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κ-卡拉胶-壳聚糖聚电解质凝胶珠的制备

[Preparation of kappa-carrageenan-chitosan polyelectrolyte gel beads].

作者信息

Zhang Yu, Zhang Yun

机构信息

Institute of Materia Medica, He'nan University, Kaifeng 475004, China.

出版信息

Zhongguo Zhong Yao Za Zhi. 2012 Feb;37(4):466-70.

Abstract

OBJECTIVE

To prepare kappa-carrageenan-chitosan polyelectrolyte gel pellets and detect the effects of formulation and preparation factors on in vitro drug release from the pellets.

METHOD

The K-carrageenan-chitosan polyelectrolyte gel pellets with baicalin as model drug were prepared by ionotropic gelation technique. The ratio of kappa-carrageenan/chitosan in pellets was determined with the composite of K-carrageenan and chitosan. The effects of the concentration of K-carrageenan, the ratio of drug/kappa-carrageenan, the concentration of gelling solution, gelling time and drying method on the release of pellets were determined by in vitro drug release.

RESULT

The mass ratio of K-carrageenan/chitosan in pellets was 6: 4. Release of the pellets in 0.1 mol x L(-1) HCl was about 10% for 2 hours and fast in PBS, indicating a typical sustained release property. The pellets released less with the increase in the concentration of K-carrageenan, the ratio of drug/kappa-carrageenan and the concentration of KCl. They also released less with the increase in gelling time, but showed little effect until 1 hour. The release of the pellets prepared by the freeze-drying method was much faster than those by vacuum drying and atmospheric drying methods which had little influence on drug release.

CONCLUSION

The K-carrageenan-chitosan polyelectrolyte gel pellets had sustained release property. Their drug release rate could be regulated with different formulation and preparation factors.

摘要

目的

制备κ-卡拉胶-壳聚糖聚电解质凝胶微丸,并考察处方及制备因素对微丸体外释药的影响。

方法

以黄芩苷为模型药物,采用离子凝胶法制备κ-卡拉胶-壳聚糖聚电解质凝胶微丸。通过κ-卡拉胶与壳聚糖的复合物测定微丸中κ-卡拉胶/壳聚糖的比例。采用体外释药法考察κ-卡拉胶浓度、药物/κ-卡拉胶比例、胶凝液浓度、胶凝时间及干燥方法对微丸释药的影响。

结果

微丸中κ-卡拉胶/壳聚糖的质量比为6∶4。微丸在0.1 mol·L-1 HCl中2 h的释放率约为10%,在PBS中释药较快,呈现典型的缓释特性。随着κ-卡拉胶浓度、药物/κ-卡拉胶比例及KCl浓度的增加,微丸释药量减少。随着胶凝时间的延长,微丸释药量也减少,但在1 h内影响较小。冷冻干燥法制备的微丸释药速度比真空干燥法和常压干燥法快得多,后两种干燥方法对药物释放影响较小。

结论

κ-卡拉胶-壳聚糖聚电解质凝胶微丸具有缓释特性,其释药速率可通过不同的处方及制备因素进行调节。

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