摘要
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（βＣＤ）包合作用的影响。方法：用相溶解度法研究了药物在βＣＤ溶液中或同时含有βＣＤ和高聚物的溶液中的热力学性质。结果：在βＣＤ溶液中水溶性高聚物的最佳浓度区域为１５～３０ｇ·Ｌ－１。低浓度ＰＶＰ或ＰＥＧ对βＣＤ溶液的粘度没有显著影响；２５ｇ·Ｌ－１ＰＥＧ的加入使βＣＤ对氯霉素的增溶效率增加了１５％，而２５ｇ·Ｌ－１ＰＶＰ则使βＣＤ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βＣＤ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βＣＤ的包合作用。
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
of β CD on chloramphenicol was improved by 15% when containing 2 5g·L -1
polyethylene glycol in the solution and on vitamininum B 2by 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.
出处
《中国药学杂志》
CAS
CSCD
北大核心
1999年第2期99-101,共3页
Chinese Pharmaceutical Journal
