| LC-MS/MS法研究瓜蒌缓释微丸在大鼠体内的药代动力学特征 |
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| 引用本文： | 卞莹莹,邹纯才,鄢海燕,孙德考,胡 倩.LC-MS/MS法研究瓜蒌缓释微丸在大鼠体内的药代动力学特征[J].南方医科大学学报,2020,40(7):995-1000. |
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| 作者姓名： | 卞莹莹 邹纯才 鄢海燕 孙德考 胡 倩 |
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| 摘 要： | 目的 建立高效液相色谱串联质谱法（LC-MS/MS）考察瓜蒌缓释微丸与瓜蒌提取物中3,29-二苯甲酰基栝楼仁三醇（3,29-DK）在大鼠体内不同时间点的血药浓度及药代动力学特征。方法 健康雄性SD大鼠分为2组：瓜蒌缓释微丸组与瓜蒌提取物组，单次灌胃给药后，瓜蒌缓释微丸组在第0、1、2、4、6、8、10、12、18、24、36、48小时眼眶取血；瓜蒌提取物组在第0、15、30、45、60、
90、120、180、240、300分眼眶取血。血浆样品预处理，采用LC-MS/MS法测定瓜蒌缓释微丸组与瓜蒌提取物组血浆中的3,29-DK浓度，建立3,29-DK含量测定标准曲线并进行专属性、最低检测限、精密度及准确度、提取回收率、稳定性、基质效应等方法学考察。测定瓜蒌缓释微丸组和瓜蒌提取物组不同时间点的3,29-DK平均血药浓度，运用Das 2.0软件处理数据，求算药代动力学参数，采用SPSS 26.0统计学软件进行统计分析。结果 3,29-DK浓度在0.5 ng/mL~32 ng/mL范围内线性关系良好，方法学验证结果均符合生物样品测定的规定。与瓜蒌提取物组相比较，瓜蒌缓释微丸组3,29-DK的AUC(0-t)、AUC（0-∞）、MRT（0-t）、MRT（0-∞）、t1/2z及Tmax差异具有统计学意义（P<0.05）。结论 瓜蒌缓释微丸提高了药物在大鼠体内的缓释效果，为瓜蒌新剂型的研究提供基础。
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| 关 键 词： | 高效液相色谱串联质谱法 瓜蒌缓释微丸 3 29-二苯甲酰基栝楼仁三醇 药代动力学 |
LC-MS/MS analysis of pharmacokinetics of 3,29-dibenzoyl karounitriol in rats following
administration of Trichosanthes sustained-release pellets |
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| Abstract: | Objective To study the plasma concentration and pharmacokinetics of 3,29-Dibenzoyl Karounitriol (3,29-DK) from
sustained- release pellets and extracts of Trichosanthes at different time points in rats using high-performance liquid
chromatography- tandem mass spectrometry (LC-MS/MS). Methods Healthy male SD rats were given a single gavage of
Trichosanthes sustained-release pellets or Trichosanthes extract, and orbital blood samples were taken at different time points
within 48 h after drug administration in the pellet group and within 5 h in Trichosanthes extract group for determination of the
plasma concentrations of 3,29-DK using LC-MS/MS. The standard curve of 3,29-DK content was established, and the
specificity, minimum detection limit, precision and accuracy, extraction recovery, stability and matrix effect of LC-MS/MS
analysis were assessed. The mean plasms levels of 3,29-DK at different time points after the drug administration were
determined and its pharmacokinetic parameters were calculated using Das 2.0 software. Results LC-MS/MS analysis showed a
good linearity of 3,29-DK concentration within the range of 0.5-32 ng/mL, and the results of methodological validation
confirmed the validity of this method for biological sample determination. Trichosanthes sustained-release pellets and
Trichosanthes extract showed significant differences in their AUC(0- t), AUC(0- ∞), MRT(0- t), MRT(0- ∞), t1/2z and Tmax of 3,29-DK after
administration in rats (P<0.05). Conclusion Trichosanthes sustained-release pellets are capable of sustained-release of 3,29-DK
in rats, and thus provides a basis for the study of new dosage forms of Trichosanthes. |
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| Keywords: | high-performance liquid chromatography-tandem mass spectrometry Trichosanthes sustained-release pellets 3 29- dibenzoyl karounitriol pharmacokinetics |
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