合成高分子化合物と医薬品との相互作用に関する研究(第2報) : スチレン無水マレイン酸共重合体とピラゾロン誘導体およびフェノチアジン誘導体との相互作用

概要

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New absorption bands were observed in the visible region of spectra for ethylene dichloride solution of styrene-maleic anhydride copolymer (SMA) containing antipyrine, aminopyrine, 4-[2-(dimethylamino)propionamido]antipyrine(aminopropylone) or chlorpromazine, indicating occurrence of interaction. The degree of binding of SMA with antipyrine, aminopyrine, aminopropylone, chlorpromazine, promethazine, levomepromazine, propericiazine, prochlorperazine and thioproperazine was evaluated by the equilibrium distribution method. It was shown that all the compounds investigated were reversibly bound with SMA, and that the binding equilibria fit a Langmuir-type equation. The degree of binding of pyrazolone derivatives with SMA appeared to be dependent upon the nature of the substituent at the 4-position of pyrazolone rings ; substitution by basic groups increased the binding constants. Except for the case of chlorpromazine, an increase in the aliphatic character of phenothiazine derivatives resulted in a decrease in the binding constants. The maximum amount (y_m) of each compounds bound to SMA indicated that one guest molecule was bound by over than 10 monomeric units of the copolymer chain. In relation to a possible binding mechanism, the significance of these results are discussed.
社団法人日本薬学会の論文
1970-04-25