| 引用本文:林上阳，周雅倩，谢辉，李伟东.杜仲极细粉与传统饮片有效成分溶出行为及大鼠药动学比较研究[J].世界中医药,2020,(21):. |
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| 杜仲极细粉与传统饮片有效成分溶出行为及大鼠药动学比较研究 |
| Comparative Study on Dissolution Behavior of Effective Ingredients from Eucommia Ultrafine Powder and Traditional Decoction Pieces and Pharmacokinetics in Rat |
| 投稿时间：2019-11-02 |
| DOI：10.3969/j.issn.1673-7202.2020.21.006 |
| 中文关键词: 杜仲 极细粉 传统饮片 溶出度 生物利用度 京尼平苷酸 高效液相色谱法 超高效色谱-串联质谱 |
| English Keywords:Eucommia ulmoides Ultra-fine powder Traditional decoction pieces Dissolution Bioavailability Geniposide acid High performance liquid chromatography Ultra performance chromatography-tandem mass spectrometry(Chinese keywords please use Chinese) |
| 基金项目:国家自然科学基金面上项目(81773902)——基于“咸入肾”,“肾主骨”理论研究青娥丸中杜仲、补骨脂盐炙增效机制 |
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| 中文摘要: |
| 目的:研究杜仲Eucommia ulmoides Oliv.极细粉与传统饮片的体外溶出度及其在大鼠体内的生物利用度,揭示杜仲极细粉碎后主要活性成分的体内外溶出的变化,为杜仲极细粉的质量标准的制定提供科学依据。方法:激光粒度分析仪测定杜仲极细粉的粒径;HPLC法测定杜仲极细粉与传统饮片有效成分在不同溶出介质中溶出度。UPLC-MS/MS测定杜仲京尼平苷酸的血药浓度变化。结果:杜仲极细粉有效成分溶出总量都显著高于杜仲传统饮片(P<0.05),杜仲传统饮片有效成分的溶出度和溶出速率均低于极细粉(P<0.05)。京尼平苷酸在大鼠体内的血药浓度-时间数据符合二室模型,权重为1,高剂量极细粉组和高剂量水煎液组的主要药动学参数为MRT(0-t)=(241.498±20.678)min和(135.084±13.571)min;Tmax=(132±26.833)min和(65±12.247)min;Cmax=(231.8±80.111)μg/L和(435.167±208.696)μg/L;AUC(0-t)=(61 947.696±27 073.105)μg/(L·min)和(63 212.803±31 981.087)μg/(L·min);AUC(0-∞)=(62 327.808±27 079.977)μg/(L·min)和(63 910.596±31 686.357)μg/(L·min)。结论:杜仲极细粉碎后能显著增加有效成分的溶出度和显著提高有效成分的溶出速率,且可以增加京尼平苷酸在大鼠体内的停留时间。杜仲传统饮片制备成极细粉具备可行性。 |
| English Summary: |
| To study the in vitro dissolution rate of Eucommia ulmoides Oliv.ultrafine powder and traditional decoction pieces and its bioavailability in rats,and to reveal the changes in the in vivo and in vitro dissolution of the main active ingredients of Eucommia ulmoides Oliv.The formulation of quality standards provides a scientific basis.Methods:Laser particle size analyzer was used to determine the particle size of Eucommia ulmoides ultrafine powder; HPLC method was used to determine the dissolution of the effective components of Eucommia ulmoides ultrafine powder and traditional decoction pieces in different dissolution media.UPLC-MS/MS was used to determine the blood concentration of Eucommia geniposide.Results:The total dissolution of active ingredients of Eucommia ulmoides extra-fine powder was significantly higher than that of traditional eucommia ulmoides(P<0.05).The dissolution rate and dissolution rate of active ingredients of eucommia ulmoides traditional decoction pieces were lower than those of ultrafine powder(P<0.05).The plasma concentration-time data of geniposide in rats conformed to the two-compartment model,with a weight of 1.The main pharmacokinetic parameters of the high-dose ultrafine powder group and the high-dose decoction group were MRT(0-t)=(241.498±20.678)and(135.084±13.571)min; Tmax=(132±26.833)and(65±12.247)min; Cmax=(231.8±80.111)and(435.167±208.696)μg/L; AUC(0-t)=(61 947.696±27 073.105)and(63 212.803±31 981.087)μg/（L·min）; AUC(0-∞)=(62 327.808±27 079.977)and(63 910.596±31 686.357)μg/（L·min）.Conclusion:Eucommia ulmoides can significantly increase the dissolution rate of the active ingredients and the dissolution rate of the active ingredients after extremely fine pulverization,and can increase the residence time of geniposide acid in rats.Traditional decoction pieces of Eucommia ulmoides can be prepared into very fine powder. |
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