FORMULATION OPTIMIZATION AND EVALUATION OF MOUTH DISSOLVING FILM OF RAMOSETRON HYDROCHLORIDE

Abstract

Objective: Ramosetron Hydrochloride is found to be more potent and having a longer duration of action with the least side effects, but the major drawback is it undergoes hepatic first-pass metabolism so our aim is to prepare mouth dissolving film (MDF) of Ramosetron hydrochloride for rapid relief in emesis.

Methods: The mouth dissolving films of Ramosetron Hydrochloride were prepared by using the solvent casting method. Films were formulated using HPMC E5 (Hydroxy Propyl Methyl Cellulose) as a film-forming agent, PEG400 (Polyethylene glycol) as a plasticizer and Aspartame as the sweetening agent. A 3² full factorial design was applied considering the concentration of HPMC E5 (X₁) and concentration of PEG400 (X₂) as independent variables and % cumulative drug release (Y₁) (CDR), disintegration time (Y₂) (DT) and tensile strength (Y₃) (TS) as dependent variables. The prepared films were evaluated for thickness, folding endurance, tensile strength, disintegration time, drug content uniformity and taste masking by E-tongue. The results indicated that factors X₁ and X₂ were found to be having a positive effect on DT and TS and negative effects on CDR.

Results: The optimized formulation was found to be the best with 94.00±0.85% in vitro drug release, 33.22±0.75 sec DT and 1.359±0.005 g/mm² tensile strength. Concentration of aspartame was optimized with E-tongue taking into consideration increased electric potential with decreasing bitterness.

Conclusion: Thus, a rapidly dissolving oral film of Ramosetron Hydrochloride with successful taste masking and immediate in vitro drug release was prepared using a solvent casting technique.