Effect of pharmaceutical additives on physicochemical properties of pharmaceutical preparations.

为了协调药品法规，药物制剂的理化性质检测非常重要。辅料的理化性质通过影响溶出度、崩解时限、片剂硬度等影响制剂的生物利用度。因此，药物制剂的设计，特别是药物添加剂和几乎不溶于水的原料药粉末之间的相互作用影响制剂的生物利用度和储存期间的稳定性。然而，目前世界各国药典中尚无关于药物添加剂对制剂影响的评价方法。因此，我们研究了药物产品的理化性质与储存期间添加剂的影响之间的关系。1）溶剂对吡瑞他尼多晶型转化的影响，2）考察了混合方式对异烟肼甲磺酸钠和吡哆醛磷酸钙复合制剂呈色的影响; 3）为了提高复合制剂的光稳定性采用动力学方法考察了脂溶性维生素K1对植物甲萘醌光降解的影响。4）考察了压片过程中辅料对卡马西平多晶型转化的影响。

In order to harmonize the regulation of pharmaceutical products, the tests for physicochemical properties of pharmaceutical preparations are important. The physicochemical properties of expicients affect their bioavailability of the preparations through effects on the dissolution rate, disintegration time, tabelt hardness. Thus, the design of pharmaceutical preparations, specially the interaction between the pharmaceutical additives and bulk drug powders which are practically insoluble in water affects on the bioavailability of the preparations, and the stability during storage period. However, there is no evaluation method concerning the effect of pharamceutical additives on the preparations in Pharmacopoeia in countries throughout the world. Therefore, we investigate the relationship between the physicochemical properties of pharmaceutical products and the effect of additives during storage period.1)Effect of solvents on polymorphic transformation of piretanide, etc during granulation process were investigated.2)Effect of mixing mode on the coloration of compound isoniazid sodium methanesulfonate and pyridoxal calcium phospate was investigeted.3)In order to improvement of the photostability (Vitamin K1) in model infusion fluids, Effect of addition of fat-soluble vitamine on the photodegradation of phytonadione was investigated by kinetics methods.4)Effect of excipients on polymorphic transformation of carbamazepine during tabletting compression was investigated.