正交设计结合药效学实验优选桂栀助眠胶囊提取工艺研究

Optimization of extraction technology of Guizhi Zhumian Capsule by orthogonal design and pharmacodynamics test

目的优选桂栀助眠胶囊最佳提取工艺。方法在单因素实验结果基础上,采取正交试验法,以干膏得率和栀子苷转移率为指标,考察加水量、提取时间、提取次数3个因素,优选桂栀助眠胶囊最佳水提工艺;以药液浓度、药液含醇量、醇沉时间为考察因素,优选桂栀助眠胶囊最佳醇沉工艺;通过改善睡眠药效学实验对醇沉前后提取物进行比较。结果桂栀助眠胶囊最佳水提工艺为加10倍量水煎煮3次,每次0.5 h;最佳醇沉工艺为水提滤液浓缩至1 mL药液相当于原药材1 g,药液含醇量为80%,醇沉时间为12 h。与阴性对照组比较,桂栀助眠胶囊水提取物能延长戊巴比妥钠小鼠睡眠时间(P<0.01),且能增加戊巴比妥钠阈下剂量小鼠入睡率(P<0.05);水提醇沉物有延长巴比妥钠小鼠睡眠时间,增加小鼠入睡率的趋势,但差异无显著性(P>0.05)。结论醇沉前后提取物药效存在差异,为不影响药效,最终选择水提工艺作为制剂的最佳提取工艺。

Objective To optimize the extraction technology of Guizhi Zhumian Capsules(GZC). Methods Based on the analysis of the single factor experiment results, the orthogonal test method was adopted to study the three factors including the amount of water added, extraction time, and extraction frequency by taking the dry extract yield of the medicinal materials and transfer rate of geniposide as indicators to optimize the water extraction process of GZC. To optimize the alcohol precipitation process of GSC, these factors including the concentration of the medicinal materials, alcohol content, and time of alcohol precipitation were investigated. The extracts before and after alcohol precipitation were compared by improving sleep pharmacodynamics. Results The best water extraction technology of GZC was decocted three times with 10 times of water, 0.5 h each time. The optimal alcohol precipitation process was to concentrate the filtrate of water extraction to 1 mL, which was equivalent to 1 g of the original medicinal materials, with 80% alcohol content and 12 h alcohol precipitation time. Compared with the negative control group, the water extract group of GZC could prolong the sleep time of pentobarbital sodium mice and increase the sleep rate of mice under the lower dose of pentobarbital sodium valve(P < 0.05). The water extract group and the water extract and alcohol precipitation showed a trend of shortening the sleep latent period of the mice with barbiturate sodium, but there was no significant difference(P > 0.05). Conclusion The pharmaceutical efficacy of the extract before and after alcohol precipitation was different. In order not to affect the drug effect, the water extraction process was finally selected as the best extraction process.