Alkhamis Khouloud A, Allaboun Hussien, Al-Momani Wafa'a Y
Faculty of Pharmacy, Jordan University of Science and Technology, Irbid, Jordan.
J Pharm Sci. 2003 Apr;92(4):839-46. doi: 10.1002/jps.10350.
It was of interest to increase the solubility of gliclazide in aqueous media. Therefore, solubilization of gliclazide in a variety of surfactants was investigated. Anionic and cationic surfactants exhibited dramatic solubilizing ability for gliclazide, whereas nonionic surfactants showed significantly lower solubilizing ability. It was found that gliclazide solubility increases with increasing the carbon chain length of cationic surfactants and decreases with increasing the carbon chain length of anionic surfactants. The solubilization data were analyzed on the basis of a pseudo-phase model with gliclazide exhibiting moderate partition coefficients into the micellar phase. The possible sites of solubilization of gliclazide in the micelle were examined by studying the effect of NaCl on solubilization and by comparing the absorption spectra of gliclazide in different solvents. The results obtained from these two experiments indicated that gliclazide is solubilized mainly in the inner core of the cationic surfactant micelles and in the outer regions of the anionic surfactant micelles.
提高格列齐特在水性介质中的溶解度很有意义。因此，研究了格列齐特在多种表面活性剂中的增溶情况。阴离子和阳离子表面活性剂对格列齐特表现出显著的增溶能力，而非离子表面活性剂的增溶能力则明显较低。研究发现，格列齐特的溶解度随阳离子表面活性剂碳链长度的增加而增加，随阴离子表面活性剂碳链长度的增加而降低。基于伪相模型分析了增溶数据，格列齐特在胶束相中的分配系数适中。通过研究氯化钠对增溶的影响以及比较格列齐特在不同溶剂中的吸收光谱，考察了格列齐特在胶束中的可能增溶位点。这两个实验得到的结果表明，格列齐特主要增溶在阳离子表面活性剂胶束的内核以及阴离子表面活性剂胶束的外部区域。
