两性霉素B平衡溶解度和表观油水分配系数的测定

Determination of equilibrium solubility of amphotericin B in various medium and its apparent oil/water partition coefficient

目的测定两性霉素B在水和表面活性剂溶液中的平衡溶解度以及在正辛醇-水/缓冲液体系中的表观油水分配系数。方法采用高效液相色谱法测定了两性霉素B在水、缓冲液和表面活性剂溶液中的浓度,采用摇瓶法测定了两性霉素B的表观油水分配系数。结果37℃下两性霉素B在水中的平衡溶解度为31.97mg/L,在酸性和碱性缓冲液中溶解度增大;曲拉通-100(OP)对两性霉素B有较强的增溶能力;两性霉素B的表观油水分配系数为56.95。结论两性霉素B的水溶性较差,提高其口服制剂的溶出度可能会提高其生物利用度。

Objective To determine the equilibrium solubility of amphotericin B in various surfactant solutions and its partition coefficients for the n-octanol-water/buffer solution systems. Methods The high performance liquid chromatography （HPLC） method was established to detect the concentrations of amphotericin B in water, buffer solutions and surfactant solutions, and shaking flash method was used to determine the partition coefficients for the n-octanol-water/buffer solution systems of amphotedcin B. Results The equilibrium solubility of amphotericin B was 31.97 mg/L in water at 37 1Z, and increased in basic and acid buffer solutions. Triton X-100 （OP） was a good solubilizer for amphotericin B. The apparent oil/water partition coefficient of amphotedcin B was 56.95. Conclusion Amphotericin B is a slightly water-soluble drug. To increase the dissolution rate of amphotedcin B for its oral drug delivery system may enhance its bioavailability.