鸦胆子油微囊的制备及体外释放性能研究
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摘要
目的探讨鸦胆子油微囊的制备工艺和质量控制方法,并研究其稳定性及体外释药特性,为开发新剂型奠定基础。方法以阿拉伯胶、明胶为囊材,采用复凝聚法制备鸦胆子油微囊,采用正交试验设计优化制备工艺并进行验证。考察所制得的鸦胆子微囊粒径分布和体外药物释放率。结果最优处方工艺为,囊心(鸦胆子油)与囊材(阿拉伯胶和明胶)质量比为1∶4,囊材质量分数为1.50%,搅拌速率为500 r/min,成囊温度为53℃。所得微囊鸦胆子油的包封率为94.60%,载药量为49.70%;最优工艺获得鸦胆子微囊外形圆整光滑,无黏连,粒径均匀,主要分布在60~90μm;30 min的累积释药率达92.00%。结论采用复凝聚法制备鸦胆子油微囊方法简便、易行,鸦胆子油微囊稳定,在人工胃液中有理想的溶出度,且此方法操作简单,适合工业化生产。
Objective To investigate the preparation technology and quality control method of Brucea javanica oil microcapsule(BOM),then study its stability and in vitro drug releasing properties,in order to lay the foundation for the development of the new dosage form of BOM. Methods With gum arabic and gelatin as capsule materials,BOM was prepared by the complex agglutination method,the preparation technology was optimized and validated by orthogonal design test,and afterwards the particle size distribution of the prepared BOM and the rate of in vitro drug release were studied. Results The optimal preparation process was as follows: core materials( Brucea javanica oil)-capsule materials(gum arabic and gelatin)(1 ∶ 4),the mass fraction of capsule material was 1. 50%,the stirring velocity was 500 r/min,and the temperature of encapsulation was 53 ℃. The encapsulation efficiency of BOM was 94. 60%,the drug loading was 49. 70%. BOM was prepared by optimal technology, which had rounded smooth surface without adhesions and uniform particle size. The average particle size was distributed in 60-90 μm,and the dissolution of the microcapsules at 30 min was about 92. 00%.Conclusion The complex agglutination method for preparing BOM is simple and convenient. BOM has good stability and ideal dissolution in the artificial gastric acid fluid. This method is easy to operate and is suitable for industrial production.
Objective To investigate the preparation technology and quality control method of Brucea javanica oil microcapsule(BOM),then study its stability and in vitro drug releasing properties,in order to lay the foundation for the development of the new dosage form of BOM. Methods With gum arabic and gelatin as capsule materials,BOM was prepared by the complex agglutination method,the preparation technology was optimized and validated by orthogonal design test,and afterwards the particle size distribution of the prepared BOM and the rate of in vitro drug release were studied. Results The optimal preparation process was as follows: core materials( Brucea javanica oil)-capsule materials(gum arabic and gelatin)(1 ∶ 4),the mass fraction of capsule material was 1. 50%,the stirring velocity was 500 r/min,and the temperature of encapsulation was 53 ℃. The encapsulation efficiency of BOM was 94. 60%,the drug loading was 49. 70%. BOM was prepared by optimal technology, which had rounded smooth surface without adhesions and uniform particle size. The average particle size was distributed in 60-90 μm,and the dissolution of the microcapsules at 30 min was about 92. 00%.Conclusion The complex agglutination method for preparing BOM is simple and convenient. BOM has good stability and ideal dissolution in the artificial gastric acid fluid. This method is easy to operate and is suitable for industrial production.
引文
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[11]朱岳鑫,饶丽明,吴立蓉.复凝聚法制备丹皮酚微囊的研究[J].中国处方药,2016,14(6):34-36.
[12]鲜敏,丁晓刚.正交设计法优选大蒜油微囊的制备工艺[J].时珍国医国药,2009,20(1):220-221.
[13]吴素香,苏璇,李智慧,等.复凝聚法制备留兰香油微囊的处方工艺研究[J].中成药,2013,35(6):1193-1199.
[14]国家药典委员会.中华人民共和国药典(四部)[M].北京:中国医药科技出版社,2015:121-124.
[15]张彬,周武,邓丹雯.超临界CO2萃取鸦胆子油研究[J].食品科学,2004,25(6):136-138.
[2]张浩中,熊启香,芦兰.紫杉醇联合鸦胆子油二线治疗晚期非小细胞性肺癌76例[J].中国药业,2016,25(1):166-169.
[3]肖勋立.我院病区抗肿瘤中药注射液合理应用分析[J].中国药业,2016,25(23):80-82.
[4]李超英,陈文文,王楚盈,等.鸦胆子油口服乳液抑制肝癌发生的实验研究[J].中国肿瘤临床,2014,41(12):762-765.
[5]吴泽榕,孔焕宇,刘朝阳,等.鸦胆子油软胶囊对裸鼠移植人小细胞肺癌LTEP-SML抑瘤作用[J].药品评价,2006,3(6):436-437.
[6]陈卓霞.鸦胆子油乳致过敏反应的护理分析[J].中国药业,2013,22(12):128-129.
[7]张骁,束梅英,张韬.微囊在医药领域的应用进展[J].中国医药情报,2004,10(1):9-14.
[8]孔繁晟,严春艳,贲永光,等.鸦胆子油自微乳的体外释放度考察[J].中国实验方剂学杂志,2012,18(12):21-23.
[9]国家药典委员会.中华人民共和国药典(一部)[M].北京:中国医药科技出版社,2015:254-255.
[10]余琰,范凌云,高建德,等.盐酸小檗碱微囊的制备及其体外释放研究[J].中国药房,2015,26(1):109-112.
[11]朱岳鑫,饶丽明,吴立蓉.复凝聚法制备丹皮酚微囊的研究[J].中国处方药,2016,14(6):34-36.
[12]鲜敏,丁晓刚.正交设计法优选大蒜油微囊的制备工艺[J].时珍国医国药,2009,20(1):220-221.
[13]吴素香,苏璇,李智慧,等.复凝聚法制备留兰香油微囊的处方工艺研究[J].中成药,2013,35(6):1193-1199.
[14]国家药典委员会.中华人民共和国药典(四部)[M].北京:中国医药科技出版社,2015:121-124.
[15]张彬,周武,邓丹雯.超临界CO2萃取鸦胆子油研究[J].食品科学,2004,25(6):136-138.