Measurement and Correlation of Solubility of Clopidogrel Hydrogen Sulfate (Metastable Form) in Lower Alcohols
Measurement and Correlation of Solubility of Clopidogrel Hydrogen Sulfate (Metastable Form) in Lower Alcohols
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DOI：
10.1021/je200067e
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发表时间：
2011-03
影响因子：
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通讯作者：
Liangcheng Song;Yuan Gao;J. Gong
中科院分区：
文献类型：
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作者：
Liangcheng Song;Yuan Gao;J. Gong
硫酸氢氯吡格雷（晶型I）的溶解度平衡是在没有晶型II成核的情况下建立的，因为晶型II的成核速率在低过饱和度下非常慢。使用激光监测技术，在（273.15至318.15）K的温度范围内测量了硫酸氢氯吡格雷（I型）在乙醇、1-丙醇、1-丁醇、1-戊醇和2-丙醇中的溶解度。采用改进的Apelblat方程对实验数据进行关联，并采用van 't霍夫曲线法计算了晶型I的溶解焓和熵。与晶型II相比，晶型I具有更高的溶解度和更低的溶解焓。因此，我们可以得出结论，在本工作的条件下，晶型I是亚稳态的形式。
The solubility equilibrium of clopidogrel hydrogen sulfate (Form I) was set up without the nucleation of Form II, as the nucleation rate of Form II is very slow under the low supersaturation. Using the laser monitoring technique, solubilities of clopidogrel hydrogen sulfate (Form I) in ethanol, 1-propanol, 1-butanol, 1-pentanol, and 2-propanol were measured at temperatures ranging from (273.15 to 318.15) K. The experimental data were correlated by the modified Apelblat equation, and the dissolution enthalpy and entropy of Form I were determined with van't Hoff plots. Compared with those of Form II, Form I exhibits a higher solubility and a lower enthalpy of dissolution. Therefore, we can draw the conclusion that Form I was the metastable form under the conditions in this work.