小蓟胶囊制备工艺及抗氧化活性研究

Study on Preparation Technology and Antioxidant Activity of Antioxidant Capsules of Cirsium Setosum

优选小蓟抗氧化胶囊的最佳辅料与制剂工艺并验证制备的胶囊的质量和抗氧化活性。通过测定不同比例辅料的吸湿率、堆密度等,筛选出最佳辅料,并确定胶囊壳的型号和装量。对蒙花苷的含量、薄层色谱、水分、装量差异进行小蓟胶囊的质量评价实验研究,以此考察制备的小蓟胶囊是否符合“中国药典2020版”的相关要求。以Vc作为对照,考察胶囊内容物对DPPH自由基的清除能力,以自由基清除率为指标,计算清除率和半数有效浓度的IC50值。小蓟胶囊浸膏粉与微晶纤维素的最佳比例为1∶1,休止角为33.69°,堆密度为0.5208 g·mL^(-1),选用0号胶囊壳,胶囊的装量为0.3489 g。质量评价实验结果显示,薄层色谱检测发现供试品与对照品色谱在相应位置显相同颜色荧光斑点,表明小蓟胶囊内容物中含有蒙花苷。含量测定得出,每粒小蓟胶囊中蒙花苷的质量应不低于115 mg。装量差异检测得到,小蓟胶囊3批次的装量差异均在±7.5%内,符合“中国药典2020版”的要求。通过抗氧化活性实验发现,小蓟胶囊和Vc对DPPH自由基的清除能力均表现为随着浓度的升高而提升,代入回归方程得出小蓟胶囊的半数有效浓度IC_(50)值为0.06 mg·mL^(-1),Vc的半数有效浓度IC_(50)值为0.13 mg·mL^(-1)。

The best excipients and preparation technology of Cirsium Setosum antioxidant capsules were selected and,the quality and antioxidant activity of the capsules were verified.By measuring the moisture absorption rate and bulk density of different proportions of auxiliary materials,the best auxiliary materials were screened out,and the model and loading quantity of capsule shell were determined.The quality evaluation experiment of Cirsium Setosum capsule was conducted on the differences in the content,TLC,water content and loading amount of mongaridin,so as to investigate whether the prepared Cirsium Setosum capsule met the relevant requirements of"Chinese Pharmacopoeia 2020 edition".With Vc as the control,the scavenging ability of the capsule contents on DPPH free radicals was investigated.The scavenging rate and IC_(50)value of half effective concentration were calculated using the free radical scavenging rate as the index.The optimal ratio of extract powder of small thistle capsule to microcrystalline cellulose was 1∶1,the angle of repose was 33.69°,the bulk density was 0.5208 g·mL^(-1),and the filling mass of capsule was 0.3489 g.The results of the quality evaluation experiment showed that the TLC detection showed the same color fluorescence spots in the corresponding positions of the test and control samples,indicating that the contents of the small thistle capsule contained montanoside.The content of mongarin in each small thistle capsule should not be less than 115 mg.The loading volume difference test showed that the loading volume difference of the three batches of Cirsium Setosum capsule was within ±7.5%,which was in line with the requirements of"Chinese Pharmacopoeia 2020 edition".The antioxidant activity experiment showed that the scavenging ability of Cirsium Setosum capsule and Vc on DPPH radical increased with the increase of concentration.The IC_(50)values of Cirsium Setosum capsule and Vc were 0.06 mg·mL^(-1)and 0.13 mg·mL^(-1),respectively,after substituting the regression equation.