Preparation and in Vitro Evaluation of Cyclodextrin Based Effervescent and Dispersible Granules of Carbamazepine

Abstract

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/β-cyclodextrin) complex and ternary (Carbamazepine/β-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 β-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.

Preparation and evaluation of a functional effervescent powder based on inclusion complexes of orange oil and β-cyclodextrin derivatives

“…Compressibility is the ability of a powder to decrease in volume under pressure. It is a simple, fast, and accurate method for predicting the powder ow characteristics [25]. Carr's index of the effervescent powder was calculated from Eq.…”

“…The owability of the selected orange avoured effervescent powder was assessed by measuring the angle of repose by a xed funnel method according to Hussain and Al-khedairy [25]. The angle of repose (θ) of the conical piles produced by allowing the sample ow through a funnel and fall freely onto a surface was calculated according to Eq.…”

“…3.5 were used for the formulation of the effervescent powder [24,25]. Each formula was dissolved in 50 mL distilled water and investigated regarding their effect on effervescent time, clarity and pH of the obtained solutions.…”

Hot liquid extrusion assisted drug-cyclodextrin complexation: a novel continuous manufacturing method for solubility and bioavailability enhancement of drugs

“…Conventionally, various methods such as physical blending [16], co-precipitation [17], spray-drying [18], freeze-drying [19], kneading [20], and solvent evaporation [15,21] have been used to form drug-CD complexes. The potential of CBZ-CD complexes in increasing the solubility and dissolution rate of CBZ has been well documented.…”

“…Previously, different carrier systems containing CBZ have been formulated in a bid to improve its dissolution and bioavailability, among which complexation with HP-β-CD showed the highest extent of absorption [ 15 ]. Conventionally, various methods such as physical blending [ 16 ], co-precipitation [ 17 ], spray-drying [ 18 ], freeze-drying [ 19 ], kneading [ 20 ], and solvent evaporation [ 15 , 21 ] have been used to form drug-CD complexes. The potential of CBZ-CD complexes in increasing the solubility and dissolution rate of CBZ has been well documented.…”