青蒿药材提取物对青蒿素生物利用度的影响

Influence of Herba Artemisiae Annuae Medicinal Material on Bioavailability of Artemisinin

目的研究青蒿药材中成分对青蒿素生物利用度的影响。方法向青蒿素中添加青蒿提取浸膏和辅料制备2种青蒿素复方。小鼠灌胃给予青蒿素复方及混悬液,用高效液相-库仑阵列电化学检测(HPLC-ECD)法测定小鼠血浆中青蒿素的浓度,以DAS3.2.8药动学软件计算相关药动学参数,探讨不同复方对青蒿素生物利用度的影响。结果 2种青蒿素复方A、B及青蒿素混悬液的相关药动学参数分别为:T_(max)为(23.86±8.18)、(33.50±13.55)、(34.00±9.66)min;C_(max)为(2.78±1.16)、(7.54±1.86)、(0.83±0.16)μg·mL^(-1);AUC_((0-t))为(152.93±24.08)、(373.06±56.52)、(23.83±5.62)μg·mL^(-1)·min;以混悬液为参比,2种青蒿素复方的相对生物利用度分别为654.00%、1582.86%。结论青蒿药材中存在某些能提高青蒿素生物利用度的成分,为青蒿素制剂研发中的配方筛选提供参考。

Objective To research the impact of the chemical composition from Herba Artemisiae Annuae medicinal material on the bioavailability of artemisinin. Methods Two kinds of artemisinin-based combinations（artemisinin recipe A and B ） were made from artemisinin with Herba Artemisiae Annuae extract and excipients added respectively. The mice were respectively given gastric gavage of the artemisinin recipes and artemisinin suspension, and then the concentration of artemisinin in mice plasma was detected by high performance liquid chromatography-electrochemical detector （HPLC-ECD）. The pharmacokinetic parameters and relative bioavailability of artemisininin different recipes were calculated by the pharmacokinetic software DAS3.2.8. Results The pharmacokinetic parameters for artemisinin inartemisinin recipe A, artemisinin recipe B and artemisinin suspension were as follows： Tmax being （23.86±8.18）, （33.50±13.55）, （34.00±9.66） min; Cm= being （2.78±1.16）, （7.54±1.86）, （0.83±0.16） μg·mL^-1; AUC（0-1） being （152.93±24.08）, （373.06±56.52）, （23.83±5.62） μg·mL^-1·min, respectively. With the suspension as reference, the relative bioavailability of artemisinin recipe A and B was 654.00 %, 1582.86 % respectively. Conclusion There exist some chemical components in Herba Artemisiae Annuae medicinal material, which can enhance the bioavailability of artemisinin. The results will provide a reference for the formulation selection in further research of the artemisinin preparation.