Evaluation of gastrointestinal transit characteristics of oral patch preparation using caffeine as a model drug in human volunteers.

Salivary caffeine excretion rate test has been proposed for the evaluation of gastrointestinal transit characteristics of an oral patch preparation after administration to human volunteers instead of measuring the plasma or serum concentration in the early stages of formulation development. Patches having a diameter of 3.0 mm and containing caffeine as a model drug were prepared.

Evaluation of oral formulations of gentamicin containing labrasol in beagle dogs.

Gentamicin (GM) is a polarized water-soluble compound having very poor intestinal membrane permeability resulting in low oral bioavailability. Labrasol was found to improve the intestinal absorption of GM in rats. In the present study, GM formulations containing labrasol were evaluated in beagle dogs after filling into hydroxypropylmethyl cellulose (HPMC) capsules wrapped with Eudragit L100 (Eud L) and Eudragit S100 (Eud S) films.

Enhanced intestinal absorption of vancomycin with Labrasol and D-alpha-tocopheryl PEG 1000 succinate in rats.

Vancomycin hydrochloride (VCM) is a glycopeptide antibiotic used for the treatment of infections caused by methicillin-resistant staphylococci. It is water soluble, having a high molecular weight, and poorly absorbed from the gastrointestinal tract. Mixtures of VCM with Labrasol and D-alpha-tocopheryl polyethylene glycol 1000 succinate (TPGS) were prepared to improve oral absorption of VCM.

Possibility of a patch system as a new oral delivery system.

A new oral patch system has been designed to increase the residence time of model drugs within the gastrointestinal tract. The system consisted of three layers (1) water-insoluble backing layer (2) drug-carrying adhesive layer composed of a model drug, fluorescein (FL) or fluorescein isothiocyanate-dextran (FD), and gel-forming polymer and (3) pH-sensitive enteric polymer. These three layers system was prepared as 3.

Absorption enhancing effect of labrasol on the intestinal absorption of insulin in rats.

The oral absorption enhancing effect of Labrasol has been studied in rats using insulin as a model peptide/protein drug. Insulin solution was prepared by dissolving insulin in pH 7.4 buffer followed by the addition of Labrasol.