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Physicochemical characterization of solid dispersions of carbamazepine formulated by supercritical carbon dioxide and conventional solvent evaporation method.
J Pharm Sci. 2002 Sep; 91(9):1948-57.JP

Abstract

Solid dispersions of carbamazepine (CBZ) were formulated by supercritical fluid processing (SCP) and conventional solvent evaporation in polyethylene glycol (PEG) 8000 with either Gelucire 44/14 or vitamin E TPGS NF (d-alpha-tocopheryl PEG 1000 succinate). Formulations were evaluated by dissolution, scanning electron microscopy, powder X-ray diffraction, and differential scanning calorimetry, and excipient cytotoxicity in Caco-2 cells by MTS [3-(4,5-dimethylthiazol-2-yl)-5-(3-carboxymethoxyphenyl)-2-(4-sulfophenyl)-2H-tetrazolium, inner salt] assay. CBZ release was enhanced from supercritical fluid-treated CBZ and the CBZ/PEG 8000 (1:5), CBZ/PEG 8000/TPGS or Gelucire 44/14 (1:4:1) solid dispersions. The radically altered morphologies of SCP samples seen by scanning electron microscopy suggested polymorphic change that was confirmed by the X-ray diffraction and differential scanning calorimetry. Disappearance of the characteristic CBZ melting peak indicated that CBZ was dissolved inside the carrier system. Polymorphic change of CBZ during SCP led to faster dissolution. Therefore, SCP provides advantages over solid dispersions prepared by conventional processes.

Authors+Show Affiliations

College of Pharmacy and Allied Health Professions, St. John's University, Jamaica, New York 11439, USA.No affiliation info available

Pub Type(s)

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

Language

eng

PubMed ID

12210042

Citation

Sethia, Sundeep, and Emilio Squillante. "Physicochemical Characterization of Solid Dispersions of Carbamazepine Formulated By Supercritical Carbon Dioxide and Conventional Solvent Evaporation Method." Journal of Pharmaceutical Sciences, vol. 91, no. 9, 2002, pp. 1948-57.
Sethia S, Squillante E. Physicochemical characterization of solid dispersions of carbamazepine formulated by supercritical carbon dioxide and conventional solvent evaporation method. J Pharm Sci. 2002;91(9):1948-57.
Sethia, S., & Squillante, E. (2002). Physicochemical characterization of solid dispersions of carbamazepine formulated by supercritical carbon dioxide and conventional solvent evaporation method. Journal of Pharmaceutical Sciences, 91(9), 1948-57.
Sethia S, Squillante E. Physicochemical Characterization of Solid Dispersions of Carbamazepine Formulated By Supercritical Carbon Dioxide and Conventional Solvent Evaporation Method. J Pharm Sci. 2002;91(9):1948-57. PubMed PMID: 12210042.
* Article titles in AMA citation format should be in sentence-case
TY - JOUR T1 - Physicochemical characterization of solid dispersions of carbamazepine formulated by supercritical carbon dioxide and conventional solvent evaporation method. AU - Sethia,Sundeep, AU - Squillante,Emilio, PY - 2002/9/5/pubmed PY - 2003/3/28/medline PY - 2002/9/5/entrez SP - 1948 EP - 57 JF - Journal of pharmaceutical sciences JO - J Pharm Sci VL - 91 IS - 9 N2 - Solid dispersions of carbamazepine (CBZ) were formulated by supercritical fluid processing (SCP) and conventional solvent evaporation in polyethylene glycol (PEG) 8000 with either Gelucire 44/14 or vitamin E TPGS NF (d-alpha-tocopheryl PEG 1000 succinate). Formulations were evaluated by dissolution, scanning electron microscopy, powder X-ray diffraction, and differential scanning calorimetry, and excipient cytotoxicity in Caco-2 cells by MTS [3-(4,5-dimethylthiazol-2-yl)-5-(3-carboxymethoxyphenyl)-2-(4-sulfophenyl)-2H-tetrazolium, inner salt] assay. CBZ release was enhanced from supercritical fluid-treated CBZ and the CBZ/PEG 8000 (1:5), CBZ/PEG 8000/TPGS or Gelucire 44/14 (1:4:1) solid dispersions. The radically altered morphologies of SCP samples seen by scanning electron microscopy suggested polymorphic change that was confirmed by the X-ray diffraction and differential scanning calorimetry. Disappearance of the characteristic CBZ melting peak indicated that CBZ was dissolved inside the carrier system. Polymorphic change of CBZ during SCP led to faster dissolution. Therefore, SCP provides advantages over solid dispersions prepared by conventional processes. SN - 0022-3549 UR - https://www.unboundmedicine.com/medline/citation/12210042/Physicochemical_characterization_of_solid_dispersions_of_carbamazepine_formulated_by_supercritical_carbon_dioxide_and_conventional_solvent_evaporation_method_ L2 - https://linkinghub.elsevier.com/retrieve/pii/S0022-3549(16)31076-0 DB - PRIME DP - Unbound Medicine ER -