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首页> 外文期刊>International Journal of Nanomedicine >Metabolic profile of puerarin in rats after intragastric administration of puerarin solid lipid nanoparticles
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Metabolic profile of puerarin in rats after intragastric administration of puerarin solid lipid nanoparticles

机译:葛根素固体脂质纳米粒胃内给药后大鼠体内葛根素的代谢特征

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Abstract: Puerarin has multiple pharmacological effects and is widely prescribed for patients with cardiovascular diseases including hypertension, cerebral ischemia, myocardial ischemia, diabetes mellitus, and arteriosclerosis. We have successfully prepared puerarin-loaded solid lipid nanoparticles (Pue-SLNs) for oral administration. Pue-SLNs are prepared using monostearin, soya lecithin, and poloxamer 188. SLNs may alter the course of puerarin absorption predominantly to and through lymphatic routes and regions, presumably following a transcellular path of lipid absorption, especially by enterocytes and polar epithelial cells of the intestine. The alteration of absorption might influence the metabolic profile of puerarin when incorporated into SLNs. In the present study, we investigated the metabolic profile of puerarin in rat plasma and urine using rapid resolution liquid chromatography–tandem mass spectrometry after a single-dose intragastric administration of Pue-SLNs in comparison with puerarin suspension. Two glucuronidated metabolites of puerarin, puerarin-4?-O-glucuronide and puerarin-7-O-glucuronide, were detected in rat plasma and urine after intragastric administration of Pue-SLNs, with the latter acting as the major metabolite. Similar results were found in rat plasma and urine after intragastric administration of puerarin suspension. The results suggest that incorporation of puerarin into SLNs does not change either the position of glucuronidation or the metabolic pathway of puerarin in rats.
机译:摘要:葛根素具有多种药理作用,被广泛用于高血压,脑缺血,心肌缺血,糖尿病和动脉硬化等心血管疾病患者。我们已经成功地制备了口服葛根素负载的固体脂质纳米颗粒(Pue-SLNs)。使用单硬脂精,大豆卵磷脂和泊洛沙姆188制备Pue-SLN。SLN可能主要通过淋巴途径和区域,尤其是通过肠上皮细胞的肠上皮细胞和极性上皮细胞,通过脂质的跨细胞途径改变葛根素的吸收过程。肠。当掺入SLNs中时,吸收的变化可能会影响葛根素的代谢特性。在本研究中,我们与葛根素混悬液相比,在单剂量胃内施用Pue-SLNs后,使用快速分离液相色谱-串联质谱法研究了葛根素在大鼠血浆和尿液中的代谢谱。胃内施用Pue-SLNs后,在大鼠血浆和尿液中检测到两种葛根素的葡糖醛酸化代谢物,葛根素4α-O-葡糖醛酸和葛根素7-O-葡糖醛酸,其中后者为主要代谢产物。胃内注射葛根素混悬液后,在大鼠血浆和尿液中发现了相似的结果。结果表明,葛根素掺入SLNs不会改变大鼠体内葡萄糖醛酸化的位置或葛根素的代谢途径。

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