Gallo F R, Pagliuca G, Multari G, Panzini G, D'amore E, Altieri I
Department of Therapeutic Research and Medicines Evaluation, Istituto Superiore di Sanità, Viale Regina Elena 299, 00161 Rome, Italy.
Service for Biotechnology and Animal Welfare, Istituto Superiore di Sanità, Viale Regina Elena 299, 00161 Rome, Italy.
Indian J Pharm Sci. 2015 Sep-Oct;77(5):530-5. doi: 10.4103/0250-474x.169031.
Natural substances present in herbal preparations should be carefully used because they can give toxic or therapeutic effects despite of their amount or the way of administration. The safety of products of vegetable origin must be assessed before commercialisation by monitoring the active ingredients and their metabolites. This study was therefore designed to identify and quantify arbutin and its metabolite hydroquinone, naturally present in Arctostaphylos uva-ursi (L.) Spreng plant in rat plasma, after an acute and subacute administration of aqueous arbutin solution in Wistar rats. For this purpose a reversed-phase high-performance liquid chromatography coupled with photodiode array detection was developed to assess the pharmacokinetic of arbutin and hydroquinone in plasma of female rats treated with aqueous arbutin solutions. The detection (arbutin: 0.0617 µg/ml and hydroquinone 0.0120 µg/ml) and quantification (arbutin: 0.2060 µg/ml and hydroquinone: 0.0400 µg/ml) limits were determined. At the arbutin concentration level of 10.7 µg/ml repeatability was 13.33% and its recovery 93.4±6.93%, while at the hydroquinone concentration level of 10.6 µg/ml repeatability was 11.66% and its recovery 92.9±7.75%. Furthermore the method was fully validated and the obtained data indicate that the new method provides good performances.
草药制剂中存在的天然物质应谨慎使用，因为无论其用量或给药方式如何，它们都可能产生毒性或治疗作用。植物源产品在商业化之前，必须通过监测活性成分及其代谢物来评估其安全性。因此，本研究旨在确定和定量熊果苷及其代谢物对苯二酚，它们天然存在于熊果叶（Arctostaphylos uva-ursi (L.) Spreng）植物中，在Wistar大鼠急性和亚急性给予熊果苷水溶液后，检测大鼠血浆中的含量。为此，开发了一种反相高效液相色谱结合光电二极管阵列检测法，以评估用熊果苷水溶液处理的雌性大鼠血浆中熊果苷和对苯二酚的药代动力学。确定了检测限（熊果苷：0.0617 µg/ml，对苯二酚：0.0120 µg/ml）和定量限（熊果苷：0.2060 µg/ml，对苯二酚：0.0400 µg/ml）。在熊果苷浓度为10.7 µg/ml时，重复性为13.33%，回收率为93.4±6.93%；而在对苯二酚浓度为10.6 µg/ml时，重复性为11.66%，回收率为92.9±7.75%。此外，该方法经过了充分验证，获得的数据表明该新方法具有良好的性能。
