Characterization of Oral Disintegrating Film Containing Donepezil for Alzheimer Disease
- 1.4k Downloads
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.
KEY WORDSAlzheimer disease donepezil HCl oral disintegrating film palatability
This author would like to thank Institute of Postgraduate Studies, Universiti Sains Malaysia for providing Fellowship.
- 1.Joseph TD, Robert LT, Gary CY, Gary RM, Barbara GW, Michael LP. Pharmacotherapy: a pathophysiologic approach. 6th ed. New York: McGraw Hill; 2005. p. 2162–87.Google Scholar
- 3.Hanawa T. Development of a new and kindly oral dosage form for elderly. JPST. 1997;13:251–8.Google Scholar
- 9.Mishra R, Amin A. Formulation development of taste-masked rapidly dissolving films of cetirizine hydrochloride. Pharmtech. 2009;33(2):48–56.Google Scholar
- 10.Pillai R, Karatgi P. Orally disintegrating tablets: the path to improved patient compliance and enhanced life cycle management. Pharmtech Europe. 2009;21(5):37–41.Google Scholar
- 11.Shimoda H, Taniguchi K, Nishimura M, Matsuura K, Tsukioka T, Yamashita H, et al. Preparation of a fast dissolving oral thin film containing dexamethasone: a possible application to antiemesis during cancer chemotherapy. Eur J Pharm Sci. 2009;73:361–5.Google Scholar
- 15.Borsadia SB, O'Halloran D, Osborne JL. Quick-dissolving films—a novel approach to drug delivery. Drug development and delivery. 2003;3(3). Available online at http://www.drugdeliverytech.com/ME2/dirmod.asp?sid=&nm=&type=Publishing&mod=Publications%3A%3AArticle&mid=8F3A7027421841978F18BE895F87F791&tier=4&id=1462E9E570724362AF256AB9CEC63126.
- 17.Bruce JK, Angela LH, Liu H, Sara KW. Olanzapine orally disintegrating tablet in the treatment of acutely ill non-compliant patients with schizophrenia. IJNP. 2003;6:97–102.Google Scholar
- 18.Raviraj P, Pradeep K. Orally disintegrating tablets: the path to improve patient compliance and enhanced life cycle management. Pharmtech Europe. 2009;21:5.Google Scholar
- 19.Emilio MC, Vincente GG, Albert NS, Jose PF, Joan HN, Jordi GC, et al. A study on the subjective compliance and acceptance of oral lanzoprazole in traumatology. The ECOFT-TR Study. Clin Rheumatol. 2009;5(2):49–54.Google Scholar
- 21.Mishra R, Amin A. Manufacturing techniques of orally dissolving films. J Pharm Sci. 2011;35(1):70–3.Google Scholar
- 23.Japanese Pharmacopoeia 15. General tests, processes and apparatus. Tokyo, Japan: The Society of Japanese Pharmacopoeia. p. 107.Google Scholar
- 26.Rowe RC, Sheskey PJ, Quinn ME. Handbook of pharmaceutical excipients. 6th ed. London: Pharmaceutical Press; 2009. p. 702.Google Scholar
- 27.Doe J. 2010 Sucralose—Technological Justification. www.food.gov.uk/multimedia/pdfs/sucraconsult2.pdf. Accessed26 Oct 2010.
- 28.Rowe R, Sheskey PJ, Quinn ME. Handbook of pharmaceutical excipients. 6th ed. London: Pharmaceutical Press; 2009. p. 48.Google Scholar
- 30.Rowe RC, Sheskey PJ, Quinn ME. Handbook of pharmaceutical excipients. 6th ed. London: Pharmaceutical Press; 2009.Google Scholar
- 31.Riera CE, Vogel H, Simon SA, Coutre Jl. Artificial sweeteners and salts producing a metallic taste sensation activate TRPV1 receptors. Am J Physiol. 2007;293:626–34.Google Scholar
- 34.Kearney P, Rathbone MJ, Hadgraft R. The Zydis oral fast-dissolving dosage form. Modified-Release Drug Delivery Technology. 2002;2:191–201.Google Scholar