PREPARATION AND IN VITRO EVALUATION OF CYCLODEXTRIN BASED EFFERVESCENT AND DISPERSIBLE GRANULES OF CARBAMAZEPINE
Objective: Carbamazepine is typically used for the treatment of seizure disorders and neuropathic pain. One of the major problems with this drug is its low solubility in water; therefore the objective of this study was to enhance the solubility of carbamazepine by complexation with cyclodextrin to be formulated as effervescent and dispersible granules.
Methods: Solvent evaporation method was used to prepare, binary (Carbamazepine/Î²-cyclodextrin) complex and ternary (Carbamazepine/Î²-cyclodextrin/hydroxypropyl methyl cellulose (HPMC E5). The more soluble complex will be further formulated as unit dose effervescent and dispersible granules. The complexes were evaluated for their solubility, drug content, percentage practical yield and differential scanning calorimetery (DSC) to confirm the formation of the complex.
Results: The ratio of effervescent components, amount of effervescent base, amount of croscarmellose sodium (superdisintegrant) within the formula were found to play a role in the percentage of drug dissolved. Among the all prepared formulas, the effervescent granules containing ternary complex equivalent to 200 or 100 carbamazepine with effervescent base of 1:2:3.4 citric acid: tartaric acid: sodium bicarbonate not less than 48% w/w and 3% w/w croscarmellose sodium within the formula may be considered as a promising formulas regarding the amount of drug dissolved within 5 min.
Conclusion: The solubility of carbamazepine was enhanced by complexation with Î²-cyclodextrin and HPMC E5 as a ternary complex. Hence effervescent and dispersible granules of carbamazepine with good flow properties can be successfully prepared by using this complex.
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