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瓜尔胶和 Eudragit ® 包衣姜黄素液体固体片剂用于结肠定位药物传递。

Guargum and Eudragit ® coated curcumin liquid solid tablets for colon specific drug delivery.

机构信息

Amrita School of Pharmacy, Amrita Institute of Medical Sciences and Research Centre, Amrita Vishwa Vidyapeetham, Kochi, Kerala, India.

Amrita School of Pharmacy, Amrita Institute of Medical Sciences and Research Centre, Amrita Vishwa Vidyapeetham, Kochi, Kerala, India.

出版信息

Int J Biol Macromol. 2018 Apr 15;110:318-327. doi: 10.1016/j.ijbiomac.2018.01.082. Epub 2018 Feb 15.

DOI:10.1016/j.ijbiomac.2018.01.082
PMID:29378277
Abstract

Colorectal cancer, also known as bowel cancer, is the uncontrolled cell growth in the colon or rectum (parts of the large intestine), or in the appendix. The colon specific drug delivery would alleviate the systemic side effects and would assure the safe therapy for colonic disorders with minimum dose and duration of therapy. The liquisolid technique refers to solubilisation of drug in a non-volatile solvent combined with inclusion of appropriate carrier and coating agent required for tableting. Colon specific degradation of natural polymer, guar gum and pH dependant degradative (pH-7) property of eudragit L100 restricts the delivery of curcumin in gastric and intestinal pH. Formulated curcumin liquisolid powder was evaluated for the micrometric properties, solubility and by differential thermal analysis, X ray powder diffraction and scanning electron microscopy. Curcumin loaded liquisolid tablet showed more anticancer activity against HCT-15 compared with free curcumin. Bioavailability study of the coated and uncoated liquisolid tablets were performed using Newzealand white rabbits. The present study concludes that liquisolid technique is a promising alternative for improving oral bioavailability and dissolution rate of water insoluble drug and coating liquisolid tablet with colon sensitive polymers showed site specific release of drug in the colon.

摘要

结直肠癌,也称为结肠癌,是指结肠或直肠(大肠的一部分)或阑尾中不受控制的细胞生长。结肠特异性药物递送可以减轻全身副作用,并通过最小剂量和最短治疗时间为结肠疾病提供安全治疗。液质技术是指将药物溶解在非挥发性溶剂中,同时加入适当的载体和包衣剂,以用于片剂制备。天然聚合物瓜尔胶的结肠特异性降解和 Eudragit L100 的 pH 依赖性降解(pH-7)特性限制了姜黄素在胃和肠道 pH 下的递送。对载有姜黄素的液质粉末进行了微观特性、溶解度以及差示热分析、X 射线粉末衍射和扫描电子显微镜的评估。与游离姜黄素相比,载有姜黄素的液质片剂对 HCT-15 表现出更强的抗癌活性。使用新西兰白兔进行了包衣和未包衣液质片剂的生物利用度研究。本研究得出结论,液质技术是提高水不溶性药物口服生物利用度和溶解速率的有前途的替代方法,用结肠敏感聚合物包衣液质片剂可以在结肠中实现药物的定位释放。

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