中枢神经系统药物树脂制备及其静态交换特性研究

以中枢神经系统药物氢溴酸美沙芬（ＤＭ）、盐酸伪麻黄碱（ＰＥ）、盐酸苯丙醇胺（ＰＭ）作为模型药物，以００１×７离子交换树脂作为药物载体，在静态条件下，考察了该树脂与上述药物的交换反应动力学和热力学．结果表明，２５℃时树脂与ＤＭ、ＰＥ和ＰＭ的反应速率常数ｋ（ｍｉｎ－１）分别为１．０４１×１０－３±２．５６×１０－５，２．２９０×１０－２±１．２４×１０－４，２．４０×１０－２±１．０２×１０－４，且随温度的升高而增加，反应活化能Ｅａ（ｋＪ／ｍｏｌ）分别为５０．２６，２１．６８，２０．８３；在２５℃反应达平衡时，表观交换反应平衡常数Ｋｅ分别为３．２３５±０．２５２，３．６８０±０．２１４，４．５１±０．３２８；其自由能变化ΔＧ°（ｋＪ／ｍｏｌ）分别为－２．９０９±０．０２０５，－３．２２８±０．０１８１，－３．７３２±０．０１２７，表明交换反应是自发的；反应热ΔＨ°（ｋＪ／ｍｏｌ）分别为８８．４４±５．５４８，４８．２９±３．２１４，４８．６６±３．１５８，即正反应为吸热反应，温度升高有利于向正反应方向进行

The Preparation and Exchange Reaction Characteristics of Central Nervous System Drugs-resin Complexes

In this paper the effect of the chemical structures of various drugs such as dextromethorphan hydrobromide(DM), pseuoephedrine hydrochloride(PE) and phenylpropanolamine hydrochloride(PM) on the exchange behavior with the strongly acidic cation exchanger(0017) was described. From experiments, it indicates that the exchange rate constants were found to be 1\^04110\+\{-3\}2\^5610\+\{-5\}, 2\^29010\+\{-2\}1\^2410\+\{-4\}, 2\^4010\+\{-2\}1\^0210\+\{-4\} min\+\{-1\} at 25 respectively. The \%K\%\-e is increased with increasing temperature. The exchange activation energies were calculated to be 50\^26, 21\^68, 20\^83 kJ\5mol\+\{-1\}, respectively. The apparent equilibrium constants(\%K\%\-e) were calculated to be 3\^2350\^252, 3\^6800\^214, 4\^5100\^328 at 25 , respectively. The exchange reactions are spontaneous according to the data of \%G\%=-2\^9090\^020 5, -3\^2280\^018 1, \{-3\^7320\^012 7\} kJ\5mol\+\{-1\}, respectively. The reaction enthalpy \%H\% were found to be 88\^445\^548, 48\^293\^214, 48\^663\^158 kJ\5mol\+\{-1\}, respectively, indicating the reaction is enthermal reaction.