三叶青藤叶配方颗粒与饮片化学等量性及抗炎等效性研究

Study on Chemical Equivalence and Anti-inflammatory Equivalence of Aerial Parts of Tetrastigma Hemsleyanum Dispensing Granules and Decoction Pieces

目的基于特征图谱探究三叶青藤叶配方颗粒与饮片汤剂间的相关性和等量性,评价二者的抗炎药理等效性。方法建立三叶青藤叶饮片汤剂、中间体及配方颗粒的HPLC特征图谱共有模式;基于特征图谱与主要效应组分含量,建立等效比数学模型,计算迁移率,综合分析比较配方颗粒与饮片汤剂间的共有特征组分群的相似性及其含量的等量关联性。采用大鼠棉球肉芽肿增生炎症模型的抗炎抑制作用的药效实验,考察三叶青藤叶配方颗粒与饮片汤剂的等同药效相关性。结果基于HPLC特征图谱共有模式,辨识归属特征共有峰10个,汤剂与配方颗粒的相似度>0.900;由饮片煎煮对照汤剂各组分平均迁移率仅14.97%~23.89%,由饮片经优化工艺制得配方颗粒各组分平均迁移率为54.61%~92.30%。3批次配方颗粒与饮片平均等量等效比为3.72,以平均值的80%计,配方颗粒与饮片的等效比是2.98倍,提示1 g三叶青藤叶配方颗粒相当于饮片3 g。与模型组相比,配方颗粒与饮片汤剂均能显著减少大鼠肉芽肿的质量(P<0.05),对大鼠棉球肉芽肿炎症组织增生的抑制率,低、高剂量组的配方颗粒分别为15.70%,37.27%,饮片汤剂分别为14.59%,35.73%,二者均具有抗炎作用且呈剂量依赖性,二者对肉芽肿炎症抑制率在统计学上无显著性差异,提示配方颗粒与饮片汤剂(1∶3)之间具有等同的药效相关性。结论三叶青藤叶配方颗粒与饮片汤剂的共有药效组分群相似,配方颗粒与饮片的量效关联性为1∶3,以此量效比例用药,二者具有等同的药效相关性。

OBJECTIVE To explore the correlation and equivalence between Tetrastigma hemsleyanum dispensing granules and decoction pieces based on the characteristic spectrum,and evaluate the anti-inflammatory pharmacological equivalence.METHODS The common pattern of the HPLC characteristic spectra of the decoction pieces,decoction,intermediates,and dispensing granules of the aerial parts of Tetrastigma hemsleyanum was established.Based on the common pattern and the content of the main active ingredients,an equivalent-ratio model was built.The migration rates were calculated.The similarity of the common active ingredient groups and the equivalent correlation between the dispensing granules and the decoction pieces were analyzed.A cotton-pellet-induced rat granuloma model was used to conduct a pharmacodynamic study on the anti-inflammatory effect.The pharmacological equivalence between the dispensing granules and the decoction pieces of the aerial parts of Tetrastigma Hemsleyanum was evaluated.RESULTS The common pattern of the HPLC characteristic spectra was established.There were 10 characteristic common peaks.The similarity between the decoction and the dispensing granules was>0.900.The control decoction was prepared from decoction pieces with an average migration rate of 14.97%-23.89%.The dispensing granules were prepared from the decoction pieces,each the average mobility of the components was 54.61%-92.30%.The average equivalent ratio of the three batches of dispensing granules and decoction pieces was 3.72.Taking 80%of the average value as the result,the equivalent ratio between the dispensing granules and the decoction pieces was 2.98.This meant that 1 g dispensing granules was equivalent to 3 g decoction pieces.Compared with the model group,the dispensing granules and the decoction of the aerial parts of Tetrastigma hemsleyanum could significantly reduce the weight of rat granuloma(P<0.05).The inhibition rate on the proliferation of inflammatory tissue of cotton ball granuloma in rats was 15.70%and 37.27%in the low and high dose groups of dispensing granules,and 14.59%and 35.73%in the low and high dose groups of decoction.This implied that both the granules and the decoction had anti-inflammatory effect.Their inhibition rates had no significant difference,and were both dose-dependent.This implied that the dispensing granules and the decoction were pharmacological equivalent.CONCLUSION The common medicinal component groups of the aerial parts of Tetrastigma hemsleyanum dispensing granules and decoction pieces,decoction are similar,and the dose-effect correlation between dispensing granules and decoction pieces is 1∶3.The dose-effect ratio of the medicine is equivalent to the same medicinal effect correlation.