非洛地平爆破型脉冲释放片制备及处方优化

Preparation of felodipine blasting type pulsed-release tablet and optimization of the prescription

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。

OBJECFIVE To prepare pulsed-release tablets with felodipine as the model drug. The prescription was optimized on purpose that the pulsed drugs could be discharged and the major drug be released quickly at the preset time. METHODS The core of tahlet was manufactured by wet-granulation squashing method and using ethyleellulose as coating stuff and filmcoating as method to prepare coated tablets. Univariate factor was used to investigate and screen the disintegrating agent, pore forming agent,plasticizer and other accessories. The prescription was optimized with homogeneous design. RESULTS The opti- mized prescription was obtained through the univariate factor investigation and homogeneous design. In the tablet core, LHPC, which was selected as disintegrating agent,occupied 10% of the total weight. In the coating solution, plasticizer（DBP） occupied 8. 50/00 weight of the EC; pore-forming （PEG6000） occupied 7%. In vitro release experiment, the time-lag of the prepared pulsed-release tablets was （4. 1 ± 0. 2） hour. In the time-lag of （1.5 ± 0. 2） hour, the cumulative drug release reached above 90%. CONCLUSION The preparation technology of blasting type felodipine is simple. After optimization,the prescription can reach the design demand that the drug be blasting released after 4 hours,which has well drug release behavior.