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Effect of composition in the development of carbamazepine hot-melt extruded solid dispersions by application of mixture experimental design.
J Pharm Pharmacol. 2014 Feb; 66(2):232-43.JP

Abstract

OBJECTIVES

This study investigates the application of hot-melt extrusion for the formulation of carbamazepine (CBZ) solid dispersions, using polyethyleneglycol-polyvinyl caprolactam-polyvinyl acetate grafted copolymer (Soluplus, BASF, Germany) and polyoxyethylene-polyoxypropylene block copolymer (Poloxamer 407). In agreement with the current Quality by Design principle, formulations of solid dispersions were prepared according to a D-optimal mixture experimental design, and the influence of formulation composition on the properties of the dispersions (CBZ heat of fusion and release rate) was estimated.

METHODS

Prepared solid dispersions were characterized using differential scanning calorimetry, attenuated total reflectance infrared spectroscopy and hot stage microscopy, as well as by determination of the dissolution rate of CBZ from the hot-melt extrudates.

KEY FINDINGS

Solid dispersions of CBZ can be successfully prepared using the novel copolymer Soluplus. Inclusion of Poloxamer 407 as a plasticizer facilitated the processing and decreased the hardness of hot-melt extrudates. Regardless of their composition, all hot-melt extrudates displayed an improvement in the release rate compared to the pure CBZ, with formulations having the ratio of CBZ : Poloxamer 407 = 1 : 1 showing the highest increase in CBZ release rate.

CONCLUSIONS

Interactions between the mixture components (CBZ and polymers), or quadratic effects of the components, play a significant role in overall influence on the CBZ release rate.

Authors+Show Affiliations

Department of Pharmaceutical Technology and Cosmetology, Faculty of Pharmacy, University of Belgrade, Belgrade, Serbia.No 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

24350884

Citation

Djuris, Jelena, et al. "Effect of Composition in the Development of Carbamazepine Hot-melt Extruded Solid Dispersions By Application of Mixture Experimental Design." The Journal of Pharmacy and Pharmacology, vol. 66, no. 2, 2014, pp. 232-43.
Djuris J, Ioannis N, Ibric S, et al. Effect of composition in the development of carbamazepine hot-melt extruded solid dispersions by application of mixture experimental design. J Pharm Pharmacol. 2014;66(2):232-43.
Djuris, J., Ioannis, N., Ibric, S., Djuric, Z., & Kachrimanis, K. (2014). Effect of composition in the development of carbamazepine hot-melt extruded solid dispersions by application of mixture experimental design. The Journal of Pharmacy and Pharmacology, 66(2), 232-43. https://doi.org/10.1111/jphp.12199
Djuris J, et al. Effect of Composition in the Development of Carbamazepine Hot-melt Extruded Solid Dispersions By Application of Mixture Experimental Design. J Pharm Pharmacol. 2014;66(2):232-43. PubMed PMID: 24350884.
* Article titles in AMA citation format should be in sentence-case
TY - JOUR T1 - Effect of composition in the development of carbamazepine hot-melt extruded solid dispersions by application of mixture experimental design. AU - Djuris,Jelena, AU - Ioannis,Nikolakakis, AU - Ibric,Svetlana, AU - Djuric,Zorica, AU - Kachrimanis,Kyriakos, Y1 - 2013/12/18/ PY - 2013/06/17/received PY - 2013/11/16/accepted PY - 2013/12/20/entrez PY - 2013/12/20/pubmed PY - 2014/9/11/medline KW - Poloxamer 407 KW - Soluplus KW - carbamazepine KW - mixture design KW - solid dispersion SP - 232 EP - 43 JF - The Journal of pharmacy and pharmacology JO - J Pharm Pharmacol VL - 66 IS - 2 N2 - OBJECTIVES: This study investigates the application of hot-melt extrusion for the formulation of carbamazepine (CBZ) solid dispersions, using polyethyleneglycol-polyvinyl caprolactam-polyvinyl acetate grafted copolymer (Soluplus, BASF, Germany) and polyoxyethylene-polyoxypropylene block copolymer (Poloxamer 407). In agreement with the current Quality by Design principle, formulations of solid dispersions were prepared according to a D-optimal mixture experimental design, and the influence of formulation composition on the properties of the dispersions (CBZ heat of fusion and release rate) was estimated. METHODS: Prepared solid dispersions were characterized using differential scanning calorimetry, attenuated total reflectance infrared spectroscopy and hot stage microscopy, as well as by determination of the dissolution rate of CBZ from the hot-melt extrudates. KEY FINDINGS: Solid dispersions of CBZ can be successfully prepared using the novel copolymer Soluplus. Inclusion of Poloxamer 407 as a plasticizer facilitated the processing and decreased the hardness of hot-melt extrudates. Regardless of their composition, all hot-melt extrudates displayed an improvement in the release rate compared to the pure CBZ, with formulations having the ratio of CBZ : Poloxamer 407 = 1 : 1 showing the highest increase in CBZ release rate. CONCLUSIONS: Interactions between the mixture components (CBZ and polymers), or quadratic effects of the components, play a significant role in overall influence on the CBZ release rate. SN - 2042-7158 UR - https://www.unboundmedicine.com/medline/citation/24350884/Effect_of_composition_in_the_development_of_carbamazepine_hot_melt_extruded_solid_dispersions_by_application_of_mixture_experimental_design_ L2 - https://doi.org/10.1111/jphp.12199 DB - PRIME DP - Unbound Medicine ER -