Kasperek Regina, Zimmer Łukasz, Szalast-Pietrzak Agnieszka, Marzec Zbigniew, Poleszak Ewa
Katedra i Zakład Farmacji Stosowanej, Wydział Farmaceutyczny, Uniwersytet Medyczny w Lublinie, Lublin, Polska.
Katedra i Zakład Żywności i Żywienia, Wydział Farmaceutyczny, Uniwersytet Medyczny w Lublinie, Lublin, Polska.
Polim Med. 2014 Oct-Dec;44(4):247-53.
In the pharmaceutical technology there is a trend to produce tablets composed of several medicinal substances to increase therapeutic effect and reduce the frequency of drug administration. In the literature there are reports concerning pharmacological studies in which a potentiation of the effects has been observed after a co-administration of antidepressant imipramine and magnesium. Currently, there is no formulation on the market comprising imipramine and magnesium, therefore, it was decided to produce uncoated tablets. In order to prepare the tablets by direct compression, it was necessary to select suitable excipients.
The aim of the study was to elaborate the composition and to prepare the tablets with imipramine and magnesium, as well as to assess the quality of the tablets by physical characteristics and by the release study of the active substances.
In order to prepare the tablets, compositions of different polymers and other excipients were added. The tablets were produced by direct compression method in a tablet press. Physical properties of the obtained tablets and the release of the active substances into an acidic medium in a paddle apparatus were tested. The contents of imipramine and magnesium were determined by different methods: spectrophotometrically and atomic absorption spectrometry, respectively.
The composition of excipients necessary to produce tablets comprising imipramine and magnesium was established. All of prepared tablets were in compliance with the pharmacopoeial requirements. The release tests showed that above 80% of imipramine was released within 20-35 min and 80-76% of magnesium up to 45 min from the composed tablets and one-ingredient tablets, respectively.
The compositions of excipients for tablets consisting of imipramine and magnesium were presented. The active substances were released within 45 min in the acidic medium, and the administration of these substances in the composed tablets did not affect pharmaceutical availability.
在制药技术领域，有一种生产由多种药用物质组成的片剂的趋势，以提高治疗效果并减少给药频率。文献中有关于药理学研究的报道，其中观察到抗抑郁药丙咪嗪和镁联合给药后效果增强。目前市场上没有包含丙咪嗪和镁的制剂，因此决定生产未包衣片剂。为了通过直接压片制备片剂，有必要选择合适的辅料。
本研究的目的是确定含丙咪嗪和镁的片剂的组成并进行制备，以及通过物理特性和活性物质释放研究来评估片剂质量。
为了制备片剂，添加了不同聚合物和其他辅料的组合物。片剂通过直接压片法在压片机中生产。测试了所得片剂的物理性质以及活性物质在桨法装置中在酸性介质中的释放情况。分别采用分光光度法和原子吸收光谱法测定丙咪嗪和镁的含量。
确定了生产含丙咪嗪和镁的片剂所需的辅料组成。所有制备的片剂均符合药典要求。释放试验表明，从复方片剂和单一组分片剂中，分别在20 - 35分钟内释放出80%以上的丙咪嗪，在45分钟内释放出80 - 76%的镁。
给出了由丙咪嗪和镁组成的片剂的辅料组成。活性物质在酸性介质中45分钟内释放，并且在复方片剂中给药这些物质不影响药物的可利用性。
