盐酸地尔硫卓药物树脂复合物的制备及其体外释药动力学研究  

THE EXCHANGE REACTIVE KINETICS AND RELEASE KINETICS OF DILTIAZEM HYDROCHLORIDE-RESIN COMPLEXES IN VITRO

作　　者：李振华[1] 皮洪琼[1] 袁直[1] 何炳林[1] 

机构地区：[1]吸附分离功能高分子材料国家重点实验室

出　　处：《离子交换与吸附》2001年第1期1-8,共8页Ion Exchange and Adsorption

基　　金：国家教育部博士点基金!(98005504)

摘　　要：本文以强酸性阳离子交换树脂为载体，制备了盐酸地尔硫卓(DH)药物树脂复合物。研究了DH与001×7树脂的交换反应动力学以及药物树脂复合物在去离子水、0.5mol/L、1.0mol/L、2.0mol/L NaCl和在0.5mol/L HCl以及0.5mol/L KCl溶液中的释药动力学。结果表明，在制备药物树脂的过程中，随温度的升高，药物与树脂的交换速率增加，及有利于反应的进行；药物树脂复合物在去离子水中不释放药物，但其释放随释放介质浓度的增加而增加，并且属于粒扩散的离子交换控制，粒扩散系数Dr随离子强度的增加而增加，DH的释药动力学过程符合对数方程（Visuanathan方程），001×7树脂可有效地控制DH在体外的释放。This paper describes the exchange reactive kinetics of diltiazem hydrochloride (DH) with the strongly acidic cation exchange resin (001×7) and the release kinetics of DH from the drug-resin complexes in deionic water, 0.5mol/L, 1.0mol/L, 2.0mol/L NaCl and 0.5mol/L HCl as well as 0.5mol/L KCl solutions. The drug-resin complexes were prepared by bath method. The content of drug was assayed spectrophotometrically at 237nm. It was found that the exchange rate and exchange reactive equilibrium constants increased with increasing of temperatures. The release studies in vitro showed that no found of DH release from drug-resin complexes when the deionic water was used as releasing medium. The release rate increases with increasing of ionic strength of the release medium, which indicates that the release of DH from the drug-resin complexes strongly depends on the ionic strength of release medium. The release of DH from drug-resin complexes can be effectively controlled by the strongly acidic cation exchange resin (001×7). A particle diffusive process controls the diffusion of DH within the resin particles based on the equation of Viswanathan. The diffusion coefficients increase with the increasing of ionic strength of the releasing media. The release kinetics of DH could be described satisfactorily by the equation of Viswanathan.

关 键 词：盐酸地尔硫卓 离子交换树脂控释给药系统 体外释药动力学 钙通道阻滞药 药物树脂复合物 

分 类 号：R972[医药卫生—药品] R944.9[医药卫生—药学]