Mura P, Faucci M T, Manderioli A, Furlanetto S, Pinzauti S
Dip. Scienze Farmaceutiche, Università di Firenze, Italy.
Drug Dev Ind Pharm. 1998 Aug;24(8):747-56. doi: 10.3109/03639049809082722.
The potential compatibilities of several commonly used pharmaceutical excipients with picotamide were evaluated using differential scanning calorimetry (DSC). The effects of aging and of mechanical treatment (blending, grinding, or kneading) of samples were also evaluated. Hot-stage microscopy (HSM) and scanning electron microscopy (SEM) were used as complementary techniques to implement and assist in interpretation of the DSC results. DSC analysis evidenced a noticeable modification of drug thermal features in the mixtures with palmitic acid, stearic acid, stearyl alcohol, polyethylene glycol (PEG) 20,000, and sorbitol, but HSM analysis showed that the DSC behavior was mainly because of the drug dissolution in the melted excipient, which allowed the presence of important solid-solid interactions to be excluded. Compatibility with Mg stearate was also found, even if sample manipulation induced the partial conversion of Mg stearate in a pseudo-polymorphic modification. Mechanical stress displayed an increased hygroscopicity of mixtures with glucose and lactose, as well as some solid-solid interactions with lactose and mannitol.
使用差示扫描量热法(DSC)评估了几种常用药用辅料与匹可他胺的潜在相容性。还评估了样品老化以及机械处理(混合、研磨或捏合)的影响。热台显微镜(HSM)和扫描电子显微镜(SEM)用作补充技术,以实施并协助解释DSC结果。DSC分析表明,在与棕榈酸、硬脂酸、硬脂醇、聚乙二醇(PEG)20000和山梨醇的混合物中,药物的热特性有明显改变,但HSM分析表明,DSC行为主要是由于药物溶解在熔融的辅料中,这排除了重要的固-固相互作用的存在。还发现了与硬脂酸镁的相容性,即使样品处理导致硬脂酸镁部分转化为假多晶型物。机械应力使与葡萄糖和乳糖的混合物吸湿性增加,以及与乳糖和甘露醇有一些固-固相互作用。