Yamamoto Keiji, Limwikrant Waree, Moribe Kunikazu
Graduate School of Pharmaceutical Sciences, Chiba University, Inohana, Chiba, Japan.
Chem Pharm Bull (Tokyo). 2011;59(2):147-54. doi: 10.1248/cpb.59.147.
The molecular states of active pharmaceutical ingredients (APIs) in pharmaceutical dosage forms strongly affect the properties and quality of a drug. Various important fundamental physicochemical studies were reviewed from the standpoint of molecular pharmaceutics. Mechanochemical effects were evaluated in mixtures of APIs and pharmaceutical additives. Amorphization, complex formation and nanoparticle formation are observed after grinding process depending on the combination of APIs and pharmaceutical additives. Sealed-heating method and mesoporous materials have been used to investigate drug molecular interactions in dosage forms. Molecular states have been investigated using powder X-ray diffraction, thermal analysis, IR, solid state fluorometry, and NMR.
药物剂型中活性药物成分（API）的分子状态强烈影响药物的性质和质量。从分子药剂学的角度对各种重要的基础物理化学研究进行了综述。在API与药用辅料的混合物中评估了机械化学效应。研磨后，根据API与药用辅料的组合情况，会观察到非晶化、复合物形成和纳米颗粒形成。密封加热法和介孔材料已被用于研究剂型中的药物分子相互作用。使用粉末X射线衍射、热分析、红外光谱、固态荧光法和核磁共振对分子状态进行了研究。
