尼莫地平柱塞型脉冲释药胶囊的制备

目的:制备尼莫地平柱塞型脉冲释药胶囊。方法:采用灌注法制备非渗透性囊体,以HPMC K15M为缓释骨架材料制备柱塞片,以PEG 6000和PEG 4000为基质制备尼莫地平滴丸,用柱塞片将滴丸密封于非渗透性囊体内制备尼莫地平柱塞型脉冲释药胶囊。结果:溶剂为丙酮/二氯甲烷/乙酸乙酯(2:0.7:0.3),醋酸纤维素溶液浓度为10.5%,柱塞片缓释骨架材料HPMC K15M和乳糖比例为1:10,制得的尼莫地平柱塞型脉冲释药胶囊体外呈明显的脉冲释放,释药时滞为4~5 h。结论:通过调节柱塞片中HPMC K15M和乳糖比例可调节脉冲胶囊的释药时滞,将尼莫地平制成滴丸可满足脉冲胶囊时滞后快速释药的要求。

Preparation of nimodipine pulsatile capsules

OBJECTIVE To prepare nimodipine pulsatile capsules controlled by time. METHODS Impermeable capsule bodies were prepared using filling method, plug tablets were prepared using HPMC K15M as matrix materials. Nimodipine dropping pills were made with PEG 6000 and PEG 4000 as matrix. Pulsatile capsules were prepared by putting dropping pills into impermeable capsule body and sealed it with plug tablets. RESULTS Concentration of acetyl cellulose was 10.5% in acetone/dichlormethane/ethyl acetate(2:0.7:0.3), plug tablet consisted of HPMC K15M and lactose(1:10), and nimodipine pulsatile capsules showed obvious pulsatile release in vitro with a lag time of 4-5 h. CONCLUSION Pulsatile capsules with a proper lag time can be achieved by adjusting HPMC K15M/lactose ratio. Nimodipine dropping pills can meet requirements of immediate-release after the lag time of pulsatile capsules.