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

Al Husban, Farhan; Perrie, Yvonne and Mohammed, Afzal R Formulation and characterisation of lyophilised rapid disintegrating tablets using amino acids as matrix forming agents. European Journal of Pharmaceutics and Biopharmaceutics, 75 (2), pp. 254-262.

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.

Publication DOI: https://doi.org/10.1016/j.ejpb.2010.03.012
Divisions: Life & Health Sciences > Pharmacy
Life & Health Sciences
Life & Health Sciences > Applied Health Research Group
Life & Health Sciences > Health Sciences
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Additional Information: Copyright 2010 Elsevier B.V. All rights reserved.
Uncontrolled Keywords: amino acids,crystallization,drug stability,excipients,freeze drying,porosity,tablets,temperature,time factors,transition temperature,wettability,Biotechnology,Pharmaceutical Science

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