Tags

Type your tag names separated by a space and hit enter

The influence of polyvinylpyrrolidone on naproxen complexation with hydroxypropyl-beta-cyclodextrin.
Eur J Pharm Sci. 2001 May; 13(2):187-94.EJ

Abstract

The combined effect of hydroxypropyl-beta-cyclodextrin (HPbetaCD) and polyvinylpyrrolidone (PVP) on the solubility of naproxen (NAP) was studied. Phase-solubility analysis at different temperatures was used to investigate interactions in aqueous solution between NAP and the carriers, either alone or in combination. Equimolar NAP-HPbetaCD solid systems, in the presence or the absence of 15% (w/w) PVP, were prepared by cogrinding, kneading, coevaporation or freeze-drying, and characterized by differential scanning calorimetry, X-ray powder diffraction analysis, infrared spectroscopy and dissolution rates. The combined use of PVP and HPbetaCD resulted in a synergistic increasing effect of the aqueous solubility of NAP (120 times that of the pure drug). The phenomenon was interpreted in terms of the strongest complexation capacity of HPbetaCD towards NAP, which was reflected by an about 65% increase in the apparent stability constant of the NAP-HPbetaCD complex in the presence of only 0.1% (w/v) PVP. Variations in thermodynamic parameters accounted for a PVP role in the formation of a NAP-HPbetaCD-PVP ternary complex. The positive effect of PVP also reflected on NAP dissolution rates from solid preparations, because all ternary systems, with the exception of physical mixtures, dissolved faster than the corresponding NAP-HPbetaCD binary systems. The results of solid state studies accounted for the occurrence of mechanically- and/or thermally-induced stronger interactions in ternary than in binary systems, that in some cases led to a complete loss of NAP crystallinity.

Authors+Show Affiliations

Dipartimento di Scienze Farmaceutiche, Via G. Capponi 9, 50121, Firenze, Italy. mura@farmafi.scifarm.unifi.itNo affiliation info availableNo affiliation info available

Pub Type(s)

Journal Article
Research Support, Non-U.S. Gov't

Language

eng

PubMed ID

11297903

Citation

Mura, P, et al. "The Influence of Polyvinylpyrrolidone On Naproxen Complexation With Hydroxypropyl-beta-cyclodextrin." European Journal of Pharmaceutical Sciences : Official Journal of the European Federation for Pharmaceutical Sciences, vol. 13, no. 2, 2001, pp. 187-94.
Mura P, Faucci MT, Bettinetti GP. The influence of polyvinylpyrrolidone on naproxen complexation with hydroxypropyl-beta-cyclodextrin. Eur J Pharm Sci. 2001;13(2):187-94.
Mura, P., Faucci, M. T., & Bettinetti, G. P. (2001). The influence of polyvinylpyrrolidone on naproxen complexation with hydroxypropyl-beta-cyclodextrin. European Journal of Pharmaceutical Sciences : Official Journal of the European Federation for Pharmaceutical Sciences, 13(2), 187-94.
Mura P, Faucci MT, Bettinetti GP. The Influence of Polyvinylpyrrolidone On Naproxen Complexation With Hydroxypropyl-beta-cyclodextrin. Eur J Pharm Sci. 2001;13(2):187-94. PubMed PMID: 11297903.
* Article titles in AMA citation format should be in sentence-case
TY - JOUR T1 - The influence of polyvinylpyrrolidone on naproxen complexation with hydroxypropyl-beta-cyclodextrin. AU - Mura,P, AU - Faucci,M T, AU - Bettinetti,G P, PY - 2001/4/12/pubmed PY - 2001/7/6/medline PY - 2001/4/12/entrez SP - 187 EP - 94 JF - European journal of pharmaceutical sciences : official journal of the European Federation for Pharmaceutical Sciences JO - Eur J Pharm Sci VL - 13 IS - 2 N2 - The combined effect of hydroxypropyl-beta-cyclodextrin (HPbetaCD) and polyvinylpyrrolidone (PVP) on the solubility of naproxen (NAP) was studied. Phase-solubility analysis at different temperatures was used to investigate interactions in aqueous solution between NAP and the carriers, either alone or in combination. Equimolar NAP-HPbetaCD solid systems, in the presence or the absence of 15% (w/w) PVP, were prepared by cogrinding, kneading, coevaporation or freeze-drying, and characterized by differential scanning calorimetry, X-ray powder diffraction analysis, infrared spectroscopy and dissolution rates. The combined use of PVP and HPbetaCD resulted in a synergistic increasing effect of the aqueous solubility of NAP (120 times that of the pure drug). The phenomenon was interpreted in terms of the strongest complexation capacity of HPbetaCD towards NAP, which was reflected by an about 65% increase in the apparent stability constant of the NAP-HPbetaCD complex in the presence of only 0.1% (w/v) PVP. Variations in thermodynamic parameters accounted for a PVP role in the formation of a NAP-HPbetaCD-PVP ternary complex. The positive effect of PVP also reflected on NAP dissolution rates from solid preparations, because all ternary systems, with the exception of physical mixtures, dissolved faster than the corresponding NAP-HPbetaCD binary systems. The results of solid state studies accounted for the occurrence of mechanically- and/or thermally-induced stronger interactions in ternary than in binary systems, that in some cases led to a complete loss of NAP crystallinity. SN - 0928-0987 UR - https://www.unboundmedicine.com/medline/citation/11297903/The_influence_of_polyvinylpyrrolidone_on_naproxen_complexation_with_hydroxypropyl_beta_cyclodextrin_ L2 - https://linkinghub.elsevier.com/retrieve/pii/S0928098701000938 DB - PRIME DP - Unbound Medicine ER -