FORMULATION DEVELOPMENT OF ORAL FAST-DISSOLVING FILMS OF RUPATADINE FUMARATE
DOI:
https://doi.org/10.22159/ajpcr.2020.v13i11.39185Keywords:
Rupatadine Fumarate, Oral Fast Dissolving Film, Solvent casting method, Beta Cyclodextrin, HPMC, Pullulan, Allergic RhinitisAbstract
Objective: Rupatadine fumarate (RF) is an anti-allergic drug indicated for the treatment of allergic rhinitis. It has low oral bioavailability due to its poor aqueous solubility and extensive hepatic first pass metabolism. In the present work, oral fast-dissolving films (OFDF) have been formulated and evaluated to facilitate dissolution in the oral cavity itself.
Methods: Pullulan and HPMC (5, 15 cps) were employed as film formers and six formulations were tried. The physicochemical compatibility between drug and the polymers was studied by FTIR spectroscopy. RF-beta-cyclodextrin (BCD) inclusion complex was initially prepared and evaluated. The inclusion complex was incorporated into the film. OFDF were formulated and prepared by solvent casting method. The film size for one dose was 2 × 2 cm. The films were evaluated for various film parameters including disintegration time and drug release.
Results: Preliminary film studies indicated % of film former solution to be between 3 and 5% for good appearance, mechanical strength, and quick disintegration. Solubility enhancement of RF is almost 40-fold from its BCD inclusion complex. Drug content in the films ranged between 83 and 90%. The pH ranged between 6 and 7 for all the formulations. All OFDF of RF disintegrated within one minute. With higher viscosity grade of HPMC, disintegration was comparatively slower and so was the drug release. Pullulan based films also showed desirable properties. F3 had disintegration time was 28 s and % drug release was 92% in 180 s.
Conclusion: OFDF of RF could be formulated employing pullulan and HPMC low viscosity grades by solvent casting method. F3 containing HPMC E5 at 37% by weight of dry film showed desirable film properties. Stability studies indicated that there was no significant change in the films with respect to physicochemical properties and in vitro release.
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References
Small P, Harold K. Allergic rhinitis. Allergy Asthma Clin Immunol 2011;7:34-41.
Wheatley LM, Togias A. Allergic rhinitis. N Engl J Med 2015;372:456-63.
Mirmoezzi MS, Yazdi MS, Gholami O. Comparative study on the efficacy of mometasone and fluticasone nasal sprays for treatment of allergic rhinitis. Int J Pharm Pharm Sci 2017;9:211-4.
Mittal PA, Godse KV, Patil SP. Second-generation antihistamines. Ind J Drug Derm 2016;2:3-12.
Vondark B, Bamhart S. Dissolvable films for flexible product format in drug delivery. PharmTech 2008;1:41-5.
Frey P. Film Strips and Pharmaceuticals. Pharmaceutical Manufacturing and Packaging Source Winter; 2006. p. 92-3.
Zhang H, Zhang J, Streis JB. Oral mucosal drug delivery: Clinical pharmacokinetics and therapeutic applications. Clin Pharmacokinet 2002;41:661-80.
Krishnaveni J, Ali MS, Vijender C, Sudheer KD. Formulation and evaluation of fast dissolving oral films of diazepam. J Pharmacovigil 2016;4:1-5.
Senthilkumar K, Vijaya K. Formulation development of mouth dissolving film of etoricoxib for pain management. Adv Pharm 2015;2015:702963.
Kathapali H, Patil A. Formulation and evaluation of orally disintegrating films of levocetirizine dihydrochloride. Ind J Pharm Sci 2017;79:204-11.
Chaudhury H, Gauri S, Rathee P, Kumar V. Development and optimization of fast dissolving oro-dispersible films of granisetron HCL using box-behnken statistical design. Bull Fac Pharm Cairo Univ 2013;51:193-201.
Castillo H, Vargas ZR, Carazo BG, Madrigal RG, Calvo GB, Baltodano VE. Development of immediate release rupatadine fumarate 10 mg tablets: A quality by design (QbD) approach. Drug Dev Ind Pharm 2019;45:1674-81.
Wasilewska K, Szekalska M, Ciosek-Skibinska P, Lenik J, Basa A, Jacyna J, et al. Ethylcellulose in organic solution or aqueous dispersion form in designing taste-masked microparticles by the spray drying technique with a model bitter drug: Rupatadine fumarate. Polymers 2019;11:522.
Ferrer MM, Capdevila MS. Liquid Formulations of Rupatadine Fumarate. European Patent Office, No. EP2402012B1; 2012.
Raj RA, Nair SS, Harindran J. Formulation and evaluation of cyclodextrin inclusion complex tablets of carvedilol. Asian J Pharm 2016;10:84-94.
Yassin GE, Abass HA. Design and evaluation of fast dissolving oro-dispersible films of metoclopramide hydrochloride using 32 multifactorial designs. Int J Pharm Pharm Sci 2016;8:218-22.
Sri KV, Ravishanker D, Rohini P, Subbarao M. Formulation and in vitro evaluation of sumatriptan succinate oral thin films. Ind Am J Pharm Res 2013;3:3016-25.
Kumar KR, Sulochona MM. Fast dissolving films a unique strategy for drug delivery. Asian J Pharm Res 2014;4:47-55.
Kumar SR. An update on fast dissolving films. World J Pharm Pharm Sci 2014;5:466-86.
Chauhan NS, Tomar A, Sharma K, Mittal A, Bajaj U. Formulation and evaluation of fast dissolving oral film of dicyclomine as potential route of buccal delivery. Int J Drug Dev Res 2012;4:408-17.
Bais PV, Upadhye KP, Dixit G. Formulation and evaluation of fast dissolving oral melt-in-mouth of lorazepam for sublingual use. World J Pharm Pharm Sci 2016;5:763-75.
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