Interaction of Chlorpromazine-Hydrochloride with Lecithin Vesicles detected by the Use of Carbon-13 Nuclear Magnetic Resonance

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The interaction of chlorpromazine-HCl with lecithin vesicles was investigated by carbon-13 nuclear magnetic resonance spectroscopy. Signal broadening of the drug induced by its addition to a vesicle-water (D_2O) solution indicated the incorporation of the drug into the vesicle membrane. In the absence of the drug, two resolved signals arising from the carbonyl carbons of the external and internal layers of the vesicle were observed with 0.3 ppm shift difference, but the difference became almost undetectable on addition of the drug. This phenomenon suggests that the incorporated chlorpromazine was located near the carbonyl carbons in the vesicle membrane. Displacement of a trivalent cation from the membrane surface by chlorpromazine-HCl was confirmed by the observation that the upfield shift of exterior choline methyl carbons initially induced by the addition of a shift reagent, Yb^<3+>, to the vesicle solution was canceled out when a sufficient amount of the drug was added to the sample solution.
公益社団法人日本薬学会の論文
1979-05-25