Interaction of Tri-O-methyl-β-cyclodextrin with Drugs. I. Effect of Tri-O-methyl-β-cyclodextrin on the Partition Coefficients of Drugs

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The partition coefficients of p-nitrophenol between 0.05N HCl and CHCl_3 were measured with or without tri-O-methyl-β-cyclodextrin (methyl-β-CD) at 15.5,20.0,and 25.0℃. The partition coefficients increased linearly with methyl-β-CD concentration. In the presence of 3.00×10^<-2>M methyl-β-CD, the value was about 2.5 times larger than that measured in the absence of methyl-β-CD. Methyl-β-CD was not detected in the aqueous phase by polarimetry, and most of the methyl-β-CD molecules were present in the CHCl_3 phase. The increase of the partition coefficients can be interpreted in terms of 1 : 1 complex formation between methyl-β-CD and p-nitrophenol. The complexes of methyl-β-CD and p-nitrophenol in the aqueous solution and the CHCl_3 solution were studied quantitatively by ultraviolet absorption measurements. The formation of inclusion complex in D_2O was also investigated by proton magnetic resonance spectroscopy.
社団法人日本薬学会の論文
1982-05-25