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一种商业藏红花(L.)提取物的生物可及性和药代动力学

Bioaccessibility and Pharmacokinetics of a Commercial Saffron ( L.) Extract.

作者信息

Almodóvar Paula, Briskey David, Rao Amanda, Prodanov Marín, Inarejos-García Antonio M

机构信息

Research and Development Department, Pharmactive Biotech Products S. L. Parque Científico de Madrid, Madrid, Spain.

School of Human Movement and Nutrition Sciences, The University of Queensland, St Lucia, QLD, Australia.

出版信息

Evid Based Complement Alternat Med. 2020 Jan 30;2020:1575730. doi: 10.1155/2020/1575730. eCollection 2020.

Abstract

There are few studies about the pharmacokinetics of the low-molecular mass carotenoids crocetin or crocin isomers from saffron ( L.). None has been performed with a galenic preparation of a standardised saffron extract. The aim of the present research work was to study the effect of digestion process on the main bioactive components of saffron extract tablets and the corresponding pharmacokinetic parameters in humans. Pharmacokinetics were calculated collecting blood samples every 30 min during the first 3 h and at 24 h after administration of two different concentrations (56 and 84 mg of the saffron extract) to 13 healthy human volunteers. Additionally, an digestion process was performed in order to determine the bioaccessibility of saffron main bioactive compounds. Identification and quantification analysis were performed by HPLC-PAD/MS. Digestion resulted in 40% of bioaccesibility for crocin isomers, whereas, safranal content followed an opposite trend increasing about 2 folds its initial concentration after the digestion process. Crocetin in plasma was detected in a maximum concentration ( ) in blood between 60 and 90 min after oral consumption with dose-dependent response kinetics, showing that crocin isomers from galenic preparation of saffron extract are rapidly transformed into crocetin. The results showed that this tested galenic form is an efficient way to administer a saffron extract, since the observed crocetin was similar and more quickly bioavailable than those obtained by other studies with much higher concentrations of crocetin.

摘要

关于藏红花(L.)中低分子量类胡萝卜素藏红花酸或藏红花苷异构体的药代动力学研究较少。尚未对标准化藏红花提取物的盖仑制剂进行过相关研究。本研究工作的目的是研究消化过程对藏红花提取物片剂主要生物活性成分的影响以及在人体中的相应药代动力学参数。对13名健康人类志愿者给予两种不同浓度(56和84毫克藏红花提取物)后,在前3小时内每30分钟采集一次血样,并在给药后24小时采集血样,计算药代动力学。此外,进行了消化过程以确定藏红花主要生物活性化合物的生物可及性。通过HPLC-PAD/MS进行鉴定和定量分析。消化导致藏红花苷异构体的生物可及性为40%,而藏花醛含量则呈现相反的趋势,消化后其初始浓度增加了约2倍。口服后,血浆中藏红花酸在60至90分钟之间的血液中达到最大浓度(),呈现剂量依赖性反应动力学,表明藏红花提取物盖仑制剂中的藏红花苷异构体迅速转化为藏红花酸。结果表明,这种测试的盖仑制剂形式是给药藏红花提取物的有效方式,因为观察到的藏红花酸与其他研究中使用高得多浓度的藏红花酸所获得的结果相似且生物利用度更高。

https://cdn.ncbi.nlm.nih.gov/pmc/blobs/3391/7013346/5dfb299d8b25/ECAM2020-1575730.001.jpg

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