Bhat B G, Chandrasekhara N
Toxicology. 1986 Jul;40(1):83-92. doi: 10.1016/0300-483x(86)90048-x.
Upon administration of piperine, the major bite factor of black pepper, to male albino rats at a dose of 30 mg (170 mg/kg) by gavage or 15 mg (85 mg/kg) intraperitoneally, about 97% was absorbed irrespective of the mode of dosing. Three per cent of the administered dose was excreted as piperine in the feces. Piperine was not detectable in urine. When everted sacs of rat intestines were incubated with 200-1000 micrograms of piperine, about 47-64% of the added piperine disappeared from the mucosal side. Only piperine was present in the serosal fluid and also the intestinal tissue, indicating that piperine did not undergo any metabolic change during absorption. Examination of the passage of piperine through the gut indicated that the highest concentration in the stomach and small intestine was attained at about 6 h. Only traces (less than 0.15%) of piperine were detected in serum, kidney and spleen from 30 min to 24 h. About 1-2.5% of the intraperitoneally administered piperine was detected in the liver during 0.5-6 h after administration as contrasted with 0.1-0.25% of the orally administered dose. The increased excretion of conjugated uronic acids, conjugated sulphates and phenols indicated that scission of the methylenedioxy group of piperine, glucuronidation and sulphation appear to be the major steps in the disposition of piperine in the rat.
给雄性白化病大鼠经口灌胃给予胡椒碱（黑胡椒的主要辛辣成分），剂量为30毫克（170毫克/千克），或腹腔注射15毫克（85毫克/千克），无论给药方式如何，约97%的胡椒碱均可被吸收。给药剂量的3%以胡椒碱形式经粪便排出。尿液中未检测到胡椒碱。当用200 - 1000微克胡椒碱孵育大鼠肠外翻囊时，约47 - 64%添加的胡椒碱从黏膜侧消失。浆膜液和肠组织中仅存在胡椒碱，表明胡椒碱在吸收过程中未发生任何代谢变化。对胡椒碱在肠道内通过情况的检查表明，胃和小肠中的最高浓度在约6小时时达到。在30分钟至24小时期间，血清、肾脏和脾脏中仅检测到微量（低于0.15%）的胡椒碱。腹腔注射的胡椒碱在给药后0.5 - 6小时内，约1 - 2.5%在肝脏中被检测到，而口服给药剂量的这一比例为0.1 - 0.25%。结合糖醛酸、结合硫酸盐和酚类排泄增加表明，胡椒碱亚甲二氧基的断裂、葡萄糖醛酸化和硫酸化似乎是大鼠体内胡椒碱代谢的主要步骤。
