Formulation and In-Vitro Evaluation of Darifenacin Hydrobromide as Buccal Films

Abstract

Darifenacin hydrobromide (DH) is the more recent uroselective M3 receptor antagonist for treating uncomplicated overactive bladder (OAB). This study was aimed to formulate DH as fast dissolving buccal films (FDBFs) using a solvent casting method to enhance patient’s compliance.
 Films were prepared by using polyvinyl alcohol (PVA) as a film forming polymer. 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.

The Development of Eletriptan Hydrobromide Immediate Release Buccal Films Using Central Composite Rotatable Design: An In Vivo and In Vitro Approach

“…As per United States Pharmacopeia (USP) guidance, drug contents could be varied between 90% to 110%. The results suggested the drug was evenly distributed throughout the film [ 65 ].…”

Drug Delivery Approaches for Managing Overactive Bladder (OAB): A Systematic Review

“…These studies were further screened by title and abstract, which resulted in the removal of 430 studies. Thus, 79 studies were subjected to full-text screening and finally 24 [ 44 , 45 , 46 , 47 , 48 , 49 , 50 , 51 , 52 , 53 , 54 , 55 , 56 , 57 , 58 , 59 , 60 , 61 , 62 , 63 , 64 , 65 , 66 , 67 ] were selected and considered eligible to be included in the systematic review for further reporting and analysis ( Figure 2 ). The main reasons for exclusion were a lack of focus on drug delivery and formulation development.…”

“…Additionally, the fast dissolving drug delivery systems have advantages for geriatric and paediatric patients due to rapid disintegration, ease of administration or self-administration, and non-requirement for chewing or water. Fast dissolving films of darifenacin hydrobromide were developed by Abbas et al, [ 67 ] using PVA, Tween 80 and glycerol. Different types and concentrations of superdisintegrants including sodium starch glycolate, croscarmellose sodium and Indion 414 were investigated.…”

Palatable Levocetirizine Dihydrochloride Solid Dispersed Fast-Dissolving Films: Formulation and In Vitro and In Vivo Characterization

“…Three 1 cm 2 films of each formulation were allowed to dissolve in 5 ml of saliva simulated phosphate buffer (pH 6.8) at room temperature, and the pH was measured by bringing a combined glass electrode into contact with the solution and allowing it to equilibrate for 1 min. [ 18 ].…”

“…One film of each formulation was put separately in a Petri dish containing 10 ml of deionized water and was agitated smoothly and continuously. The time at which the FDFs started to disintegrate or break was recorded in seconds as disintegration times [ 18 ].…”