難溶性医薬品結晶の超微細化方法の開発に関する研究(第5報)フェニトイン, フェノバルビタールの微細化

抄録

In this study a new size reduction method was applied to slightly soluble medicinal compound having an acidic group in a molecule other than oxolinic acid. Phenytoin (PHT) and phenobarbital (PB) were chosen as medicinal compounds to be reduced, then effects of kinds or concentration of surfactants or polymers on size reduction were investigated. Changes of crystal form by powder X-ray diffraction measurements and dissolution rates of various microparticles were studied. The results obtained were as follows : i) PHT and PB crystallines were reduced so far as 3μm and 4μm (median diameter), respectively. ii) No change in crystal form of PTH microparticles was found, but there were changes in crystal form of PB microparticles in comparison with original crystallines. In the case of PB, original crystallines were anydride, but the microparticles were hydrate. iii) Dissolution rates of both microparticles of PHT and PB were increased remarkably.