索法酮海藻酸盐微胶囊的制备及释放性的研究

周锦霞 伍林 王建国 童玲 易德莲 齐小燕 刘敏 彭功名

中国药学杂志 ›› 2011, Vol. 46 ›› Issue (10) : 766-770.

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中国药学杂志 ›› 2011, Vol. 46 ›› Issue (10) : 766-770.
论著

索法酮海藻酸盐微胶囊的制备及释放性的研究

  • 周锦霞1,伍林1*,王建国1,2,童玲3,易德莲1,齐小燕1,刘敏1,彭功名1
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Preparation of Sofalcone Alginate Microcapsules and Their Release Profile

  • ZHOU Jin-xia1,WU Lin1*,WANG Jian-guo1,2,TONG Ling3,YI De-lian1,QI Xiao-yan1,LIU Min1,PENG Gong-ming1
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摘要

目的 研究了以索法酮药物为囊芯海藻酸钠盐微胶囊的制备方法及其体外释药性能。方法 采用乳化法制备了索法酮微胶囊,通过正交实验确定了最佳的制备条件。利用光学显微镜观测了微胶囊的形态;双目倒置显微镜测定微胶囊尺寸;用紫外分光光度法测定索法酮的含量,包封率和回收率;利用傅里叶红外光谱和X射线衍射光谱验证了微胶囊的包覆效果,并进行了体外释放实验。结果 在搅拌速度为1 000 r·min-1,海藻酸钠浓度为3%,Span80与Tween80质量比为2.5,水油体积比为4,芯壁的质量比为1的条件下制备的微胶囊表面光滑,粒度分布均匀。得到微胶囊的平均包封率78.3%,平均载药量为5.54%,平均粒径为400 μm。微胶囊在模拟肠液,模拟胃液中释放曲线显示微胶囊在模拟肠液中9 h达到最高释放度64%,并且能持续保持平稳,而在模拟胃液中达到平稳释放度为8.5%。结论 以海藻酸钠为壁材,乳化法可以制备出结构良好,释放规律符合药物在体内作用效果的微胶囊。

Abstract

ABSTRACT: OBJECTIVE To study the preparation of sofalcone alginate microcapsules and their in vitro release.MTTHODS Sofalcone microcapsules were prepared by emulsion method. The best preparation condition was determined by orthogonal experiment.The appearance of the microcapsules was observed by optical microscope, and the microcapsule size was measured by binocular inverted microscope. Sofalcone content, encapsulation efficiency and recovery efficiency were determined using ultraviolet spectrophotometer.The embedding effect of microcapsules was proved by IR and X-ray diffraction. Besides, in viro release experiments were carried out in simulated intestinal fluid and gastric fluid.RESULTS At a stirring speed of 1 000 r·min-1, sodium alginate concentration of 3%, Span80 and Tween80 mass ratio of 2.5, andwater-oil volume ratio of 4 and core-wall ratio of 1,the microcapsules had good shape and smooth surface. The average encapsulation efficiency was 78.3%. The average drug loading was 5.54%, and the average particle size was 400 μm. The release of microcapsules in simulated intestinal fluid reached maximum value of 64% at 9 h,and remained stable thereafter, while in simulated gastric juice, the microcapsules achieved a smooth release of 8.5%. CONCLUSION Using sodium alginate as wall material microcapsules with good structure can be prepared by emulsion method. Theie in vitro release is in line with the in vivo effect.

关键词

索法酮 / 微胶囊 / 模拟肠液 / 模拟胃液 / 体外释药性

Key words

sofalcone / microcapsules / simulated intestinal fluid / simulated gastric fluid / release profile in vitro

引用本文

导出引用
周锦霞 伍林 王建国 童玲 易德莲 齐小燕 刘敏 彭功名. 索法酮海藻酸盐微胶囊的制备及释放性的研究[J]. 中国药学杂志, 2011, 46(10): 766-770
ZHOU Jin-xi;WU Lin;WNG Jin-guo;TONG Ling;YI De-lin;QI Xio-yn;LIU Min;PENG Gong-ming. Preparation of Sofalcone Alginate Microcapsules and Their Release Profile[J]. Chinese Pharmaceutical Journal, 2011, 46(10): 766-770

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