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Characterization of physicochemical properties of naproxen systems with amorphous beta-cyclodextrin-epichlorohydrin polymers.
J Pharm Biomed Anal. 2002 Aug 01; 29(6):1015-24.JP

Abstract

Ground mixtures of naproxen with amorphous beta-cyclodextrin-epichlorohydrin soluble (betaCd-EPS) or insoluble cross-linked (betaCd-EPI) polymers were investigated for both solid phase characterization (Differential Scanning Calorimetry, powder X-ray Diffractometry) and dissolution properties (dispersed amount method). The effect of different grinding conditions and of drug-to-carrier ratio was also evaluated. Co-grinding induced a decrease in drug crystallinity to an extent which depended on the grinding time, and was most pronounced for the cross-linked insoluble polymer, particularly in combinations at the lowest drug content. Both cyclodextrin polymers were more effective in improving the naproxen dissolution properties, not only than the parent betaCd but also than hydroxyalkyl-derivatives, and their performance was almost comparable to that of methyl-derivatives, previously found as the best carriers for naproxen. Dissolution efficiencies of naproxen from physical mixtures with betaCd-EPS, thanks to the high water solubility of this Cd-derivative, were up to three times higher than those from the corresponding products with betaCd-EPI. However this difference in their performance became much less evident in co-ground products and tended to progressively diminish with increasing the polymer content in the mixture, according to the better amorphizing power shown by betaCd-EPI during the co-grinding process. The 10/90 (w/w) drug-carrier co-ground products exhibited the best dissolution properties, giving dissolution efficiencies about 30 times higher than that of naproxen alone.

Authors+Show Affiliations

Dipartimento di Scienze Farmaceutiche, Università di Firenze, Via G. Capponi 9, Firenze, Italy. mura@farmfi.scifarm.unifi.itNo 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

12110386

Citation

Mura, P, et al. "Characterization of Physicochemical Properties of Naproxen Systems With Amorphous Beta-cyclodextrin-epichlorohydrin Polymers." Journal of Pharmaceutical and Biomedical Analysis, vol. 29, no. 6, 2002, pp. 1015-24.
Mura P, Faucci MT, Maestrelli F, et al. Characterization of physicochemical properties of naproxen systems with amorphous beta-cyclodextrin-epichlorohydrin polymers. J Pharm Biomed Anal. 2002;29(6):1015-24.
Mura, P., Faucci, M. T., Maestrelli, F., Furlanetto, S., & Pinzauti, S. (2002). Characterization of physicochemical properties of naproxen systems with amorphous beta-cyclodextrin-epichlorohydrin polymers. Journal of Pharmaceutical and Biomedical Analysis, 29(6), 1015-24.
Mura P, et al. Characterization of Physicochemical Properties of Naproxen Systems With Amorphous Beta-cyclodextrin-epichlorohydrin Polymers. J Pharm Biomed Anal. 2002 Aug 1;29(6):1015-24. PubMed PMID: 12110386.
* Article titles in AMA citation format should be in sentence-case
TY - JOUR T1 - Characterization of physicochemical properties of naproxen systems with amorphous beta-cyclodextrin-epichlorohydrin polymers. AU - Mura,P, AU - Faucci,M T, AU - Maestrelli,F, AU - Furlanetto,S, AU - Pinzauti,S, PY - 2002/7/12/pubmed PY - 2002/10/4/medline PY - 2002/7/12/entrez SP - 1015 EP - 24 JF - Journal of pharmaceutical and biomedical analysis JO - J Pharm Biomed Anal VL - 29 IS - 6 N2 - Ground mixtures of naproxen with amorphous beta-cyclodextrin-epichlorohydrin soluble (betaCd-EPS) or insoluble cross-linked (betaCd-EPI) polymers were investigated for both solid phase characterization (Differential Scanning Calorimetry, powder X-ray Diffractometry) and dissolution properties (dispersed amount method). The effect of different grinding conditions and of drug-to-carrier ratio was also evaluated. Co-grinding induced a decrease in drug crystallinity to an extent which depended on the grinding time, and was most pronounced for the cross-linked insoluble polymer, particularly in combinations at the lowest drug content. Both cyclodextrin polymers were more effective in improving the naproxen dissolution properties, not only than the parent betaCd but also than hydroxyalkyl-derivatives, and their performance was almost comparable to that of methyl-derivatives, previously found as the best carriers for naproxen. Dissolution efficiencies of naproxen from physical mixtures with betaCd-EPS, thanks to the high water solubility of this Cd-derivative, were up to three times higher than those from the corresponding products with betaCd-EPI. However this difference in their performance became much less evident in co-ground products and tended to progressively diminish with increasing the polymer content in the mixture, according to the better amorphizing power shown by betaCd-EPI during the co-grinding process. The 10/90 (w/w) drug-carrier co-ground products exhibited the best dissolution properties, giving dissolution efficiencies about 30 times higher than that of naproxen alone. SN - 0731-7085 UR - https://www.unboundmedicine.com/medline/citation/12110386/Characterization_of_physicochemical_properties_of_naproxen_systems_with_amorphous_beta_cyclodextrin_epichlorohydrin_polymers_ L2 - https://linkinghub.elsevier.com/retrieve/pii/S0731708502001425 DB - PRIME DP - Unbound Medicine ER -