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壳聚糖乳清酸盐对胆汁酸的吸附作用及其作为口服制剂的应用。

Adsorption of bile acid by chitosan-orotic acid salt and its application as an oral preparation.

作者信息

Murata Yoshifumi, Kudo Sayuri, Kofuji Kyouko, Miyamoto Etsuko, Kawashima Susumu

机构信息

Faculty of Pharmaceutical Science, Hokuriku University, Kanazawa, Japan.

出版信息

Chem Pharm Bull (Tokyo). 2004 Oct;52(10):1183-5. doi: 10.1248/cpb.52.1183.

DOI:10.1248/cpb.52.1183
PMID:15467231
Abstract

The orotic acid (OT) salt of chitosan (CS), CS-OT, and that of a CS derivative, CP, were prepared, and the adsorption of primary or secondary bile acid was investigated. Calcium-induced alginate gel beads (Alg-Ca) containing CS-OT were also prepared and autoclaved, and the possibility of these beads to act as a vehicle for oral administration to prevent hyperlipidemia was investigated. When taurocholate (TCA) and glycocholate (GCA) were present together in the medium, CS-OT adsorbed identical amounts of both bile acids. This trend was seen in all CPs, although the capacity to adsorb bile acid was affected by the number and/or structure of the amino groups in the CP. On the other hand, taurodeoxycholate, a secondary bile acid was preferentially adsorbed over TCA and GCA. Alg-Ca containing CS-OT took up bile acids in a similar manner as CS-OT irrespective of the water content of the gel matrix. As all elements can be taken as a food, Alg-Ca containing CS-OT could serve as a useful dietary agent for the prevention of hyperlipidemia, which is a lifestyle-related disease.

摘要

制备了壳聚糖(CS)的乳清酸(OT)盐(CS-OT)以及CS衍生物CP的乳清酸盐,并研究了它们对一级或二级胆汁酸的吸附作用。还制备了含有CS-OT的钙诱导海藻酸盐凝胶珠(Alg-Ca)并进行了高压灭菌,研究了这些珠子作为口服给药载体预防高脂血症的可能性。当牛磺胆酸盐(TCA)和甘氨胆酸盐(GCA)同时存在于培养基中时,CS-OT对两种胆汁酸的吸附量相同。所有CP都呈现出这种趋势,尽管CP中氨基的数量和/或结构会影响其吸附胆汁酸的能力。另一方面,二级胆汁酸牛磺脱氧胆酸盐比TCA和GCA更易被优先吸附。含有CS-OT的Alg-Ca无论凝胶基质的含水量如何,都以与CS-OT相似的方式摄取胆汁酸。由于所有成分都可作为食物,含有CS-OT的Alg-Ca可作为预防高脂血症的有用膳食剂,高脂血症是一种与生活方式相关的疾病。

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