氯磷酸二钠缓释微丸工艺与处方的优化

Optimization of preparation and formulation of the sustained-release pellets of disodium clodronate

目的 :优化氯磷酸二钠缓释微丸的工艺以及处方中辅料的配方。方法 :以20 mg氯膦酸二钠为一个微丸的剂量,优化滚制速度、时间和干燥温度、微晶纤维素和润滑剂的加入量及乙基纤维素和硬脂酸的比例。结果 :最佳微丸制备工艺为:高档速度下滚制6 min,干燥温度为60℃。微丸的最佳配方为:20 mg氯膦酸二钠,不加微晶纤维素,乙基纤维素和硬脂酸比例为1∶2,24μl的10%Eudragit L30D-55。结论 :该工艺和配方可以作为制备氯磷酸二钠缓释微丸的较佳方案。

Objective： To optimize the preparation and formulation process of clodronate sustained-release pellets. Methods：Taking 20 mg of clodronate as a dose of pellet, the preparation processes such as speed and time of ball rolling, drying temperature and dosage of excipients and lubricant were optimized. Anion exchange chromatography was used to determine the release amount of the clodronate pellets prepared under different conditions at different time points. Results：The best processes for preparation and formulation of pellets were as follows：rolling for 6 min at high speed and 60℃, adding 20 mg of clodronate disodium, ethyl cellulose and stearic acid at ratio of 1：2 and 24 μl of 10%Eudragit L30D-55 without microcrystalline cellulose. Conclusion：The process above-mentioned is a better one for preparation of sustained-release pellets of disodium clodronate.