Solubilities of 5-fluorouracil and ß-estradiol in supercritical carbon dioxide
Solubilities of 5-fluorouracil and ß-estradiol in supercritical carbon dioxide
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DOI：
10.1021/je000110l
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发表时间：
2000-11-01
期刊：
影响因子：
--
通讯作者：
Akgerman, A
中科院分区：
文献类型：
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作者：
Guney, O;Akgerman, A
控释药物产品在制药工业中越来越重要。通过超临界流体浸渍是生产这些产品的潜在技术。测量药物在超临界二氧化碳中的溶解度，因为它们控制可由移动的相携带的药物组分的量，并因此控制浸渍时间和程度。分别用于化学疗法和雌激素疗法的5-氟尿嘧啶和β-雌二醇的溶解度在100巴至220巴和308 K至328 K的压力下测量。这些药物具有10（-6）至10（-4）量级的质量分数溶解度，其足够高以使超临界浸渍方法成为使用有机溶剂的浸渍的可行替代方案。的溶解度作为溶剂密度的函数，并表明在较高的温度下的药物更高的溶解度。β-雌二醇的溶解度也报告在选定的条件下与乙醇作为共溶剂。
Controlled release drug products are gaining importance in the pharmaceutical industry. Impregnation via supercritical fluids is a potential technique for the production of these products. The solubilities of the drugs in supercritical carbon dioxide are being measured, since they control the amount of drug component that can be carried by the mobile phase and therefore the impregnation period and extent. The solubilities of 5-fluorouracil and beta -estradiol, used in chemotherapy and estrogen hormone therapy, respectively, are measured at pressures ranging from 100 bar to 220 bar and at 308 K to 328 K. These drugs have mass fraction solubilities of the order 10(-6) to 10(-4), which are high enough to make the supercritical impregnation process a feasible alternative to impregnation employing organic solvents. The solubilities are presented as a function of solvent density and indicate higher solubilities at higher temperatures for both of the drugs. Solubilities of beta -estradiol are also reported at select conditions with ethanol as a cosolvent.