【摘要】 目的：研究吸收促进剂对大鼠胰岛素溶液(insulin solution, INS-SOL)口腔给药的吸收促进作用。方法：以血糖水平为指标，考察在各种吸收促进剂的影响下INS-SOL经正常大鼠口腔给药后的降血糖作用，以皮下注射为对照，计算不同条件下INS-SOL的药理生物利用度(pharmacological bioavailability, PA)。结果：不加吸收促进剂的条件下，10 U·kg-1的INS-SOL 经口腔给药后的生物利用较低(PA=6.9%)。十二烷基硫酸钠(5%，PA=14.5%)，苄泽 78(5%， PA=20.6%)，脱氧胆酸钠(5%，PA=16.5%)和卵磷酯(10%, PA=13.8%)均显著地增加INS-SOL的降血糖作用。苄泽 78 (5%)可使INS-SOL(5 U·kg-1 ) 的PA最高达到33%。结论：在适当的吸收促进剂的作用下INS-SOL经口腔给药后具有显著的降血糖效果。更多还原

【Abstract】 Effects of several transmucosal and transdermal absorption promoters on buccal insulin delivery in rats were evaluated. Insulin absorption has been assessed from cumulative response of serum glucose concentrations and by comparison with a s.c. insulin dose/response curve. In the absence of absorption promoters, buccal insulin was less than 7% as effective as s.c. insulin. The non-ionic surfactant, Brij78, obviously improved buccal insulin absorption, using phosphate buffer solution at pH 7.4 containing 5% adjuvant. One steroidal detergent, sodium deoxycholate, tested as absorption promoter was also effective. Another effective absorption promoter was sodium lauryl sulfate. In the presence of the most effective absorption-promoting systems, the pharmacological availability (PA) of buccal insulin was about one third as effective as s.c. insulin.更多还原