Studies on rapidly disintegrating tablets containing taste masked venlafaxine polymer complex

Venlafaxine is a phenethylamine bicyclic derivative chemically unrelated to tricyclic, tetracyclic or other available antidepressant agents, having bitter taste. Thus, in the work undertaken, an attempt was made to mask the taste by complexing venlafaxine HCl with Eudragit EPO and to formulate into a rapid disintegrating tablet. The drug polymer complexes were prepared using precipitation method by taking drug: Eudragit EPO ratios 1:1, 1:2, 1:2.5, 1:3, 1:3.5 and 1:4. The drug polymer complexes were evaluated for the drug content, Fourier transform infrared spectroscopy , X-ray diffraction, in-vitro and in-vivo taste evaluation. The optimum drug: polymer ratio was selected based on in-vitro taste evaluation. Rapid disintegrating tablets (RDTs) were developed from optimum drug: polymer ratios of 1:3. RDTs were evaluated for hardness, tensile strength, friability, weight variation, drug content, wetting time, water absorption ratio, in-vivo disintegration time, in-vivo disintegration time, and sensory evaluation of roughness and taste evaluation. RDTs prepared using spray dried lactose, spray dried mannitol and microcrystalline cellulose in the ratio 1:1 and 8 % w/w crospovidone XL-10 (F4), showed faster disintegration (within 8 sec.) and complete bitter taste masking of Venlafaxine. Human volunteers rated formulation F4 non-bitter with score 0. Tablets of batch F4 also revealed rapid release (t90, 60 sec) in simulated gastric fluid. Thus, results conclusively demonstrated successful masking of taste and rapid disintegration of the formulated tablets in the oral cavity with improved dissolution
Author(s): Jayshree S. Hadke, Shagufta Khan and Dilesh J Singhavi

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