水溶性高聚物对药物-环糊精包合作用的影响

 目的：研究水溶性高聚物聚乙烯吡咯烷酮（PVP）和聚乙二醇（PEG）对药物与β-环糊精（β-CD）包合作用的影响。方法：用相溶解度法研究了药物在β-CD溶液中或同时含有β-CD和高聚物的溶液中的热力学性质。结果：在β-CD溶液中水溶性高聚物的最佳浓度区域为1.5～3.0g·L^-1。低浓度PVP或PEG对β-CD溶液的粘度没有显著影响；2.5g·L-1PEG的加入使β-CD对氯霉素的增溶效率增加了15％，而2. 5g·L^-1PVP则使β-CD对核黄素的增溶效率增加了98％。说明水溶性高聚物可以增强β-CD对药物的增溶效率；在包合介质中加入高聚物使得包合反应的ΔH负值增大，同时ΔS负值也增大，说明焓效应是包合作用的原动力。结论：水溶性高聚物可以增加药物与β-CD的包合作用。

Effect of water-soluble polymers on drug-cyclodextrin complexation

OBJECTIVES:The effect of water-soluble polymers polyvinylpyrrolidone(PVP) and polyethylene glycol(PEG)on the complexation of drugs with β-cyclodextrin were investigated.METHODS:the thermodynamic properties of drugs in aqueous β-CD solution and in aqueous solut.RESULTS:The maximum solubilization concentration of PVP or PEG appeared from 1.5g.L－1 to 3.0g.L－1.At this low concentration,PVP or PEG had insignificant effect on the viscosity of the aqueous β-CD solution.The solubilising effect ofβ-CD on chloramphenicol was improved by 15% when containing 2.5g.L－1 polyethylene glycol in the solution and on vitamininum B2by 98%when containing 2.5g.L－1 polyvinylpyrrolidone.In aqueous solutions water-soluble polymers were shown to increase the solubilising effect of β-CD on drugs.Additing of PEG or PVP to the aqueous complexation medium resulted in an increased negative enthalpy change,together with an increased negative entropy change.CONCLUSION：Water-soluble polymers were shown to increase the solubilising effect of β-CD on drugs.