Research paperIntranasal absorption of different aqueous formulations of angiopeptin (cas 113294-82-9): In vivo bioavailability study

Add time:08/12/2019    Source:sciencedirect.com

The bioavailability of angiopeptin in rabbits after intranasal administration of three aqueous formulations has been studied. In each case a total amount of 750 μg angiopeptin was administered. A simple aqueous solution and an aqueous solution supplemented with 5% glycofurol 75 (GF) resulted in bioavailabilities of 133%, whereas the bioavailability of angiopeptin was 53%, when 1% sodium glycocholate (GC) was added to the aqueous solution. The observed reduction in bioavailability from this formulation may be due to precipitation of angiopeptin in the nasal mucus layer, as the formulation containing GC tended to precipitate. The main indication of angiopeptin is inhibition of restenose of cononary arteries after angioplasty or heart transplantation. The pharmacokinetics of angiopeptin could be described by a two-compartment model, and the plasma half-life was about 1.5 h. Addition of GF and GC resulted in faster absorption, the tmax being 16 and 14 min, respectively, as compared with 31 min for the simple aqueous solution. The faster absorption with GF and GC is not considered of therapeutic importance, but rapid absorption may give rise to more reproducible dosing in the clinical situation. Cmax was about 2.8 ng/ml for all three formulations.

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