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| 洛索洛芬钠缓释微球的制备及体外释药特性考察 | |
| 引用本文： | 韩 枫,徐 凯,王中彦,闫永波,李 妍,莫凤奎. 洛索洛芬钠缓释微球的制备及体外释药特性考察[J]. 沈阳药科大学学报, 2009, 26(5): 331-334 |
| 作者姓名： | 韩 枫 徐 凯 王中彦 闫永波 李 妍 莫凤奎 |
| 作者单位： | 韩枫,徐凯,王中彦,李妍,莫凤奎,HAN Feng,XU Kai,WANG Zhong-yan,LI Yan,MO Feng-kui(沈阳药科大学,药学院,辽宁,沈阳,110016);闫永波,YAN Yong-bo(沈阳药科大学,药学院,辽宁,沈阳,110016;本溪市中心医院,辽宁,本溪,117000) |
| 摘 要： | 目的延缓洛索洛芬钠在局部的作用时间,了解洛索洛芬钠缓释微球的体外释药特性。方法采用乳化-化学交联法制备明胶微球,采用正交试验优化明胶微球的处方和制备工艺;采用流化床包衣技术制备缓释微球;采用透析法考察体外释药特性。结果制备明胶微球最优处方和工艺为:洛索洛芬钠5.0 g,质量分数为20%的明胶溶液100 mL作为水相,含质量分数0.5%Span 80的液体石蜡混合液400 mL作为油相,55℃搅拌下将水相缓缓加入至油相中,500 r.min-1乳化20 min,冰水浴20 min,加入戊二醛使体积分数为50%,交联90 min,4000 r.min-1离心分离10 min,用丙酮、乙醚交替洗涤3次,40℃真空干燥12 h;制备的明胶微球平均粒径为18.25μm,载药量为19.37%,包封率为87.72%,包衣后质量增加25%;洛索洛芬钠缓释微球体外释药过程符合Higuchi方程。结论制备的洛索洛芬钠缓释微球具有明显的缓释作用。 |
| 关 键 词： | 洛索洛芬钠 明胶微球 缓释微球 体外释药 |
| 收稿时间： | 2008-05-19 |
Preparation and in vitro release of sustained-release microspheres of loxoprofen sodium |
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| HAN Feng,XU Kai,WANG Zhong-yan,YAN Yong-bo,LI Yan,MO Feng-kui. Preparation and in vitro release of sustained-release microspheres of loxoprofen sodium[J]. Journal of Shenyang Pharmaceutical University, 2009, 26(5): 331-334 | |
| Authors: | HAN Feng XU Kai WANG Zhong-yan YAN Yong-bo LI Yan MO Feng-kui |
| Affiliation: | （1. School of Pharmacy, Shenyang Pharmaceutical University, Shenyang 110016,China, 2. Benxi Central Hospital, Benxi 117000, China ） |
| Abstract: | Objective To prepare sustained-release microspheres of loxoprofen sodium, and investigate its in vitro release property. Methods The microspheres were prepared by emulsify-chemical cross linking method, and its formulation and technique were optimized by means of orthogonal experiments. Fluid-bed coating technique was utilized to prepare sustained-release microspheres. The dialysis method was used to investigate its in vitro release property. Results The optimum formulation and technique to prepare the gelatin microspheres were determined as follows: loxoprofen sodium (5.0 g) was added to the 20 %(m:m) gelatin solution (100 mL) as the water phase, paraffin oil (400 mL) within 0.5 %(m:m) Span 80 was made to be the oil phase, then the water phase was added slowly to the oil phase at 55 ℃ under constant stirring using a mechanical stirrer at the rotation speed of 500 r•min-1 for emulsifying of 20 min. Glutaral was added to the emulsion made its concentration of 50 % (V:V) to crosslink for 90 min in order to form solid microspheres after iced bath of 20 min. The microspheres was centrifuged at 4 000 r•min-1 to isolate the solid microspheres, and then washed alternately using acetone and ether for three times, and dried by vacuum drying oven for 12 h to obtain dry microspheres. The microspheres prepared by the selected procedure had a mean diameter of 18.25 μm. The drug loading was about 19.37 %, and the entrapment efficiency was 87.32 %. The weight of coating of sustained-release microspheres was increased by 25 %, and its in vitro release profile property fitted the Higuchi equation. Conclusion The sustained-release mirospheres prepared by the selected procedure have distinct sustained release action. |
| Keywords: | oxoprofen sodium gelatin microsphere sustained-release microsphere in vitro release |
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