1种微粒分散型盐酸维拉帕米脉冲制剂的研究

Preparation A Novel Verapamil Hydrochloride Polydispersity Pulsatile Released Dosage Form

目的制备1种微粒分散型pH敏感型离子交换树脂并将其应用于脉冲制剂。方法采用自由基聚合反应制备pH敏感型离子交换树脂;并采用红外光谱仪、激光衍射粒径分析仪对所制得的pH敏感型离子交换树脂进行表征;进一步在pH敏感型离子交换树脂上载药-盐酸维拉帕米,在模拟胃肠液的环境中进行pH敏感型离子交换树脂溶胀和盐酸维拉帕米药物树脂复合物体外释放实验。结果成功制备了平均粒径范围在200～210μm的pH敏感型离子交换树脂。在pH6.8溶液中,盐酸维拉帕米在15 min内快速释放,在30 min内完全释放。而在pH1.2溶液中,几乎没有药物释放。随着缓冲溶液的pH从1.2增加到7.4,微球的吸水量也显著增加。结论 pH敏感型离子交换树脂可应用于脉冲制剂的制备。

Objective To develop a polydispersity pH-sensitive ion exchange resin,and to apply it to the pulsatile released dosage form.Methods A novel pH-sensitive ion exchange resin was synthesized by the suspension polymerization and the sulfonation reaction.Microspheres of this resin were characterized by FTIR and laser scanning particle size analyzer.The pH-sensitive microspheres were loaded with Verapamil hydrochloride.The drug-release and swelling characteristics were studied under both simulated gastric and intestinal pH conditions.Results The pH-sensitive ion exchange resins were successfully prepared with the average particle range in 200~210 μm.The microspheres showed a pulsatile swelling behavior when the pH of the media changed.The drug released fast in the stimulated intestinal medium,almost all the drug released in 30 minutes.But in the gastric medium,there was nearly no drug released.The results showed that the drug-resinates had a clear pulsatile character.Conclusion The novel pH-sensitive ion exchange resin was successfully developed and can be applied to prepare pulsatile released dosage form.