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Estimation of the percolation thresholds in lobenzarit disodium native dextran matrix tablets.
AAPS PharmSciTech. 2007 Dec 28; 8(4):E115.AP

Abstract

The objective of the present work is to estimate for the first time the percolation threshold of a new series of dextran (native dextran of high molecular weight [B110-1-2, Mw = 2 x 10(6)]), in matrices of lobenzarit disodium (LBD) and to apply the obtained result to the design of hydrophilic matrices for the controlled delivery of this drug. The formulations studied were prepared with different amounts of excipient in the range of 20% to 70% wt/wt. Dissolution studies were performed using the paddle method (100 rpm) and one face water uptake measurements were performed using a modified Enslin apparatus. The Higuchi, zero-order, and Hixson-Crowell models as well as the nonlinear regression model were employed as empiric methods to study the release data. Values of diffusion exponent 0.563 < n < 0.786 (Korsmeyer equation) for dissolution profile and water uptake mechanism 0.715 < n < 1 (Davidson and Peppas equation) suggested anomalous or complex mechanisms. On the other hand, the contribution of the relaxation or erosion and of the diffusive mechanism in Peppas-Sahlin equation indicated that the main mechanism for drug delivery from tablets is swelling controlled delivery (K(r)/K(d) < 1). The critical points observed in kinetic parameters above 58.63% vol/vol of native dextran B110-1-2 plus initial porosity in the LBD-dextran matrices with a relative polymer/drug particle size of 4.17 were attributed to the existence of an excipient percolation threshold.

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Authors+Show Affiliations

Gil EC
Center of Pharmaceutical Chemistry, Calle 200, esq 21, Atabey, Playa, Havana, Cuba. eddy02cu@yahoo.es
Colarte AI
No affiliation info available
Bataille B
No affiliation info available
Caraballo I
No affiliation info available

MeSH

Antirheumatic AgentsChemistry, PharmaceuticalDelayed-Action PreparationsDextransDiffusionDrug CompoundingExcipientsKineticsModels, ChemicalModels, StatisticalMolecular WeightParticle SizePorosityResearch DesignSolubilityTabletsTechnology, PharmaceuticalWaterortho-Aminobenzoates

Pub Type(s)

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

Language

eng

PubMed ID

18181536

Citation

Gil, Eddy Castellanos, et al. "Estimation of the Percolation Thresholds in Lobenzarit Disodium Native Dextran Matrix Tablets." AAPS PharmSciTech, vol. 8, no. 4, 2007, pp. E115.
Gil EC, Colarte AI, Bataille B, et al. Estimation of the percolation thresholds in lobenzarit disodium native dextran matrix tablets. AAPS PharmSciTech. 2007;8(4):E115.
Gil, E. C., Colarte, A. I., Bataille, B., & Caraballo, I. (2007). Estimation of the percolation thresholds in lobenzarit disodium native dextran matrix tablets. AAPS PharmSciTech, 8(4), E115. https://doi.org/10.1208/pt0804115
Gil EC, et al. Estimation of the Percolation Thresholds in Lobenzarit Disodium Native Dextran Matrix Tablets. AAPS PharmSciTech. 2007 Dec 28;8(4):E115. PubMed PMID: 18181536.
* Article titles in AMA citation format should be in sentence-case
TY - JOUR T1 - Estimation of the percolation thresholds in lobenzarit disodium native dextran matrix tablets. AU - Gil,Eddy Castellanos, AU - Colarte,Antonio Iraizoz, AU - Bataille,Bernard, AU - Caraballo,Isidoro, Y1 - 2007/12/28/ PY - 2008/1/10/pubmed PY - 2008/1/25/medline PY - 2008/1/10/entrez SP - E115 EP - E115 JF - AAPS PharmSciTech JO - AAPS PharmSciTech VL - 8 IS - 4 N2 - The objective of the present work is to estimate for the first time the percolation threshold of a new series of dextran (native dextran of high molecular weight [B110-1-2, Mw = 2 x 10(6)]), in matrices of lobenzarit disodium (LBD) and to apply the obtained result to the design of hydrophilic matrices for the controlled delivery of this drug. The formulations studied were prepared with different amounts of excipient in the range of 20% to 70% wt/wt. Dissolution studies were performed using the paddle method (100 rpm) and one face water uptake measurements were performed using a modified Enslin apparatus. The Higuchi, zero-order, and Hixson-Crowell models as well as the nonlinear regression model were employed as empiric methods to study the release data. Values of diffusion exponent 0.563 < n < 0.786 (Korsmeyer equation) for dissolution profile and water uptake mechanism 0.715 < n < 1 (Davidson and Peppas equation) suggested anomalous or complex mechanisms. On the other hand, the contribution of the relaxation or erosion and of the diffusive mechanism in Peppas-Sahlin equation indicated that the main mechanism for drug delivery from tablets is swelling controlled delivery (K(r)/K(d) < 1). The critical points observed in kinetic parameters above 58.63% vol/vol of native dextran B110-1-2 plus initial porosity in the LBD-dextran matrices with a relative polymer/drug particle size of 4.17 were attributed to the existence of an excipient percolation threshold. SN - 1530-9932 UR - https://www.unboundmedicine.com/medline/citation/18181536/Estimation_of_the_percolation_thresholds_in_lobenzarit_disodium_native_dextran_matrix_tablets_ DB - PRIME DP - Unbound Medicine ER -