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药物-丝胶固体制剂的筛选,以提高其溶解度和溶出度。

Screening of drug-sericin solid dispersions for improved solubility and dissolution.

机构信息

Department of Pharmaceutics, Bharati Vidyapeeth College of Pharmacy, Kolhapur 416013, Maharashtra State, India.

Department of Pharmaceutics, Bharati Vidyapeeth College of Pharmacy, Kolhapur 416013, Maharashtra State, India.

出版信息

Int J Biol Macromol. 2018 Feb;107(Pt B):1683-1691. doi: 10.1016/j.ijbiomac.2017.10.035. Epub 2017 Oct 10.

Abstract

The aim of present attempt deals with preparation of binary dispersion of sericin, waste of sericulture industry in order to enhance solubility and dissolution of poorly soluble drugs. Solid dispersions (SDs) of BCS-II drugs were prepared by spray drying, solvent evaporation, ball milling and physical mixing in ratio of drug:sericin (1:0.5, 1:1, 1:1.5, 1:2, 1:2.5 and 1:3). Further, SDs were investigated by solubility, ATR-FTIR, XRD, DSC, micromeritics and tablettability, surface morphology and in-vitro dissolution. Results demonstrated that, sericin improves solubility of drugs by 8-10 fold. The ATR-FTIR showed the slight shifting/broadening of principle peaks corresponding to NH and OH. Spray dried (1:2w/w) SDs showed maximum reduction in crystallinity of drugs indicating drug was molecularly distributed and was in amorphous state. Spray dried SDs of meloxicam showed better compressibility and compactibility. The microphotograph of spray dried SDs of lornoxicam and meloxicam showed bowl shaped and blend of bowl and spherical particles respectively, while spray dried SDs of felodepine showed spherical shape. The spray dried SDs (1:2w/w) displayed better dissolution performance than other methods Conclusively, sericin offers a hydrophilic matrix to deliver poor water soluble drugs and its aerodynamic shape may show a great potential for various drug deliveries.

摘要

本研究旨在制备丝胶的二元分散体,以提高丝织工业废物中难溶性药物的溶解度和溶解性能。采用喷雾干燥、溶剂蒸发、球磨和物理混合的方法,以药物:丝胶(1:0.5、1:1、1:1.5、1:2、1:2.5 和 1:3)的比例制备了 BCS-II 类药物的固体分散体(SDs)。进一步通过溶解度、ATR-FTIR、XRD、DSC、微粉学和可压性、表面形态和体外溶出度对 SDs 进行了研究。结果表明,丝胶可将药物的溶解度提高 8-10 倍。ATR-FTIR 显示出对应于 NH 和 OH 的主要峰的轻微移动/展宽。喷雾干燥(1:2w/w)SDs 显示出药物结晶度的最大降低,表明药物呈分子分布且处于无定形状态。美洛昔康的喷雾干燥 SDs 显示出更好的可压缩性和可压缩性。洛索洛芬和美洛昔康的喷雾干燥 SDs 的微观照片分别显示为碗状和碗状与球状颗粒的混合物,而非洛地平的喷雾干燥 SDs 则呈球形。喷雾干燥 SDs(1:2w/w)的溶出性能优于其他方法。总之,丝胶提供了一种亲水基质,用于输送难溶性药物,其空气动力学形状可能为各种药物输送提供巨大潜力。

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