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通过等离子体处理改善非诺贝特片剂的润湿性和溶出度。

Improvement of the wettability and dissolution of fenofibrate compacts by plasma treatment.

机构信息

Institute for Pharmacy and Biochemistry, Johannes Gutenberg University, Staudinger Weg 5, Mainz, Germany.

出版信息

Int J Pharm. 2011 Sep 15;416(1):49-54. doi: 10.1016/j.ijpharm.2011.05.074. Epub 2011 Jun 12.

Abstract

The goal of this study was to investigate the effect of plasma treatment on the wettability and dissolution of fenofibrate compacts. Contact angle measurements and intrinsic dissolution rate studies of untreated and plasma-treated fenofibrate compacts were conducted. The contact angle data clearly show that the wettability of the tablet surface increased with the duration of plasma treatment. Analyses of stability revealed that the surfaces which were plasma-treated for more than 1min regained some degree of hydrophobicity after storage in air. Since their hydrophobic recovery finally reached the level observed with 1min plasma-treated fenofibrate compacts it was deduced that permanent incorporation of hydrophilic groups had already attained saturation upon plasma irradiation for 1min. Dissolution studies revealed the advantages of the hydrophilized surface of plasma-treated fenofibrate compacts. Due to the improved wettability of plasma-treated fenofibrate its intrinsic dissolution rate was vastly increased compared to untreated fenofibrate. This study thus demonstrates the potential of plasma treatment to enhance the wettability and dissolution behavior of poorly water-soluble drugs.

摘要

本研究旨在探讨等离子体处理对非诺贝特压片的润湿性和溶解性能的影响。测量了未经处理和等离子体处理的非诺贝特压片的接触角,并对其进行了内在溶解速率研究。接触角数据清楚地表明,随着等离子体处理时间的延长,片剂表面的润湿性增加。稳定性分析表明,经过 1 分钟以上等离子体处理的表面在空气中储存后会恢复一定程度的疏水性。由于它们的疏水性恢复最终达到了与经过 1 分钟等离子体处理的非诺贝特压片相同的水平,可以推断出在 1 分钟的等离子体辐照下,亲水性基团的永久掺入已经达到饱和。溶解研究揭示了等离子体处理的非诺贝特润湿性提高的优势。由于等离子体处理的非诺贝特的润湿性得到改善,其内在溶解速率与未经处理的非诺贝特相比大大提高。因此,本研究证明了等离子体处理可以提高疏水性药物的润湿性和溶解行为。

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