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多孔淀粉:提高卡马西平溶解度的新型载体。

Porous starch: a novel carrier for solubility enhancement of carbamazepine.

机构信息

Department of Pharmaceutical Sciences and Technology, Institute of Chemical Technology, Matunga (E), Mumbai, 400019, India.

出版信息

AAPS PharmSciTech. 2013 Sep;14(3):919-26. doi: 10.1208/s12249-013-9985-6. Epub 2013 May 29.

Abstract

To circumvent the solubility-related issues associated with Biopharmaceutics Classification System class II drugs, a novel porous carrier has been developed. In the present study, a process for preparation of porous starch (PS) is demonstrated. The process briefly comprises of translucent gel preparation followed by solvent replacement, drying, and sizing. Carbamazepine (CBZ) was used as a drug candidate to exhibit solubility enhancement potential of PS. PS and CBZ-loaded PS (CBZ-PS) systems were characterized with respect to IR, DSC, XRD, SEM, and dissolution kinetic studies. PS-CBZ was found to follow a Fickian behavior during dissolution. In vivo studies conducted in mice displayed a superior performance of CBZ-PS as compared to neat CBZ.

摘要

为了解决生物药剂学分类系统 II 类药物相关的溶解度问题,开发了一种新型多孔载体。在本研究中,展示了一种多孔淀粉(PS)的制备工艺。该工艺包括半透明凝胶的制备,随后进行溶剂置换、干燥和筛分。卡马西平(CBZ)被用作药物候选物,以展示 PS 的溶解度增强潜力。对 PS 和载有 CBZ 的 PS(CBZ-PS)系统进行了特征描述,包括 IR、DSC、XRD、SEM 和溶解动力学研究。PS-CBZ 的溶解行为符合菲克定律。在小鼠体内研究中,CBZ-PS 的性能优于纯 CBZ。

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