Adachi Y, Wakisaka G, Yamamoto T
Gastroenterol Jpn. 1975;10(2):120-31. doi: 10.1007/BF02774839.
Salicylamide glucuronide (SAMG) in 0-6 and 6-12 hours-urine specimens was determined after oral administration of salicylamide in 7 normal volunteers (NV), in 51 cases of various liver diseases and hyperbilirubinemias, and in 19 cases after drug administration, to predict the in vivo drug metabolism in man and its change by drugs. Maximal glucuronide formation was obtained by 1.0 g of salicylamide administered to NV; thus, this dosage was used in the present study. SAMG as percent of total salicylamide, the percent of SAMG, from 0-6 hours-urine specimens was high and constant in NV (71.3 +/- 8.3 (Mean +/- S.D.)). 0-0.08% of the total salicylamide was confirmed as free salicylamide in 0-12 hours-urine specimens of NV. The percent of SAMG of 0-6 hours-urine specimens was 57.2 +/- 8.6 in acute hepatitis, 66.6 +/- 10.9 in chronic hepatitis, and 48.6 +/- 10.7 in liver cirrhosis (mean +/- S.D.). Free salicylamide increased slightly in liver diseases. Serum bilirubin levels tended to be inversely correlated with the percent of SAMG. In most cases of Gilbert's syndrome, the percent of SAMG remained at a normal level. The percent of SAMG in cases with unconjugated hyperbilirubinemias of other geneses were almost within normal limits. Bucolome and phenobarbital increased the percent of SAMG in patients with various liver diseases. After rifampicin or phenytoin administration, the percent of SAMG of the patients with lung tuberculosis or epilepsy did not surpass that of NV.
在7名正常志愿者(NV)、51例各种肝脏疾病和高胆红素血症患者以及19例用药后患者口服水杨酰胺后,测定了0 - 6小时和6 - 12小时尿液样本中的水杨酰胺葡萄糖醛酸苷(SAMG),以预测人体体内药物代谢及其受药物的影响。给正常志愿者服用1.0 g水杨酰胺可获得最大葡萄糖醛酸苷形成量;因此,本研究采用该剂量。以总水杨酰胺的百分比表示的SAMG,在正常志愿者0 - 6小时尿液样本中占比高且恒定(71.3±8.3(平均值±标准差))。在正常志愿者0 - 12小时尿液样本中,总水杨酰胺的0 - 0.08%被确认为游离水杨酰胺。急性肝炎患者0 - 6小时尿液样本中SAMG的百分比为57.2±8.6,慢性肝炎患者为66.6±10.9,肝硬化患者为48.6±10.7(平均值±标准差)。肝脏疾病患者中游离水杨酰胺略有增加。血清胆红素水平与SAMG百分比呈负相关趋势。在大多数吉尔伯特综合征病例中,SAMG百分比保持在正常水平。其他病因的非结合性高胆红素血症患者中SAMG百分比几乎在正常范围内。布可隆和苯巴比妥增加了各种肝脏疾病患者的SAMG百分比。服用利福平或苯妥英后,肺结核或癫痫患者的SAMG百分比未超过正常志愿者。