Formulation and characterisation of lyophilised rapid disintegrating tablets using amino acids as matrix forming agents

Farhan Al Husban, Yvonne Perrie, Afzal R Mohammed

Research output: Contribution to journalArticle

Abstract

Despite recent advances in the formulation of lyophilised rapid disintegrating tablets (RDTs), the inclusion of matrix supporting/disintegration enhancing agents has been limited to the use of saccharides and polyols. In this study, the feasibility of using amino acids as matrix forming agents in lyophilised RDTs was investigated. Twelve amino acids were chosen (alanine, arginine, threonine, glycine, cysteine, serine, histidine, lysine, valine, asparagine, glutamine and proline), and the suitability for freeze drying, mechanical properties and disintegration time after inclusion of the amino acids at varied concentration were studied. In addition, the porosity of the RDTs and wettability profile of the amino acids were investigated to understand the mechanisms of disintegration. The results suggest the suitability of these amino acids for the lyophilisation regime, as they displayed satisfactory safety margin between the glass transition and shelf temperature (-40 degrees C), except proline-based formulations. Moreover, the crystallisation behavior of alanine, glycine, cysteine and serine at high concentration increased the stability of the formulation. The characterisation of the RDTs suggests that high concentration of the amino acids is required to enhance the mechanical properties, whereas only optimum concentrations promote the disintegration. Moreover, wetting time of the amino acid and porosity of the tablet are the two factors that control the disintegration of RDTs.
LanguageEnglish
Pages254-262
Number of pages9
JournalEuropean Journal of Pharmaceutics and Biopharmaceutics
Volume75
Issue number2
Early online date21 Mar 2010
DOIs
Publication statusPublished - Jun 2010

Fingerprint

Tablets
Amino Acids
Freeze Drying
Porosity
Proline
Alanine
Glycine
Serine
Cysteine
Wettability
Transition Temperature
Asparagine
Valine
Threonine
Crystallization
Glutamine
Histidine
Lysine
Glass
Arginine

Keywords

  • amino acids
  • crystallization
  • drug stability
  • excipients
  • freeze drying
  • porosity
  • tablets
  • temperature
  • time factors
  • transition temperature
  • wettability

Cite this

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abstract = "Despite recent advances in the formulation of lyophilised rapid disintegrating tablets (RDTs), the inclusion of matrix supporting/disintegration enhancing agents has been limited to the use of saccharides and polyols. In this study, the feasibility of using amino acids as matrix forming agents in lyophilised RDTs was investigated. Twelve amino acids were chosen (alanine, arginine, threonine, glycine, cysteine, serine, histidine, lysine, valine, asparagine, glutamine and proline), and the suitability for freeze drying, mechanical properties and disintegration time after inclusion of the amino acids at varied concentration were studied. In addition, the porosity of the RDTs and wettability profile of the amino acids were investigated to understand the mechanisms of disintegration. The results suggest the suitability of these amino acids for the lyophilisation regime, as they displayed satisfactory safety margin between the glass transition and shelf temperature (-40 degrees C), except proline-based formulations. Moreover, the crystallisation behavior of alanine, glycine, cysteine and serine at high concentration increased the stability of the formulation. The characterisation of the RDTs suggests that high concentration of the amino acids is required to enhance the mechanical properties, whereas only optimum concentrations promote the disintegration. Moreover, wetting time of the amino acid and porosity of the tablet are the two factors that control the disintegration of RDTs.",
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Formulation and characterisation of lyophilised rapid disintegrating tablets using amino acids as matrix forming agents. / Al Husban, Farhan; Perrie, Yvonne; Mohammed, Afzal R.

In: European Journal of Pharmaceutics and Biopharmaceutics, Vol. 75, No. 2, 06.2010, p. 254-262.

Research output: Contribution to journalArticle

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AU - Al Husban, Farhan

AU - Perrie, Yvonne

AU - Mohammed, Afzal R

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