In situ cross-linking of sodium alginate with calcium and aluminum ions to sustain the release of theophylline from polymeric matrices.
Small matrices of calcium alginate or aluminium alginate have been investigated as possible controlled release systems for drugs. The objective of the present study was to sustain the release of theophylline from alginate matrices using different concentrations of aluminium chloride and calcium chloride in presence and absence of HPMC. Tablets containing differing concentrations of aluminium and calcium chloride were produced and the release rate of theophylline was tested using the basket dissolution apparatus over 8 h. Increasing amounts of aluminium chloride from 0.0001 to 0.00068 moles decreased the release of theophylline from 95.1 +/- 0.27 to 29.5 +/- 1.5, indicating a significant effect of aluminium ions on a reduction in the release rate of theophylline from sodium alginate matrices. In the case of matrices containing different concentrations of calcium ions, as the concentration of calcium chloride increased, the release rate increased to an optimum then declined after this. This was due to insufficient calcium ions being available to cross-link with the sodium alginate to form an insoluble gel. The effect of aluminium ions, as this is a trivalent ion compared to calcium, which is a divalent ion, aluminium ions are able to decrease the release rate with a smaller concentration compared to calcium ions. The results also showed that the presence of HPMC caused a reduction in release rate of theophylline from alginate matrices containing calcium chloride. Whereas, in the case of alginate matrices containing aluminium chloride the release rate of theophylline increased in presence of HPMC. For comparing the dissolution data, dissolution efficiency (DE) was used. The values of DE are consistent with the dissolution data. The results show that within a formulation series, DE values generally decrease when the cation concentration increases and this criterion can be used to describe the effect of calcium and aluminium ions on the release behaviour of theophylline from polymeric matrices.
Nokhodchi
Ali
A
Pharmacy Department, Kings College London, 150 Stamford Street, Franklin-Wilkins Building, London SE1 9NN, UK. ali.nokhodchi@kcl.ac.uk
Tailor
Anish
A
D000464:Alginates / Q000737:chemistry / Q000493:pharmacokinetics*; D000535:Aluminum / Q000737:chemistry / Q000493:pharmacokinetics; D002118:Calcium / Q000737:chemistry / Q000493:pharmacokinetics; D003432:Cross-Linking Reagents / Q000737:chemistry / Q000493:pharmacokinetics*; D003692:Delayed-Action Preparations / Q000737:chemistry / Q000493:pharmacokinetics; D020723:Glucuronic Acid / Q000737:chemistry / Q000493:pharmacokinetics*; D006603:Hexuronic Acids / Q000737:chemistry / Q000493:pharmacokinetics*; D011108:Polymers / Q000737:chemistry / Q000493:pharmacokinetics*; D012995:Solubility; D013806:Theophylline / Q000737:chemistry / Q000493:pharmacokinetics*
D000464:Alginates; D003432:Cross-Linking Reagents; D003692:Delayed-Action Preparations; D006603:Hexuronic Acids; D011108:Polymers; D020723:Glucuronic Acid; D013806:Theophylline; D000535:Aluminum; D002118:Calcium