Toskić-Radojcić Marija, Pavlović Marija, Gazikalović Emilija, Arandjelović Aleksandra, Kovacević Aleksandra
Sektor za farmaciju, Vojnomedicinska akademija, Beograd, Srbija.
Vojnosanit Pregl. 2012 Aug;69(8):675-80. doi: 10.2298/vsp101015006t.
BACKGROUND/AIM: Hydrophilic matrix tablets represent the most commonly used oral dosage form. Carbomers used in the concentration of 10%-30% for preparation of matrix tablets, may significantly affect the profile of drug release due to the formation of hydrogel matrix tablets. The aim of this study was to compare the influence of different types of Carbopol (carbomers in the pharmacopoeia) on the release rate of lithium-carbonate and other pharmaceutical, technological, physical and chemical properties of the prepared formulations of matrix tablets.
Three different formulations of matrix tablets were made according to direct compression method. The tablets were of the following composition: carbomer, lactose monohydrate, magnesium-stearate, lithium-carbonate in the proportion 75:120: 5 : 300. The first formulation was made with Carbopol 971P NF, the second one with Carbopol 974 P NF and the third one with Carbopol 71G NF. The quantity of lithium-carbonate was determined according to the BP 2009, pharmaceutical and tecnological properties were examined in accordance with the regulations of Ph. Jug. V, whereas the release rate of lithium-carbonate from the formulations was examined by the application of dissolution test, prescribed in the monography 'Lithium Carbonate Extended-Release Tablets' in USP 26.
The profile of lithium-carbonate release from matrix tablets with Carbopol 974P NF entirely complies with the regulations of USP 26, whereas the values obtained from the analysis of matrix tablets with Carbopol 971P NF and Carbopol 71G NF were considerably lower than the prescribed ones. In all the investigated formulations the content of the drug, mass variation and tablet hardness comply with the regulations set in pharmacopoeia.
In the formulation of matrix tablets with lithium-carbonate, by the application of carbomers in the concentration of 15%, with Carbopol 974 P NF a favourable lithium-carbonate release profile was achieved, whereas in the formulations with Carbopol 971P NF and Carbopol 71G NF, the release rate was significantly lower than that given in the USP 26 monography.
背景/目的：亲水性基质片剂是最常用的口服剂型。用于制备基质片剂的卡波姆浓度为10%-30%时，由于形成水凝胶基质片剂，可能会显著影响药物释放曲线。本研究的目的是比较不同类型的卡波普（药典中的卡波姆）对碳酸锂释放速率以及所制备的基质片剂制剂的其他药学、工艺、物理和化学性质的影响。
根据直接压片法制备了三种不同的基质片剂制剂。片剂的组成如下：卡波姆、一水乳糖、硬脂酸镁、碳酸锂，比例为75:120:5:300。第一种制剂用卡波普971P NF制备，第二种用卡波普974P NF制备，第三种用卡波普71G NF制备。碳酸锂的含量根据BP 2009测定，药学和工艺性质按照Ph. Jug. V的规定进行检查，而碳酸锂从制剂中的释放速率通过应用USP 26中“碳酸锂缓释片”专论规定的溶出度试验进行检查。
含卡波普974P NF的基质片剂中碳酸锂的释放曲线完全符合USP 26的规定，而从含卡波普971P NF和卡波普71G NF的基质片剂分析中获得的值明显低于规定值。在所有研究的制剂中，药物含量、质量差异和片剂硬度均符合药典规定。
在含碳酸锂的基质片剂制剂中，应用浓度为15%的卡波姆，使用卡波普974P NF可实现良好的碳酸锂释放曲线，而在含卡波普971P NF和卡波普71G NF的制剂中，释放速率明显低于USP 26专论中的规定。
