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Physicochemical characterization of solid dispersions of three antiepileptic drugs prepared by solvent evaporation method.
J Pharm Pharmacol. 2007 May; 59(5):645-53.JP

Abstract

We have investigated the solid dispersion and dissolution profiles of three antiepileptic drugs (carbamazepine (CBZ), oxcarbazepine (OXC) and rufinamide (RFN)) with different aqueous solubilities, prepared by the solvent evaporation method. Solid dispersions of the three drugs in hydroxy-propylmethylcellulose (HPMC), with drug:polymer ratios of 1:4, were prepared and characterized by differential scanning calorimetry (DSC), Fourier transformation infrared (FTIR) spectroscopy, X-ray diffraction (XRD) and scanning electron microscopy. The release mechanism was also investigated and the kinetic order of the solid dispersions was evaluated. It appeared that the dissolution behaviour depended on the physicochemical properties of the drug and drug-polymer interactions. DSC thermographs showed amorphous forms for all drugs confirmed by XRD patterns. The FTIR spectra of CBZ and OXC demonstrated drug interactions with HPMC through hydrogen polymer bonds. Thus, solid dispersions of these drugs had an improved dissolution profile. In contrast, solid dispersions of RUF showed modest enhancement of dissolution, suggesting negligible drug-polymer interactions. The different dissolution behaviour is attributed to the extent of interactions between the polymer hydroxyl group and the drug amide groups.

Authors+Show Affiliations

Phoqus Pharmaceutical Ltd, 10 Kings Hill Avenue, Kings Hill, West Malling, ME19 4PQ, Kent, UK. dionysios.douroumis@phoqus.comNo affiliation info availableNo affiliation info available

Pub Type(s)

Journal Article

Language

eng

PubMed ID

17524229

Citation

Douroumis, Dionysios, et al. "Physicochemical Characterization of Solid Dispersions of Three Antiepileptic Drugs Prepared By Solvent Evaporation Method." The Journal of Pharmacy and Pharmacology, vol. 59, no. 5, 2007, pp. 645-53.
Douroumis D, Bouropoulos N, Fahr A. Physicochemical characterization of solid dispersions of three antiepileptic drugs prepared by solvent evaporation method. J Pharm Pharmacol. 2007;59(5):645-53.
Douroumis, D., Bouropoulos, N., & Fahr, A. (2007). Physicochemical characterization of solid dispersions of three antiepileptic drugs prepared by solvent evaporation method. The Journal of Pharmacy and Pharmacology, 59(5), 645-53.
Douroumis D, Bouropoulos N, Fahr A. Physicochemical Characterization of Solid Dispersions of Three Antiepileptic Drugs Prepared By Solvent Evaporation Method. J Pharm Pharmacol. 2007;59(5):645-53. PubMed PMID: 17524229.
* Article titles in AMA citation format should be in sentence-case
TY - JOUR T1 - Physicochemical characterization of solid dispersions of three antiepileptic drugs prepared by solvent evaporation method. AU - Douroumis,Dionysios, AU - Bouropoulos,Nikolaos, AU - Fahr,Alfred, PY - 2007/5/26/pubmed PY - 2007/7/24/medline PY - 2007/5/26/entrez SP - 645 EP - 53 JF - The Journal of pharmacy and pharmacology JO - J. Pharm. Pharmacol. VL - 59 IS - 5 N2 - We have investigated the solid dispersion and dissolution profiles of three antiepileptic drugs (carbamazepine (CBZ), oxcarbazepine (OXC) and rufinamide (RFN)) with different aqueous solubilities, prepared by the solvent evaporation method. Solid dispersions of the three drugs in hydroxy-propylmethylcellulose (HPMC), with drug:polymer ratios of 1:4, were prepared and characterized by differential scanning calorimetry (DSC), Fourier transformation infrared (FTIR) spectroscopy, X-ray diffraction (XRD) and scanning electron microscopy. The release mechanism was also investigated and the kinetic order of the solid dispersions was evaluated. It appeared that the dissolution behaviour depended on the physicochemical properties of the drug and drug-polymer interactions. DSC thermographs showed amorphous forms for all drugs confirmed by XRD patterns. The FTIR spectra of CBZ and OXC demonstrated drug interactions with HPMC through hydrogen polymer bonds. Thus, solid dispersions of these drugs had an improved dissolution profile. In contrast, solid dispersions of RUF showed modest enhancement of dissolution, suggesting negligible drug-polymer interactions. The different dissolution behaviour is attributed to the extent of interactions between the polymer hydroxyl group and the drug amide groups. SN - 0022-3573 UR - https://www.unboundmedicine.com/medline/citation/17524229/Physicochemical_characterization_of_solid_dispersions_of_three_antiepileptic_drugs_prepared_by_solvent_evaporation_method_ L2 - https://doi.org/10.1211/jpp.59.5.0004 DB - PRIME DP - Unbound Medicine ER -