骨架型别嘌醇缓释微丸的制备及其质量评价

目的：优化骨架型别嘌醇缓释微丸的处方及制备工艺，并对其进行质量评价。方法：采用挤出滚圆法制备微丸；以得率为指标，考察骨架材料、致孔剂、崩解剂及制备工艺过程的滚圆速度和滚圆时间对释放度的影响，并验证处方；以圆整度及粒度分布、流动性、脆碎度为指标，对其进行质量考察。结果：优化的处方以微晶纤维素（Mcc）为骨架材料，以乳糖为致孔剂，交联羧甲基纤维素钠为崩解剂，控制滚圆速度为50Hz，滚圆时间为20rain。通过调节MCC、乳糖和崩解剂的配伍使用，可以起到调节药物释放的作用，得到释放度符合要求的微丸。验证试验所得微丸的平均圆整度为10．2，粒度分布在22~26目最多，占95．63％；平均休止角为23．15，流动性良好；脆碎度为0．08％；其他各项质量指标良好。结论：所选处方及制备工艺合理、可行，所制备微丸质量良好。

Preparation and Quality Evaluation of Matrix Type Allopurinol Sustained-release Pellets

OBJECTIVE： To optimize the formulation and preparation technology of matrix type Allopurinol sustained-release pellets, and to evaluate the quality of it. METHODS： The extrusion-spberonisation method was applied to prepare the pellets. The effects of matrix materials, diluents, disintegrants, spheronization speed and spheronization time on release rate of pellets were in- vestigated with yield as index, and validation test of presq~ription was conducted. The quality of product was assessed through inves-~ tigating sphericity, size distribution, flexibility and friab! lity. RESULTS： The optimized formulation was as follows： microcrystal- line cellulose （MCC）, lactose and croscarmellose sodiu~ as matrix material, diluents and disintegrants; spheronization speed of 50 Hz, spheronization time of 20 rain. By adjusting the prol~ortion of MCC, lactose and croscarmellose sodium, drug release could be adjusted, and yield and release rate of pellets met the release requirement. Validation test showed sphericity of 10.2 ~ ; particle size of 22-26 mesh, accounting for 95.63%; angle of repose of 23.15 o, with sound flexibility; friability of 0.08 %; other quality index- es were satisfactory. CONCLUSIONS： The formulation and preparation technology are reasonable and feasible, and the quality of prepared pellets is satisfactory.