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用核磁共振定量测定茶儿茶素沉淀中利培酮的含量。

Quantification of Risperidone Contained in Precipitates Produced by Tea Catechins Using Nuclear Magnetic Resonance.

机构信息

Faculty of Pharmacy and Pharmaceutical Sciences, Fukuyama University.

出版信息

Chem Pharm Bull (Tokyo). 2023;71(2):134-139. doi: 10.1248/cpb.c22-00651.

Abstract

A mixture of risperidone and eight major tea catechins: (-)-epicatechin-3-O-gallate (ECg), (-)-epigallocatechin-3-O-gallate (EGCg), (-)-catechin-3-O-gallate (Cg), (-)-gallocatechin-3-O-gallate (GCg), (-)-epicatechin (EC), (-)-epigallocatechin (EGC), (+)-catechin (CA), or (+)-gallocatechin (GC), in tartaric acid buffer (pH 3.0) afforded a precipitate. Amounts of risperidone and these catechins in the precipitate were measured by quantitative H-NMR (qNMR). About half or more of risperidone used was precipitated by gallated catechins ECg, EGCg, Cg, and GCg; on the other hand, it was precipitated little by non-gallated catechins EC, EGC, CA, and GC. Furthermore, risperidone was precipitated more by 2,3-trans gallated catechins Cg and GCg than 2,3-cis gallated catechins ECg and EGCg. Regarding the amount of tea catechins in the precipitate obtained by a mixture of risperidone and Catechin Mixture, the amounts of 2,3-cis gallated catechins EGCg and ECg were much larger than those of the other green tea catechins GCg, EC, EGC, CA, and GC. It was considered that risperidone was mainly precipitated by EGCg and ECg in Catechin Mixture. Therefore, it can be concluded that when patients take risperidone with catechin-rich beverages, the efficacy of risperidone reduces, mainly because the 2,3-cis gallated catechins EGCg and ECg form complexes with risperidone and precipitate.

摘要

在酒石酸缓冲液(pH 3.0)中,利培酮与 8 种主要的茶儿茶素混合:(-)-表儿茶素-3-O-没食子酸酯(ECg)、(-)-表没食子儿茶素-3-O-没食子酸酯(EGCg)、(-)-儿茶素-3-O-没食子酸酯(Cg)、(-)-没食子儿茶素-3-O-没食子酸酯(GCg)、(-)-表儿茶素(EC)、(-)-表没食子儿茶素(EGC)、(+)-儿茶素(CA)或(+)-表没食子儿茶素(GC),会产生沉淀。沉淀中利培酮和儿茶素的含量通过定量核磁共振(qNMR)进行测量。使用的利培酮约有一半或更多被 ECg、EGCg、Cg 和 GCg 这些没食子酸儿茶素沉淀;另一方面,它很少被非没食子酸儿茶素 EC、EGC、CA 和 GC 沉淀。此外,利培酮与 2,3-反式没食子酸儿茶素 Cg 和 GCg 的沉淀比 2,3-顺式没食子酸儿茶素 ECg 和 EGCg 更多。关于利培酮与儿茶素混合物混合沉淀中茶儿茶素的含量,2,3-顺式没食子酸儿茶素 EGCg 和 ECg 的含量远大于其他绿茶儿茶素 GCg、EC、EGC、CA 和 GC。可以认为利培酮主要是由儿茶素混合物中的 EGCg 和 ECg 沉淀的。因此,可以得出结论,当患者服用富含儿茶素的饮料与利培酮时,利培酮的疗效会降低,主要是因为 2,3-顺式没食子酸儿茶素 EGCg 和 ECg 与利培酮形成复合物并沉淀。

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