FORMULATION DEVELOPMENT OF SUBLINGUAL FILM OF ANTIPSYCHOTIC DRUG WITH DIFFERENT POLYMERS AND PLASTICIZERS
Kiran B. Patel
Department of Chemistry, Sheth M. N. Science College, Patan-Gujarat, India , IN
Piyush J. Vyas
Department of Chemistry, Sheth M. N. Science College, Patan-Gujarat, India , IN
Deep S. Joshi
Department of Chemistry, Sheth M. N. Science College, Patan-Gujarat, India , IN
Dharmesh Patel
Department of Chemistry, Sheth M. N. Science College, Patan-Gujarat, India , IN
Zalak Patel
Department of Chemistry, Sheth M. N. Science College, Patan-Gujarat, India , IN
Keywords: Asenapine, Schizophrenia, Bipolar disorder, drug substance
Abstract
Asenapine Maleate was selected for evaluation of different polymer for preparation of fast dissolving sublingual film. Asenapine Maleate, antagonist activity at Histamine 5-HT2A and dopamine D2 receptors is a new psychopharmacologic drug with high potency and affinity for blocking dopamine, serotonin, α-adrenergic and histamine receptors, which has oral bioavailability of only 2% due to first pass metabolism. This research work performed for developing Asenapine Maleate sublingual films with satisfactory drug dissolution in the oral cavity, thus bypassing hepatic first pass metabolism to provide rapid onset of action of the drug and comparable effect as reference listed drug product Saphris. The sublingual films were prepared by solvent casting method. Different combination of polymers was used with plasticizer to develop palatable and stable film. Cherry flavor is used as
flavouring agent, Aspartame is used as sweetening agent and Poloxamer 188 was used as penetration enhancer. All the films formulations was evaluated for their thickness, weight variations, tensile strength, percentage elongation, folding endurance, surface pH, in-vitro disintegration, drug content and in-vitro drug release. Disintegration time showed by the formulations was found to be less than 2 minutes. Formulations showed 80% in-vitro drug dissolution within 4 min was finalized. The film showed an excellent stability for one month when stored at temperature 40˚C and 75% in humidity and room temperature.
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