Enhanced absorption of insulin and (Asu(1,7))eel-calcitonin using novel azopolymer-coated pellets for colon-specific drug delivery

Citation
H. Tozaki et al., Enhanced absorption of insulin and (Asu(1,7))eel-calcitonin using novel azopolymer-coated pellets for colon-specific drug delivery, J PHARM SCI, 90(1), 2001, pp. 89-97
Citations number
19
Language
INGLESE
art.tipo
Article
Categorie Soggetti
Pharmacology & Toxicology
Journal title
JOURNAL OF PHARMACEUTICAL SCIENCES
ISSN journal
0022-3549 → ACNP
Volume
90
Issue
1
Year of publication
2001
Pages
89 - 97
Database
ISI
SICI code
0022-3549(200101)90:1<89:EAOIA(>2.0.ZU;2-9
Abstract
The objective of this study was to estimate colon-specific delivery of insu lin and (Asu(1,7))eel-calcitonin using novel azopolymer-coated pellets. In vitro drug-release experiments from the azopolymer-coated pellets containin g fluorescein isothiocyanate dextran (MW 4400; FD-4) were carried out by th e Japanese Pharmacopoeia (J.P.) XIII rotating basket method with some sligh t modifications. Little release of FD-4 from the pellets was observed in ph osphate buffered saline. However, the release of FD-4 was markedly increase d in the presence of rat cecal contents. The intestinal absorption of insul in and (Asu(1,7) )eel-calcitonin after oral administration of the azopolyme r-coated pellets containing these peptides with camostat mesilate was evalu ated by measuring the hypoglycemic and hypocalcemic effects, respectively. A slight decrease in plasma glucose levels was observed following the oral administration of these pellets containing 12.5 IU of insulin compared with the same dose of insulin solution. Camostat mesilate, a protease inhibitor that is incorporated with insulin in these pellets, further decreased the plasma glucose levels in a dose-dependent manner. Similar results were also obtained with the oral administration of pellets containing (Asu(1,7))eel- calcitonin. These findings suggest that azopolymer-coated pellets may be us eful carriers for the colon-specific delivery of peptides including insulin and (Asu(1,7))eel-calcitonin. (C) 2001 Wiley-Liss, Inc. and the American P harmaceutical Association.