Development and Evaluation of High Loading Oral Dissolving Film of Aspirin and Acetaminophen

Abstract

The objective of this research was to develop and evaluate physicochemical properties of acetaminophen and aspirin orally disintegrating strips with high loading dose. The strips were compared with conventional over the counter strips and chewable tablets for their mechanical and chemical properties. Aspirin (81 mg) and acetaminophen (80 mg) oral dissolving films were developed with 50-55% of drug loading and were compared with GAS-X ® (62.5 mg) and chewable tablets (aspirin and acetaminophen). Orally dissolving films were developed using a solvent casting method. Sonication was proven to be a more competent step in order to load a high amount of active drug substance in the thin film strips. Different film formulations were prepared by varying concentration of polymers and plasticizers. Optimization of formulation was done by conducting studies for various mechanical properties using TA-XT plus texture analyzer. Dissolution of optimized formulation was performed in 250 ml of pH 1.2 and artificial saliva (pH 6.8). The study was conducted by stirring the dissolution media at 50 rpm, 37 C for 30 minutes and was analyzed using UV/Vis spectroscopy. The dimensions of orally dissolving films were determined with the help of vernier calipers. Modulated Differential Scanning Calorimetry (MDSC) was also performed for the filmstrips to check the compatibility. The film strip was evaluated for imperfections and cuts, peelability without rupturing, folding and cracking endurance, surface roughness, tensile strength, film burst and disintegration time with the help of TA-XT plus texture analyzer. Moisture content was performed, on the fresh, as well as stability samples. Dissolution of filmstrips showed much faster release as compared to respective chewable tablets in artificial saliva as well as in pH 1.2. Disintegration times for filmstrips were also comparable to Gas-X ® and Listerine ® . After one month stability of filmstrips at room temperature, dissolution profiles perceived with negligible change. Other mechanical properties of the filmstrips were also comparable to Gas-X ® . DSC results suggest miscibility in polymer, which explains the increase in dissolution rate of filmstrips at high dose loading. Hence, in conclusion we develop a new in house method to formulate a stable and more efficient formulation for high loading dose of aspirin and acetaminophen.

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