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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: To study the protective effect of insulin on enteric microcapsules (PLAMCI) after being orally ingested by polylactide-coated insulin without being degraded by intestinal enzymes. Methods: PLAMCI in vitro release of insulin was measured by Folin method. In vivo activity is reflected by changes in blood glucose in diabetic rats after oral administration. Results: In vitro release experiment showed that PLAMCI started to release from 30min, release of 65% ~ 80% in 6 ~ 10h and sustained release of 108h. The released supernatant was injected into diabetic rabbits, in which the insulin still maintained hypoglycemic biological activity. In 34 non-fasting diabetic rats, oral administration of PLAMCI (containing 2.5 mg of insulin) resulted in a mean blood glucose drop (57 ± 21)% at peak time of 7 to 12 hours and sustained effect (8 ± 4) h. Conclusion: PLAMCI maintains insulin bioactivity and has a new pharmacological model.