摘要
目的研究甲苯达唑在几种油相和水相介质中的溶解度，通过观察溶解度的变化情况，为药物生物利用度的提高奠定基础。方法将甲苯达唑分散于大豆油、甘油三油酸酯以及油酸等9种油相介质中，并以1％西黄耆胶和去离子水作为对照，于25℃或37cC的恒温水浴中以100r／min的速度机械振荡24h后离心，取上清液采用高效液相色谱法（HPLC）测定甲苯达唑在上述介质中的浓度。结果在25℃时甲苯达唑在大豆油、甘油三油酸酯以及油酸中的溶解度分别为（2．1±0．2）μg／ml、（54．1±1．9）μg/ml以及（329．4±9．7）μg／ml，均高于在去离子水（1．0±0．1）μg／ml和1％西黄芪胶（5．5±0．7）μg/ml的溶解度。当介质温度升高到37℃，甲苯达唑在上述溶剂中的溶解度均随着介质温度的升高而增加，其中在3种油相中的溶解度为（34．1±1．9）～（900．7±57．1）μg／ml，而在1％西黄耆胶和去离子水中增加到（7．2±0．7）μg/m1和（3．7±1．2）μg／ml。结论与传统的水相给药介质相比，将甲苯达唑分散于油相溶剂中，可显著增加其溶解度。
Objective To study the solubility of mebendazole in several solvents. Methods Mebendazole was suspended in 9 kinds of oil, such as soybean oil, glycerol trioleate, oleic acid and so on, and in 1% tragacanth and deionized water as control. Then after being kept at 25 ℃ and 37 ℃ water bath for 24 h by 100 r/min, the saturated solution was centrifuged and then assayed by high performance liquid chromatograph （HPLC） to estimate the solubility of mebendazole in each solvent. Results The solubility of mebendazole in soybean oil, glycerol trioleate, oleic acid was （2.1 ± 0.2） μg/ml, （54.1 ± 1.9） μg/ml and （329.4 ± 9.7 ） μg/ml respectively, significantly higher than that in 1% tragacanth [ （5.5 ± 0.7 ） μg/ml） and deionized water （ 1.0 ±0.1 ） μg/ml]. And as the temperature raised to 37 ℃, the solubility of mebendaozle in those solvents was all improved, which was from （34.1± 1.9） - （900.7 ± 57.1 ） ±g/ml in three oil solvents mentioned above and was （7.2 ± 0.7） ±g/ml and （3.7 ±1.2） ±g/ml in 1% tragacanth and deionized water. Conclusion The study showed that the solubility of mebendazole could be increased by suspending in oils comparing with the classic aqueous solutions, and provided the way to promote drug absorption and achieve the ultimate purpose of improving curative effect.
出处
《国际医学寄生虫病杂志》
CAS
2012年第5期292-295,共4页
International JOurnal of Medical Parasitic Diseases
