基体形成剂,制备的固体分散颗粒也仅通过将吐温80涂在允许溶剂蒸发的容器表面即可。主要发现:与未包被的固体分散颗粒(103 μg/ml)和瑞格列奈(3.82 μg/ml)相比,80包被颗粒的最大溶解度提高为1982 μg/ml。通过DSC、X-RD、FT-IR和SEM图像证实了药物的结晶转变为非晶态。溶出度研究表明,90%的药物在溶出后30分钟内释放。结论:溶解度评价数据证实了新方法在颗粒剂配制中的有效性,是提高溶解度的最佳方法。
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