A Pharmacokinetic Evaluation of a Pectin-Based Oral Multiparticulate Matrix Carrier of Carbamazepine
Date
2021
Journal Title
Journal ISSN
Volume Title
Publisher
Hindawi
Abstract
Background. Carbamazepine is a drug used in the treatment of neurological disorders such as epilepsy. However, due to its erratic
absorption, oral bioavailability is often poor. There is, therefore, the need to develop alternative formulations for carbamazepine
with better pharmacokinetic characteristics. Aim. .e aim of this study was to formulate an oral modified-release multiparticulate
matrix of carbamazepine from cocoa pod husk (CPH) pectin and evaluate the pharmacokinetic profile of this formulation using in
vitro and in vivo models. Methods. CPH pectin was extracted from cocoa pod husks with hot aqueous and citric acid solutions.
Oral multiparticulate carbamazepine matrices were formulated from CPH pectin cross-linked with calcium. .e formulation was
evaluated for carbamazepine content and release profile in vitro. For in vivo pharmacokinetic profile estimation, rats were put into
4 groups of 5 animals each to receive carbamazepine multiparticulate matrix formulations A and B, carbamazepine powder, and
Tegretol CR®. Animals in each group received 200 mg/kg of each drug via the oral route. Maximum plasma concentration (Cmax),
area under the concentration-time curve (AUC), elimination rate constant (Ke), and terminal half-life (t1/2) of the formulations
were estimated by noncompartmental analysis. Results. .e pectin extraction from fresh cocoa pod husks using hot aqueous and
citric acid solutions gave pectin yields of 9.63% and 11.54%, respectively. .e drug content of carbamazepine in CPH pectin
formulations A and B was 95% and 96%, respectively. .ere was controlled and sustained release of carbamazepine for both
formulations A and B in vitro. AUC0⟶36 (176.20 ± 7.97 µg.h/mL), Cmax (8.45 ± 0.71 μg/mL), Tmax (12 ± 1.28 h), and t1/2
(13.75 ± 3.28 h) of formulation A showed a moderately enhanced and comparable pharmacokinetic profile to Tegretol CR®
(AUC0⟶36: 155 ± 7.15 µg.h/mL, Cmax: 8.24 ± 0.45 μg/mL, Tmax: 8.0 ± 2.23 h, and t1/2: 13.51 ± 2.87 h). Conclusion. Findings from
the study suggest that formulations of CPH pectin had the potential to control and maintain therapeutic concentrations of
carbamazepine in circulation over a period of time in the rat model.
Description
Research Article