Characterization of Oral Disintegrating Film Containing Donepezil for Alzheimer Disease

Abstract

Abstract. The aim of this study was to develop a taste-masked oral disintegrating film (ODF) containing donepezil, with fast disintegration time and suitable mechanical strength, for the treatment of Alzheimer's disease. Hydroxypropyl methylcellulose, corn starch, polyethylene glycol, lactose monohydrate and crosspovidone served as the hydrophilic polymeric bases of the ODF. The uniformity, in vitro disintegration time, drug release and the folding endurance of the ODF were examined. The in vitro results showed that 80% of donepezil hydrochloride was released within 5 minutes with mean disintegration time of 44 seconds. The result of the film flexibility test showed that the number of folding time to crack the film was 40 times, an indication of sufficient mechanical property for patient use. A single-dose, fasting, four-period, eight-treatment, double-blind study involving 16 healthy adult volunteers was performed to evaluate the in situ disintegration time and palatability of ODF. Five parameters, namely taste, aftertaste, mouthfeel, ease of handling and acceptance were evaluated. The mean in situ disintegration time of ODF was 49 seconds. ODF containing 7 mg of sucralose were more superior than saccharin and aspartame in terms of taste, aftertaste, mouthfeel and acceptance. Furthermore, the ODF was stable for at least 6 months when stored at 40°C and 75% relative humidity.

In vitro/in vivo evaluation of an optimized fast dissolving oral film containing olanzapine co-amorphous dispersion with selected carboxylic acids

“…The disintegration time of the films was in the ranged of 4.00-51.00 s which is less than 1 min and considered acceptable time as reported in previous studies (Liew et al, 2012). It was clear that the time was increased as the polymer concentration increased.…”

Characterization of low cost orally disintegrating film (ODF)

“…Oral strips produced with maltodextrin presented in vivo disintegration of only 10 s [30] . For ODF based on hydroxypropyl methylcellulose, corn starch, polyethylene glycol, and lactose monohydrate with donepezil a disintegration mean time of 49 s [32] . For drug delivery by oral route, an ODF with hydroxy-propyl methyl cellulose and carbopol had a residence time of 23 min [9] .…”

Effect of Backing Films on the Transdermal Delivery of Donepezil from Patches

“…), a new class of acetylcholinesterase inhibitor, is the second drug approved by FDA for treatment of mild to moderate Alzheimer's diseases (1,2). It is superior to other cholinesterase inhibitors due to its high potency and selectivity for the enzyme AChE in central nervous system (3).…”