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Assessment of solid-state interactions of naproxen with amorphous cyclodextrin derivatives by DSC.
J Pharm Biomed Anal. 2002 Nov 07; 30(4):1173-9.JP

Abstract

A microcalorimetric method based on differential scanning calorimetry (DSC) of drug-additive binary systems to assess kneading-induced interactions was applied to naproxen (NAP) in combinations with amorphous hydroxypropyl beta-cyclodextrin (HPbetaCd), beta-cyclodextrin sulfobutyl ether, sodium salt ((SBE)(7m)-betaCd), acetyl beta-cyclodextrin (AcbetaCd) and acetyl gamma-cyclodextrin (AcgammaCd). Modifications of thermal parameters of NAP in DSC curves of physical mixtures indicate heating-induced interactions which resulted in a broadening of the NAP melting endotherm in the combinations with HPbetaCd, AcbetaCd and AcgammaCd. The effect of kneading on the interaction was particularly pronounced for the NAP-HPbetaCd and NAP-(SBE)(7m)-betaCd systems, which show a similar drug-to-carrier interaction ratio (1:2 by weight) as that of the other systems. Drug-to-carrier ratios, calculated considering the amount of NAP which recrystallizes from the melted mixtures equivalent to NAP not bound to the carrier, show a distinctly lower affinity in solid-state of the drug for the anionically charged (SBE)(7m)-betaCd with respect to other neutral carriers. The similar affinity of NAP for AcbetaCd and AcgammaCd demonstrates that the geometry of the cavity, which is a determinant factor for the inclusion complexation in liquid state, does not influence the interaction process in solid-state.

Authors+Show Affiliations

Dipartimento di Chimica Farmaceutica, Università di Pavia, Viale Taramelli 12, I-27100, Pavia, Italy. gpbettinetti@unipv.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

12408907

Citation

Bettinetti, G P., et al. "Assessment of Solid-state Interactions of Naproxen With Amorphous Cyclodextrin Derivatives By DSC." Journal of Pharmaceutical and Biomedical Analysis, vol. 30, no. 4, 2002, pp. 1173-9.
Bettinetti GP, Sorrenti M, Rossi S, et al. Assessment of solid-state interactions of naproxen with amorphous cyclodextrin derivatives by DSC. J Pharm Biomed Anal. 2002;30(4):1173-9.
Bettinetti, G. P., Sorrenti, M., Rossi, S., Ferrari, F., Mura, P., & Faucci, M. T. (2002). Assessment of solid-state interactions of naproxen with amorphous cyclodextrin derivatives by DSC. Journal of Pharmaceutical and Biomedical Analysis, 30(4), 1173-9.
Bettinetti GP, et al. Assessment of Solid-state Interactions of Naproxen With Amorphous Cyclodextrin Derivatives By DSC. J Pharm Biomed Anal. 2002 Nov 7;30(4):1173-9. PubMed PMID: 12408907.
* Article titles in AMA citation format should be in sentence-case
TY - JOUR T1 - Assessment of solid-state interactions of naproxen with amorphous cyclodextrin derivatives by DSC. AU - Bettinetti,G P, AU - Sorrenti,M, AU - Rossi,S, AU - Ferrari,F, AU - Mura,P, AU - Faucci,M T, PY - 2002/11/1/pubmed PY - 2003/4/23/medline PY - 2002/11/1/entrez SP - 1173 EP - 9 JF - Journal of pharmaceutical and biomedical analysis JO - J Pharm Biomed Anal VL - 30 IS - 4 N2 - A microcalorimetric method based on differential scanning calorimetry (DSC) of drug-additive binary systems to assess kneading-induced interactions was applied to naproxen (NAP) in combinations with amorphous hydroxypropyl beta-cyclodextrin (HPbetaCd), beta-cyclodextrin sulfobutyl ether, sodium salt ((SBE)(7m)-betaCd), acetyl beta-cyclodextrin (AcbetaCd) and acetyl gamma-cyclodextrin (AcgammaCd). Modifications of thermal parameters of NAP in DSC curves of physical mixtures indicate heating-induced interactions which resulted in a broadening of the NAP melting endotherm in the combinations with HPbetaCd, AcbetaCd and AcgammaCd. The effect of kneading on the interaction was particularly pronounced for the NAP-HPbetaCd and NAP-(SBE)(7m)-betaCd systems, which show a similar drug-to-carrier interaction ratio (1:2 by weight) as that of the other systems. Drug-to-carrier ratios, calculated considering the amount of NAP which recrystallizes from the melted mixtures equivalent to NAP not bound to the carrier, show a distinctly lower affinity in solid-state of the drug for the anionically charged (SBE)(7m)-betaCd with respect to other neutral carriers. The similar affinity of NAP for AcbetaCd and AcgammaCd demonstrates that the geometry of the cavity, which is a determinant factor for the inclusion complexation in liquid state, does not influence the interaction process in solid-state. SN - 0731-7085 UR - https://www.unboundmedicine.com/medline/citation/12408907/Assessment_of_solid_state_interactions_of_naproxen_with_amorphous_cyclodextrin_derivatives_by_DSC_ L2 - https://linkinghub.elsevier.com/retrieve/pii/S0731708502004211 DB - PRIME DP - Unbound Medicine ER -