Pueraria mirifica is an endemic Thai plant that has been used for rejuvenation and in the relief of various aging diseases. Puerarin is one of the major isoflavones found in this plant and shows several pharmacological activities in relation to the Thai traditional use of P. mirifica. Therefore, comparative pharmacokinetics of pure puerarin alone and that in a P. mirifica extract in cynomolgus monkeys were conducted in order to investigate the pharmacokinetic profiles of the 2 preparations. To this end, puerarin and P. mirifica extract, at an equivalent dose of 10 mg/kg of puerarin, were orally dosed to adult female monkeys for 7 consecutive days. A single intravenous injection of puerarin at a dose of 1 mg/kg was also peformed. Serial blood samples and excreta were collected from 0 - 24 h and 0 - 48 h after dosing. Determination of the puerarin levels and its metabolites in biological samples was conducted by liquid chromatography tandem mass spectrometry. Plasma levels of aspartate aminotransferase, alanine aminotransferase, and creatinine fluctuated in the normal range, with no abnormal physical signs in the animal. The absolute oral bioavailability of puerarin was approximately 1% in both preparations. Accumulation of puerarin was found after oral dosing for 7 consecutive days in both groups. Major metabolites of puerarin found in monkeys were hydroxylation and deglycosylation products. A negligible amount of unchanged puerarin was detected in urine and feces. Pharmacokinetic profiles obtained from this study could help to design the prescribed remedy of puerarin and P. mirifica extract phytopharmaceutical products for human use.

中文翻译：

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单独葛根素和野葛根提取物在雌性食蟹猴体内的药代动力学比较

Pueraria mirifica 是一种泰国特有植物，已被用于恢复活力和缓解各种衰老疾病。葛根素是在这种植物中发现的主要异黄酮之一，并显示出与泰国传统用途 P. mirifica 相关的几种药理活性。因此，为了研究两种制剂的药代动力学特征，对单独的纯葛根素和猕猴桃提取物在食蟹猴中的药代动力学进行了比较。为此，将葛根素和山茱萸提取物以 10 mg/kg 葛根素的等效剂量连续 7 天口服给药于成年雌性猴。还进行了剂量为1mg/kg的葛根素的单次静脉注射。在给药后 0-24 小时和 0-48 小时收集系列血样和排泄物。生物样品中葛根素含量及其代谢物的测定采用液相色谱串联质谱法。血浆天冬氨酸转氨酶、丙氨酸转氨酶和肌酐水平在正常范围内波动，动物体征未见异常。两种制剂中葛根素的绝对口服生物利用度约为 1%。两组均连续7天口服后发现葛根素蓄积。在猴子中发现的葛根素的主要代谢物是羟基化和去糖基化产物。在尿液和粪便中检测到可忽略不计的原形葛根素。从这项研究中获得的药代动力学特征可以帮助设计用于人类使用的葛根素和 P. mirifica 提取物植物药物产品的处方药。