盐肤木总酚酸微丸的处方优化及制备工艺研究
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摘要
应用挤出滚圆法制备盐肤木总酚酸微丸,优化处方组成及其制备工艺。以收率、外观以及成丸性能为评价指标对处方因素(载药量、稀释剂、润湿剂和抗黏剂)进行单因素考察,优选处方组成;采用Box-Behnken设计与响应面法,以挤出速度、滚圆速度、滚圆时间为自变量,收率、脆碎度和圆整度的总评归一化值为因变量,优化制备工艺。单因素试验确定的最佳处方组成:载药量为28. 7%,微晶纤维素-乳糖9∶1,二氧化硅为抗黏剂,60%乙醇为润湿剂; Box-Behnken试验优化的制备工艺参数:挤出速度43 r·min-1,滚圆速度1 800 r·min-1,滚圆时间4 min,在此条件下,预测值和测定值偏差绝对值<5. 0%,与模型拟合程度较高,得到的制备工艺参数准确可靠,重复性良好。在扫描电镜下观察该工艺制备的盐肤木总酚酸微丸,粒径较均一,表面圆整光滑。该研究优化筛选出的处方组成及制备工艺稳定可行,可用于盐肤木总酚酸微丸的制备。
Extrusion-spheronisation method was used to prepare Rhus chinensis total phenolic acid pellets. The formula and preparation of R. chinensis total phenolic acid pellets were optimized. The formulas( drug loading capacity,diluent,wetting agent and anti-sticking agent) were determined by the single factor test with yield,appearance and performance as the indexes. The preparation was optimized by Box-Behnken design and response surface method,with the rate of extrusion,rate of spheronization and time of spheronization as the independent variables and the overall desirability value of yield,friability and roundness as the dependent variables. The optimal formula of pellets was as follows: drug loading capacity 28. 7%,MCC-lactose 9 ∶1,silicon dioxide as anti-sticking agent,and 60% ethanol as wetting agent. The optimal preparation was determined as follows: the rate of extrusion was 43 r·min-1,the rate of spheronization was 1 800 r·min-1,and the time of spheronization was 4 min. The absolute deviation between predicted value and estimated value under the conditions was less than 5. 0%,with a high degree of model fit. The preparation parameters obtained were accurate,reliable and reproducible. Under scanning electron microscopy( SEM),R. chinensis total phenolic acid pellets were uniform in diameter,round and smooth. The optimal formulation and process are stable and feasible for preparing R. chinensis total phenolic acid pellets.
Extrusion-spheronisation method was used to prepare Rhus chinensis total phenolic acid pellets. The formula and preparation of R. chinensis total phenolic acid pellets were optimized. The formulas( drug loading capacity,diluent,wetting agent and anti-sticking agent) were determined by the single factor test with yield,appearance and performance as the indexes. The preparation was optimized by Box-Behnken design and response surface method,with the rate of extrusion,rate of spheronization and time of spheronization as the independent variables and the overall desirability value of yield,friability and roundness as the dependent variables. The optimal formula of pellets was as follows: drug loading capacity 28. 7%,MCC-lactose 9 ∶1,silicon dioxide as anti-sticking agent,and 60% ethanol as wetting agent. The optimal preparation was determined as follows: the rate of extrusion was 43 r·min-1,the rate of spheronization was 1 800 r·min-1,and the time of spheronization was 4 min. The absolute deviation between predicted value and estimated value under the conditions was less than 5. 0%,with a high degree of model fit. The preparation parameters obtained were accurate,reliable and reproducible. Under scanning electron microscopy( SEM),R. chinensis total phenolic acid pellets were uniform in diameter,round and smooth. The optimal formulation and process are stable and feasible for preparing R. chinensis total phenolic acid pellets.
引文
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[2]方琴,何晓梅,陈存武.盐肤木原料林可持续经营措施[J].安徽农业科学,2018,46(23):69.
[3]李斌,高洁莹,龚力民,等.盐肤木果粕化学成分研究[J].中药材,2015,38(6):1209.
[4]王立,马维阳,张文君.微丸的研究进展[J].药学研究,2014(9):528.
[5]金浩,王立,张文君,等.缓控释微丸制备方法的研究进展[J].黑龙江医药,2015(1):93.
[6] Pan X,Chen M,Han K,et al. Novel compaction techniques with pellet-containing granules[J]. Eur J Pharm Biopharm,2010,75(3):436.
[7]程玲,郑娟,沈刚,等. pH依赖型黄芩苷纳米晶体结肠靶向微丸的制备及体外释药研究[J].中成药,2016,38(2):298.
[8]王勇,岳国超,王红军,等.挤出滚圆法在中药微丸中的应用[J].中国药业,2013,22(11):1.
[9]罗开沛,李小芳,罗佳,等.水飞蓟素纳米结晶微丸的表征及稳定性考察[J].中国实验方剂学杂志,2017,23(4):7.
[10]熊志伟,罗云,廖正根,等.丹参提取物混合粉的粉体学性质与微丸成型的相关性研究[J].中国中药杂志,2014,39(22):4317.
[11]孙强,李小芳,罗开沛,等.基于CRITIC权重赋值的Box-Behnken响应面法优化甘草黄酮纳米海绵制备工艺[J].中国中药杂志,2018,43(24):4855.
[12]赵锋,闫森,赵梦瑶,等.Box-Behnken法优化渗透泵微丸丸芯的制备工艺[J].中国医院药学杂志,2018,38(13):1377.
[13]茹庆国,彭宇,马书伟,等.响应面分析法优化当归超临界提取物结肠定位微丸的制备工艺研究[J].中国中药杂志,2016,41(13):2442.
[14]叶永华.盐肤木抗冠心病活性部位筛选及化学成分研究[D].福州:福建中医药大学,2018.
[15]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.
[16]冷静,林大胜,杨华蓉,等.三七三醇皂苷微丸的处方优化及制备工艺研究[J].中国药房,2013,24(23):2141.
[17]赵呈雷,曹鹏.响应面法优化葛根素微丸片的处方及工艺[J].中国新药杂志,2018,27(1):84.
[18]李雪,洪燕龙,鲜洁晨,等.基于转矩流变性的中药微丸润湿剂用量筛选研究[J].中国中药杂志,2017,42(17):3341.
[19]黄元红,邹和平,吕志勇,等.复方枣仁微丸的制备和体外溶出度研究[J].中成药,2014,36(5):1085.
[20]黄洋,贾晓斌,陈斌.水/乙醇在挤出滚圆法制备微丸中的作用与影响[J].中草药,2010,41(5):845.
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