Formulation and Evaluation of Doxofylline Sublingual Tablets Using Sodium Starch Glycolate and Crosscarmellose Sodium as Superdisintegrant


Asthma and COPD (Chronic Obstructive Pulmonary Disease) are the most common life threatening pulmonary disease that requires constant monitoring. Xanthine derivatives are used since a long period of time for treatment of Asthma and COPD. Doxofylline is a new generation xanthine derivative that works by inhibition of phosphodiesterase activities with no cardiovascular side effects that usually seen in case of theophylline and other xanthine derivatives due to decreased affinities towards adenosine A1 and A2 receptors. Doxofylline is an anti-tussive and bronchodilator used for maintenance therapy in patients suffering with asthma and chronic obstructive pulmonary disease (COPD) and is highly metabolised by liver to an extent of 80-90%. Doxofylline is coming under class III of BCS classification and water soluble. Present work studies were carried on the formulation and evaluation of sublingual tablets of Doxofylline using super disintegrant like sodium starch glycolate and crosscarmellose with a view to obtain rapid disintegration when held beneath the tongue, permitting direct absorption of the active ingredient by the oral mucosa and it also by passes fast pass metabolism and improve the bioavailability. Different Precompression and post compression characterization of tablet was carried out and the result satisfied according to the pharmacopoeia specifications. In-vitro release studies were carried out in USP II paddle type dissolution apparatus for different formulations. In-vitro release kinetic studies were carried out for zero order, first order and Higuchi kinetic model. FTIR studies were carried out for pure drug Doxofylline, MCC, PVPK30, SSG, crosscarmellose and for optimised formulation to confirm that there is no interaction between drug and different excipients used in the formulation. DSC studies were carried out to know the thermal stabilities of drug and optimised formulation. Accelerated stability studies were carried out to confirm the stability of dosage forms.