OBJECTIVE To investigate feasibility of the insulin absorption via the buccal mucous of an buccal spray formulation.METHODS
The hypoglycemic effect and the changes of insulin concentration in vivo of an insulin buccal spray formulation in rats and rabbits were investigated.Compared with subcutaneous administration of insulin solution,the
relative pharmacological bioavailability and the
relative bioavailability of insulin buccal spray were determined and the pharmacokinetic parameters were calculated by means of 3P87.RESULTS The relative pharmacological bioavailabilities of insulin spray in rats and rabbits were 30.8% and 40.3%,respectively.According to the data of insulin concentration,the relative bioavailabilities of insulin spray in rats and rabbits were 22.5% and 23.9%,respectively.The concentration time data of buccal and sc adminstration of insulin in rats and rabbits were all fitted to one compartment model with a weight of 1/C/C.The absorption of buccal insulin spray was found more rapid than that of subcutaneous administration.The absorption and elimination of buccal insulin spray in rabbits were rapid than those in rats.CONCLUSION It showed that the insulin buccal spray formulation played a role in reducing the blood glucose level and increasing the plasma insulin concentration.This proved the possibility of insulin delivery via the buccal route.