Fernández N, Diez M J, Terán M T, García J J, Calle A P, Sierra M
Department of Physiology, Pharmacology and Toxicology, University of León, León, Spain.
J Pharmacol Exp Ther. 1998 Aug;286(2):870-4.
Fiber formulations are used in human nutrition owing to their beneficial properties for health. It is probable that ingestion of fiber coincides with the oral administration of drugs, and a modification of its oral absorption, and therefore of its pharmacokinetics, can appear. In the present study, the compartmental and noncompartmental pharmacokinetic parameters of ethinylestradiol (EE) in rabbits after oral administration were determined. It was also studied whether the presence of two different fiber formulations [A, wheat bran (76.5%), fruit fiber (12%) and guar gum (2%) and B, Plantago ovata seeds (65%) and P. ovata seed cuticles (2.2%)] in the gastrointestinal tract modified the pharmacokinetics of EE when administered at the same time. Three groups of rabbits were used: control, fiber A and fiber B. The animals in all three groups received 1 mg/kg b. wt. EE. The estrogen was administered alone in the control group and in the presence of 4 g of fiber A and fiber B, respectively, in the other two groups. After compartmental (two-compartment open model) and noncompartmental analyses of plasma concentrations, statistical analysis revealed that the presence of fiber (both A and B) decreased between 29% and 35% the extent of EE absorbed (represented by the pharmacokinetic parameters area under the curve and the maximum plasma concentration) without affecting the rate of the absorption process (represented by the time to reach maximum concentration and the absorption rate constant).
纤维制剂因其对健康有益的特性而被用于人类营养。摄入纤维可能与口服药物同时发生,进而可能出现其口服吸收的改变,以及由此导致的药代动力学改变。在本研究中,测定了炔雌醇(EE)经口给药后在兔体内的房室和非房室药代动力学参数。还研究了胃肠道中两种不同的纤维制剂(A,麦麸(76.5%)、水果纤维(12%)和瓜尔胶(2%);B,卵叶车前种子(65%)和卵叶车前种子表皮(2.2%))同时存在时是否会改变EE的药代动力学。使用了三组兔子:对照组、纤维A组和纤维B组。所有三组动物均接受1mg/kg体重的EE。对照组单独给予雌激素,另外两组分别在存在4g纤维A和纤维B的情况下给予雌激素。在对血浆浓度进行房室(二室开放模型)和非房室分析后,统计分析表明,纤维(A和B)的存在使EE的吸收程度(由药代动力学参数曲线下面积和最大血浆浓度表示)降低了29%至35%,但不影响吸收过程的速率(由达峰时间和吸收速率常数表示)。