盐酸倍他洛尔-树脂混悬剂制备工艺研究

Study on Preparation Technology of Betaxolol Hydrochloride Resin Suspension

目的:考察药物-树脂混悬剂的制备工艺。方法:以阳离子交换树脂(大、小粒径)为载体,盐酸倍他洛尔为模型药物,设计正交试验考察药物与大、小粒径树脂结合的复合物的包封率和载药量,以沉降体积比和再分散性为评价指标筛选出合适的助悬剂,并在人工泪液中比较包衣后药物-树脂混悬剂盐酸倍他洛尔滴眼液的释药动力学。结果:制备的药物-树脂(小粒径)复合物包封率为82.86%、载药量为41.43%,优于大粒径(78.95%、39.48%);以加入卡波姆为助悬剂时混悬剂沉降体积比大,再分散性好,混悬剂稳定。由包衣后的药物-树脂复合物所制备的混悬剂,在人工泪液中的释药动力学与盐酸倍他洛尔滴眼液相似。结论:初步建立了药物-树脂混悬剂的制备工艺,为进一步制备出安全、有效、稳定的药物-树脂眼用混悬剂提供了一定的参考。

OBJECTIVE： To investigate the preparation technology of Betaxolol hydrochloride resin suspension.METHODS： Encapsulation coefficency and drug-loading amount of compound of drugs combined with resin of big and small particle size were investigated by orthogonal experiment using cation exchange resin（big and small particle size） as carrier and betaxolol hydrochloride as model drug.The suspension was selected with sedimentation volume ratio and redispersibility as index.The drug release kinetics was compared between drug-resin suspension and Betaxolol hydrochloride eye drops in artificial tear.RESULTS： Encapsulation coefficency of small size complexes was 82.86% with drug-loading rate of 41.43%,which was superior to those of large size complexes（78.95% and 39.48%）.Great sedimentation volume ratio and sound redispersibility of stable suspension were obtained using carbomer as suspending agent.Suspension was prepared from the coated drug-resin complexes,and drug release kinetics of complexes was similar to that of Betaxolol hydrochloride eye drops in artificial tear.CONCLUSION： The preparation technology of drug-resin suspension has been established preliminary,which offers some reference for the preparation of safe,effective,stable Betaxolol hydrochloride-resin ophthalmic suspension.