González-Esquivel D F, Rubio-Donnadieu F, Carvajal-Sandoval G, Jung H C
Laboratorio de Neuropsicofarmacología, Instituto Nacional de Neurología y Neurocirugía, México, DF, México.
Biopharm Drug Dispos. 1998 Dec;19(9):583-7. doi: 10.1002/(sici)1099-081x(199812)19:9<583::aid-bdd139>3.0.co;2-y.
The pharmacokinetics and the dose proportionality of a new anticonvulsant compound, HEPP (D,L-3-hydroxy-3-ethyl-3-phenylpropionamide) was studied in healthy male volunteers as part of the pharmacological evaluation for new drugs. Study was performed administering doses of 250, 375, 500 and 625 mg of HEPP to six male volunteers. Blood and urine samples were collected for 72 h postdose and analysed by HPLC. Results showed that in man HEPP is rapidly absorbed from the gastrointestinal tract. Tmax values were between 1.5 and 6.0 h. Plasma mean terminal half-life after the different doses ranged between 15.83 and 27.62 h with an overall harmonic mean value of 22.8. The mean AUC0-infinity and Cmax increased linearly with doses of 250, 375 and 500 mg but not with the dose of 625 mg. The amount of unchanged drug excreted in urine was between 3 and 6% of administered dose which shows an extensive metabolism of the drug.
作为新药药理学评估的一部分，在健康男性志愿者中研究了一种新型抗惊厥化合物HEPP（D，L-3-羟基-3-乙基-3-苯基丙酰胺）的药代动力学和剂量比例关系。对六名男性志愿者给予250、375、500和625mg的HEPP进行研究。给药后72小时收集血液和尿液样本，并通过高效液相色谱法进行分析。结果表明，在人体中，HEPP可迅速从胃肠道吸收。达峰时间值在1.5至6.0小时之间。不同剂量后的血浆平均终末半衰期在15.83至27.62小时之间，总体调和平均值为22.8。250、375和500mg剂量时，平均药时曲线下面积（AUC0-∞）和峰浓度（Cmax）与剂量呈线性增加，但625mg剂量时并非如此。尿液中排泄的原形药物量占给药剂量的3%至6%，这表明该药物有广泛的代谢。
