Abstract

ENHANCEMENT OF BIOAVAILABILITY OF ASENAPINE MALEATE BY INCORPORATING IN MELT-IN-MOUTH SUBLINGUAL FILMS

S. N. H. Pratap* and A. Krishna Kishore

ABSTRACT

Asenapine Maleate is an atypical antipsychotic drug used in the treatment of schizophrenia. The melt-in-mouth sublingual films (SLF’s) of Asenapine Maleate were prepared with an objective of immediate release; improve bioavailability of drug and patient compliance.In this study, Asenapine maleate is initially complexed with hydroxy propyl-β- cyclodextrin (HP-β-CD) using kneading method followed by molding into thin films. Poly ethylene glycol (PEG-400) and propylene glycol (PG) are used as plasticizers and ethanol-water mixture is used as solvent. Sublingual films were prepared by solvent casting method using various concentrations of hydrophilic polymers like sodium carboxy methyl cellulose (Na-CMC), poly vinyl alcohol (PVA) and HPMC E5-lv. The prepared formulations were evaluated for various parameters like thickness, folding endurance, uniformity of weight, drug content, disintegration time, in vitro dissolution study, stability study and drug excipients compatibility. The thickness ranges from 2-4 mm with a folding endurance of more than 300 for all the formulations. The drug content present in the prepared films was in the range of 95% to 105% and the drug release from all the films was less than 3 minutes.

Keywords: Asenapine Maleate, HP- ?-Cyclodextrin, Sublingual films, Bioavailability, in-vitro release studies.