[關(guān)鍵詞]
[摘要]
在新藥研發(fā)早期階段,將候選化合物成鹽是一種重要手段,可改善候選化合物的理化性質(zhì),如溶解度、結(jié)晶度、吸濕性、熔點(diǎn)和固態(tài)穩(wěn)定性等。藥物鹽型的篩選首先從反離子的選擇開始,然后篩選結(jié)晶條件制備其相應(yīng)的鹽型,最后根據(jù)結(jié)晶度、熔點(diǎn)、吸濕性、物理化學(xué)穩(wěn)定性和晶型等因素確定藥物的最終鹽型。藥物鹽型的篩選對(duì)選擇具有適宜藥學(xué)性質(zhì)的固態(tài)劑型有重要的指導(dǎo)作用。
[Key word]
[Abstract]
During the early stage of new drug research and development, to make the candidate compounds be salt is an important method for developing new drug, which could modify the physicochemical properties, such as solubility, crystallinity, hygroscopicity, melting point, and solid state stability. Salt type screening starts with the selection of possible counter ions, followed by the screening of crystallization conditions and the preparation of different salts. The final salt is determined by the crystallinity, melting point, hygroscopicity, physicochemical stability, crystal type, and some other factors. The salt type selection of new drugs could provide the guides for the selection of proper solid dosage forms with appropriate pharmaceutical properties.
[中圖分類號(hào)]
[基金項(xiàng)目]
國家重點(diǎn)基礎(chǔ)研究發(fā)展計(jì)劃(973計(jì)劃)課題(2012CB724000,2012CB724002);國家生物醫(yī)藥國際創(chuàng)新園(天津)創(chuàng)新藥物孵化基地建設(shè)(2010ZX09401)