Formulation and in-vitro evaluation of Darifenacin Hydrobromide as buccal films

Abstract EN

Overactive bladder (OAB) affects about 16% of the adults and rises with increasing age.

OAB lead to various symptoms such as urgency, incontinence, urinary frequency and nocturia.

Darifenacin hydrobromide (DH) is the more recent uroselective M3 receptor antagonist for treating uncomplicated OAB.

Fast dissolving buccal films are the most innovative oral solid dosage form because of their flexibility and comfort.

This study aims to formulate DH as fast dissolving buccal films (FDBFs) using a solvent casting method to increase its bioavailability by reducing the effect of first pass metabolism in the liver.

Films were prepared by using polyvinyl alcohol as a film forming polymer, glycerol and tween 80.

Different types and concentrations of superdisintegrants (croscarmellose sodium, sodium starch glycolate, indion 414) were used to select the best formula by studying the physicochemical properties of the films, disintegration time (DT) and percent drug release.

The results revealed that formula (F9) that containing 7.5mg DH, 2%w/v PVA, 30%w/w glycerol, 0.5%w/v tween 80, 4%w/w indion 414 was the preferred formula.

F9 showed the shortest in-vitro disintegration time (31.28sec).

In-vitro dissolution profile showed the lowest T80% of the drug in 3.05 min and the highest release of the drug (94%) within 5 min (D5min %).It was concluded that the FDBFs of DH could be considered as a promising drug delivery system with an enhanced disintegration and dissolution rate and better patient compliance.