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Content Provider | World Health Organization (WHO)-Global Index Medicus |
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Author | Itoh, Kunihiko Hatakeyama, Tomoaki Shimoyama, Tetsuya Miyazaki, Shozo D'Emanuele, Antony Attwood, David |
Description | Country affiliation: Japan Author Affiliation: Itoh K ( Faculty of Pharmaceutical Sciences, Health Sciences University of Hokkaido, Ishikari-Tobetsu, Hokkaido, Japan. itou@hoku-iryo-u.ac.jp) |
Abstract | BACKGROUND: Oral-sustained release gel formulations with suitable rheological properties have been proposed as a means of improving the compliance of dysphagic and geriatric patients who have difficulties with handling and swallowing oral dosage forms. AIM: We have modified the rheological and release properties of thermally reversible methylcellulose solutions by admixture with pectin, the gelation of which is ion-responsive, with the aim of formulating an in situ gelling vehicle suitable for oral-sustained drug delivery. METHOD: Gels formed by solutions containing methylcellulose (1.0-2.0%) and pectin (0.5-2.0%) were assessed for suitable gel strength, and in vitro and in vivo release of paracetamol. RESULTS: Addition of 1.5% pectin to a 2.0% methylcellulose formulation containing 20% d-sorbitol and calcium ions in complexed form increased the gel strength and provided a formulation with a suitable viscosity for ease of swallowing by dysphagic patients. Gels formed in situ after oral administration of this formulation retained their integrity in the rat stomach for sufficient time for sustained release to be achieved. In vitro release of paracetamol from methylcellulose, pectin, and methylcellulose/pectin gels was diffusion-controlled. Plasma levels of paracetamol after oral administration to rats (gastric pH 2.6 and 5.5) of a solution including 2.0% methylcellulose/1.5% pectin showed improved sustained release compared with that from both 2.0% methylcellulose and 1.5% pectin solutions. CONCLUSIONS: The addition of suitable concentrations of pectin to methylcellulose solutions produces in situ gelling formulations with suitable viscosity for administration to dysphagic patients and improved sustained release characteristics. |
File Format | HTM / HTML |
ISSN | 03639045 |
Issue Number | 7 |
Volume Number | 37 |
e-ISSN | 15205762 |
Journal | Drug Development and Industrial Pharmacy |
Language | English |
Publisher | Taylor & Francis |
Publisher Date | 2011-07-01 |
Publisher Place | Great Britain (UK) |
Access Restriction | Subscribed |
Subject Keyword | Discipline Pharmacology Deglutition Disorders Drug Therapy Delayed-action Preparations Administration & Dosage Drug Delivery Systems Methods Acetaminophen Pharmacokinetics Administration, Oral Animals Drug Compounding Gels Humans Male Methylcellulose Pectins Rats Rats, Wistar Rheology Stomach Metabolism Viscosity Journal Article Research Support, Non-u.s. Gov't |
Content Type | Text |
Resource Type | Article |
Subject Domain (in MeSH) | Digestive System Eukaryota Digestive System Diseases Organic Chemicals Macromolecular Substances Carbohydrates Complex Mixtures Pharmaceutical Preparations Therapeutics Investigative Techniques Chemical Phenomena |
Subject | Organic Chemistry Pharmaceutical Science Pharmacology Drug Discovery |
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