<abstract xml:lang="en" xmlns="http://www.w3.org/1999/xhtml"><p>Dissolution behaviour of a poorly water-soluble drug, tadalafil, from its solid dispersion systems with poloxamer 407 has been investigated. Solid dispersion systems of tadalafil were prepared with poloxamer 407 in 1:0.5, 1:1.5 and 1:2.5 ratios using the melting method. Characterization of binary systems with FTIR and XRPD studies demonstrated the presence of strong hydrogen bonding interactions, a significant decrease in crystallinity and the possibility of existence of amorphous entities of the drug. In the binary systems tested, 1:0.5 proportion of tadalafil/poloxamer 407 showed rapid dissolution of tadalafil (<italic>DE</italic><sub>30</sub> 70.9 ± 3.6 %). In contrast, higher proportions of poloxamer 407 (1:1.5 and 1:2.5) offered no advantage towards dissolution enhancement of the drug, indicating altered rheological characteristics of the polymer at its higher concentration, which might have retarded the release rate of tadalafil.</p></abstract>

Dissolution behaviour of a poorly water-soluble drug, tadalafil, from its solid dispersion systems with poloxamer 407 has been investigated. Solid dispersion systems of tadalafil were prepared with poloxamer 407 in 1:0.5, 1:1.5 and 1:2.5 ratios using the melting method. Characterization of binary systems with FTIR and XRPD studies demonstrated the presence of strong hydrogen bonding interactions, a significant decrease in crystallinity and the possibility of existence of amorphous entities of the drug. In the binary systems tested, 1:0.5 proportion of tadalafil/poloxamer 407 showed rapid dissolution of tadalafil (DE30 70.9 ± 3.6 %). In contrast, higher proportions of poloxamer 407 (1:1.5 and 1:2.5) offered no advantage towards dissolution enhancement of the drug, indicating altered rheological characteristics of the polymer at its higher concentration, which might have retarded the release rate of tadalafil.

Physicochemical characterization of solid dispersion systems of tadalafil with poloxamer 407

Department of Pharmaceutical Chemistry, Government College of Pharmacy, Karad Maharashtra-415124, India

Acta Pharmaceutica

Dissolution behaviour of a poorly water-soluble drug, tadalafil, from its solid dispersion systems with poloxamer 407 has been investigated. Solid dispersion...

Physicochemical characterization of solid dispersion systems of tadalafil with poloxamer 407

Publié en ligne: 16 nov. 2009

Pages: 453 - 461

DOI: https://doi.org/10.2478/v10007-009-0037-4

Mots clés
tadalafil, čvrsta disperzija, poloksamer 407, oslobađanje

This content is open access.

Physicochemical characterization of solid dispersion systems of tadalafil with poloxamer 407

Publié en ligne: 16 nov. 2009

Pages: 453 - 461

DOI: https://doi.org/10.2478/v10007-009-0037-4

Mots cléstadalafil, čvrsta disperzija, poloksamer 407, oslobađanje

This content is open access.

Mots clés
tadalafil, čvrsta disperzija, poloksamer 407, oslobađanje