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绝经后泰国女性摄入大豆饮料与大豆提取物胶囊后异黄酮、大豆苷元和染料木黄酮的药代动力学比较

Pharmacokinetics of isoflavones, daidzein and genistein, after ingestion of soy beverage compared with soy extract capsules in postmenopausal Thai women.

作者信息

Anupongsanugool Ekasin, Teekachunhatean Supanimit, Rojanasthien Noppamas, Pongsatha Saipin, Sangdee Chaichan

机构信息

Department of Pharmacology, Faculty of Medicine, Chiang Mai University, Thailand.

出版信息

BMC Clin Pharmacol. 2005 Mar 3;5:2. doi: 10.1186/1472-6904-5-2.

Abstract

BACKGROUND

Isoflavones from soybeans may provide some beneficial impacts on postmenopausal health. The purpose of this study was to compare the pharmacokinetics and bioavailability of plasma isoflavones (daidzein and genistein) after a single dose of orally administered soy beverage and soy extract capsules in postmenopausal Thai women.

METHODS

We conducted a randomized two-phase crossover pharmacokinetic study in 12 postmenopausal Thai women. In the first phase, each subject randomly received either 2 soy extract capsules (containing daidzin : genistin = 7.79 : 22.57 mg), or soy beverage prepared from 15 g of soy flour (containing daidzin : genistin = 9.27 : 10.51 mg). In the second phase, the subjects received an alternative preparation in the same manner after a washout period of at least 1 week. Blood samples were collected immediately before and at 0.5, 1, 2, 4, 6, 8, 10, 12, 24 and 32 h after administration of the soy preparation in each phase. Plasma daidzein and genistein concentrations were determined by using high performance liquid chromatography (HPLC). The pharmacokinetic parameters of daidzein and genistein, i.e. maximal plasma concentration (Cmax), time to maximal plasma concentration (Tmax), area under the plasma concentration-time curve (AUC) and half-life (t1/2), were estimated using the TopFit version 2.0 software with noncompartmental model analysis.

RESULTS

There were no significant differences in the mean values of Cmax/dose, AUC0-32/dose, AUC0- proportional, variant/dose, Tmax, and t1/2 of genistein between both preparations. For pharmacokinetic parameters of daidzein, the mean values of Cmax/dose, Tmax, and t1/2 did not significantly differ between both preparations. Nonetheless, the mean AUC0-32/dose and AUC0- proportional, variant/dose after administration of soy extract capsules were slightly (but significantly, p < 0.05) higher than those of soy beverage.

CONCLUSION

The bioavailability of daidzein, which was adjusted for the administered dose (AUC/dose), following a single oral administration of soy beverage was slightly (but significantly) less than that of soy extract capsules, whereas, the bioavailability adjusted for administered dose of genistein from both soy preparations were comparable. The other pharmacokinetic parameters of daidzein and genistein, including Cmax adjusted for the dose, Tmax and t1/2, were not different between both soy preparations.

摘要

背景

大豆中的异黄酮可能对绝经后健康产生一些有益影响。本研究的目的是比较绝经后泰国女性单次口服大豆饮料和大豆提取物胶囊后血浆异黄酮(大豆苷元和染料木黄酮)的药代动力学和生物利用度。

方法

我们对12名绝经后泰国女性进行了一项随机两阶段交叉药代动力学研究。在第一阶段,每位受试者随机接受2粒大豆提取物胶囊(含大豆苷:染料木苷 = 7.79 : 22.57毫克),或由15克大豆粉制备的大豆饮料(含大豆苷:染料木苷 = 9.27 : 10.51毫克)。在第二阶段,经过至少1周的洗脱期后,受试者以相同方式接受另一种制剂。在每个阶段给予大豆制剂前及给药后0.5、1、2、4、6、8、10、12、24和32小时立即采集血样。采用高效液相色谱法(HPLC)测定血浆大豆苷元和染料木黄酮浓度。使用TopFit 2.0软件通过非房室模型分析估算大豆苷元和染料木黄酮的药代动力学参数,即最大血浆浓度(Cmax)、达最大血浆浓度的时间(Tmax)、血浆浓度 - 时间曲线下面积(AUC)和半衰期(t1/2)。

结果

两种制剂之间染料木黄酮的Cmax/剂量、AUC0 - 32/剂量、AUC0 - 比例、变异/剂量、Tmax和t1/2的平均值无显著差异。对于大豆苷元的药代动力学参数,两种制剂之间的Cmax/剂量、Tmax和t1/2平均值无显著差异。然而,服用大豆提取物胶囊后的平均AUC0 - 32/剂量和AUC0 - 比例、变异/剂量略高于(但显著,p < 0.05)大豆饮料。

结论

单次口服大豆饮料后,经给药剂量校正的大豆苷元生物利用度(AUC/剂量)略低于(但显著)大豆提取物胶囊,而两种大豆制剂中经给药剂量校正的染料木黄酮生物利用度相当。大豆苷元和染料木黄酮的其他药代动力学参数,包括经剂量校正的Cmax、Tmax和t1/2,在两种大豆制剂之间无差异。

https://cdn.ncbi.nlm.nih.gov/pmc/blobs/ead1/555741/6a1338b60d77/1472-6904-5-2-1.jpg

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