Gossai D, Lau-Cam C A
Department of Pharmaceutical Sciences, St. John's University, College of Pharmacy and Allied Health Professions, Jamaica, New York 11439, USA.
Pharmazie. 2009 Mar;64(3):202-9.
This study has examined the effects of type of dairy product (whole milk, skim milk, heavy cream) and chocolate matrix (baking, dark, dairy milk, white) on the oral absorption of the chocolate flavanols (+)-catechin and (-)-epicatechin in a small animal model. In the study, each flavanol compound, as a solution in water or a dairy product or as a chocolate dispersion in water, was administered intragastrically to male Sprague-Dawley rats in an amount equal to or equivalent to 350 mg/kg. In each instance, blood samples were collected over a 5 h period, and used to measure plasma total catechin concentrations by HPLC after enzymatic hydrolysis of flavanol conjugates. Pharmacokinetic data were evaluated using a one compartment approach. Whole milk and heavy cream, and to a much lesser extent skim milk, lowered the oral absorption of both (+)-catechin and (-)-epicatechin and altered the AUC, C(max), k(a), k(e) and t1/2 values in direct proportion to their fat, but not to their protein, content. In addition, the t(max) for solutions of (-)-epicatechin in water and skim milk occurred 2 h earlier than from solutions in whole milk and heavy cream. Similarly, dispersions of baking chocolate in water and in whole milk yielded plasma levels of monomeric catechins that were, respectively, about equal to and much lower than those from aqueous solutions of authentic flavanols. A determining role for a chocolate matrix (dark, dairy milk or white chocolate) on the oral absorption of its constitutive monomeric flavanols was suggested by the apparent variability in plasma total catechins levels that existed among them both before and after their spiking with equal amounts of exogenous (+)-catechin and (-)-epicatechin. Such a variability could reflect differences among different chocolates in terms of their physical properties, matrix components, and matrix characteristics imposed by the manufacturing process used for each type of chocolate. In all the experiments, (+)-catechin demonstrated a higher oral absorption than (-)-epicatechin.
本研究在小动物模型中考察了乳制品类型(全脂牛奶、脱脂牛奶、浓奶油)和巧克力基质(烘焙巧克力、黑巧克力、牛奶巧克力、白巧克力)对巧克力黄烷醇(+)-儿茶素和(-)-表儿茶素口服吸收的影响。在该研究中,每种黄烷醇化合物以水溶液、乳制品溶液或巧克力水分散液的形式,以等于或相当于350 mg/kg的量灌胃给予雄性斯普拉格-道利大鼠。在每种情况下,在5小时内采集血样,并在黄烷醇结合物酶解后通过HPLC测定血浆总儿茶素浓度。使用一室模型方法评估药代动力学数据。全脂牛奶和浓奶油,以及程度小得多的脱脂牛奶,降低了(+)-儿茶素和(-)-表儿茶素的口服吸收,并改变了AUC、C(max)、k(a)、k(e)和t1/2值,其与脂肪含量成正比,而非与蛋白质含量成正比。此外,(-)-表儿茶素水溶液和脱脂牛奶溶液的t(max)比全脂牛奶和浓奶油溶液早2小时出现。同样,烘焙巧克力在水和全脂牛奶中的分散液产生的单体儿茶素血浆水平分别约等于和远低于真实黄烷醇水溶液的水平。在添加等量外源性(+)-儿茶素和(-)-表儿茶素前后,它们之间血浆总儿茶素水平存在明显差异,这表明巧克力基质(黑巧克力、牛奶巧克力或白巧克力)对其组成单体黄烷醇的口服吸收具有决定性作用。这种差异可能反映了不同巧克力在物理性质、基质成分以及每种巧克力制造工艺所赋予的基质特性方面的差异。在所有实验中,(+)-儿茶素的口服吸收均高于(-)-表儿茶素。