阿苯达唑纳米微粉平衡溶解度和表观脂水分配系数的测定

发布时间：2018-01-08 08:19

本文关键词：阿苯达唑纳米微粉平衡溶解度和表观脂水分配系数的测定　出处：《中国医药导报》2016年33期 　论文类型：期刊论文

【摘要】：目的测定阿苯达唑纳米微粉在不同介质中的平衡溶解度以及表观脂水分配系数。方法采用高效液相色谱法测定阿苯达唑的浓度,采用摇瓶法测定阿苯达唑纳米微粉在不同极性溶剂和不同p H缓冲液中的平衡溶解度及表观脂水分配系数。结果不同极性溶剂中,阿苯达唑纳米微粉在甲醇中溶解度最大[(2564.28±38.73)μg/m L],在水中的溶解度最小[(125.25±1.45)μg/m L]。在pH=1.2~6.8缓冲液中,阿苯达唑纳米微粉溶解度从(551.33±19.00)μg/m L下降到(155.84±5.52)μg/m L;在pH=7.0~7.8缓冲液中,溶解度从(137.53±4.87)μg/m L上升到(168.94±5.63)μg/m L。纳米微粉的表观脂水分配系数在p H=1.2~2.0条件下lgP在0~2之间,pH=5.0~7.8条件下lgP在3~4之间。结论本研究测定了阿苯达唑纳米微粉在不同介质中的平衡溶解度以及表观脂水分配系数,为预测该纳米微粉体内外吸收的改善奠定了基础。
[Abstract]:Objective to determine the equilibrium solubility and apparent lipids water partition coefficient of albendazole nano-powder in different media. Methods the concentration of albendazole was determined by HPLC. The equilibrium solubility and apparent lipid-water partition coefficient of albendazole nano-powder in different polar solvents and pH buffer solution were determined by shaking flask method. Maximum solubility of albendazole nanoparticles in methanol. [2564.28 卤38.73 渭 g / mL], with the lowest solubility in water. [125.25 卤1.45 渭 g / mL]. In pH=1.2~6.8 buffer. The solubility of albendazole nanoparticles decreased from 551.33 卤19.00 渭 g / mL to 155.84 卤5.52 渭 g / mL; In pH=7.0~7.8 buffer. Solubility increased from 137.53 卤4.87 渭 g / mL to 168.94 卤5.63). The apparent lipids and water partition coefficients of 渭 g / m 路L 路渭 g / m 路L 路渭 g / m 路nano-powder were between 0 and 2 under the condition of pH 1.2 and 2.0. Conclusion the equilibrium solubility and apparent lipids water partition coefficient of albendazole nano-powder in different media were determined. It lays a foundation for predicting the improvement of the absorption inside and outside of the nanometer powder.
【作者单位】：新疆医科大学药学院;新疆医科大学第一附属医院药学部;
【基金】：新疆维吾尔自治区重大疾病医学重点实验室开放课题(SKLIB-XJMDR-2014-10)
【分类号】：R927
【正文快照】： 阿苯达唑(albendazole,ABZ)又名丙硫咪唑,为苯并咪唑类广谱抗寄生虫药,其在抗棘球蚴领域卓越的疗效、毒性作用小以及药物经济学方面明显优于其他药物,成为细粒棘球蚴病药物治疗中的首选[1-2],也是WHO推荐抗包虫病的一线药物[3-4]。但其在水和多数有机溶剂中不溶,影响了其体内

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