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作 者:马星[1] 戎善康[2] 吴秋前[1] 周国信[2]
机构地区:[1]兰州医学院药学系,兰州730000 [2]化工部涂料研究所,兰州730000
出 处:《药学学报》1992年第2期144-149,共6页Acta Pharmaceutica Sinica
摘 要:用X线衍射(XRD)对甲苯磺了脲(D860)与脲、聚乙烯吡咯烷酮(PVP)和聚乙烯二醇6000(PEG 6000)的固体分散物进行较详细的研究,并与它们的溶出速率进行关联。D860—PVP分散物为无定形态,溶出速率大。用熔融法制备的固体分散物中,D860在D860—脲,D860—PEG中为部分互溶,部分呈微晶析出,为过饱和状态,活性强,溶出速率快。而用溶剂法制备的D860—PEG近似物理混合状态,大部分以微晶形态分散,溶出速率较慢。陈化试验表明D860分散物在贮存期间无晶体结构变异,溶出速率的下降估计是由于药剂活性改变所致。D860 (tolbutamide)solid dispersions prepared with urea, polyvinylpyrrolidone (PVP), and polyethylene glycal (PEG) 6000 as carriers were studied byX- ray diffraction, relating to their dissolution rates. D860 in D860- PVP dispersion wasshown to be in an amorphous state and to have greater dissolution rate. D860- urea andD860-PEG melts were found to be partly in miscible solid solution state and partlyin microcrystal state and possess higher activity and greater dissolution rate. D860- PEGcoprecipitate was a physical mixture and its dissolution rate is slower than its melt. No va-riation in the crystal structure of the D860 dispersions was observed during the ageingtest.
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