Studies to enhance dissolution properties of carbamazepine

Abstract

Carbamazepine a dibenzapine derivative with structural resembling to the tricyclic antidepressant, it is used to control some types of seizures in the treatment of epilepsy. It is also used to relieve pain due to trigeminal neuralgia. One of the major problems with this drug is its very low solubility in biological fl uids, which results into poor bioavailability after oral administration. Hence present study was carried out to enhance dissolution properties of carbamazepine. Physical mixtures and solid dispersions of carbamazepine were prepared to enhance its water solubility. Physical mixtures and solid dispersions of carbamazepine were prepared by using polyvinyl pyrrolidone K-30, polyethylene glycol 4000 and polyethylene glycol 6000 as water-soluble carrier at various proportion (1:0.1, 1:0.2, 1:0.4, 1:0.6, 1:0.8, by weight) by employing solvent evaporation method. The drug release profi le was studied according to USP XXIII monograph in 1% sodium lauryl sulphate solution. It was found that the dissolution rate and the dissolution parameters of the drug from the physical mixture as well as solid dispersion were higher than those of the intact drug. The degree of the dissolution rate enhancement depended on the nature and the amount of the carrier, i.e., the higher amount of the carrier used, the higher dissolution rate was obtained except for polyvinyl pyrrolidone K-30 and PEG 4000 solid dispersions. Among carrier studied solid dispersion of Carbamazepine: PVP K-30 at 1:0.2 (drug:carrier ratio) gave highest dissolution. The increase in dissolution rate of the drug may be due to increase wettability, hydrophilic nature of the carrier and also possibility due to reduction in drug crystalinity.

To enhance dissolution rate of poorly water-soluble drugs: Glucosamine hydrochloride as a potential carrier in solid dispersion formulations

“…This could be another reason for high dissolution rate of solid disper- sion samples containing low concentration of carrier in comparison with the samples containing high concentration of carrier. Similar results were reported for CBZ solid dispersion samples when the concentration of PVP-K30 was increased from 40 to 160 mg [17]. The figures shows that no further improvement in dissolution of CBZ occurred when the amount of carrier was increased from 33.3% (ratio of drug to carrier 2:1) to 80% (ratio of drug:carrier 1:4) (Fig.…”

Improvement of solubility and dissolution properties of clotrimazole by solid dispersions and inclusion complexes

“…It can be observed that the dissolution of pure CLOT in distilled water was very low with less than 14% of the drug was dissolved within 120 min. This is could be ascribed to poor wettability and/or agglomeration or particle size[ 33 ]. Co-habitation of carriers with CLOT in physical mixtures, clearly improved the dissolution rate of the drug and this could be attributed to wettability improvement of CLOT particles[ 34 ].…”

Solid Dispersion (Kneading) Technique: A Platform for Enhancement Dissolution Rate of Valsartan Poorly Water Soluble Drug

“…12 Powder X-ray Diffraction Studies Using of XRD patterns were recorded using BRUKER-axs D8-ADVANCE, model generator Powder, X-ray diffraction patterns, were used to determine intensities and position of diffraction peaks were considered for comparison and identification of crystallinity of the drug or carrier. 13,14 Scanning Electron Microscopy Using scanning electron microscopy to determine the external morphology of pure drug and solid dispersion. Solid dispersion was coated with gold-palladium alloy using coat ion sputter.…”