国际医学寄生虫病杂志
國際醫學寄生蟲病雜誌
국제의학기생충병잡지
INTERNATIONAL JOURNAL OF MEDICAL PARASITIC DISEASES
2012年
5期
292-295
,共4页
棘球蚴病%甲苯达唑%溶解度%酸碱度%酸度值
棘毬蚴病%甲苯達唑%溶解度%痠堿度%痠度值
극구유병%갑분체서%용해도%산감도%산도치
Echinococcosis%Mebendazole%Solubility%pH%Acid value
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37℃的恒温水浴中以100 r/min的速度机械振荡24 h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/ml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.
目的 研究甲苯達唑在幾種油相和水相介質中的溶解度,通過觀察溶解度的變化情況,為藥物生物利用度的提高奠定基礎.方法 將甲苯達唑分散于大豆油、甘油三油痠酯以及油痠等9種油相介質中,併以1％西黃耆膠和去離子水作為對照,于25℃或37℃的恆溫水浴中以100 r/min的速度機械振盪24 h後離心,取上清液採用高效液相色譜法(HPLC)測定甲苯達唑在上述介質中的濃度.結果 在25℃時甲苯達唑在大豆油、甘油三油痠酯以及油痠中的溶解度分彆為(2.1±0.2)μg/ml、(54.1±1 9)μg/ml以及(329.4 +9.7) μg/ml,均高于在去離子水(1.0±0.1) μg/ml和1％西黃芪膠(5.5±0.7) μg/ml的溶解度.噹介質溫度升高到37℃,甲苯達唑在上述溶劑中的溶解度均隨著介質溫度的升高而增加,其中在3種油相中的溶解度為(34.1 ± 1.9) ～(900.7±57.1)μg/ml,而在1％西黃耆膠和去離子水中增加到(7.2±0.7)μg/ml和(3.7±1.2)μg/ml.結論 與傳統的水相給藥介質相比,將甲苯達唑分散于油相溶劑中,可顯著增加其溶解度.
목적 연구갑분체서재궤충유상화수상개질중적용해도,통과관찰용해도적변화정황,위약물생물이용도적제고전정기출.방법 장갑분체서분산우대두유、감유삼유산지이급유산등9충유상개질중,병이1％서황기효화거리자수작위대조,우25℃혹37℃적항온수욕중이100 r/min적속도궤계진탕24 h후리심,취상청액채용고효액상색보법(HPLC)측정갑분체서재상술개질중적농도.결과 재25℃시갑분체서재대두유、감유삼유산지이급유산중적용해도분별위(2.1±0.2)μg/ml、(54.1±1 9)μg/ml이급(329.4 +9.7) μg/ml,균고우재거리자수(1.0±0.1) μg/ml화1％서황기효(5.5±0.7) μg/ml적용해도.당개질온도승고도37℃,갑분체서재상술용제중적용해도균수착개질온도적승고이증가,기중재3충유상중적용해도위(34.1 ± 1.9) ～(900.7±57.1)μg/ml,이재1％서황기효화거리자수중증가도(7.2±0.7)μg/ml화(3.7±1.2)μg/ml.결론 여전통적수상급약개질상비,장갑분체서분산우유상용제중,가현저증가기용해도.
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 hby 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 ) μg/ml in three oil solvents mentioned above and was ( 7.2 ± 0.7 ) μg/ml and (3.7 + 1.2) μg/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.
