Egen-Schwind C, Eckard R, Jekat F W, Winterhoff H
Institut für Pharmakologie und Toxikologie, Westfälischen Wilhelms-Universität Münster, Federal Republic of Germany.
Planta Med. 1992 Feb;58(1):8-13. doi: 10.1055/s-2006-961379.
The pharmacokinetic behaviour of vinyldithiins, the main constituents of oily preparations of garlic (Allium sativum L.), was investigated after oral administration of 27 mg 2-vinyl-4H-1,3-dithiin and 9 mg 3-vinyl-4H-1,2-dithiin to rats. In serum, kidney, and fat tissue, both vinyldithiins could be detected by GC-MS over a period of 24 h, whereas in liver only 1,3-vinyldithiin was found. Pharmacokinetic parameters (t1/2, ke, Cltot, AUC, and Vd) were determined using compartment models, elucidating the different pharmacokinetic behaviour of both vinyldithiins. 1,3-Vinyldithiin seems to be less lipophilic and is rapidly eliminated from serum, kidney, and fat tissue, whereas 1,2-vinyldithiin is more lipophilic and shows a tendency to accumulate in fat tissue. Experiments with liver homogenate confirmed the in vivo findings on the different degradation rates of both vinyldithiins. Allicin, the precursor of the vinyldithiins, is metabolized more rapidly in liver homogenate than the vinyldithiins.
在给大鼠口服27毫克2-乙烯基-4H-1,3-二硫醚和9毫克3-乙烯基-4H-1,2-二硫醚后，对大蒜（葱属植物）油制剂的主要成分乙烯基二硫醚的药代动力学行为进行了研究。在血清、肾脏和脂肪组织中，在24小时内都可以通过气相色谱-质谱联用仪检测到这两种乙烯基二硫醚，而在肝脏中仅发现了1,3-乙烯基二硫醚。使用房室模型确定了药代动力学参数（t1/2、ke、Cltot、AUC和Vd），阐明了两种乙烯基二硫醚不同的药代动力学行为。1,3-乙烯基二硫醚似乎亲脂性较低，能迅速从血清、肾脏和脂肪组织中消除，而1,2-乙烯基二硫醚亲脂性更强，有在脂肪组织中蓄积的倾向。肝脏匀浆实验证实了两种乙烯基二硫醚在体内不同降解速率的研究结果。乙烯基二硫醚的前体大蒜素在肝脏匀浆中的代谢速度比乙烯基二硫醚更快。
