Orally disintegrating tablet containing carbamazepine and levetiracetam: formulation and in vitro and in vivo characterization


Kandilli B., UĞUR KAPLAN A. B., ÇETİN M., Taspınar N., Genc S., Yeni Y., ...More

Drug Development and Industrial Pharmacy, vol.47, no.7, pp.1153-1165, 2021 (SCI-Expanded) identifier identifier

  • Publication Type: Article / Article
  • Volume: 47 Issue: 7
  • Publication Date: 2021
  • Doi Number: 10.1080/03639045.2021.1988094
  • Journal Name: Drug Development and Industrial Pharmacy
  • Journal Indexes: Science Citation Index Expanded (SCI-EXPANDED), Scopus, Biotechnology Research Abstracts, Business Source Elite, Business Source Premier, CAB Abstracts, Chemical Abstracts Core, EMBASE, International Pharmaceutical Abstracts, MEDLINE, Veterinary Science Database
  • Page Numbers: pp.1153-1165
  • Keywords: Carbamazepine, epilepsy, levetiracetam, orally disintegrating tablet, seizure score
  • Ondokuz Mayıs University Affiliated: No

Abstract

This study aimed to prepare and characterize the orally disintegrating tablet (ODT) formulations containing the combination of levetiracetam (LEV) and carbamazepine (CBZ) (CBZ + LEV combination) for the treatment of epilepsy. The ODT formulations were prepared using the lyophilization (L) and direct compression (DC) methods. The flowability of the mixed powders used for DC formulation was evaluated. The quality control tests for the ODTs were performed. Also, the antiepileptic effects of pure drugs, their combination, and the suspension of CBZ + LEV-DC-ODT formulation were evaluated in the rats with pentylenetetrazole (PTZ)-induced epilepsy model. The obtained results for the mixed powders of the DC formulation (angle of repose: 26.18 ± 0.794°; compressibility index: 15.24 ± 0.764%) suggest that the flow properties of the powder blend were suitable for the preparation of CBZ + LEV-ODT using DC method. The mean values of diameter and hardness of L-ODTs and DC-ODTs were found to be 16.87 mm and 16.18 mm and 11.96 N and 30.11 N, respectively. The friability of both formulations was <1%. Both formulations were disintegrated in seconds. Drugs in L-ODT had faster dissolution than those in DC-ODT. Compared to the seizure scores obtained for the groups treated with LEV or CBZ, generally, there was a higher decrease in seizure scores in the groups treated with CBZ + LEV combination or the suspension of CBZ + LEV-DC-ODTs. Consequently, the ODT formulations containing the CBZ + LEV combination might be beneficial in the treatment of epilepsy.