富马酸美托洛尔爆破型脉冲片体外实验研究

 目的以富马酸美托洛尔为模型药物,研制爆破型脉冲片并考察其体外释药特性。方法以乙基纤维素和丙烯酸树脂(Eudragit L100)为包衣材料,聚乙二醇6000(PEG 6000)为增塑剂,采用薄膜包衣法,制备含富马酸美托洛尔50 mg的脉冲片;通过体外释放实验,考察处方因素对脉冲片体外释放的影响;通过吸水实验分析脉冲片的释药机制。结果片芯崩解剂种类、包衣组成与厚度、增塑剂种类与用量影响富马酸美托洛尔的脉冲释放。该制剂在体外延迟释放时间为4.5 h,时滞后3.5 h累积释药达90%。结论富马酸美托洛尔爆破型脉冲片在体外具有脉冲释放特性。

Studies on Explosion Pulsatile-Release Tablets of Metoprolol Fumarate in vitro

OBJECTIVE To prepare the explosion pulsatile-release tablets of metoprolol fumarate(MF) and to investigate the release characteristics in vitro.METHODS The pulsatile-release tablets containing MF 50 mg was prepared by film-coated methods using ethylcellulose(EC)and Eudragit L100 as coating materials and PEG 6000 as plasticizer.The relationship between the formulation composition and the releasing rate of the MF pulsatile-release tablets was investigated.The pulsatile-release mechanism of the tablets was proved by the water take-up experiments.RESULTS The release characters of the MF pulsatile-release tablets were related to the disintegrant in the core and the composition and the thickness of the coating films as well as the varieties and amounts of plasticizer.The delayed-release time was 4.5 h in vitro,the accumulated amouts of release was 90% when the pulse-release time was 3.5 h.CONCLUSION The pulsatile-release character of the MF pulsatile-release tablets is confirmed in vitro.