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Thiago Caon,Ricardo Augusto Konig,Ariadne Cristiane Cabral da Cruz,Simone Gonc¸alves Cardoso,Carlos Eduardo Maduro Campos,Silvia Lucia Cuffini,Letı´cia Scherer Koester,Cla´udia Maria Oliveira Simo˜es 대한약학회 2013 Archives of Pharmacal Research Vol.36 No.9
Solid dispersions of saquinavir mesylate containingeither Gelucire 44/14 or poly(ethylene glycol)(PEG) 4000, or mixtures of each carrier with Tween 80 orpolyvinyl pyrrolidone (PVP) K30 were prepared in order toenhance the drug dissolution rate. These systems wereprepared by the melting method and characterized by X-raypowder diffraction, microscopical techniques, and Ramanspectroscopy aiming to establish a relationship betweenphysicochemical and dissolution properties under differentcooling conditions. Modifications in degree of crystallineorder/disorder over time were observed in preparationswith both carriers. Overall, formulations cooled and stored at -20 C showed less variation in dissolution rates thanthose at 25 C. Although Tween 80 has enhanced theknown self-emulsifying properties of Gelucire 44/14, itscombination with PEG 4000 displayed miscibility problems. The addition of PVP K30 was not the most effectiveapproach in enhancing the dissolution in early steps;however, the drug dissolution was stable after 7 days ofstorage at 25 C. The combination of PEG 4000 and PVPK30 maintained the dissolution properties for 60 and90 days at 25 C/95 % relative humidity and 40 C/75 %(f2 values[50), respectively.