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用于结肠靶向给药系统的果胶-硼酸大米珠的制剂、评价与优化

Formulation, evaluation and optimization of pectin- bora rice beads for colon targeted drug delivery system.

作者信息

Ramteke Kuldeep Hemraj, Nath Lilakant

机构信息

Modern College of Pharmacy (for Ladies), Moshi, Pune, Maharashtra.

Department of Pharmaceutical Sciences, Dibrugarh University, Dibrugagh, Assam.

出版信息

Adv Pharm Bull. 2014;4(2):167-77. doi: 10.5681/apb.2014.025. Epub 2013 Dec 24.

Abstract

PURPOSE

The purpose of this research was to established new polysaccharide for the colon targeted drug delivery system, its formulation and in vitro and in vivo evaluation.

METHODS

Microspheres containing pectin and bora rice were prepared by ionotropic gelation technique using zinc acetate as cross linking agent and model drug used was glipizide. A 3(2) full factorial design was employed to study the effect of independent variables, polymer to drug ratio (A), and concentration of cross linking agent (B) on dependent variables, particle size, swelling index, drug entrapment efficiency and percentage drug release.

RESULTS

RESULTS of trial batches indicated that polymer to drug ratio and concentration of cross linking agent affects characteristics of beads. Beads were discrete, spherical and free flowing. Beads exhibited small particle size and showed higher percentage of drug entrapment efficiency. The optimized batch P2 exhibited satisfactory drug entrapment efficiency 68% and drug release was also controlled for more than 24 hours. The polymer to drug ratio had a more significant effect on the dependent variables. In vivo gamma scintigraphy study of optimized pectin-bora rice beads demonstrated degradation of beads whenever they reached to the colon.

CONCLUSION

Bora rice is potential polysaccharide for colon targeted drug delivery system.

摘要

目的

本研究的目的是建立一种用于结肠靶向给药系统的新型多糖、其制剂以及体外和体内评价。

方法

以醋酸锌为交联剂,采用离子凝胶技术制备了含果胶和硼稻的微球,所用模型药物为格列吡嗪。采用3(2)全因子设计研究自变量聚合物与药物比例(A)和交联剂浓度(B)对因变量粒径、溶胀指数、药物包封率和药物释放百分比的影响。

结果

试验批次结果表明,聚合物与药物比例和交联剂浓度影响微球特性。微球离散、呈球形且流动性好。微球粒径小,药物包封率较高。优化后的批次P2表现出令人满意的药物包封率68%,药物释放也能控制超过24小时。聚合物与药物比例对因变量的影响更为显著。优化后的果胶-硼稻微球的体内γ闪烁扫描研究表明,微球到达结肠时会发生降解。

结论

硼稻是用于结肠靶向给药系统的潜在多糖。

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