Development and characterization of a gastroretentive dosage form composed of chitosan and hydroxyethyl cellulose for alendronate

Ying Chen Chen, Hsiu O. Ho, Chiao Chi Chiu, Ming Thau Sheu

Research output: Contribution to journalArticle

7 Citations (Scopus)

Abstract

In this study, alendronate, the most commonly used biphosphonate for treating osteoporosis, was formulated as gastroretentive dosage form (GRDF) tablets to enhance its oral bioavailability. GRDF tablets were characterized with the effects of different molecular weights (MWs) of chitosan (CS) and hydroxyethyl cellulose (HEC) at various ratios on swelling, floating, and physical integrity. The CS component was formed using various acids: acetic, lactic, malic, succinic, and citric, and a high viscosity grade of HEC was selected. The results demonstrated that the swelling ratios of the formulations comprising high MW CS were lower than those of low or medium MW CS when salts were formed with any countering acids except for acetic acid. The decreasing ranking of the swelling rates was: CS-citrate > CS-malate > CS-lactate > CS-succinate > CS-acetate. A negative correlation was found between the pKa of the respective countering acid and the swelling rate. The swelling rate was promoted if an acidic salt of CS with a lower water content was incorporated, while it became slower when tablet hardness was higher or the compression force to form tablets was increased. Although HEC did not contribute to swelling or floating, it played a role in maintaining structural integrity. A prolonged dissolution profile of alendronate GRDF tablets developed in this study was observed.

Original languageEnglish
Pages (from-to)67-78
Number of pages12
JournalDrug Design, Development and Therapy
Volume8
DOIs
Publication statusPublished - Dec 27 2013

Fingerprint

Alendronate
Dosage Forms
Chitosan
Cellulose
Tablets
Molecular Weight
Acetates
Salts
Acids
Hardness
Succinic Acid
Viscosity
Acetic Acid
Biological Availability
Osteoporosis
Lactic Acid
Milk
Water

Keywords

  • Alendronate
  • Chitosan
  • Gastroretentive dosage form
  • Hydrogel
  • Hydroxyethyl cellulose
  • Swelling

ASJC Scopus subject areas

  • Pharmaceutical Science
  • Pharmacology
  • Drug Discovery
  • Medicine(all)

Cite this

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abstract = "In this study, alendronate, the most commonly used biphosphonate for treating osteoporosis, was formulated as gastroretentive dosage form (GRDF) tablets to enhance its oral bioavailability. GRDF tablets were characterized with the effects of different molecular weights (MWs) of chitosan (CS) and hydroxyethyl cellulose (HEC) at various ratios on swelling, floating, and physical integrity. The CS component was formed using various acids: acetic, lactic, malic, succinic, and citric, and a high viscosity grade of HEC was selected. The results demonstrated that the swelling ratios of the formulations comprising high MW CS were lower than those of low or medium MW CS when salts were formed with any countering acids except for acetic acid. The decreasing ranking of the swelling rates was: CS-citrate > CS-malate > CS-lactate > CS-succinate > CS-acetate. A negative correlation was found between the pKa of the respective countering acid and the swelling rate. The swelling rate was promoted if an acidic salt of CS with a lower water content was incorporated, while it became slower when tablet hardness was higher or the compression force to form tablets was increased. Although HEC did not contribute to swelling or floating, it played a role in maintaining structural integrity. A prolonged dissolution profile of alendronate GRDF tablets developed in this study was observed.",
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AU - Sheu, Ming Thau

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