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Polymer percolation threshold in HPMC extended release formulation of carbamazepine and verapamil HCl.
AAPS PharmSciTech. 2010 Jun; 11(2):558-62.AP

Abstract

The principles of the percolation theory were applied to further understand and design hydroxypropyl methylcellulose (HPMC) extended release matrix tablets containing carbamazepine and verapamil HCl. This statistical theory studies disordered or chaotic systems where the components are randomly distributed in a lattice. The application of this theory to study the hydration and drug release of hydrophilic matrices allows describing the changes in hydration and drug release kinetics of swellable matrices. The aim of this work was to study and develop extended release matrix formulations for carbamazepine and verapamil HCl, containing hypromellose (HPMC, METHOCEL Premium K100M CR) as rate controlling polymer using the concepts of percolation theory. The knowledge of the percolation threshold of the components of the matrix formulations contributes to improve their design. First, reducing the time to market and second, avoiding to formulate in the nearby of the percolation threshold, which will result in a lower variability. Therefore these formulations will be more robust when they are prepared at industrial scale. The HPMC percolation threshold for drugs with very different water solubilities was determined and it was shown that there was no significant influence of drug solubility on the HPMC critical concentration threshold (excipient percolation threshold). This may be related to the versatility and broad functionality of the swelling hydrophilic matrices.

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Authors+Show Affiliations

Gonçalves-Araújo T
Department of Pharmacy and Pharmaceutical Technology, Faculty of Pharmacy, University of Seville, Seville, Spain. tamara@ufc.br
Rajabi-Siahboomi AR
No affiliation info available
Caraballo I
No affiliation info available

MeSH

Analgesics, Non-NarcoticAnti-Arrhythmia AgentsCarbamazepineCombinatorial Chemistry TechniquesComputer SimulationData Interpretation, StatisticalDelayed-Action PreparationsDiffusionDrug CombinationsDrug DesignLactoseMethylcelluloseModels, ChemicalModels, StatisticalPolymersVerapamil

Pub Type(s)

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

Language

eng

PubMed ID

20352536

Citation

Gonçalves-Araújo, Tamara, et al. "Polymer Percolation Threshold in HPMC Extended Release Formulation of Carbamazepine and Verapamil HCl." AAPS PharmSciTech, vol. 11, no. 2, 2010, pp. 558-62.
Gonçalves-Araújo T, Rajabi-Siahboomi AR, Caraballo I. Polymer percolation threshold in HPMC extended release formulation of carbamazepine and verapamil HCl. AAPS PharmSciTech. 2010;11(2):558-62.
Gonçalves-Araújo, T., Rajabi-Siahboomi, A. R., & Caraballo, I. (2010). Polymer percolation threshold in HPMC extended release formulation of carbamazepine and verapamil HCl. AAPS PharmSciTech, 11(2), 558-62. https://doi.org/10.1208/s12249-010-9408-x
Gonçalves-Araújo T, Rajabi-Siahboomi AR, Caraballo I. Polymer Percolation Threshold in HPMC Extended Release Formulation of Carbamazepine and Verapamil HCl. AAPS PharmSciTech. 2010;11(2):558-62. PubMed PMID: 20352536.
* Article titles in AMA citation format should be in sentence-case
TY - JOUR T1 - Polymer percolation threshold in HPMC extended release formulation of carbamazepine and verapamil HCl. AU - Gonçalves-Araújo,Tamara, AU - Rajabi-Siahboomi,Ali R, AU - Caraballo,Isidoro, Y1 - 2010/03/30/ PY - 2009/10/26/received PY - 2010/02/19/accepted PY - 2010/3/31/entrez PY - 2010/3/31/pubmed PY - 2010/10/12/medline SP - 558 EP - 62 JF - AAPS PharmSciTech JO - AAPS PharmSciTech VL - 11 IS - 2 N2 - The principles of the percolation theory were applied to further understand and design hydroxypropyl methylcellulose (HPMC) extended release matrix tablets containing carbamazepine and verapamil HCl. This statistical theory studies disordered or chaotic systems where the components are randomly distributed in a lattice. The application of this theory to study the hydration and drug release of hydrophilic matrices allows describing the changes in hydration and drug release kinetics of swellable matrices. The aim of this work was to study and develop extended release matrix formulations for carbamazepine and verapamil HCl, containing hypromellose (HPMC, METHOCEL Premium K100M CR) as rate controlling polymer using the concepts of percolation theory. The knowledge of the percolation threshold of the components of the matrix formulations contributes to improve their design. First, reducing the time to market and second, avoiding to formulate in the nearby of the percolation threshold, which will result in a lower variability. Therefore these formulations will be more robust when they are prepared at industrial scale. The HPMC percolation threshold for drugs with very different water solubilities was determined and it was shown that there was no significant influence of drug solubility on the HPMC critical concentration threshold (excipient percolation threshold). This may be related to the versatility and broad functionality of the swelling hydrophilic matrices. SN - 1530-9932 UR - https://www.unboundmedicine.com/medline/citation/20352536/Polymer_percolation_threshold_in_HPMC_extended_release_formulation_of_carbamazepine_and_verapamil_HCl_ L2 - https://dx.doi.org/10.1208/s12249-010-9408-x DB - PRIME DP - Unbound Medicine ER -