可待因树脂复合物的表征及其药物释放

目的探讨可待因树脂复合物的形成机理,并考察其药物释放行为的影响因素。方法采用批式离子交换法制备可待因树脂复合物,通过扫描电镜、激光衍射粒度分析考察药物树脂复合物的形态外观;通过红外光谱、X-ray衍射、差示扫描量热分析探讨药物树脂复合物的形成机理;通过释放度试验考察离子种类、离子强度及不同pH值对可待因树脂复合物药物释放行为的影响。结果扫描电镜和粒度分析结果表明,药物树脂复合物的表面形态和粒径大小都与起始的离子交换树脂非常相似。红外光谱、X-ray衍射及DSC分析结果证实,药物树脂复合物所载药物是以化学键的形式结合到离子交换树脂上的,而且和离子交换树脂一样呈现无定型状态。可待因树脂复合物的释放度随着释放介质中离子强度的增加而增大,其释药动力学过程可用Viswanathan方程进行表征。结论可待因树脂复合物是通过化学键形成的,其药物释放行为受释放介质中离子种类、离子强度及不同pH值的影响。

Characterization of codeine-resinate complex and its drug release behavior

ObjectiveTo prepare and characterize the codeine-resinate complex, and study its drug release behavior. Methods Using an ion exchange resin as a carrier, the codeine-resinate complex was prepared by a batch process. The codeine-resinate complex was characterized by the morphology which was observed using a scanning electron microscope, and the particle size distribution was determined using a laser diffraction particle size analyzer. Fourier-transformed infrared analysis, x-ray diffraction analysis, differential scanning calorimetry analysis were employed to confirm the formation mechanism of the codeine-resinate complex. The release behavior of the codeine-resinate complex in different media was investigated which includes various kinds of ion, ionic strength, and pH values. Results Scanning electron microscope analysis and laser particle size analysis proved that the codeine-resinate complex had the same appearance and characters as the initiative ion exchange resin. Through fourier-transformed infrared analysis, x-ray diffraction analysis and differential scanning calorimetry analysis, it’s found that the drug in codeine-resinate complex was combined with ion-exchange resins by chemical bond. The drug-resinate complex, like ion exchange resin, was in amorphous state. The increased ionic strength generally accelerated the drug release from the codeine-resinate complex, and its in-vitro release kinetics conformed to viswanathan performance. Conclusion The codeine-resinate complex is formed through the reaction between the drug and ion-exchange resin by chemical bond. The release behavior is mainly correlated with composition and ionic strength of the release media.