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美托洛尔酒石酸盐贴片的游离体积与释放度的相关性。

Correlation between the free volume and the metoprolol tartrate release of Metolose patches.

机构信息

Semmelweis University, School of PhD Studies, Budapest, Hungary.

出版信息

J Pharm Biomed Anal. 2010 Jan 5;51(1):244-7. doi: 10.1016/j.jpba.2009.07.011. Epub 2009 Jul 15.

Abstract

The correlation between the release characteristics of metoprolol tartrate and the free volumes of Metolose patches containing Metolose 90SH 100.000SR (hypromellose) and Metolose SM 4000 (methylcellulose) of various proportions was studied. Positron annihilation lifetime spectroscopy (PALS) measurements were performed in parallel with the metoprolol tartrate release study to track the free volume changes of patches. Second-order polynomial relationship was found, with good correlation, between the metoprolol tartrate released at the 6th hour, the o-positronium lifetime, indicating the free volume of the polymer, and the Metolose SM 4000 relative proportions. The main reason for this correlation is the change in the free volume size of the polymer patches embedding metoprolol tartrate as a function of the relative proportion of Metolose 90SH 100.000SR containing hydroxypropoxy substitution. Since there were no significant changes between the free volumes of Metolose polymers at any ratio of the constituents in the case of lack of metoprolol tartrate, the free volume changes refer to a possible intermolecular interaction between the polymer and the active agent.

摘要

研究了酒石酸美托洛尔释放特性与含有不同比例 Metolose 90SH 100.000SR(羟丙甲纤维素)和 Metolose SM 4000(甲基纤维素)的 Metolose 贴片的自由体积之间的相关性。在进行酒石酸美托洛尔释放研究的同时,还进行了正电子湮没寿命谱(PALS)测量,以跟踪贴片的自由体积变化。发现酒石酸美托洛尔在第 6 小时释放量、o-正电子素寿命(表示聚合物的自由体积)和 Metolose SM 4000 的相对比例之间存在二次多项式关系,相关性良好。这种相关性的主要原因是,作为含有羟丙氧基取代的 Metolose 90SH 100.000SR 相对比例函数的嵌入酒石酸美托洛尔的聚合物贴片的自由体积大小发生了变化。由于在缺乏酒石酸美托洛尔的情况下,任何成分比例的 Metolose 聚合物的自由体积都没有明显变化,因此自由体积的变化是指聚合物与活性剂之间可能存在的分子间相互作用。

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