Chow S L, Sims B E
J Pharm Sci. 1981 Aug;70(8):924-6. doi: 10.1002/jps.2600700823.
Cetaben sodium solubilities were evaluated by micellar solubilization in various surfactants and lipid solvents. At pH 8, the relationship between cetaben sodium solubility and surfactant concentration delineated apparent saturable kinetics; at pH 4.9, the relationship between the two parameters was linear. In the presence of 0.5% sodium taurocholate and polysorbate 80, cetaben sodium solubility increased as the medium pH was increased; however, in the presence of 0.5% poloxamer 188, cetaben sodium solubility revealed a hyperbola when the pH was changed from 4.9 to 8.0. Cetaben sodium solubility was enhanced greatly by mixed physiological surfactants, full-strength caprylic-capric monodiglycerides or monodiglycerides, when compared to a single surfactant system. Cetaben sodium solubility is influenced by pH, surfactant type, surfactant concentration, lipid solvent type, and the simultaneous presence of surfactants or phospholipids.
通过在各种表面活性剂和脂质溶剂中的胶束增溶作用评估了西他苯钠的溶解度。在pH 8时，西他苯钠溶解度与表面活性剂浓度之间的关系呈现出明显的饱和动力学；在pH 4.9时，这两个参数之间的关系是线性的。在存在0.5%牛磺胆酸钠和聚山梨酯80的情况下，随着介质pH值的升高，西他苯钠溶解度增加；然而，在存在0.5%泊洛沙姆188的情况下，当pH值从4.9变为8.0时，西他苯钠溶解度呈现出双曲线关系。与单一表面活性剂体系相比，混合生理表面活性剂、全强度辛酸 - 癸酸甘油单酯或甘油单酯可大大提高西他苯钠的溶解度。西他苯钠溶解度受pH值、表面活性剂类型、表面活性剂浓度、脂质溶剂类型以及表面活性剂或磷脂的同时存在影响。
