Dissolution properties and in vivo behaviour of triamterene in solid dispersions with polyethylene glycols

The applicability of the solid dispersion technique as a method for enhancing the GI absorption of a drug has been explored in order to procure better dissolution characteristics and better bioavailability for triamterene. The physicochemical characterization of the systems has shown the absence of...

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Bibliographic Details
Published in:Pharmaceutica acta Helvetiae 1996-10, Vol.71 (4), p.229-235
Main Authors: Arias, M.J., Ginés, J.M., Moyano, J.R., Rabasco, A.M.
Format: Article
Language:English
Subjects:
Animals
Biological Availability
Chemical Phenomena
Chemistry, Pharmaceutical
Chemistry, Physical
Diuretics - chemistry
Diuretics - pharmacokinetics
Female
Intestinal Absorption
Male
Polyethylene glycol
Polyethylene Glycols - chemistry
Polyethylene Glycols - pharmacokinetics
Rats
Rats, Wistar
Solid dispersion
Solutions
Triamterene
Triamterene - chemistry
Triamterene - pharmacokinetics
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Summary:The applicability of the solid dispersion technique as a method for enhancing the GI absorption of a drug has been explored in order to procure better dissolution characteristics and better bioavailability for triamterene. The physicochemical characterization of the systems has shown the absence of chemical reaction between the drug and the polymers during the solid dispersion elaboration process (melting carrier method). In vitro release profiles have been studied and quantified in terms of dissolution efficiency over the first 30 min (DE30) and dissolution percentage over the first 30 min (DP30). The results have shown that there were no significant differences between the three polyethylene glycols (PEGs) under test. The in vivo effectiveness of the different preparations was also investigated by means of the urinary volumetric excretion (UVE) — pharmacologie effect — and by the estimation of Kc, tmax, and MRT — pharmacokinetic parameters. At end, an analysis of the relative bioavailabilities between formulations has been performed.
ISSN:0031-6865
DOI:10.1016/S0031-6865(96)00017-9