Effect of pharmaceutical additives on physicochemical properties of pharmaceutical preparations.

药物添加剂对药物制剂理化性质的影响。

• 批准号: 08672491
• 负责人: MATSUDA Yoshihsa
• 金额: $ 1.41万
• 依托单位: Kobe Pharmaceutical University
• 依托单位国家: 日本
• 项目类别: Grant-in-Aid for Scientific Research (C)
• 财政年份: 1996
• 资助国家: 日本
• 起止时间: 1996 至 1997
• 项目状态: 已结题
• 来源: https://kaken.nii.ac.jp/grant/KAKENHI-PROJECT-08672491/
• 关键词: Polymorphism; additives; international harmonization; excipients; reaction rate; powder characteristics; pharmaceutical properties; kinetics

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.

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）考察了混合方式对复合异烟肼甲磺酸钠和吡哆醛磷酸钙显色的影响; 3）为了提高复合异烟肼甲磺酸钠和吡哆醛磷酸钙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。

项目成果

R.TERAOKA,Y.MATSUDA,et al.: "Improvement of the photostability of phytonadione (Vitamin K1) in model infusion fluids : Effect of addition of fat-soluble vitamine on the photodegradation of phytonadione" Jpn.J.Hosp.Pharm.22(5). 449-456 (1996)

R.TERAOKA,Y.MATSUDA,et al.：“模型输注液中植物萘二酮（维生素 K1）光稳定性的改善：添加脂溶性维生素对植物萘二酮光降解的影响”Jpn.J.Hosp.Pharm。

R.TERAOKA,M.OTSUKA,et al.: "Effect of mixing mode on the coloration of compound isoniazid sodium methanesulfonate and pyridoxal calcium phospate" Jpn.J.Hosp.Pharm.22(2). 198-205 (1996)

R.TERAOKA，M.OTSUKA，等：“混合方式对复方异烟肼甲磺酸钠与吡哆醛磷酸钙显色的影响”Jpn.J.Hosp.Pharm.22(2)。

M.Otsuka and Y.Matsuda: "Comparative Evaluation of Mean Particle Size of Bulk Drug Powder in Pharmaceutical Preparations by Fourier-Transformed Powder Diffuse Reflectance Infrared Spectroscopy and Dissolution Kinetics," J.Pharm.Sci.,. 85(1),. 112-116 (199

M.Otsuka 和 Y.Matsuda：“通过傅里叶变换粉末漫反射红外光谱和溶解动力学对药物制剂中原料药粉末的平均粒径进行比较评估”，J.Pharm.Sci.，。