Katayama H, Watanabe M, Yoshitomi H, Yoshida H, Kimoto H, Kamiya A, Hayashi T, Akimura T
Fukuyama University, Faculty of Pharmacy and Pharmaceutical Sciences, Hiroshima, Japan.
Biol Pharm Bull. 1998 Mar;21(3):304-7. doi: 10.1248/bpb.21.304.
The urinary excretion of valproic acid (VPA) and its metabolites (3-keto VPA, 3-OH VPA, and VPA-glucuronide) in 6 epileptic patients was studied using gas chromatography-mass spectrometry. The amount of VPA and 3-OH VPA excreted in the urine was low (0.1-0.5% of the dose of VPA and 0.6-1.5% of the dose of 3-OH administered). The amount of 3-keto VPA and glucuronide (VPA-Glu) excreted was marked (5.8-26.2% and 13.1-88.7% of the dose of VPA administered, respectively). The urinary excretion of VPA and its metabolites by patients who have taken a normal amount of a VPA preparation was almost the same as that of healthy volunteers. Two epileptic patients who took a large amount of the VPA preparation showed a high excretion of VPA-Glu without an increase in their plasma VPA-Glu.
采用气相色谱 - 质谱联用技术研究了6例癫痫患者体内丙戊酸(VPA)及其代谢产物(3 - 酮基VPA、3 - 羟基VPA和VPA - 葡萄糖醛酸苷)的尿排泄情况。尿液中排泄的VPA和3 - 羟基VPA量较低(分别为VPA给药剂量的0.1 - 0.5%和3 - 羟基VPA给药剂量的0.6 - 1.5%)。排泄的3 - 酮基VPA和葡萄糖醛酸苷(VPA - Glu)量显著(分别为VPA给药剂量的5.8 - 26.2%和13.1 - 88.7%)。服用正常剂量VPA制剂的患者VPA及其代谢产物的尿排泄情况与健康志愿者几乎相同。两名服用大量VPA制剂的癫痫患者显示VPA - Glu排泄量高,但其血浆VPA - Glu并未增加。