摘要
目的:为保护胰岛素口服后不被肠道酶分解,用聚丙交酯包裹胰岛素制成口服型微囊(PLAMCI),对其活性进行初步研究。方法:PLAMCI体外释药胰岛素测定用福林酚法。体内活性通过糖尿病大鼠口服后血糖变化反映。结果:体外释药实验显示PLAMCI自30min开始释药,6～10h已释放65%～80%,持续释药达108h。将释药后的上清液注入糖尿病兔,其中的胰岛素仍保持降血糖的生物活性。34只非空腹糖尿病大鼠口服PLAMCI(含胰岛素2.5mg),平均血糖下降(57±21)%,峰时为7～12h,持续作用(8±4)h,血糖下降幅度与剂量正相关。结论:PLAMCI保持了胰岛素生物活性,具有新的药理作用模式。
OBJECTIVE:In order to protect insulin from degradation in gastrointestinal tract by proteolytic enzyme, polylactide was used to encapsulate the insulin. The insulin release profile from microspheres in vitro and characteristics after oral administration in vivo were studied. METHODS:Insulin entrapped in polylactide microcapsulated insulin (PLA MCI) was determined by Follin phenol method by UV spectrophotometer. The hypoglycemic effects were determined by periodically assaying blood glucose levels in diabetic rats.RESULTS: In vitro insulin began to release from PLA MCI since 30 min in 10 mmol·L -1 PBS buffer (pH 7.4) , it released for 65%～80% after 6～10 hours. The above buffer contained released insulin was injected into diabetic rabbits.It showed similar hypoglycemic profile to insulin. 34 unfasting diabetic rats were gavaged by PLA MCI (contained insulin 2.5 mg).Their peripheral blood glucose decreased to (-57±-21)% of control levers for (8±4)h.The peak action was in 7～12 hours after oral administration. The hypoglycemic effects were positively related to the doses of PLA MCI. CONCLUSION:PLA MCI kept the hypoglycemic effects of native insulin but showed a new pharmacologic model.
出处
《中国药学杂志》
CAS
CSCD
北大核心
2000年第2期99-102,共4页
Chinese Pharmaceutical Journal
关键词
口服型
胰岛素
聚丙交酯
微囊化
insulin,polylactide acid,microcapsulated insulin
