CAJ | 학술논문

目的：测定西他沙星在不同溶剂中的溶解度以及表观油水分配系数,为剂型研究和制备工艺提供依据。方法采用高效液相色谱(HPLC)法,Dikma Diamonsil C18(2)色谱柱(4.6 mm×250 mm,5μm)；流动相：0.05 mol·L-1磷酸二氢钾溶液(用磷酸调节 pH 至2.4)乙腈=7030；柱温：室温；流速1.0 mL·min-1；检测波长：295 nm；进样量10μL。考察西他沙星在 pH 为2.0,4.3,5.8,6.6,7.4,8.0,10.0,11.2磷酸盐缓冲液中溶解度和表观油水分配系数。结果在(37±2)℃条件下,西他沙星在水中的平衡溶解度为0.44 mg·mL-1,表观油水分配系数( P)为0.23( lgP =-0.64)；在不同 pH 磷酸盐缓冲液中,西他沙星在 pH 7.4的中性条件下溶解度最低,仅为0.13 mg·mL-1,表观油水分配系数最大,在 pH>10及 pH<5.8,西他沙星平衡溶解度显著增大,表观油水分配系数相应减小。结论西他沙星难溶于水,脂溶性也较差,但在酸性和碱性条件下有较高的溶解度。
목적：측정서타사성재불동용제중적용해도이급표관유수분배계수,위제형연구화제비공예제공의거。방법채용고효액상색보(HPLC)법,Dikma Diamonsil C18(2)색보주(4.6 mm×250 mm,5μm)；류동상：0.05 mol·L-1린산이경갑용액(용린산조절 pH 지2.4)을정=7030；주온：실온；류속1.0 mL·min-1；검측파장：295 nm；진양량10μL。고찰서타사성재 pH 위2.0,4.3,5.8,6.6,7.4,8.0,10.0,11.2린산염완충액중용해도화표관유수분배계수。결과재(37±2)℃조건하,서타사성재수중적평형용해도위0.44 mg·mL-1,표관유수분배계수( P)위0.23( lgP =-0.64)；재불동 pH 린산염완충액중,서타사성재 pH 7.4적중성조건하용해도최저,부위0.13 mg·mL-1,표관유수분배계수최대,재 pH>10급 pH<5.8,서타사성평형용해도현저증대,표관유수분배계수상응감소。결론서타사성난용우수,지용성야교차,단재산성화감성조건하유교고적용해도。
Objective To determine the solubility and apparent oil/ water partition coefficient of sitafloxacin in different solvents. Methods High performance liquid chromatography (HPLC) was used. The column was Dikma Diamonsil C18 (2) (4. 6 mmí250 mm,5 μm). The mobile phase was 0. 05 mol·L-1 KH2 PO4 solution (pH was adjusted with H3 PO4 to 2. 4)-acetonitrile (7030). The column temperature was set at room temperature. The flow rate was 1. 0 mL·min-1 . The detection wavelength was 295 nm and the injection volume was 10 μL. The solubility of sitafloxacin and the apparent oil/ water partition coefficient at pH 2. 0,4. 3,5. 8,6. 6,7. 4,8. 0,10. 0 and 11. 2 were determined. Results The equilibrium solubility of sitafloxacin in water was 0. 44 mg·mL-1 and the apparent oil/ water partition coefficient was 0. 23 (lgP= -0. 64) at (37±2) ℃ . Sitafloxacin has the lowest equilibrium solubility (0. 13 mg·mL-1 ) and the highest apparent oil/ water partition coefficient in pH7. 4 buffer solution system. At pH>10 and pH<5. 8,the solubility of sitafloxacin increased obviously and apparent oil/ water partition coefficient decreased. Conclusion Sitafloxacin is insoluble in water and also poorly soluble in oil,but its solubility could be improved significantly in acidic or alkaline solution.