Abstract
Purpose: To investigate the effect of co-administration of two absorption enhancing bile alts, sodium glycocholate (NaGc) and sodium salicylate (NaSal), on insulin absorption via intestinal targeted delivery system.Methods: Insulin (10 IU/kg), associated with and without absorption enhancers (5 % enhancer solution of NaGc or NaSal), was administered to the duodenum, jejunum, and ileum part of the diabetic rat's gastrointestinal (GI) tract by surgical technique. The insulin absorbed from the GI tract was evaluated by its hypoglycemic effect at 45 and 60 min post-administration.Results: The results showed that insulin formulations containing NaGc or NaSal administered into the duodenum and with little quantity in the jejunum decreased blood glucose levels, compared to the reference formulations (p < 0.05). It was also observed that formulations containing cellulose acetate phthalate (CAP) protectors and enhancers may protect insulin during transit through the stomach for 180 min.Conclusion: Thus, the results of this study demonstrate that duodenum-specific delivery of insulin with NaGc and NaSal was achievable by oral administration compared to the other parts of small intestine. Furthermore, NaGc has a greater enhancing effect on duodenal, and to some extent, jejunal absorption of insulin.Keywords: Bile salts, Sodium glycocholate, Sodium salicylate, Insulin, Gastrointestinal administration
Highlights
Insulin is still the principal hypoglycemic medication in diabetes mellitus treatment but administration of these peptide drugs so far have been almost exclusively limited to the parenteral route [1]
Alternative specific insulin delivery systems have been tried to improve the low availability of insulin following oral administration Various absorption promoters such as surfactants, bile salts, chelating agents, fatty acids, protease inhibitor and soy bean trypsin inhibitor have been used for improving the absorption of poorly absorbable drugs such as insulin [2]
In this study NaGc with NaSal were used as model bile salts due to their absorption enhancing effects for insulin [8] and other peptides [9] to overcome the low availability of insulin oral administration
Summary
Insulin is still the principal hypoglycemic medication in diabetes mellitus treatment but administration of these peptide drugs so far have been almost exclusively limited to the parenteral route [1]. In this study NaGc with NaSal were used as model bile salts due to their absorption enhancing effects for insulin [8] and other peptides [9] to overcome the low availability of insulin oral administration.
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