体外评估可可荚果果胶作为载体用于肾上腺皮质功能不全症的氢化可的松慢性给药。

Journal of drug delivery Pub Date : 2017-01-01 Epub Date: 2017-12-24 DOI:10.1155/2017/8284025
Ofosua Adi-Dako, Kwabena Ofori-Kwakye, Mariam El Boakye-Gyasi, Samuel Oppong Bekoe, Samuel Okyem
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引用次数: 0

摘要

本研究评估了可可荚果(CPH)果胶作为用于肾上腺皮质功能不全的氢化可的松 chronodel 给药载体的体外潜力。傅立叶变换红外光谱研究发现,药物与 CPH 果胶之间没有相互作用,化学计量分析表明,纯氢化可的松与热水可溶性果胶(HWSP)中的氢化可的松相比,与柠檬酸可溶性果胶(CASP)中的氢化可的松更为相似。采用直接压缩和湿法制粒技术制备了 CPH 果胶基氢化可的松基质片剂(约 300 毫克),片芯采用 15%的 HPMC 制剂包膜以实现定时释放,然后再采用 12.5% 的 Eudragit® S100 制剂包膜以实现耐酸性。在模拟胃肠道条件下对未包衣和包衣基质片剂进行的体外药物释放研究表明,湿法制粒片剂比直接压制片剂在水介质中表现出更强的药物释放延缓能力。CASP 比 HWSP 更能抑制药物在水介质中的释放。对基于 HWSP 的湿法制粒基质片剂进行了优化,最终包衣增重约为 25% w/w,用于氢化可的松在结肠中的 chronodel 给药。优化后的片剂表现出约 6 小时的滞后期,随后药物在结肠区域加速释放,具有控制肾上腺功能不全患者夜间皮质醇水平的潜力。
本文章由计算机程序翻译,如有差异,请以英文原文为准。

In Vitro Evaluation of Cocoa Pod Husk Pectin as a Carrier for Chronodelivery of Hydrocortisone Intended for Adrenal Insufficiency.

In Vitro Evaluation of Cocoa Pod Husk Pectin as a Carrier for Chronodelivery of Hydrocortisone Intended for Adrenal Insufficiency.

In Vitro Evaluation of Cocoa Pod Husk Pectin as a Carrier for Chronodelivery of Hydrocortisone Intended for Adrenal Insufficiency.

In Vitro Evaluation of Cocoa Pod Husk Pectin as a Carrier for Chronodelivery of Hydrocortisone Intended for Adrenal Insufficiency.

This study evaluated the in vitro potential of cocoa pod husk (CPH) pectin as a carrier for chronodelivery of hydrocortisone intended for adrenal insufficiency. FTIR studies found no drug-CPH pectin interactions, and chemometric analysis showed that pure hydrocortisone bears closer similarity to hydrocortisone in hot water soluble pectin (HWSP) than hydrocortisone in citric acid soluble pectin (CASP). CPH pectin-based hydrocortisone matrix tablets (~300 mg) were prepared by direct compression and wet granulation techniques, and the tablet cores were film-coated with a 15% HPMC formulation for timed release, followed by a 12.5% Eudragit® S100 formulation for acid resistance. In vitro drug release studies of the uncoated and coated matrix tablets in simulated gastrointestinal conditions showed that wet granulation tablets exhibit greater retardation of drug release in aqueous medium than directly compressed tablets. CASP showed greater suppression of drug release in aqueous medium than HWSP. Wet granulation HWSP-based matrix tablets coated to a final coat weight gain of ~25% w/w were optimized for chronodelivery of hydrocortisone in the colon. The optimized tablets exhibited a lag phase of ~6 h followed by accelerated drug release in the colonic region and have potential to control night time cortisol levels in patients with adrenal insufficiency.

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Journal of drug delivery
Journal of drug delivery PHARMACOLOGY & PHARMACY-
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