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辅酶Q10微粒的制备、体外和体内表征:电喷雾法提高生物利用度

Preparation, in-vitro and in-vivo characterisation of CoQ10 microparticles: electrospraying-enhanced bioavailability.

作者信息

Fung Wai Yee, Liong Min Tze, Yuen Kah Hay

机构信息

School of Pharmaceutical Sciences, UniversitiSains Malaysia, Penang, Malaysia.

School of Industrial Technology, Universiti Sains Malaysia, Penang, Malaysia.

出版信息

J Pharm Pharmacol. 2016 Feb;68(2):159-69. doi: 10.1111/jphp.12502. Epub 2016 Jan 4.

Abstract

OBJECTIVES

This study aimed to prepare Coenzyme Q10 (CoQ10) microparticles using electrospraying technology, and evaluate the in-vitro properties and in-vivo oral bioavailability.

KEY FINDINGS

Electrospraying was successfully used to prepare CoQ10 to enhance its solubility and dissolution properties. In-vitro evaluation of the electrosprayed microparticles showed bioavailability-enhancing properties such as reduced crystallinity and particle size. The formulation was evaluated using dissolution study and in-vivo oral bioavailability using rat model. The dissolution study revealed enhanced dissolution properties of electrosprayed microparticles compared with physical mixture and raw material. The absorption profiles showed increasing mean plasma levels CoQ10 in the following order: raw material < physical mixture < electrosprayed microparticles.

CONCLUSION

Based on the findings in this study, electrospraying is a highly prospective technology to produce functional nano- and micro-structures as delivery vehicles for drugs with poor oral bioavailability due to rate-limiting solubility.

摘要

目的

本研究旨在利用电喷雾技术制备辅酶Q10(CoQ10)微粒,并评估其体外性质和体内口服生物利用度。

主要发现

成功利用电喷雾技术制备CoQ10,以提高其溶解度和溶解性质。对电喷雾微粒进行的体外评估显示出生物利用度增强的性质,如结晶度降低和粒径减小。使用溶出度研究对该制剂进行评估,并使用大鼠模型评估体内口服生物利用度。溶出度研究表明,与物理混合物和原料药相比,电喷雾微粒的溶解性质增强。吸收曲线显示CoQ10的平均血浆水平按以下顺序升高:原料药<物理混合物<电喷雾微粒。

结论

基于本研究的结果,电喷雾是一种极具前景的技术,可用于生产功能性纳米和微观结构,作为因溶解度限制而口服生物利用度差的药物的递送载体。

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