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目的:测定VBE-1的平衡溶解度和表观油水分配系数,并考察其酸碱稳定性,为药物的制剂设计提供实验依据。方法:采用平衡法和摇瓶法测定VBE-1在不同溶剂中的平衡溶解度以及在正辛醇-水/缓冲溶液中的表观油水分配系数,采用高效液相色谱法测定两者的浓度,并用紫外分光光度法考察VBE-1的酸碱稳定性。结果:VBE-1在PEG-400中的溶解度较大,为(677.47±48.09)g·L~(-1)。在pH4.0~8.0范围内,pH对VBE-1的表观油水分配系数有影响,表现出表观油水分配系数随着pH升高而降低的趋势。pH的升高会引起VBE-1颜色的改变,但此变化为可逆反应。结论:VBE-1具有一定的透过能力,可满足经皮给药的一般要求,其对pH较敏感,实验过程中应避免在强碱条件下操作。
OBJECTIVE: To determine the equilibrium solubility and apparent oil-water partition coefficient of VBE-1 and study its acid-base stability to provide experimental evidence for drug formulation design. Methods: The equilibrium solubility of VBE-1 in different solvents and the apparent oil-water partition coefficient in n-octanol-water / buffer solution were determined by equilibrium method and shake-flask method. The concentrations of VBE- The acid-base stability of VBE-1 was investigated by UV spectrophotometry. Results: The solubility of VBE-1 in PEG-400 was (677.47 ± 48.09) g · L -1. In the range of pH4.0 ~ 8.0, pH had an influence on the apparent oil-water partition coefficient of VBE-1, indicating that the apparent oil-water partition coefficient decreased with the increase of pH. Elevated pH causes changes in VBE-1 color, but this change is reversible. Conclusion: VBE-1 has a certain ability to transmit, which can meet the general requirements of transdermal drug delivery. It is sensitive to pH and should be avoided during operation under strong alkaline conditions.