本文選題：格列美脲 + 過飽和溶液�。� 參考：《沈陽藥科大學(xué)學(xué)報》2017年06期

【摘要】：目的快速地篩選格列美脲的結(jié)晶抑制劑,比較不同結(jié)晶抑制劑對其制備的格列美脲固體分散體的影響。方法通過溶劑改變法制備格列美脲的過飽和溶液,篩選出藥物具有明顯沉降趨勢的過飽和度。進一步考察Soluplus、VA64、HPMC-E5、PVP K30、F68、PEG6000和PEG4000等聚合物抑制格列美脲的過飽和溶液的沉降能力,選擇有抑晶作用的聚合物制備格列美脲固體分散體�？疾烊艹鲚^好的固體分散體在非漏槽條件,pH4.5的PBS溶液中維持藥物過飽和溶液的能力,并用偏光顯微鏡法、差示掃描量熱法、X-射線衍射法和紅外光譜法考察藥物在載體中的存在狀態(tài)。結(jié)果格列美脲過飽和溶液在過飽和度約為68.20時,沉降趨勢明顯。聚合物對格列美脲的抑晶作用強弱為:SoluplusHPMC-E5PVP K30≥VA64F68PEG4000≥PEG6000,選取Soluplus、VA64、HPMC-E5和PVP K30為載體。采取溶劑法制備格列美脲固體分散體,不同載體制備的固體分散體都可在藥物與聚合物的質(zhì)量比為1∶4或1∶7時,在pH7.8PBS溶液中達到最大累計溶出量,且4h不沉降。固體分散體在非漏槽條件pH4.5的PBS溶液中維持藥物過飽和溶液的能力同結(jié)晶抑制劑篩選的結(jié)果一致,而且只有VA64制備的固體分散體的抑晶作用和載體量成正相關(guān)。根據(jù)偏振光顯微鏡法、差示掃描量熱、X-射線衍射和紅外光譜考察結(jié)果,格列美脲在對其具有抑晶作用的載體制備的固體分散體中以無定型或分子形式存在。結(jié)論格列美脲結(jié)晶抑制劑能夠在4h內(nèi)維持其固體分散體溶液相對穩(wěn)定的過飽和狀態(tài)。藥物在有抑晶作用的載體中以無定型或分子形式存在。
[Abstract]:Aim to screen the crystal inhibitors of glimepiride and compare the effects of different crystal inhibitors on the solid dispersion of glimepiride prepared by glimepiride. Methods the supersaturated solution of glimepiride was prepared by solvent change method. The inhibition ability of Soluplusus VA64 (HPMC-E5) PVP K30F68PEG6000 and PEG4000 on the sedimentation of supersaturated solution of glimepiride was investigated. The solid dispersion of glimepiride was prepared by using the suppressive polymer. The ability of dissolving solid dispersions to maintain supersaturated drug solution in PBS solution with pH 4.5 was investigated by polarizing microscope. Differential scanning calorimetry (DSC) and X-ray diffraction (XRD) and infrared spectroscopy (IR) were used to investigate the existence of drugs in the carrier. Results when supersaturated solution of glimepiride was about 68.20, the settlement trend was obvious. The inhibitory effect of polymer on glimepiride was as follows: Soluplus HPMC-E5PVP K30 鈮，

本文編號：1989246