1Department of Pharmaceutics, Faculty of Pharmacy, Zagazig University, Egypt
2Department of Pharmacology, Faculty of Pharmacy, Zagazig University, Egypt
Online published on 7 February, 2013.
The pharmacologic efficacy of benzodiazepines (as clonazepam, CZP) in controlling seizures is directly associated with their plasma concentration. An emergent epileptic situation necessitates rapid drug absorption. parentral administration is not convenient in epileptic emergency and oral bioavailability of CZP is limited by its poor water solubility.
Solid dispersion formulations were developed by physical mixture and solvent evaporation using CZP with the carriers polyvinyl pyrrolidone K30 (PVP K30, 1:4) or polyethylene glycol 4000 (PEG 4000, 1:4).
Analysis of the solid dispersions by FTIR, DSC, XRD and dissolution studies showed that CZP was molecularly dispersed in an amorphous form and indicate increased dissolution rate.
In addition, the oral bioavailability of the formulations was significantly improved reaching therapeutic levels within 30 and 60 min in case of PEG 4000 and PVP K30 respectively following oral administration to mice.
In conclusion; PVP K 30 and PEG 4000 can be utilized to increase the solubility of CZP and enhance its oral bioavailability.
