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作为亲水性和亲脂性化合物的代表,依曲替酯对D-木糖和植物甲萘醌(维生素K1)肠道吸收无影响。

Lack of influence of etretinate on the intestinal absorption of D-xylose and of phytomenadione (vitamin K1) as representatives of hydrophilic and lipophilic compounds.

作者信息

Hartmann D, Crevoisier C, Dubach U C, Forgo I, Heizmann P

机构信息

Pharma Clinical Research Department, F. Hoffmann-La Roche & Co. AG, Basle Switzerland.

出版信息

Arzneimittelforschung. 1987 Dec;37(12):1392-6.

PMID:3449069
Abstract

The possible influence of the aromatic retinoid etretinate (Tigason ) on the intestinal absorption of D-xylose and phytomenadione (vitamin K1) has been studied in 7 healthy male volunteers between 22 and 25 years of age. D-xylose and phytomenadione were selected as being representative of water-soluble and fat-soluble test compounds, respectively. Following an oral dose of 25 g D-xylose the plasma levels and urinary excretion pattern of the compound were followed over 6 h. The plasma concentrations of phytomenadione after an oral dose of 20 mg of the vitamin were measured over 14 h. These absorption tests were performed before (baseline) and at the end of a 3-week treatment period with 25 mg b.i.d. etretinate. In addition some parameters on the serum lipid status pre and post etretinate treatment were monitored. The pharmacokinetic and biochemical determinants after treatment with etretinate were referenced to the pretreatment values and nonparametric confidence intervals (a less than 0.05) for these ratios were calculated. With respect to the area, AUC, under the D-xylose plasma concentration--time curve (0.79 less than or equal to RAUC = 1.00 less than or equal to 1.17) as well as to the cumulative amount excreted into urine over 6 h (0.90 less than or equal to RSUM = 1.04 less than or equal to 1.28) and to renal clearance (0.91 less than or equal to Rcl = 1.05 less than or equal to 1.25), no effect of etretinate on absorption and/or renal handling of D-xylose was discernible.(ABSTRACT TRUNCATED AT 250 WORDS)

摘要

已在7名年龄在22至25岁之间的健康男性志愿者中研究了芳香维甲酸依曲替酯(银屑灵)对D-木糖和植物甲萘醌(维生素K1)肠道吸收的可能影响。分别选择D-木糖和植物甲萘醌作为水溶性和脂溶性测试化合物的代表。口服25 g D-木糖后,在6小时内跟踪该化合物的血浆水平和尿排泄模式。口服20 mg该维生素后,在14小时内测量植物甲萘醌的血浆浓度。这些吸收测试在服用依曲替酯25 mg,每日两次,为期3周的治疗期之前(基线)和结束时进行。此外,还监测了依曲替酯治疗前后血清脂质状态的一些参数。将依曲替酯治疗后的药代动力学和生化指标参考治疗前的值,并计算这些比率的非参数置信区间(小于0.05)。关于D-木糖血浆浓度-时间曲线下的面积、AUC(0.79≤RAUC = 1.00≤1.17),以及6小时内累积尿排泄量(0.90≤RSUM = 1.04≤1.28)和肾清除率(0.91≤Rcl = 1.05≤1.25),未发现依曲替酯对D-木糖的吸收和/或肾脏处理有影响。(摘要截断于250字)

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