Document Detail


In-vitro and in-vivo erosion profiles of hydroxypropylmethylcellulose (HPMC) matrix tablets.
MedLine Citation:
PMID:  20600400     Owner:  NLM     Status:  MEDLINE    
Abstract/OtherAbstract:
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.
Authors:
Manish Ghimire; Lee Ann Hodges; Janet Band; Bridget O'Mahony; Fiona J McInnes; Alexander B Mullen; Howard N E Stevens
Publication Detail:
Type:  Journal Article; Randomized Controlled Trial; Research Support, Non-U.S. Gov't     Date:  2010-06-23
Journal Detail:
Title:  Journal of controlled release : official journal of the Controlled Release Society     Volume:  147     ISSN:  1873-4995     ISO Abbreviation:  J Control Release     Publication Date:  2010 Oct 
Date Detail:
Created Date:  2010-09-13     Completed Date:  2011-02-02     Revised Date:  -    
Medline Journal Info:
Nlm Unique ID:  8607908     Medline TA:  J Control Release     Country:  Netherlands    
Other Details:
Languages:  eng     Pagination:  70-5     Citation Subset:  IM    
Copyright Information:
Copyright © 2010 Elsevier B.V. All rights reserved.
Affiliation:
Strathclyde Institute of Pharmacy and Biomedical Sciences, University of Strathclyde, Glasgow G4 0NR, UK. mghimire@colorcon.co.uk
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MeSH Terms
Descriptor/Qualifier:
Adult
Charcoal / chemistry
Cross-Over Studies
Delayed-Action Preparations / administration & dosage*,  chemistry,  pharmacokinetics
Drug Carriers / administration & dosage,  chemistry*,  pharmacokinetics
Drug Compounding
Humans
Lactose / administration & dosage,  analogs & derivatives*,  chemistry,  pharmacokinetics
Male
Methylcellulose / administration & dosage,  analogs & derivatives*,  chemistry,  pharmacokinetics
Radionuclide Imaging
Solubility
Tablets
Technetium Tc 99m Pentetate
Viscosity
Young Adult
Chemical
Reg. No./Substance:
0/Delayed-Action Preparations; 0/Drug Carriers; 0/Tablets; 0/hydroxypropylmethylcellulose-lactose matrix; 16291-96-6/Charcoal; 63-42-3/Lactose; 65454-61-7/Technetium Tc 99m Pentetate; 9004-67-5/Methylcellulose

From MEDLINE®/PubMed®, a database of the U.S. National Library of Medicine


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