title: 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.
authors.affiliation: Department of Pharmaceutical Sciences, Shenyang Pharmaceutical University, 103 Wenhua Road, Shenyang, Liaoning 110016, China.
authors.forename: Yuan
authors.initials: Y
authors.lastname: Zhao
authors.affiliation: Department of Pharmaceutical Sciences, Shenyang Pharmaceutical University, 103 Wenhua Road, Shenyang, Liaoning 110016, China.
authors.forename: Peng
authors.initials: P
authors.lastname: Quan
authors.affiliation: Department of Pharmaceutical Sciences, Shenyang Pharmaceutical University, 103 Wenhua Road, Shenyang, Liaoning 110016, China. Electronic address: fangliang2003@yahoo.com.
authors.forename: Liang
authors.initials: L
authors.lastname: Fang
mesh_terms: D000284:Administration, Oral; D000818:Animals; D004337:Drug Carriers / Q000008:administration & dosage* / Q000138:chemical synthesis* / Q000378:metabolism; D004339:Drug Compounding / Q000379:methods; D004353:Drug Evaluation, Preclinical / Q000379:methods; D008297:Male; D008468:Meclizine / Q000008:administration & dosage* / Q000097:blood / Q000138:chemical synthesis*; D051381:Rats; D017208:Rats, Wistar; D013718:Tensile Strength / Q000502:physiology; D014961:X-Ray Diffraction
chemical_list: D004337:Drug Carriers; D008468:Meclizine
keywords: Bioequivalence; Dissolution rate; Drug-polymer interaction; Meclizine hydrochloride; Oral thin film; Tensile strength