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首页> 外文期刊>RSC Advances >Pharmacokinetics of rosmarinic acid in rats by LC-MS/MS: absolute bioavailability and dose proportionality
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Pharmacokinetics of rosmarinic acid in rats by LC-MS/MS: absolute bioavailability and dose proportionality

机译：LC-MS / MS法测定迷迭香酸在大鼠中的药代动力学：绝对生物利用度和剂量比例

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Rosmarinic acid (RA), one of the main bioactive compounds of Rosmarinus officinalis L., exhibits diverse pharmacological effects. However, its oral absolute bioavailability and dose proportionality in vivo have not been comprehensively studied. In the present study, a validated LC-MS/MS method was developed for the determination of RA in rat plasma. Pharmacokinetic parameters were obtained following oral and intravenous dosing using DAS 3.0 software. Absolute bioavailability in rats was determined by comparing pharmacokinetic data after administration of single oral (12.5, 25 and 50 mg kg?1) and intravenous (0.625 mg kg?1) doses of RA. The dose proportionality of AUC and Cmax were analyzed using a power model. After single-dose oral administration of RA, Cmax values for groups with 12.5, 25 and 50 mg kg?1 doses ranged from 215.29 to 790.96 ng mL?1, with AUC0–t values from 41?789.84 to 96?070.00 min ng mL?1, while Tmax and t1/2 values ranged from 8.33 to 18.33 and from 332.34 to 295.32 min, respectively. The power model showed RA lacked dose proportionality over the dose range from 12.5–50 mg kg?1. Oral absolute bioavailability was calculated to range from 0.91% to 1.69%. All the results demonstrated that the pharmacokinetic properties of RA in rats after oral administration were characterized as rapid absorption, middle-speed elimination and poor absolute bioavailability. Systemic exposure exhibited lack of dose proportionality over the dose range from 12.5 to 50 mg kg?1. These presented data could provide useful information for the rational clinical application and optimal dosage form design of RA.
机译：迷迭香（Rosmarinus officinalis L.）的主要生物活性化合物之一迷迭香酸（RA）具有多种药理作用。然而，其口服绝对生物利用度和体内剂量比例尚未得到全面研究。在本研究中，开发了一种经过验证的LC-MS / MS方法来测定大鼠血浆中的RA。在使用DAS 3.0软件口服和静脉内给药后获得药代动力学参数。通过比较单次口服（12.5、25和50 mg kg ？1 ）和静脉内（0.625 mg kg <）后的药代动力学数据，确定大鼠的绝对生物利用度sup>？1 ）剂量的RA。使用功效模型分析了AUC和 C max 的剂量比例。单剂量口服RA后，12.5、25和50 mg kg 的组的 C max 值？ 1 剂量范围为215.29到790.96 ng mL ？1 ，AUC 0– t 值从41？789.84到96？070.00 min ng mL ？1 ，而 T max 和 t 1/2 值的范围为8.33至18.33和332.34至295.32分钟，分别。功效模型显示RA在12.5–50 mg kg ？1 的剂量范围内缺乏剂量比例性。口服绝对生物利用度的计算范围为0.91％至1.69％。所有结果表明，口服给药后RA在大鼠体内的药代动力学特征是吸收快，中速消除和绝对生物利用度差。在12.5至50 mg kg ？1 的剂量范围内，全身暴露均没有剂量比例性。这些提供的数据可以为RA的合理临床应用和最佳剂型设计提供有用的信息。

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