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水飞蓟宾葡甲胺片和甘草酸二铵肠溶胶囊治疗抗结核药物性肝损伤的疗效比较

Comparative bioavailability of curcuminoids from a water-dispersible high curcuminoid turmeric extract against a generic turmeric extract: a randomized, cross-over, comparative, pharmacokinetic study.

机构信息

Inventia Healthcare Ltd., Mumbai, Maharashtra, India.

Laila Nutraceuticals, Vijayawada, Andhra Pradesh, India.

出版信息

J Pharm Pharmacol. 2021 Apr 27;73(6):816-823. doi: 10.1093/jpp/rgab028.

Abstract

OBJECTIVES

The therapeutic utility of turmeric (Curcuma longa L., Zingiberaceae) is limited due to low bioavailability of its active principal curcuminoids. This study evaluates the pharmacokinetic characteristics of a natural, water-dispersible turmeric extract containing 60% curcuminoids (TurmXtra 60N), referred to as WDTE60N, compared to standard turmeric extract 95% (STE95).

METHODS

This open-label, two-way crossover, single oral dose, comparative pharmacokinetic study, randomized 14 subjects to receive one capsule of WDTE60N (150 mg curcuminoids) or three capsules of STE95 (500 mg curcuminoids each). The resulting dose ratio of actives for WDTE60N:STE95 was 1:10.

KEY FINDINGS

Peak plasma levels of free curcumin, total curcuminoids, tetrahydrocurcumin and demethoxycurcumin were similar (P > 0.05). Cmax of total curcumin was higher (P = 0.0253) for WDTE60N at a 10-fold lower dose compared to STE95 (43.5 ± 28.5 vs. 21.3 ± 10.7 ng/ml). Mean AUC0-t was higher (P < 0.001) for free curcumin and comparable for total curcumin and total curcuminoids with WDTE60N than with STE95. Five adverse events were reported in three subjects (mild in severity) and were unrelated to study products.

CONCLUSION

WDTE60N showed higher absorption and comparable exposure for free curcumin, total curcumin and total curcuminoids at a 10-fold lower dose than STE95.

摘要

目的

姜黄(姜科姜黄属植物)的治疗功效受到其活性主要姜黄素类物质生物利用度低的限制。本研究评估了一种天然、水分散性姜黄提取物(TurmXtra 60N)的药代动力学特征,该提取物含有 60%的姜黄素类物质,简称 WDTE60N,与标准姜黄提取物 95%(STE95)进行比较。

方法

这是一项开放标签、两周期、单次口服剂量、比较药代动力学研究,将 14 名受试者随机分为两组,分别服用 1 粒 WDTE60N(150mg 姜黄素类物质)或 3 粒 STE95(每粒 500mg 姜黄素类物质)。WDTE60N 的活性药物剂量比为 1:10。

主要发现

游离姜黄素、总姜黄素类物质、四氢姜黄素和脱甲氧基姜黄素的血浆峰浓度相似(P>0.05)。与 STE95 相比,WDTE60N 的总姜黄素 Cmax 更高(P=0.0253),尽管剂量低 10 倍(43.5±28.5 与 21.3±10.7ng/ml)。与 STE95 相比,WDTE60N 的游离姜黄素 AUC0-t 更高(P<0.001),总姜黄素和总姜黄素类物质的 AUC0-t 也更高。在 3 名受试者中报告了 5 起不良事件(轻度),与研究产品无关。

结论

与 STE95 相比,WDTE60N 以低 10 倍的剂量显示出更高的吸收和相似的游离姜黄素、总姜黄素和总姜黄素类物质的暴露量。

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