罗布麻双层漂浮型脉冲释药片的制备

Preparation of bilayer floating gogbane tablets for pulsatile release

目的制备用于节律性高血压治疗的罗布麻提取物漂浮型脉冲释药片。方法以崩解时间和溶出度为指标,筛选罗布麻提取物速释片芯的崩解剂,用混料设计优选最佳漂浮层处方,体外释药试验考察对时滞的影响。结果优选的处方和工艺条件为:交联聚维酮(PVPP)作为片芯崩解剂;包衣处方中羟丙甲基纤维素(HPMC K4M)作为凝胶材料,乳糖用量为20%;漂浮层以30%卡波姆(carbopol)、36.3%羟丙甲基纤维素、33.7%碳酸氢钠组合最优。体外释放试验表明,罗布麻双层漂浮型脉冲片在经6 h滞期后药物脉冲释放。结论罗布麻双层漂浮型脉冲片达到瞬间起漂并持续到预定的时滞期脉冲释药,满足节律性疾病的治疗要求。

AIM To develop a floating godbane leaf（ Apocynum venetum L.） extract tablets with pulsatile drug delivery system for circadian rhythmic hypertension treatment. METHODS The disintegration time and dissolution rate were taken as indexes for selection of the disintegrating agent for a quick release tablet core and the mixing design to screen the optimal formula for the bilayer. The in vitro test was applied to evaluating the lag time of tablet release. RESULTS The optimum prescription and process conditions were made up by PVPP as the disintegrate agent for core materiel,HPMC K4 M with 20% lactose for gel material,30% carbopol,36. 3% HPMC K4 M,and 33. 7% sodium bicarbonate were employed for the pulsatile layer. In vitro release test showed that the release from bilayer floating pulsatile gogbane tablets began after six-hour time lag. CONCLUSION The bilayer floating godbane tablets for pulsatile release reach the target for instant floating and start the release at the expected time after the designed lag,and this qualifies the treatment of rhythmic diseases.