CAJ | 학술논문

研究了Pluronic F127胶团溶液对药物布洛芬(IBU)的增溶作用.通过芘探针荧光法测定了不同温度下F127在水溶液和0.01 mol·L-1 pH 7.4磷酸盐缓冲生理(PBS)溶液中的临界胶束浓度(cmc),采用高效液相色谱(HPLC)测定了F127溶液中布洛芬的溶解度,并依据公式计算了增溶参数(摩尔增溶量X和胶团-水分配系数K),考察了温度、溶剂和F68的加入对F127胶团化行为及其对布洛芬增溶作用的影响.结果表明:布洛芬的溶解度随F127质量分数的提高线性增加:随着温度升高,cmc急剧下降,胶团内核的疏水性增强,X和K稍有增大;与水溶液相比,在PBS溶液中cmc减小,X乎不变,K显著降低;F68的加入对F127胶团的性质几乎无影响,对增溶的影响也不明显.对增溶参数的分析表明,K反映的是药物布洛芬的性质,X则可反映嵌段共聚物F127的溶解效能,并证实了布洛芬是通过F127胶团的内核和栅栏层而实现增溶的.
연구료Pluronic F127효단용액대약물포락분(IBU)적증용작용.통과비탐침형광법측정료불동온도하F127재수용액화0.01 mol·L-1 pH 7.4린산염완충생리(PBS)용액중적림계효속농도(cmc),채용고효액상색보(HPLC)측정료F127용액중포락분적용해도,병의거공식계산료증용삼수(마이증용량X화효단-수분배계수K),고찰료온도、용제화F68적가입대F127효단화행위급기대포락분증용작용적영향.결과표명:포락분적용해도수F127질량분수적제고선성증가:수착온도승고,cmc급극하강,효단내핵적소수성증강,X화K초유증대;여수용액상비,재PBS용액중cmc감소,X호불변,K현저강저;F68적가입대F127효단적성질궤호무영향,대증용적영향야불명현.대증용삼수적분석표명,K반영적시약물포락분적성질,X칙가반영감단공취물F127적용해효능,병증실료포락분시통과F127효단적내핵화책란층이실현증용적.
We studied the effect of Pluronic F127 micelle solution on the solubility of ibuprofen (IBU). The critical micelle concentration (cmc) of F127 in both water and 0.01 mol-L-1 pH 7.4 phosphate buffer salt (PBS) solution at different temperatures was determined by the pyrene fluorescence method. The concentration of the solubilized IBU was determined using high-performance liquid chromatography (HPLC). We calculated the solubility descriptors (molar solubilization capacity,X,and micelle-water partition coefficient,K). The influences of temperature, medium properties, and additional copolymer F68 on the micellization of F127 and the solubilization of IBU were also investigated. The results showed that the solubility of IBU increased linearly with an increase in the F127 mass fraction. With an increase in temperature, a significant decrease in the cmc was apparent and a less polar microenvironment was present in the micelle core. Slight increases in X and K were found with an increase in temperature. The cmc of F127 in PBS solution was much less than that in water, x was essentially the same and K decreased significantly in PBS solution. F127 micelle property and the solubilization capacity of the F127 micelles were only slightly affected in the presence of F68. An analysis of the solubility descriptors indicates that the K is particularly unique for the drug IBU, and the % is useful in determining the solubility effectiveness of copolymer F127. We also demonstrated that IBU was predominantly in the micelle core and core-corona interface.