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Solid-state characterization and dissolution properties of naproxen-arginine-hydroxypropyl-beta-cyclodextrin ternary system.
Eur J Pharm Biopharm. 2005 Jan; 59(1):99-106.EJ

Abstract

The effect of ternary complexation of naproxen, a poorly water soluble anti-inflammatory drug, with hydroxypropyl-beta-cyclodextrin and the basic aminoacid L-arginine on the drug dissolution properties has been investigated. Equimolar binary (drug-cyclodextrin or drug-arginine) and ternary (drug-cyclodextrin-arginine) systems were prepared by blending, cogrinding, coevaporation, and characterized by differential scanning calorimetry, thermogravimetric analysis, FT-IR spectroscopy, X-ray diffractometry. The dissolution behavior of naproxen from the different products was evaluated by means of a continuous flow through method. The results of solid state studies indicated the presence of strong interactions between the components in ternary coevaporated and coground systems, which were both of totally amorphous nature. In contrast, the presence of either free drug or free arginine was detected when the third component (cyclodextrin or aminoacid) was physically mixed, respectively, to the drug-arginine binary system (as physical mixture, coevaporate, or coground product) or to the drug-cyclodextrin binary system (as physical mixture, coevaporate, or coground product). All ternary combinations were significantly (P<0.001) more effective than the corresponding binary drug-cyclodextrin and drug-arginine systems in improving the naproxen dissolution rate. The best performance in this respect was given by the ternary coevaporate, with about 15 times increase in terms of both drug relative dissolution rate and dissolution efficiency. The synergistic effect of the simultaneous use of arginine and cyclodextrin on the dissolution rate of naproxen was attributed to the combined effects of inclusion in cyclodextrin and salt formation, as well as to a specific role played by arginine in this interaction.

Authors+Show Affiliations

Dipartimento di Scienze Farmaceutiche, Università di Firenze, Firenze, Italy. mura@unifi.itNo affiliation info availableNo affiliation info availableNo affiliation info availableNo affiliation info availableNo affiliation info available

Pub Type(s)

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

Language

eng

PubMed ID

15567306

Citation

Mura, Paola, et al. "Solid-state Characterization and Dissolution Properties of Naproxen-arginine-hydroxypropyl-beta-cyclodextrin Ternary System." European Journal of Pharmaceutics and Biopharmaceutics : Official Journal of Arbeitsgemeinschaft Fur Pharmazeutische Verfahrenstechnik E.V, vol. 59, no. 1, 2005, pp. 99-106.
Mura P, Bettinetti GP, Cirri M, et al. Solid-state characterization and dissolution properties of naproxen-arginine-hydroxypropyl-beta-cyclodextrin ternary system. Eur J Pharm Biopharm. 2005;59(1):99-106.
Mura, P., Bettinetti, G. P., Cirri, M., Maestrelli, F., Sorrenti, M., & Catenacci, L. (2005). Solid-state characterization and dissolution properties of naproxen-arginine-hydroxypropyl-beta-cyclodextrin ternary system. European Journal of Pharmaceutics and Biopharmaceutics : Official Journal of Arbeitsgemeinschaft Fur Pharmazeutische Verfahrenstechnik E.V, 59(1), 99-106.
Mura P, et al. Solid-state Characterization and Dissolution Properties of Naproxen-arginine-hydroxypropyl-beta-cyclodextrin Ternary System. Eur J Pharm Biopharm. 2005;59(1):99-106. PubMed PMID: 15567306.
* Article titles in AMA citation format should be in sentence-case
TY - JOUR T1 - Solid-state characterization and dissolution properties of naproxen-arginine-hydroxypropyl-beta-cyclodextrin ternary system. AU - Mura,Paola, AU - Bettinetti,Gian Piero, AU - Cirri,Marzia, AU - Maestrelli,Francesca, AU - Sorrenti,Milena, AU - Catenacci,Laura, PY - 2003/10/20/received PY - 2004/05/10/revised PY - 2004/05/10/accepted PY - 2004/11/30/pubmed PY - 2005/4/20/medline PY - 2004/11/30/entrez SP - 99 EP - 106 JF - European journal of pharmaceutics and biopharmaceutics : official journal of Arbeitsgemeinschaft fur Pharmazeutische Verfahrenstechnik e.V JO - Eur J Pharm Biopharm VL - 59 IS - 1 N2 - The effect of ternary complexation of naproxen, a poorly water soluble anti-inflammatory drug, with hydroxypropyl-beta-cyclodextrin and the basic aminoacid L-arginine on the drug dissolution properties has been investigated. Equimolar binary (drug-cyclodextrin or drug-arginine) and ternary (drug-cyclodextrin-arginine) systems were prepared by blending, cogrinding, coevaporation, and characterized by differential scanning calorimetry, thermogravimetric analysis, FT-IR spectroscopy, X-ray diffractometry. The dissolution behavior of naproxen from the different products was evaluated by means of a continuous flow through method. The results of solid state studies indicated the presence of strong interactions between the components in ternary coevaporated and coground systems, which were both of totally amorphous nature. In contrast, the presence of either free drug or free arginine was detected when the third component (cyclodextrin or aminoacid) was physically mixed, respectively, to the drug-arginine binary system (as physical mixture, coevaporate, or coground product) or to the drug-cyclodextrin binary system (as physical mixture, coevaporate, or coground product). All ternary combinations were significantly (P<0.001) more effective than the corresponding binary drug-cyclodextrin and drug-arginine systems in improving the naproxen dissolution rate. The best performance in this respect was given by the ternary coevaporate, with about 15 times increase in terms of both drug relative dissolution rate and dissolution efficiency. The synergistic effect of the simultaneous use of arginine and cyclodextrin on the dissolution rate of naproxen was attributed to the combined effects of inclusion in cyclodextrin and salt formation, as well as to a specific role played by arginine in this interaction. SN - 0939-6411 UR - https://www.unboundmedicine.com/medline/citation/15567306/Solid_state_characterization_and_dissolution_properties_of_naproxen_arginine_hydroxypropyl_beta_cyclodextrin_ternary_system_ L2 - https://linkinghub.elsevier.com/retrieve/pii/S0939641104001377 DB - PRIME DP - Unbound Medicine ER -