静态法与动态法测定药物水中溶解度的探讨..docxVIP

静态法与动态法测定药物水中溶解度的探讨 作者：袁飞，何琳，丁沐淦，龙晓 英，李志棠，梁静敏，林小玲【摘要】 目的比较采用静态法与动态法对药物 水中平衡溶解度测定结果的影响。 方法 静态法：超声1 h、25 C水浴恒温24 h, 25 C气浴振荡24 h , 25 C水浴恒温放置7 d及16 d;动态法：超声1 h、 25 C气浴振荡24 h , 25 C气浴振荡24 h , 25 C水浴搅拌24 h，分别测定布 洛芬、盐酸小檗碱、葛根素、对乙酰氨基酚在水中的溶解度。 结果25 C条件 下采用静态法及动态法测得药物在水中的平衡溶解度如下：布洛芬为 0.067~0.078 mg/mL(RSD 11.94%~22.18%)和 0.063~0.078 mg/mL(RSD 3.2%~7.8%); 盐酸小檗碱为 7.072~8.230 mg/mL(RSD 3.4%~14.5%)和 7.654~9.771 mg/mL(RSD 2.2%~5.0%)，葛根素为 7.305~9.479 mg/mL(RSD 7.5%~14.5%)和 6.057~8.046 mg/mL(RSD 2.5%~6.8%); 对乙酰氨基酚为 8.708~9.771 mg/mL(RSD 3.2%~13.6%)和 8.965~10.932 mg/mL(RSD 1.5%~6.6%)。结论 4 种药物在水中的平衡溶解度以动态法重现性较好，其中采 用水浴搅拌24 h测得的结果重现性最好，最低 RSD值为1.5%;而采用超声与恒 温气浴振荡结合法，除溶解度特别小的药物造成误差较大外，基本能满足大部 分药物溶解度测定的要求(RSDV2.5%)而且，相对于水浴搅拌，该法处理样品 量大，可广泛应用。 【关键词】 静态法;动态法;平衡溶解度 Abstract:ObjectiveTo compare the effect of stationary method and dynamic method on the results of drugs equilibrium solubility in water.Methods The solubility of ibuprofen,berberine,puerarin and paracetamol in water were determined by stationary method,i.e.,ultraso und 1 h,the n stay in water bath 24 h at 25 °C or oscillated in air bath 24 h at 25 C ,then stay 7 d and 16 d at the same temperature; and by dynamic method,i.e.,oscillated in air bath h at 25 C ,ultrasound 1 h and then oscillated in air bath 24 h at C,or agitated in water bar 24 h at 25 C,respectively.Results The solubility of ibuprofen,berberine,puerarin and paracetamol by stationary and dynamic method were 0.067~0.078 mg/mL(RSD=11.94%~22.18%)and 0.063~0.078 mg/mL(RSD=3.2%~7.8%),7.072~8.230 mg/mL(RSD=3??4%~14.50%)and 7.654~9.771 mg/mL(RSD=2.2%~5.0%),7.305~9.479 mg/mL(RSD=7??5%~14.50%)and 6.057~8.046 mg/mL(RSD=2.5%~6.8%),8.708~9.771 mg/mL(RSD=3??2%~13.6%)and 8.965~10.932 mg/mL(RSD=1.5%~6.6%),respectively.Conclusion The solubility data of four drugs in water exhibits good reproducibility by dynamic method,especially with agitating in water bar 24 h and the lowest RSD is 1.5%.The RSD of combination of ultrasound and oscillation of air bath is less than 2.5%,which satisf