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目的:以非洛地平为模型药物,制备脉冲释放片,通过优化处方,使脉冲片在预设时间爆破,有效快速释放药物。方法:采用湿法制粒压片法,制备含药片芯;以乙基纤维素(EC)为包衣材料,薄膜包衣法对片芯进行包衣;单因素考察筛选崩解剂、致孔剂、增塑剂等辅料;均匀设计法优化处方工艺。结果:经过单因素考察及均匀设计优化得到最佳处方,片芯中崩解剂为低取代羟丙基纤维素(L-HPC),含量占片芯重10%;包衣液中增塑剂为邻苯二甲酸二丁酯(DBP),含量为8.5%(占EC的量),致孔剂为PEG6000,含量为7%(占EC的量);通过体外释放试验,制备的脉冲片,时滞为(4.1±0.2)h,在时滞后(1.5±0.2)h内,药物累积释药达到90%以上。结论:非洛地平爆破型脉冲片制备工艺简单,优化后处方可达到4 h爆破设计要求,具有良好的释药行为。
OBJECTIVE: To felodipine as a model drug preparation of pulsatile release tablets, by optimizing the prescription, the pulsar burst in the preset time, effective and rapid release of drugs. Methods: The tablet core was prepared by wet granulation method. The core was coated with ethyl cellulose (EC) as the coating material and the film coating method. The single factor was used to screen the disintegrator and porogen , Plasticizers and other accessories; uniform design optimization prescription process. Results: The optimum prescription was obtained through single factor investigation and uniform design optimization. The disintegrating agent in tablet cores was low-substituted hydroxypropyl cellulose (L-HPC), accounting for 10% of the tablet core weight. The plasticizer As dibutyl phthalate (DBP), the content is 8.5% (the amount of EC), the porogen is PEG6000, the content is 7% (the amount of EC); by in vitro release test, The time lag was (4.1 ± 0.2) h. After the lag time (1.5 ± 0.2) h, the accumulated drug release reached more than 90%. Conclusion: The preparation method of felodipine bursting pulse sheet is simple, and the optimized formulation can reach the requirements of 4 h blasting design with good release behavior.