Controlled-release carbamazepine matrix granules and tablets comprising lipophilic and hydrophilic components.
The objective of this study was to investigate the effect of lipophilic (Compritol 888 ATO) and hydrophilic components (combination of HPMC and Avicel) on the release of carbamazepine from granules and corresponding tablet. Wet granulation followed by compression was employed for preparation of granules and tablets. The matrix swelling behavior was investigated. The dissolution profiles of each formulation were compared to those of Tegretol CR tablets and the mean dissolution time (MDT), dissolution efficiency (DE%), and similarity factor (f(2) factor) were calculated. It was found that increase in the concentration of HPMC results in reduction in the release rate from granules and achievement of zero-order is difficult from the granules. The amount of HPMC plays a dominant role for the drug release. The release mechanism of CBZ from matrix tablet formulations follows non-Fickian diffusion shifting to Case II by the increase of HPMC content, indicating significant contribution of erosion. Increasing in drug loading resulted in acceleration of the drug release and in anomalous controlled-release mechanism due to delayed hydration of the tablets. These results suggest that wet granulation followed by compression could be a suitable method to formulate sustained release CBZ tablets.
Barakat
Nahla S
NS
Department of Pharmaceutics, College of Pharmacy, King Saud University, Riyadh, Saudi Arabia. nsybarakat@yahoo.com
Elbagory
Ibrahim M
IM
Almurshedi
Alanood S
AS
D000927:Anticonvulsants / Q000008:administration & dosage* / Q000737:chemistry; D002220:Carbamazepine / Q000008:administration & dosage* / Q000737:chemistry; D002482:Cellulose / Q000737:chemistry; D002626:Chemistry, Pharmaceutical / Q000379:methods; D003692:Delayed-Action Preparations; D005079:Excipients / Q000737:chemistry*; D005227:Fatty Acids / Q000737:chemistry; D065347:Hypromellose Derivatives; D008747:Methylcellulose / Q000031:analogs & derivatives / Q000737:chemistry; D012995:Solubility; D013607:Tablets
D000927:Anticonvulsants; D003692:Delayed-Action Preparations; D005079:Excipients; D005227:Fatty Acids; D013607:Tablets; C086409:glyceryl behenate; D002220:Carbamazepine; D065347:Hypromellose Derivatives; D002482:Cellulose; D008747:Methylcellulose; C109691:microcrystalline cellulose