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使用天然聚合物进行结肠靶向递送槲皮素以提高其生物利用度。

Colon-targeted quercetin delivery using natural polymer to enhance its bioavailability.

作者信息

Singhal Anil, Jain H, Singhal Vipin, Elias Edwin J, Showkat Ahmad

机构信息

B. R. Nahata College of Pharmacy, BRNSS-Contract Research Center, Mhow-Neemuch Road, Mandsaur, Madhya Pradesh, India.

出版信息

Pharmacognosy Res. 2011 Jan;3(1):35-9. doi: 10.4103/0974-8490.79113.

Abstract

The aim of the present study is to develop a polymer (Guar Gum)-based matrix tablet (using quercetin as a model drug) with sufficient mechanical strength, and promising in vitro mouth-to-colon release profile. By definition, an oral colonic delivery system should retard drug release in the stomach and small intestine, and allow complete release in the colon. By drug delivery to the colon would therefore ensure direct treatment at the disease site, lower dosing, and fewer systemic side effects. Quercetin is antioxidant in nature and used to treat colon cancer, but they have poor absorption in the upper part of the gastrointestinal tract (GIT). As a site for drug delivery, the colon offers a near neutral pH, reduced digestive enzymatic activity, a long transit time, and an increased responsiveness to absorption enhancers. By achieving a colon-targeted drug delivery system, the absorption of quercetin may be increased, which leads to better bioactivity in fewer doses.

摘要

本研究的目的是开发一种基于聚合物(瓜尔胶)的基质片剂(以槲皮素作为模型药物),使其具有足够的机械强度,并具有良好的体外口腔至结肠释放特性。根据定义,口服结肠给药系统应延缓药物在胃和小肠中的释放,并使药物在结肠中完全释放。因此,通过将药物递送至结肠可确保在疾病部位进行直接治疗、降低给药剂量并减少全身副作用。槲皮素具有抗氧化性质,可用于治疗结肠癌,但其在胃肠道(GIT)上部的吸收较差。作为药物递送部位,结肠具有接近中性的pH值、降低的消化酶活性、较长的转运时间以及对吸收促进剂的反应性增加。通过实现结肠靶向给药系统,槲皮素的吸收可能会增加,从而以较少的剂量实现更好的生物活性。

https://cdn.ncbi.nlm.nih.gov/pmc/blobs/a3f4/3119269/bae32e670c62/PR-3-35-g003.jpg

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