基于药效筛选乌鳖颗粒中间体的醇沉工艺

Optimization of Alcohol Precipitation Technology of Wubie Granules Intermediates Based on Pharmacodynamic Screening

目的：优选乌鳖颗粒中间体的醇沉工艺,降低该制剂的日服用量。方法：通过考察卵巢摘除大鼠雌二醇（E2）,卵泡刺激素（FSH）,黄体生成素（LH）的活性和幼鼠子宫、卵巢发育情况,评价乌鳖颗粒中间体醇沉工艺的合理性。以二苯乙烯苷、川续断皂苷Ⅵ和固含物转移率为指标,通过单因素试验确定最佳醇沉工艺。采用HPLC测定二苯乙烯苷、川续断皂苷Ⅵ含量。结果：乌鳖颗粒中间体醇沉前后对药效试验无显著性差异。最佳醇沉工艺为何首乌组提取液浓缩至相对密度1.10（60℃）,加乙醇使含醇量达60%,静置时间〉12 h,上清液减压浓缩至相对密度1.20～1.23（60℃）。结论：药效评价结合单因素试验确定的何首乌组醇沉工艺更加合理、可靠,降低乌鳖颗粒日服用量的同时,还保证了该制剂的有效性。

Objective： To optimize alcohol precipitation technology of Wubie granules intermediates for reducing the daily dose of this preparation. Method： The rationality of alcohol precipitation technology of Wubie granules intermediates was determined by investigating activities of estradiol（ E2）,follicle stimulating hormone（ FSH）,luteinizing hormone（ LH） of ovariectomized rats and uterus,ovaries of mice. Taking transfer rates of stilbene glucoside,asperosaponin Ⅵ and solid content as indexes,single factor tests were adopted to optimize alcohol precipitation technology. Contents of stilbene glucoside and asperosaponin Ⅵ were determined by HPLC.Result： Optimum alcohol precipitation process was as follows： concentrated extracting liquid of Polygoni Multiflori Radix praeparata group to relative density of 1. 10（ 60 ℃）,added ethanol until the concentration of ethanol to 60%,standing time of 12 h,concentrated supernatant to relative density of 1. 20-1. 23（ 60 ℃）. Conclusion： Optimal alcohol precipitation technology is reasonable and reliable,which determines by pharmacodynamic screening and single-factor tests. This process can reduce the daily dose and ensure the effectiveness of Wubie granules.