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利用伽马闪烁扫描法研究可蚀片体外和体内侵蚀行为的相关性。

Correlation between in vitro and in vivo erosion behaviour of erodible tablets using gamma scintigraphy.

机构信息

Strathclyde Institute of Pharmacy and Biomedical Sciences, University of Strathclyde, Glasgow, UK.

出版信息

Eur J Pharm Biopharm. 2011 Jan;77(1):148-57. doi: 10.1016/j.ejpb.2010.10.005. Epub 2010 Oct 29.

Abstract

In vitro and in vivo erosion behaviour of erodible tablets consisting of glyceryl behenate and low-substituted hydroxypropylcellulose manufactured using three different methods: direct compression (DC), melt granulation (MG) and direct solidification (DS) was investigated. In vitro erosion behaviour was studied using gravimetric and scintigraphic methods. For scintigraphic investigations, the radiolabel was adsorbed onto activated charcoal and incorporated into tablets at a concentration that did not affect the erosion profile. A clinical study was carried out in six healthy volunteers using gamma scintigraphy. Tablet erosion was affected by the preparation method and was found to decrease in the order of preparation method, DC>MG>DS tablets. The mean in vivo onset time for all tablets (DC: 6.7±3.8 min, MG: 18.3±8.1 min, DS: 67±18.9 min) did not differ significantly from in vitro onset time (DC: 5.3±1 min, MG: 16.8±3.9 min, DS: 61.8±4.7 min). The mean in vivo completion times were found to be 36.6±9.7 (DC tablets), 70±18.3 min (MG tablets) and 192.5±39.9 min (DS tablets). Among the three different erodible tablets, MG tablets showed the highest correlation between in vitro and in vivo mean erosion profile and suggested a potential platform to deliver controlled release of water-insoluble compounds.

摘要

采用直接压片(DC)、熔融制粒(MG)和直接固化(DS)三种不同方法制备的由山嵛酸甘油酯和低取代羟丙基纤维素组成的可蚀性片剂的体外和体内侵蚀行为进行了研究。采用重量法和闪烁照相法研究了体外侵蚀行为。对于闪烁照相研究,将放射性标记物吸附到活性炭上,并以不影响侵蚀曲线的浓度掺入片剂中。在 6 名健康志愿者中进行了一项临床研究,使用伽马闪烁照相术。片剂的侵蚀受到制备方法的影响,发现其顺序为 DC>MG>DS 片剂。所有片剂的体内起始时间(DC:6.7±3.8 min,MG:18.3±8.1 min,DS:67±18.9 min)与体外起始时间(DC:5.3±1 min,MG:16.8±3.9 min,DS:61.8±4.7 min)无显著差异。体内完成时间分别为 36.6±9.7(DC 片剂)、70±18.3 min(MG 片剂)和 192.5±39.9 min(DS 片剂)。在三种不同的可蚀性片剂中,MG 片剂在体外和体内平均侵蚀曲线之间表现出最高的相关性,这表明它有可能成为一种输送水不溶性化合物的控释平台。

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