均匀设计法优化葛根素白蛋白微球处方工艺
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摘要
为优化葛根素白蛋白微球处方工艺。以牛血清白蛋白为载体,采用乳化热固化法制备葛根素白蛋白微球。以包封率和载药量为综合评价指标,以牛血清白蛋白用量、葛根素用量、司盘80用量为考察因素,在单因素实验的基础上,利用均匀设计法优化葛根素白蛋白微球的处方工艺。葛根素白蛋白微球最优处方为:牛血清白蛋白0.20 g,葛根素30.00 mg,司盘80为0.80 m L,验证处方的包封率为76.75%±2.09%,载药量为9.81%±0.14%。采用均匀设计优化法制备的葛根素白蛋白微球综合评分高,模型预测性良好。
To optimize the formulation of puerarin albumin microspheres. The microspheres were prepared by emulsion-heat stabilization techniques using albumin as carrier. The encapsulation efficiency and drug loading rate of the puerarin albumin microspheres were selected as comprehensive evaluation indexes.The amount of bovine serum albumin,the amount of puerarin and the amount of span-80 were selected as factors.Uniform design method were used to optimize the formulation process of puerarin albumin microspheres.Optimum formulation of puerarin albumin microspheres was as follows: Bovine serum albumin was 0.20 g,puerarin was 30.00 mg,span-80 was 0.80 m L.The entrapment efficiency of optimum formulation was 76.75% ± 2.09% and the drug loading was 9.81% ± 0.14%. The formulation process of the puerarin albumin microspheres optimized by uniform design method was effective and feasible with a good prediction,and the results showed a high comprehensive score.
To optimize the formulation of puerarin albumin microspheres. The microspheres were prepared by emulsion-heat stabilization techniques using albumin as carrier. The encapsulation efficiency and drug loading rate of the puerarin albumin microspheres were selected as comprehensive evaluation indexes.The amount of bovine serum albumin,the amount of puerarin and the amount of span-80 were selected as factors.Uniform design method were used to optimize the formulation process of puerarin albumin microspheres.Optimum formulation of puerarin albumin microspheres was as follows: Bovine serum albumin was 0.20 g,puerarin was 30.00 mg,span-80 was 0.80 m L.The entrapment efficiency of optimum formulation was 76.75% ± 2.09% and the drug loading was 9.81% ± 0.14%. The formulation process of the puerarin albumin microspheres optimized by uniform design method was effective and feasible with a good prediction,and the results showed a high comprehensive score.
引文
[1]曹毅.中药葛根的相关药理药效研究综述[J].中国处方药,2018,16(2):27-28.
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[19]黄羲颖,庄启范,黄凤华,等.应用均匀设计法优化佛手蜜炙工艺的研究[J].海峡药学,2018,30(1):15-17.
[20]陈永顺,吴珍,董永成,等.沙美特罗白蛋白微球的制备与体外释放度考察[J].中国药师,2011,14(11):1624-1626.
[21]陈永顺,吴珍,董永成,等.去甲斑蝥素白蛋白微球的制备[J].中国医院药学杂志,2011,31(14):1174-1177.
[22]樊继波,陈永斌,周洁.白蛋白微球的制备方法及质量评价的研究进展[J].天津药学,2009,23(3):58-61.
[23]Li H F,Cheng C F,Liao W J,et al.ATF3-mediated epigenetic regulation protects against acute kidney injury[J].JAm Soc Nephrol,2010,21(6):1003-1013.
[2]郭丽君,张静,肖冬,等.不同生长时期葛根光合特性及其与淀粉积累的关系[J].南方农业学报,2018,49(4):662-668.
[3]李远辉,刘佃飞,杨永福.葛根提取物的化学成分及其临床应用研究综述[J].中药与临床,2015,6(4):47-48.
[4]楚纪明,马树运,李海峰,等.葛根有效成分及其药理作用研究进展[J].食品与药品,2015,17(2):142-146.
[5]杨书山,刘莉,刘丽娜,等.葛根素微球的制备及其体外释放研究[J].中华高血压杂志,2015,3(23):357-358.
[6]Liu X J,Zhao J,Gu X Y.The effects of genistein and puerarin on the activation of nuclear factor-kappa B and the production of tumor necrosis factor-alpha in asthma patients[J].Pharmazie,2010,65(2):127-131.
[7]Gao L,Ji X,Song J,et al.Puerarin protects against ischemic brain injury in a rat model of transient focal ischemia[J].Neurol Res,2009,31(4):402-406.
[8]尹乐斌,夏秋良,赵良忠,等.葛根药理作用研究进展[J].现代农业科技,2016,45(4):68-69.
[9]李宁,郝志梅,崔书霞,等.葛根素对心肌细胞氧化应激损伤的保护作用[J].中国中医基础医学杂志,2014,20(11):1501-1503.
[10]闫雪生,程立方.葛根素新型制剂的研究概况[J].中国医院药学杂志,2011,31(15):1294-1297.
[11]张智舟,姜守刚,祖元刚,等.多西紫杉醇白蛋白微球的制备及优化实验研究[J].植物研究,2011,31(3):381-384.
[12]王秋芳,杨且翟,胡晋,等.白蛋白微球剂的研究进展[J].沈阳药学院学报,1992,2(9):140-143.
[13]Xue J L,Danineis F,Star Ra,et al.Incidence and mortality of acute renal failure in medicare beneficiaries,1992 to 2001[J].Jam Soc Nephrol,2006,17(4):1135-1142.
[14]殷悦,阎雪莹,马艳南,等.白蛋白微球的制备方法及质量评价的研究进展[J].黑龙江医药,2015,28(1):43-46.
[15]周雪,贺智勇,薛雨晨,等.葛根素缓释微球的高分子材料考察及工艺优化[J].中国实验方剂杂志,2015,21(9):14-18.
[16]吴静澜,陈红汝,陈白霜,等.三七总皂苷白蛋白微球的制备工艺[J].中国实验方剂学杂志,2011,17(19):17-20.
[17]李岸,刘丹,周捷,等.多西他赛人血清白蛋白微球的制备及体外释药性质的评价[J].中国医院药学杂志,2017,37(12):1149-1152.
[18]陈锋,李春忠,抗癌丝裂霉素白蛋白微球的制备及体外释药性能[J].华东理工大学学报,2006,32(2):184-187,192.
[19]黄羲颖,庄启范,黄凤华,等.应用均匀设计法优化佛手蜜炙工艺的研究[J].海峡药学,2018,30(1):15-17.
[20]陈永顺,吴珍,董永成,等.沙美特罗白蛋白微球的制备与体外释放度考察[J].中国药师,2011,14(11):1624-1626.
[21]陈永顺,吴珍,董永成,等.去甲斑蝥素白蛋白微球的制备[J].中国医院药学杂志,2011,31(14):1174-1177.
[22]樊继波,陈永斌,周洁.白蛋白微球的制备方法及质量评价的研究进展[J].天津药学,2009,23(3):58-61.
[23]Li H F,Cheng C F,Liao W J,et al.ATF3-mediated epigenetic regulation protects against acute kidney injury[J].JAm Soc Nephrol,2010,21(6):1003-1013.
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