Preparation of an oral thin film containing meclizine hydrochloride: In vitro and in vivo evaluation

Abstract

Oral thin film (OTF) is a preparation of postage stamp size, with advantages of flexible, tasty and without water for oral administration. A commercial product (Zentrip®) was developed for people who suffered from motion sickness. In order to improve the mechanical strength of Zentrip®, OTF containing meclizine hydrochloride (MH) was designed and prepared using the solvent casting method. The characteristics of the prepared OTF were evaluated using micrometer, auto stripping tester, DSC, X-ray diffraction. ATR-FTIR was employed to investigate the interaction between drug and polymer. The thickness of MH OTF obtained was 0.116±0.004mm, the tensile strength was 17.37±1.54Nmm−2 and the drug dissolution at 5min was more than 80% both in distilled water and 0.1mol/L HCL. DSC and XRD showed MH was amorphous in the polymer. ATR-FTIR indicated the MH molecules inserted into the network structure of polymer, which resulted in an inhibition of drug recrystallization. The Cmax of Zentrip® and MH OTF were 1.46±0.44μg/mL and 1.91±0.51μg/mL, and the AUC were 10.38±2.93μgh/mL and 13.74±3.23μgh/mL, respectively. Compared with Zentrip®, MH OTF successfully overcome the weakness of mechanical strength, possessed faster dissolution profile and showed bioequivalence in pharmacokinetics, deserving to a further development.