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目的:制备5-氨基水杨酸结肠定位柱塞型脉冲胶囊并对其体外释药行为进行评价。方法:用灌注法制备非渗透性胶囊体,粉末直接压片法压制柱塞片,湿法制粒法制备含药速崩片,将速崩片与柱塞片密封于非渗透性胶囊体内制备脉冲胶囊,考察影响释药时滞的各种因素。结果:胶囊在体外呈明显的脉冲释放,释药时滞随柱塞片中高酯果胶-乳糖或羟丙甲纤维素-低酯果胶比例的增加而增加,具有相同处方柱塞片的脉冲胶囊在模拟结肠溶出介质中释药时滞明显缩短,当高酯果胶-乳糖为4∶6和6∶4,低酯果胶/羟丙甲纤维素为9.5∶0.5和9∶1时,可达到结肠定位所需的4~5h释药时滞。结论:调节柱塞片处方组成可获得具有适当释药时滞的脉冲胶囊,以满足结肠定位释药的目的。
OBJECTIVE: To prepare 5-aminosalicylic acid colon-positioned plunger pulse capsule and evaluate its in vitro drug release. Methods: The non-permeable capsule body was prepared by perfusion method. The powder tablets were directly compressed to compress the plunger tablets. The wet granulation method was used to prepare the drug-containing rapidly disintegrating tablets. The disintegrating tablets and the plunger tablets were sealed in non-permeable capsules to prepare the pulse Capsule, investigate the various factors that affect the drug release delay. Results: The capsule showed obvious pulse release in vitro. The release delay increased with the increase of the proportion of high-ester pectin-lactose or hypromellose-low ester pectin in the plunger slice. The pulses with the same prescription plunger The delayed release of the capsule in the simulated colon dissolution medium was significantly shortened when the high ester pectin-lactose was 4: 6 and 6: 4, the low ester pectin / hypromellose was 9.5: 0.5 and 9: 1, Colonization can reach the required 4 ~ 5h drug release delay. Conclusion: Adjusting the composition of the plunger tablets prescription can be obtained with appropriate release delay pulse capsule to meet the purpose of colon-specific release.