厚朴不同粒径粉体溶出行为比较研究

目的:比较厚朴不同粒径粉体中主要活性成分厚朴酚、和厚朴酚溶出情况,为厚朴超微粉体的粒径控制与制剂生产提供实验依据。方法:采用高效液相色谱法分别对厚朴超微粉体和普通粉体中所含主要活性成分的提取率及不同溶出介质的相对累积溶出率进行定量研究。色谱条件:采用ZORBX-C₁₈(4.6 mm×150 mm,5 μm)色谱柱,流动相为甲醇-水(75:25),流速1 mL·min^-1,检测波长294 nm,柱温30 ℃,进样量10 μL。结果:厚朴超声提取的厚朴酚及和厚朴酚的相对提取率较回流提取高,且不同粒度粉体的相对提取率大小为60 Hz超微粉体 > 23 Hz超微粉体 > 42 Hz超微粉 > 常规粉体,厚朴不同粒度粉体在不同溶出介质中的相对累积溶出率大小为人工胃液 > 蒸馏水 > 人工肠液;在本次试验所选4个粒度粉体中,60 Hz超微粉体为最佳粒度粉体。厚朴超微粉体与普通粉体主要活性成分的提取率以及在水、人工胃液、人工肠液中的相对累积溶出率差异显著。结论:适度的微粉化能促进厚朴有效成分的溶出,其溶出行为还受到不同溶出介质的影响,超微粉碎技术应用于厚朴药材具有可行性。

Objective:To compare the differences in the dissolution behavior of magnolol and honokiol between ultrafine powder and common powder of Magnolia officinalis to provide experimental evidence for the control of particle size and preparation production of the ultrafine powder.Methods:The relative extraction rates and relative cumulative dissolution rates of powders of Magnolia officinalis in different dissolution mediums were quantitatively studied by HPLC.The chromatographic column was ZORBX-C₁₈ (4.6 mm×150mm,5 μm),the mobile phase was methanol-water (75:25),the detection wavelength was 294 nm at the flow rate of 1.0 mL·min^-1,the column temperature was 30 ℃ and the volume of injection was 10 μL.Results:The relative ultrasonic extraction rate was higher than the reflux extraction rate.The order of the different powders of Magnolia officinalis by extraction rate was 60 Hz ultrafine powder > 23 Hz ultrafine powder > 42 Hz ultrafine powder > common powder.The order of different dissolution mediums for powders by relative cumulative dissolution rate was simulated gastric fluid > distilled water > simulated intestinal fluid,and the best particle size of the four sizes selected in this experiment was 60Hz ultrafine powder.There were significant differences between ultrafine and common powders in the extraction rates and relative cumulative dissolution rates in distilled water,simulated gastric fluid and simulated intestinal fluid.Conclusion:An appropriate degree of ultrafine grinding can promote the dissolution of active ingredients of Magnolia officinalis and the dissolution is influenced by the dissolution medium.The application of ultrafine grinding technology to Magnolia officinalis was proved to be feasible.