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In-vitro and in-vivo erosion profiles of hydroxypropylmethylcellulose (HPMC) matrix tablets.
J Control Release. 2010 Oct 01; 147(1):70-5.JC

Abstract

The purpose of this study was to evaluate and compare the in-vitro and in-vivo erosion profiles of two tablet formulations primarily consisting of hydroxypropylmethylcellulose (HPMC) and lactose. HPMC was used at concentrations below and above the reported values for polymer percolation threshold in controlled release matrix formulations: 20 and 40% (w/w) HPMC. In-vitro erosion behaviour was studied using traditional gravimetric and scintigraphic methods, with radiolabelled charcoal used as a marker to quantify erosion profiles in scintigraphic studies. Six healthy male subjects participated in a randomised crossover scintigraphic erosion study. Both in-vitro and in-vivo erosion profiles determined using the gravimetric and/or scintigraphic method for matrix tablets were dependent upon the concentration of HPMC, and erosion was faster for tablets containing 20% (w/w) HPMC than those containing 40% (w/w) HPMC. Good correlation was found between in-vitro gravimetric and scintigraphic erosion profiles for both tablets. Tablets containing 40% (w/w) HPMC (polymer level above percolation threshold) demonstrated robust in-vivo performance and showed stronger correlation with in-vitro erosion profiles. The study demonstrated that a matrix formulation with a lower concentration of HPMC and higher lactose concentration is more likely to perform poorly in the in-vivo environment.

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Authors+Show Affiliations

Ghimire M
Strathclyde Institute of Pharmacy and Biomedical Sciences, University of Strathclyde, Glasgow G4 0NR, UK. mghimire@colorcon.co.uk
Hodges LA
No affiliation info available
Band J
No affiliation info available
O'Mahony B
No affiliation info available
McInnes FJ
No affiliation info available
Mullen AB
No affiliation info available
Stevens HN
No affiliation info available

MeSH

AdultCharcoalCross-Over StudiesDelayed-Action PreparationsDrug CarriersDrug CompoundingHumansLactoseMaleMethylcelluloseRadionuclide ImagingSolubilityTabletsTechnetium Tc 99m PentetateViscosityYoung Adult

Pub Type(s)

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

Language

eng

PubMed ID

20600400

Citation

Ghimire, Manish, et al. "In-vitro and In-vivo Erosion Profiles of Hydroxypropylmethylcellulose (HPMC) Matrix Tablets." Journal of Controlled Release : Official Journal of the Controlled Release Society, vol. 147, no. 1, 2010, pp. 70-5.
Ghimire M, Hodges LA, Band J, et al. In-vitro and in-vivo erosion profiles of hydroxypropylmethylcellulose (HPMC) matrix tablets. J Control Release. 2010;147(1):70-5.
Ghimire, M., Hodges, L. A., Band, J., O'Mahony, B., McInnes, F. J., Mullen, A. B., & Stevens, H. N. (2010). In-vitro and in-vivo erosion profiles of hydroxypropylmethylcellulose (HPMC) matrix tablets. Journal of Controlled Release : Official Journal of the Controlled Release Society, 147(1), 70-5. https://doi.org/10.1016/j.jconrel.2010.06.015
Ghimire M, et al. In-vitro and In-vivo Erosion Profiles of Hydroxypropylmethylcellulose (HPMC) Matrix Tablets. J Control Release. 2010 Oct 1;147(1):70-5. PubMed PMID: 20600400.
* Article titles in AMA citation format should be in sentence-case
TY - JOUR T1 - In-vitro and in-vivo erosion profiles of hydroxypropylmethylcellulose (HPMC) matrix tablets. AU - Ghimire,Manish, AU - Hodges,Lee Ann, AU - Band,Janet, AU - O'Mahony,Bridget, AU - McInnes,Fiona J, AU - Mullen,Alexander B, AU - Stevens,Howard N E, Y1 - 2010/06/23/ PY - 2010/03/29/received PY - 2010/06/11/revised PY - 2010/06/17/accepted PY - 2010/7/6/entrez PY - 2010/7/6/pubmed PY - 2011/2/3/medline SP - 70 EP - 5 JF - Journal of controlled release : official journal of the Controlled Release Society JO - J Control Release VL - 147 IS - 1 N2 - The purpose of this study was to evaluate and compare the in-vitro and in-vivo erosion profiles of two tablet formulations primarily consisting of hydroxypropylmethylcellulose (HPMC) and lactose. HPMC was used at concentrations below and above the reported values for polymer percolation threshold in controlled release matrix formulations: 20 and 40% (w/w) HPMC. In-vitro erosion behaviour was studied using traditional gravimetric and scintigraphic methods, with radiolabelled charcoal used as a marker to quantify erosion profiles in scintigraphic studies. Six healthy male subjects participated in a randomised crossover scintigraphic erosion study. Both in-vitro and in-vivo erosion profiles determined using the gravimetric and/or scintigraphic method for matrix tablets were dependent upon the concentration of HPMC, and erosion was faster for tablets containing 20% (w/w) HPMC than those containing 40% (w/w) HPMC. Good correlation was found between in-vitro gravimetric and scintigraphic erosion profiles for both tablets. Tablets containing 40% (w/w) HPMC (polymer level above percolation threshold) demonstrated robust in-vivo performance and showed stronger correlation with in-vitro erosion profiles. The study demonstrated that a matrix formulation with a lower concentration of HPMC and higher lactose concentration is more likely to perform poorly in the in-vivo environment. SN - 1873-4995 UR - https://www.unboundmedicine.com/medline/citation/20600400/In_vitro_and_in_vivo_erosion_profiles_of_hydroxypropylmethylcellulose__HPMC__matrix_tablets_ L2 - https://linkinghub.elsevier.com/retrieve/pii/S0168-3659(10)00439-6 DB - PRIME DP - Unbound Medicine ER -