熱熔擠出技術(shù)制備泊沙康唑固體分散體及其體外評價
發(fā)布時間:2018-03-10 01:22
本文選題:熱熔擠出 切入點(diǎn):固體分散體 出處:《中國藥科大學(xué)學(xué)報》2015年03期 論文類型:期刊論文
【摘要】:采用熱熔擠出(HME)技術(shù)制備難溶性藥物泊沙康唑(POS)固體分散體,提高其溶出度。利用溶解度參數(shù)、玻璃化轉(zhuǎn)變溫度和熔融法,初步篩選載體。進(jìn)一步運(yùn)用HME技術(shù)制備POS固體分散體,以溶出度為指標(biāo)考察載體Kollidon VA64、Soluplus、Eudragit L100以及混合載體Kollidon VA64-Eudragit L100對藥物的增溶能力?疾煊绊懝腆w分散體溶出度的處方以及工藝因素、不同載體、擠出溫度、增塑劑和載藥量對溶出度的影響。采用差示掃描量熱法(DSC)進(jìn)行物相分析,并通過影響因素實(shí)驗初步分析固體分散體的穩(wěn)定性。結(jié)果顯示以Kollindon VA64-Eudragit L100(2∶8)為載體,10%檸檬酸三乙酯為增塑劑,150℃擠出溫度下制備的POS固體分散體,顯著提高了POS的溶出度,DSC結(jié)果顯示藥物以無定形或分子形式存在于載體中;旌陷d體的比例、擠出溫度、載藥量以及增塑劑均能影響藥物的溶出。固體分散體對濕度敏感,高溫和強(qiáng)光條件下穩(wěn)定。采用HME技術(shù)制備的固體分散體可以顯著提高POS的溶出度。
[Abstract]:The insoluble drug posaconazole (POS) solid dispersion was prepared by hot melt extrusion (HME-HME) technique, and its dissolution was improved. The solubility parameters, glass transition temperature and melting method were used. HME technology was used to prepare POS solid dispersion. The solubilization ability of the carrier Kollidon VA64 Soluplusus Eudragit L100 and the mixed carrier Kollidon VA64-Eudragit L100 was investigated. The formulation and technological factors affecting the dissolution of solid dispersions, different carriers and extrusion temperature were investigated. Effect of plasticizer and drug loading on dissolution. Phase analysis was performed by differential scanning calorimetry (DSC). The stability of the solid dispersion was preliminarily analyzed by the experiment of influencing factors. The results showed that the solid dispersion of POS was prepared by extrusion at 150 鈩,
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