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Evaluation of hydroxypropyl methylcellulose matrix systems as swellable gastro-retentive drug delivery systems (GRDDS).
J Pharm Sci. 2011 Jan; 100(1):150-63.JP

Abstract

Utilizing gastro-retentive drug delivery systems (GRDDS) to increase absorption of weakly basic drugs by extending their transit time is a promising approach. Swellable systems were evaluated for this purpose. Such systems demonstrate dual mechanism of release-diffusion and erosion. GRDDS requires maintaining its dimensions, which demands diffusion as a predominant mechanism of release (Fickian). In this work, dypyridamole, a weakly basic drug, together with various grades of hydroxypropyl methylcellulose and different excipients were evaluated for release and swelling properties. Dissolution data were analyzed by curve fitting to various models to estimate predominant release mechanism. It was found that matrices containing a swellable diluent like microcrystalline cellulose demonstrated predominantly Fickian mechanism of release, whereas soluble diluents (lactose and mannitol) contributed to a mixed mechanism of release. Addition of copovidone increased the swelling and survivability, whereas sodium chloride altered the erosion behavior. A correlation between matrix weight loss and drug release was obtained, which further consolidated the analysis. Correlation for the soluble excipients was linear, whereas that for the swellable excipient was nonlinear, implying predominance of Fickian release mechanism for the latter. Hence, the selection of excipients can influence matrix survivability and release kinetics, which can be used for developing GRDDS.

Links

Publisher Full Text
linkinghub.elsevier.com
onlinelibrary.wiley.com

Authors+Show Affiliations

Matharu AS
Division of Pharmaceutical Sciences, Arnold & Marie Schwartz College of Pharmacy and Health Sciences, Long Island University, Brooklyn, New York 11201, USA.
Motto MG
No affiliation info available
Patel MR
No affiliation info available
Simonelli AP
No affiliation info available
Dave RH
No affiliation info available

MeSH

AcetatesAlgorithmsCelluloseChemistry, PharmaceuticalDelayed-Action PreparationsDiffusionDipyridamoleDrug Delivery SystemsExcipientsGastrointestinal TransitHydrogen-Ion ConcentrationHypromellose DerivativesKineticsMethylcelluloseModels, ChemicalPovidoneSolubilityTabletsWater

Pub Type(s)

Comparative Study
Journal Article

Language

eng

PubMed ID

20572054

Citation

Matharu, Amol S., et al. "Evaluation of Hydroxypropyl Methylcellulose Matrix Systems as Swellable Gastro-retentive Drug Delivery Systems (GRDDS)." Journal of Pharmaceutical Sciences, vol. 100, no. 1, 2011, pp. 150-63.
Matharu AS, Motto MG, Patel MR, et al. Evaluation of hydroxypropyl methylcellulose matrix systems as swellable gastro-retentive drug delivery systems (GRDDS). J Pharm Sci. 2011;100(1):150-63.
Matharu, A. S., Motto, M. G., Patel, M. R., Simonelli, A. P., & Dave, R. H. (2011). Evaluation of hydroxypropyl methylcellulose matrix systems as swellable gastro-retentive drug delivery systems (GRDDS). Journal of Pharmaceutical Sciences, 100(1), 150-63. https://doi.org/10.1002/jps.22252
Matharu AS, et al. Evaluation of Hydroxypropyl Methylcellulose Matrix Systems as Swellable Gastro-retentive Drug Delivery Systems (GRDDS). J Pharm Sci. 2011;100(1):150-63. PubMed PMID: 20572054.
* Article titles in AMA citation format should be in sentence-case
TY - JOUR T1 - Evaluation of hydroxypropyl methylcellulose matrix systems as swellable gastro-retentive drug delivery systems (GRDDS). AU - Matharu,Amol S, AU - Motto,Michael G, AU - Patel,Mahendra R, AU - Simonelli,Anthony P, AU - Dave,Rutesh H, Y1 - 2010/06/22/ PY - 2009/12/04/received PY - 2010/04/21/revised PY - 2010/04/22/accepted PY - 2010/6/24/entrez PY - 2010/6/24/pubmed PY - 2011/4/1/medline SP - 150 EP - 63 JF - Journal of pharmaceutical sciences JO - J Pharm Sci VL - 100 IS - 1 N2 - Utilizing gastro-retentive drug delivery systems (GRDDS) to increase absorption of weakly basic drugs by extending their transit time is a promising approach. Swellable systems were evaluated for this purpose. Such systems demonstrate dual mechanism of release-diffusion and erosion. GRDDS requires maintaining its dimensions, which demands diffusion as a predominant mechanism of release (Fickian). In this work, dypyridamole, a weakly basic drug, together with various grades of hydroxypropyl methylcellulose and different excipients were evaluated for release and swelling properties. Dissolution data were analyzed by curve fitting to various models to estimate predominant release mechanism. It was found that matrices containing a swellable diluent like microcrystalline cellulose demonstrated predominantly Fickian mechanism of release, whereas soluble diluents (lactose and mannitol) contributed to a mixed mechanism of release. Addition of copovidone increased the swelling and survivability, whereas sodium chloride altered the erosion behavior. A correlation between matrix weight loss and drug release was obtained, which further consolidated the analysis. Correlation for the soluble excipients was linear, whereas that for the swellable excipient was nonlinear, implying predominance of Fickian release mechanism for the latter. Hence, the selection of excipients can influence matrix survivability and release kinetics, which can be used for developing GRDDS. SN - 1520-6017 UR - https://www.unboundmedicine.com/medline/citation/20572054/Evaluation_of_hydroxypropyl_methylcellulose_matrix_systems_as_swellable_gastro_retentive_drug_delivery_systems__GRDDS__ L2 - https://linkinghub.elsevier.com/retrieve/pii/S0022-3549(15)32332-7 DB - PRIME DP - Unbound Medicine ER -