Preparation, optimization and in vivo evaluation of Eletriptan HBR fast dissolving oral films

Pavan Kumar Kothapuvari, Swati Rawat, DVRN Bhikshapathi

Abstract


The present investigation was aimed with the objective of developing fast dissolving oral films of Eletriptan HBr in order to attain quick onset of action for the better management of migraine attack. Twenty five formulations were prepared by solvent casting method using different polymer types, plasticizer types, surfactant concentrations and different ratio of hydroxypropyl methyl cellulose and maltodextrin. The prepared films were evaluated for folding endurance, thickness, drug content, in vitro/in vivo disintegration time, drug release and tensile test. The optimized formulation F17 containing HPMC 15cp and maltodextrin showed minimum in vitro disintegration time 11 seconds, highest dissolution rate i.e. 98.5% of drug within 10 min. The optimized film was further evaluated for bioavailability compared with a marketed product (Relpax-20mg). The pharmacokinetic results revealed that the fast dissolving oral films has higher peak blood concentration (Cmax, 0.455±0.1µg/ml) within shorter time (Tmax, 0.5 hours), indicating rapid absorption and faster onset of action with acceptable bioavailability value. Therefore, the oral fast dissolving film is considered to be potentially useful for the treatment of migraine disease where quick onset of action is desired, also improved patient compliance.


Keywords


Eletriptan HBr, Migraine, Fast dissolving oral films, disintegration time, HPMC, Pharmacokinetics.

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References


. Liang AC, Chen LH. Fast-dissolving intraoral drug delivery systems. Exp Opin Ther Patents. 2001; 11: 981–6;

. Borsadia S, Halloran D, Osborne JL. Quick dissolving films A novel approach to drug delivery. Drug Deliv Technol. 2003; 3:63 6.

. Klancke J. Dissolution testing of orally disintegrating tablets. Dissolut Technol. 2003; 10:6–8.

. Parakh SR, Gothoskar AV. Review of mouth dissolving tablet technologies. Pharm Tech. 2003; 27:92–100.

. Swapnil LP,Paresh RM, Madhavi AS, Shradha ST, Ketan VP, Prashant NS. Fast dissolving oral films: an innovative drug delivery system. Int J Res Rev Pharm Appl Sci. 2012; 2(3): 482-96.

. Bhupinder B, Sarita J, Mandeep K, Harmanpreet S. Orally fast dissolving films:innovations in formulations and technology. Int J Pharm Sci Rev Res. 2011; 9(2):50-7.

. Revathi V. Fast Dissolving drug delivery system. Pharma Times 2007; 39: 22-3.

. Koland M, Sandeep VP, Charyulu NR. Fast Dissolving Sublingual Films of Ondansetron Hydrochloride: Effect of Additives on in vitro Drug Release and Mucosal Permeation. J Young Pharm. 2010; 2(3): 216–22.

. Sheryl Haut R, Marcelo Bigal E, Richard Lipton B. Chronic disorders with episodic manifestations: focus on epilepsy and migraine. Lancet Neurol. 2006; 5: 148–57.

. Lipton RB, Bigal ME. The epidemiology of migraine. Am J Med. 2005; 1 18: 3-10.

. Himabindu S, Sathish D, Shaik Shayeda. Formulation and Ex Vivo Evaluation of Buccal Tablets of Eletriptan Hydrobromide. Am. J. PharmTech Res. 2012; 2(3), 919-930.

. Zeina Salman D, Nidhal Maraie K, Mustafa Alabbassi G, Mowafaq Ghareeb M. In Vitro/In Vivo Evaluation and Bioavailability Study of Amitriptyline Hydrochloride from the Optimized Oral Fast Dissolving Films. UK Journal of Pharmaceutical and Biosciences. 2014; 2(6): 32-42.

. Kumar GV, Krishna RV, William GJ, Konde A. Formulation and evaluation of buccal films of salbutamol sulphate. Indian J Pharm Sci. 2005; 67:160–4.

. Mona Nagar, Mayank Nagar, Vikram Chopra. Formulation and evaluation of mouth dissolving film of antipsychotic drug aripiprazole. Der Pharmacia Lettre. 2012; 4 (4):1221-1227.

. Prabhakara P, Ravi M, Marina K, Vijaynarayana K, Ullas Souza D, Harish NM, Shastry CS. Formulation and evaluation of fast dissolving films of levocitirizine dihydrochloride. Int J Pharm Inves. 201; 1(2): 99–104.

. Nafee NA, Boraie MA, Ismail FA, Mortada LM. Design and characterization of mucoadhesive buccal patches containing cetylpyridinium chloride. Acta Pharm. 2003; 53:199–212.

. Mashru RC, Sutariya VB, Sankalia MG, Parikh PP. Development and evaluation of fast dissolving film of salbutamol sulphate. Drug Dev Ind Pharm. 2005; 31: 25–34.

. Hiroyoshi S, Kazumi T, Misao N, Katsuhiko M, Tadao T, Hirotaka Y, Naoki I, Kazuyuki H, Mayumi Y, Yasutomi K, Yoshinori I. Preparation of a fast dissolving oral thin film containing dexamethasone: A possible application to antiemesis during cancer chemotherapy. Eur J Pharm Biopharm. 2009; 73(3): 361-5.


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Copyright (c) 2015 Pavan Kumar Kothapuvari, Swati Rawat, DVRN Bhikshapathi

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