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Comparative efficacy and bioequivalence of novel h1-antihistamine bepotastine salts (nicotinate and salicylate).
- Source :
-
Journal of toxicology and environmental health. Part A [J Toxicol Environ Health A] 2014; Vol. 77 (22-24), pp. 1451-66. - Publication Year :
- 2014
-
Abstract
- Bepotastine salts (nicotinate and salicylate) were investigated for their physicochemical properties to develop novel salt forms of bepotastine, bioequivalent to the bepotastine besilate-loaded tablet (Talion). These bepotastine salts of either nicotinate- or salicylate-loaded tablets were prepared by conventional wet granulation method, and dissolution profiles and pharmacokinetics in beagle dogs were compared to those of Talion. A novel bepotastine nicotinate has a higher solubility at varying pH levels (1.2, 4, or 6.8) than salicylate-loaded or besilate-loaded salt. In addition, those bepostastine salt forms (nicotinate and salicylate) are stable in heat, light, and water. Further, the novel nicotinate- and salicylate-loaded tablets showed similar dissolution rates to Talion in several selected dissolution media and were bioequivalent to Talion in beagle dogs in terms of area under the concentration-time curve (AUC) and maximum observed concentration (Cmax). A pharmacokinetic study performed in beagle dogs demonstrated that test and reference products were found to be bioequivalent in terms of safety, efficacy, and pharmacokinetic properties. These results suggest that bepostastine nicotinate and salicylate formulations are considered applicable candidates and are well tolerated versus the conventional bepostastine besilate formulation.
- Subjects :
- Animals
Chemical Phenomena
Chromatography, Liquid
Dogs
Female
Guinea Pigs
Hydrogen-Ion Concentration
Male
Rats
Rats, Sprague-Dawley
Tablets chemistry
Tandem Mass Spectrometry
Therapeutic Equivalency
Histamine Antagonists pharmacokinetics
Niacin pharmacokinetics
Piperidines pharmacokinetics
Pyridines pharmacokinetics
Salicylates pharmacokinetics
Subjects
Details
- Language :
- English
- ISSN :
- 1528-7394
- Volume :
- 77
- Issue :
- 22-24
- Database :
- MEDLINE
- Journal :
- Journal of toxicology and environmental health. Part A
- Publication Type :
- Academic Journal
- Accession number :
- 25343294
- Full Text :
- https://doi.org/10.1080/15287394.2014.955833