Preparation, optimisation and characterisation of lyophilised rapid disintegrating tablets based on gelatin and saccharide

Farhan AlHusban, Yvonne Perrie, Afzal R. Mohammed

Research output: Contribution to journalArticle

Abstract

Despite recent success, rapidly disintegrating lyophilized tablets still face problems of low mechanical strength and higher disintegration times resulting in poor patient compliance. The aim of the current work was to carry out a systematic study to understand the factors controlling mechanical properties of these formulations. The work investigated the influence of two bloom strengths of gelatin: low (60 bloom) and high (225 bloom) at different stock solution concentrations (2, 5, 7.5, and 10 %w/w). This was followed by investigation of addition of five saccharides (xylitol, glucose, trehalose, maltotriose and mannitol) at varied concentration range (10-80 %w/w) to decipher their influence on disintegration time, mechanical and thermal properties of the formulation. The results indicated that the disintegration time of the tablets dramatically decreased by decreasing the concentration and bloom strength of gelatin in the stock solution. However the mechanical properties of the tablets were mainly influenced by the concentration of gelatin rather than the bloom strength. The addition of saccharides resulted in enhancement of tablet properties and was concentration dependent. All the saccharides improved the fractubility of the tablets significantly at high concentration (equal or higher than 40% w/w). However, only high concentration (equal or higher than 40% w/w) of trehalose, maltotriose and mannitol significantly enhanced the hardness. Additionally, mannitol crytallised during freeze drying and consequently produced elegant tablets, whilst the other saccarides exhibited lyoprotectant activity as they were able to retain amorphous status. Based on the above findings, an optimized formulation was also successfully developed and characterized to deliver 100 microg dose of Clonidine HCl.
LanguageEnglish
Pages65-75
Number of pages11
JournalCurrent Drug Delivery
Volume7
Issue number1
Publication statusPublished - Jan 2010

Fingerprint

Gelatin
Tablets
Mannitol
Trehalose
Xylitol
Freeze Drying
Hardness
Clonidine
Patient Compliance
Hot Temperature
Glucose

Keywords

  • adrenergic alpha-agonists
  • differential scanning calorimetry
  • carbohydrates
  • pharmaceutical chemistry
  • high pressure liquid chromatography
  • clonidine
  • freeze drying
  • gelatin
  • hydrogen-ion concentration
  • materials testing
  • tablets
  • viscosity

Cite this

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abstract = "Despite recent success, rapidly disintegrating lyophilized tablets still face problems of low mechanical strength and higher disintegration times resulting in poor patient compliance. The aim of the current work was to carry out a systematic study to understand the factors controlling mechanical properties of these formulations. The work investigated the influence of two bloom strengths of gelatin: low (60 bloom) and high (225 bloom) at different stock solution concentrations (2, 5, 7.5, and 10 {\%}w/w). This was followed by investigation of addition of five saccharides (xylitol, glucose, trehalose, maltotriose and mannitol) at varied concentration range (10-80 {\%}w/w) to decipher their influence on disintegration time, mechanical and thermal properties of the formulation. The results indicated that the disintegration time of the tablets dramatically decreased by decreasing the concentration and bloom strength of gelatin in the stock solution. However the mechanical properties of the tablets were mainly influenced by the concentration of gelatin rather than the bloom strength. The addition of saccharides resulted in enhancement of tablet properties and was concentration dependent. All the saccharides improved the fractubility of the tablets significantly at high concentration (equal or higher than 40{\%} w/w). However, only high concentration (equal or higher than 40{\%} w/w) of trehalose, maltotriose and mannitol significantly enhanced the hardness. Additionally, mannitol crytallised during freeze drying and consequently produced elegant tablets, whilst the other saccarides exhibited lyoprotectant activity as they were able to retain amorphous status. Based on the above findings, an optimized formulation was also successfully developed and characterized to deliver 100 microg dose of Clonidine HCl.",
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Preparation, optimisation and characterisation of lyophilised rapid disintegrating tablets based on gelatin and saccharide. / AlHusban, Farhan; Perrie, Yvonne; Mohammed, Afzal R.

In: Current Drug Delivery, Vol. 7, No. 1, 01.2010, p. 65-75.

Research output: Contribution to journalArticle

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AU - Perrie, Yvonne

AU - Mohammed, Afzal R.

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KW - gelatin

KW - hydrogen-ion concentration

KW - materials testing

KW - tablets

KW - viscosity

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