Abstract
Tolbutamide PEG 6000 solid dispersions as well as tolbutamide β-cyclodextrin complexes were prepared with a view to increasing the bioavailability of this poorly soluble drug. Absolute and relative bioavailabilities were determined by comparison with the administration of a commercial solution of the drug. The study was carried out in rabbits ( n = 5 per dosage form). The aqueous solution of tolbutamide (Dolipol ®) was administered either intravenously (10 mg/kg) or orally (20 mg/kg). Bulk powder, comelt, coprecipitate and solid complex of tolbutamide were administered orally at a dose of 20 mg/kg. Plasma tolbutamide concentrations were measured by an HPLC method. Our results indicate that the absorption of tolbutamide is not increased in comparison with either bulk powder or a solution of the drug. However, there are obvious differences in the kinetics of absorption: indeed, tolbutamide is absorbed rapidly from the complex and the bulk powder. The process of absorption is much slower for the other dosage forms. Finally, even if the quantitative part of bioavailability is not modified, complexation with cyclodextrins could be interesting in order to increase the kinetic process of absorption of poorly soluble drugs.
Published Version
Talk to us
Join us for a 30 min session where you can share your feedback and ask us any queries you have
Schedule a callDisclaimer: All third-party content on this website/platform is and will remain the property of their respective owners and is provided on "as is" basis without any warranties, express or implied. Use of third-party content does not indicate any affiliation, sponsorship with or endorsement by them. Any references to third-party content is to identify the corresponding services and shall be considered fair use under The CopyrightLaw.
