Chakraborty Subhashis, Shukla Dali, Jain Achint, Mishra Brahmeshwar, Singh Sanjay
Department of Pharmaceutics, Institute of Technology, Banaras Hindu University, Varanasi 221 005, India.
J Colloid Interface Sci. 2009 Jul 15;335(2):242-9. doi: 10.1016/j.jcis.2009.03.047. Epub 2009 Apr 5.
The effect of surfactants on the solubility of a new phosphate salt of carvedilol was investigated at different biorelevent pH to evaluate their solubilization capacity. Solutions of different classes of surfactants viz., anionic-sodium dodecyl sulfate (SDS) and sodium taurocholate (STC), cationic-cetyltrimethylammonium bromide (CTAB) and non-ionic-Tween 80 (T80) were prepared in the concentration range of 5-35 mmol dm(-3) in buffer solutions of pH 1.2, 3.0, 4.5, 5.8, 6.8 and 7.2. The solubility data were used to calculate the solubilization characteristics viz. molar solubilization capacity, water micelle partition coefficient, free energy of solubilization and binding constant. Solubility enhancement in basic pH was in following order: CTAB>T80>SDS>STC. CTAB and T80 showed remarkable solubility enhancement in acidic pH as well. Among the anionic surfactants, solubility in acidic medium was retarded except at pH 1.2 in case of SDS. Cationic and non-ionic surfactants were found to be suitable for enhancing the solubility of CP which can be employed for maintaining the in vitro sink condition in the basic dissolution medium. While anionic surfactants showed solubility retardant behavior which may be exploited in increasing the drug entrapment efficiency of a colloidal drug delivery system formulated by emulsification technique.
在不同的生物相关pH值下研究了表面活性剂对卡维地洛新磷酸盐溶解度的影响,以评估它们的增溶能力。制备了不同类型表面活性剂的溶液,即阴离子型十二烷基硫酸钠(SDS)和牛磺胆酸钠(STC)、阳离子型十六烷基三甲基溴化铵(CTAB)和非离子型吐温80(T80),浓度范围为5 - 35 mmol dm(-3),分别置于pH 1.2、3.0、4.5、5.8、6.8和7.2的缓冲溶液中。溶解度数据用于计算增溶特性,即摩尔增溶能力、水 - 胶束分配系数、增溶自由能和结合常数。在碱性pH条件下,溶解度增强顺序为:CTAB>T80>SDS>STC。CTAB和T80在酸性pH条件下也显示出显著的溶解度增强。在阴离子表面活性剂中,除了在pH 1.2时的SDS外,在酸性介质中的溶解度均受到抑制。发现阳离子和非离子表面活性剂适合增强卡维地洛新磷酸盐的溶解度,可用于在碱性溶出介质中维持体外漏槽条件。而阴离子表面活性剂表现出溶解度抑制行为,这可用于提高通过乳化技术制备的胶体药物递送系统的药物包封效率。