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Abstract
Objective: To characterize the in vitro release of carbamazepine tablets and benzoyl metronidazole suspensions using the flow-through cell apparatus and simulated gastrointestinal fluids.Methods: Tegretol® tablets, Flagyl® suspension, and generic formulations of each were tested. Release studies were performed using an automated flow-through cell apparatus. Simulated gastric fluid (with and without pepsin) and simulated intestinal fluid (without pancreatin) at 16 ml/min and fasted state simulated intestinal fluid at 8 ml/min, all at 37.0±0.5 °C, were used as dissolution media. The quantity of dissolved carbamazepine and benzoyl metronidazole was determined at 5-min intervals until 60 min at 285 and 278 nm, respectively. Percentage dissolved at 60 min, mean dissolution time, dissolution efficiency values, and t10%, t25%, t50% and t63.2% were calculated. Mean values for all parameters were compared between the reference and generic formulations using Studentʼs t-test. Dissolution data were fitted to different kinetic models.Results: Simulated gastric fluid without pepsin showed no discriminative capability for carbamazepine tablets. Significant differences were observed between the reference and generic formulations for almost all parameters (*P<0.05). In some cases, the logistic model best described the in vitro release of both drugs.Conclusion: Using an apparatus and media that best simulates the gastrointestinal environment, we identified differences in the rate and extent of dissolution of both drugs that could help to optimise the design of interchangeable formulations. Based on the physicochemical characteristics of carbamazepine and benzoyl metronidazole and the conditions in which the formulations were tested, these differences could be of clinical relevance.
Highlights
Carbamazepine, an antiepileptic drug with a narrow range of therapeutic efficacy, is widely used to control seizures [1]
Both carbamazepine drug products met the requirements of the content uniformity test, and the carbamazepine and benzoyl metronidazole drug products met the requirements of the assay tests specified in the United States Pharmacopeia (USP)
The flow-through cell method (16 ml/min) with 1.0% sodium lauryl sulphate aqueous solution as dissolution medium was reported to be more discriminative for carbamazepine generic products than the use of USP Apparatus 2 [31]
Summary
Carbamazepine, an antiepileptic drug with a narrow range of therapeutic efficacy, is widely used to control seizures [1]. Kasim et al [5] have classified metronidazole as a Class III drug (high solubility/low permeability), and a private company specializing in drug delivery studies [6, 7] has classified it as a Class IV drug (low solubility/low permeability). Both compounds are manufactured as generic tablets and suspensions, and to determine whether these drugs are safely interchangeable, evaluation of their in vitro release under conditions that simulate the natural environment of the gastrointestinal tract is very important. An official dissolution test for carbamazepine tablets, using a USP Apparatus 2 at 75 rpm with 900 ml of 1.0% sodium lauryl sulphate aqueous solution as the dissolution medium, has been reported, but no official dissolution test for benzoyl metronidazole suspension is defined in the USP [9]
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