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响应面法优化葛根素微丸片的处方及工艺
响应面法优化葛根素微丸片的处方及工艺
赵呈雷,曹 鹏

南京中医药大学附属中西医结合医院/江苏省中医药研究院,南京 210028
Optimizing the formulation process of puerarin pellets-type tablets by response surface method
(Hospital of Integrated Traditional Chinese and Western Medicine Affiliated to Nanjing University of Chinese Medicine & Jiangsu Province Academy of Traditional Chinese Medicine, Nanjing 210028, China)

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起始页:84

摘要:[摘要] 目的:优化葛根素微丸片的处方及制备工艺,并对其体外溶出度进行评价,为葛根素微丸片的应用奠定基础。方法:采用挤出-滚圆法制备葛根素微丸,粉末直接压片法制备葛根素微丸片。在单因素考察葛根素微丸处方的基础上,以收率和圆整度为综合评价指标,黏合剂用量、挤出速度、滚圆速度为考察因素,利用Box-Behnken响应面法优化葛根素微丸的制备工艺。再以微晶纤维素(microcrystalline cellulose, MCC)、交联聚维酮(polyvinylpolypyrrolidone, PVPP)、低取代羟丙纤维素(low-substituted hydroxypropylcellulose, L-HPC)用量为考察因素,微丸片崩解时限、硬度为综合评价指标,采用Box-Behnken响应面法筛选葛根素微丸片最优处方。结果:葛根素微丸最佳处方和制备工艺为葛根素载药量40%,MCC-101加入量45%,羧甲基淀粉纳加入量10%,乳糖加入量5%,6%聚乙烯吡咯烷酮K30溶液加入量46.2%(v/w),挤出速度38.6 Hz,滚圆速度37.8 Hz,滚圆时间7 min。微丸片的最佳处方为葛根素微丸8 g,MCC-102 8 g,PVPP 3 g,L-HPC 0.5 g,SiO2 0.4 g制得的葛根素微丸片在6 s内崩解,硬度95.5 N,脆碎度<0.2%,葛根素在60 min累积溶出率>82%,微丸压片前后溶出行为无明显变化。结论:采用Box-Behnken效应面法优化法制备的葛根素微丸及微丸片综合评分高,模型预测性良好,确定的处方和工艺是有效、可行的。

关键词:[关键词] 葛根素;微丸片;Box-Behnken;响应面法

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Abstract:[Abstract] Objective: To optimize the formulation process of puerarin pellets-type tablets, and to evaluate the in vitro dissolution rate. Methods: Puerarin pellets were prepared by extrusion-spheronization method, and puerarin pellets-type tablets were prepared by direct powder tableting technology. The yield and sphericity of the puerarin pellets were selected as comprehensive evaluation indexes. Adhesive percentage, extrusion speed, and spheronization speed were selected as factors. Then the hardness and disintegration time of puerarin pellets-type tablets were selected as comprehensive evaluation index. The amounts of MCC-102, PVPP and L-HPC (LH22) were selected as factors. Box-Behnken design and response surface method were used to optimize the formulation process of puerarin pellets and puerarin pellets-type tablets. Results: The optimized formulation process of puerarin pellets was as follows: puerarin content was 40%, MCC-101 content was 45%, CMS-Na content was 10%, lactose content was 5%, 6% PVP K30 content was 46.2% (v/w), extrusion speed was 38.6 Hz, spheronization speed was 37.8 Hz, and rolling time was 7 min. Optimum formulation of puerarin pellets-type tablets was as follows: puerarin pellets was 8 g, MCC-102 was 8 g, PVPP was 3 g, L-HPC (LH22) was 0.5 g, and SiO2 was 0.4 g. The prepared tablets were disintegrated in 6 s, and the hardness was 95.5 N. The degree of fragmentation was less then 0.2%, and the dissolution rate of puerarin in 60 min was over 82%. The dissolution behaviors of pellets before and after compression had no significant difference. Conclusion: The formulation process of the puerarin pellets and pellets-type tablets optimized by Box-Behnken design and response surface method is effective and feasible with a good prediction, and the results show a high comprehensive score.

Key words:[Key words] puerarin; pellets-type tablet; Box-Behnken; response surface method

    [1] 宋清安,陈志标,陈丹.葛根素合纳洛酮治疗外伤性脑梗死的临床疗效观察[J].中国中西医结合急救杂志,2006,13(1):57-59.
    [2] 张年宝,程慧珍,崔卫东,等.葛根素对肾性高血压大鼠的降压作用及对肾组织ANGⅡ的影响[J].中药药理与临床,2010,26(2):26-29.
    [3] 林吉,候少贞.葛根素注射液的不良反应及口服制剂开发的探讨[J].世界科学技术-中药现代化,2005,140(15):48-50.
    [4] 姚丹,丁选胜.葛根素药理作用机制探讨及临床应用[J].中国临床药理学与治疗学,2008,13(4):468-474.
    [5] DASHEVSKY A, KOLTER K, BODMEIER R. Compression of pellets coated with various aqueous polymer dispersions[J].Int J Pharm,2004,279(1-2):19-26.
    [6] CHAROENTHAI N,KLEINEBUDDE P,PUTTIPIPATKHACHORN S. Influence of chitosan type on the properties of extruded pellets with low amount of microcrystalline cellulose[J].AAPS Pharm Sci Tech,2007,8(3): E99-E109.
    [7] 张婧,李翔,廖正根,等.高载药量二十五味肺病微丸的制备及其性能考察[J].中国实验方剂学杂志,2016,22(1):1-5.
    [8] 刘志华,方瑜,吴晓辉,等.兰索拉唑肠溶微丸片的研制[J].中国医药工业杂志,2013,44(11):1106-1110.
    [9] 赵晓宏,陈迪华,斯建勇,等.多指标综合评分法研究中药新药片剂成型处方[J].中成药,2002,24(8):579-581.
    [10] 国家药典委员会.中华人民共和国药典[S].2015年版.四部.北京:中国医药科技出版社,2015:通则010.
    [11] 冯飞飞,王明浩,黄春玉,等.k-卡拉胶在挤出滚圆法制备缬沙坦速释微丸中的应用[J].中国药科大学学报,2015,46(2):214-218.
    [12] 王双双,刘睿,何新.星点设计-效应面法优化桔梗泡腾片的处方[J].中国实验方剂学杂志,2016,22(12):23-27.
    [13] 苏珊珊,陈文,方贺,等. Box-Behnken效应面法优化松果菊苷PLGA 纳米粒处方工艺[J].中国新药杂志,2016,25(9):1069-1074.
    [14] 谢鹏,秦鹏,赵培静,等. 采用响应面法优化替考拉宁的层析工艺

    [J].今日药学,2014,24(2):73-77.
    [15] 昌水平,余香,梁志云,等. 响应面法优化火炭母中总黄酮的提取工艺研究

    [J].今日药学,2016,26(1):36-38,50.
    [16] 刘萍,程轩轩,张旭红,等. 响应面法优化龙眼核多糖的酶法提取工艺研究

    [J].今日药学,2016,26(5):331-334.