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Biol Pharm Bull ; 47(6): 1123-1127, 2024.
Article in English | MEDLINE | ID: mdl-38839364

ABSTRACT

This study aimed to validate the In vitro Dissolution Absorption System 2 (IDAS2) containing a biological barrier of Caco-2 or Madin-Darby canine kidney (MDCK) cell monolayer through dose sensitivity studies. Metoprolol and propranolol were selected as Biopharmaceutics Classification System (BCS) Class I model drugs, and atenolol as a Class III model drug. The IDAS2 is comprised of a dissolution vessel (500 mL) and two permeation chambers (2 × 8.0 mL) mounted with Caco-2 or MDCK cell monolayer. One or two immediate-release tablet(s) of the model drug were added to the dissolution vessel, and the time profiles of dissolution and permeation were observed. Greater than 85% of metoprolol and propranolol (tested at two dosing concentrations) were dissolved by 15 min, and all drugs were fully dissolved by 30 min. All three drugs were more permeable across Caco-2 cells than MDCK cells with a linear increase in permeation across both cells at both dose concentrations. Thus, the dose sensitivity of the IDAS2 was demonstrated using both cell barriers. These results indicate a successful qualification of IDAS2 for the development/optimization of oral formulations and that MDCK cells can be utilized as a surrogate for Caco-2 cells.


Subject(s)
Atenolol , Metoprolol , Propranolol , Solubility , Dogs , Caco-2 Cells , Humans , Animals , Madin Darby Canine Kidney Cells , Propranolol/pharmacokinetics , Metoprolol/pharmacokinetics , Metoprolol/administration & dosage , Atenolol/pharmacokinetics , Atenolol/administration & dosage , Dose-Response Relationship, Drug , Biopharmaceutics/methods , Permeability , Intestinal Absorption
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