• Abeer Ahmed Kassem Faculty of Pharmacy, Princess Nourah bint Abdulrahman University, Riyadh, Saudi Arabia
  • Gihan Salah Labib Department of Pharmaceutics, Faculty of Pharmacy, Alexandria University, Alexandria, Egypt




Almotriptan, Lyophilization, Sublingual, Fast-dissolving, Migraine


Objective: Development of sublingual fast dissolving lyophilized almotriptan tablets, to enhance its pre-gastric absorption and so alleviating the gastrointestinal dysmotility that is commonly associated with migraineurs.

Methods: Primary almotriptan lyophilized tablets (Alm-lyotab), were prepared using polyvinyl alcohol (PVA), polyvinyl pyrrolidone (PVP), gelatin, or sodium alginate, as a bulk forming agent and mannitol as a disintegrant, cryoprotectant and taste improver. Physical properties, wetting time, in vitro dissolution and disintegration behaviour, were investigated. A combination of PVP, gelatin and chitosan in different ratios with mannitol were developed and characterised for further improvement. Optimised formula was examined by scanning electron microscope (SEM), differential scanning calorimetry (DSC) and Fourier-transform infrared spectroscopy (FTIR).

Results: Both PVP and gelatin primary formulations showed elegant appearance with fast in vitro disintegration time of 5.67 and 5.64 sec, short wetting time of 4.06 and 4.05 sec, respectively, and high in vitro release rate of about 80% after 1 min, thus they were selected for further improvement. Optimised formula from polymer blend formulations (F8) which consisted of PVP: gelatin: chitosan in a ratio of its constituting solutions of 1:5:0.5, exhibited an elegant appearance, drug content of 98.75 %, in vivo disintegration time of 1.85 sec and complete drug release within 1 min. SEM micrographs revealed spongy, highly porous structure. DSC results indicated the presence of the drug in its crystalline form. FTIR studies revealed no interaction between the drug and excipients.

Conclusion: Sublingual instantly dissolving Almo-lyotab was successfully developed and may constitute an advance in the management of acute migraine attacks.


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Chu J. Goldfrank's toxicologic emergencies. In: Nelson LS, Lewin NA, Howland MA, Hoffman RS, Goldfrank LR, Flomenbaum NE. editors. McGraw-Hill Medical New York; 2010. p. 763-9.

Ali AM, Awad TG, Al-Adl NM. Efficacy of combined topiramate/thioctic acid therapy in migraine prophylaxis. Saudi Pharm J 2010;18:239-43.

Minor DS, Jackson D. Pharmacotherapy in primary care. In: Linn WD. Wofford MR, O'keefe M, Posey L. editors. McGraw Hill: New York; 2009. p. 219-32.

Sanders-Bush E, Hazelwood L. Goodman and Gilman's the pharmacological basis of therapeutics. In: Brunton LL, Chabner BA, Knollmann BC. editors. McGraw-Hill Medical New York; 2011. p. 381-417.

Saxena PR, Ferrari MD. Monthly update: central and peripheral nervous systems: pharmacology of antimigraine 5-HT1D receptor agonists. Expert Opin Invest Drugs 1996;5:581-93.

Keam S, Goa K, Figgitt D. Almotriptan: a review of its use in a migraine. Headache: J Head Face Pain 2003;43:300-1.

Gras J, Llenas J, Jansat JM, Jáuregui J, Cabarrocas X, Palacios JM. Almotriptan, a new antiâ€migraine agent: a review. CNS Drug Rev 2002;8:217-34.

Aubets J, Cardenas A, Salva M, Jansat J, Martinez-Tobed A, Palacios J. Disposition and metabolism of almotriptan in rats, dogs and monkeys. Xenobiotica 2006;36:807-23.

Jansat JM, Costa J, Salvà P, Fernandez FJ, Martinezâ€Tobed A. Absolute bioavailability, pharmacokinetics, and urinary excretion of the novel antimigraine agent almotriptan in healthy male volunteers. J Clin Pharmacol 2002;42:1303-10.

Pradhan V, Gaikwad R, Samad A, Prabhakar B. Formulation and evaluation of almotriptan malate nasal drops. Indian J Pharm Sci 2009;71:727.

Abbas Z, Marihal S. Gellan gum-based mucoadhesive microspheres of almotriptan for nasal administration: formulation optimisation using factorial design, characterization, and in vitro evaluation. J Pharm Bioallied Sci 2014;6:267-77.

Calatayud-Pascual M, Balaguer-Fernandez C, Serna-Jimenez C, Del Rio-Sancho S, Femenia-Font A, Merino V, et al. Effect of iontophoresis on in vitro transdermal absorption of almotriptan. Int J Pharm 2011;416:189-94.

Pauletti GM, Wilson M, Soderstrom R, Kishorkumar DJ, Ritschel WA. Coated vaginal device for delivery of anti-migraine and anti-nausea drugs; 2010.

Main MJ, Pulmonary formulations of triptans; 2011.

Kassem A. Formulation approaches of triptans for the management of a migraine. Curr Drug Delivery 2016;13:882-98.

Safarab R, Abdelwahed W, Chehna MF, Degobert G, Fessi H. Preparation and characterization of new oral lyophilizates containing a non-steroidal anti-inflammatory drug. Int J Pharm Pharm Sci 2011;3:108-14.

Mishra DN, Bindal M, Singh SK, Vijaya Kumar SG. Spray dried excipient base: a novel technique for the formulation of orally disintegrating tablets. Chem Pharm Bull 2006;54:99-102.

Narmada G, Mohini K, Prakash Rao B, Gowrinath D, Kumar K. Formulation, evaluation and optimisation of fast dissolving tablets containing amlodipine besylate by a sublimation method. Ars Pharm 2009;50:129-44.

Sharma S, Gupta G. Formulation and characterization of a fast-dissolving tablet of promethazine theoclate. Asian J Pharm 2014;2:70-2.

Singh SK, Mishra DN, Jassal R, Soni P. Fast disintegrating combination tablets of omeprazole and domperidone. Asian J Pharm Clin Res 2009;2:74-82.

Amipara LV. A review on fast dissolving tablet technology. J Biomed Pharm Res 2013;2:8-18.

Dey P, Ghosh A. Wafers: an innovative advancement of oro-dispersible films. Int J Appl Pharm 2016;8:1-7.

McLaughlin R, Banbury S, Crowley K. Orally disintegrating tablets: the effect of recent FDA guidance on ODT technologies and applications. Pharm Technol 2009;Suppl 2:1-7.

Swarbrick J. Encyclopedia of pharmaceutical technology. Informa Healthcare USA. Inc., New York. Informa Healthcare USA; 2007.

Luppi B, Bigucci F, Abruzzo A, Corace G, Cerchiara T, Zecchi V. Freeze-dried chitosan/pectin nasal inserts for antipsychotic drug delivery. Eur J Pharm Biopharm 2010;75:381-7.

Labib GS. Novel levocetirizine HCl tablets with enhanced palatability: synergistic effect of combining taste modifiers and effervescence technique. Drug Des Dev Ther 2015;9:5135–46.

Siddiqui MN, Garg G, Sharma PK. Fast dissolving tablets: preparation, characterization and evaluation: an overview. Int J Pharm Sci Rev Res 2010;4:87-96.

Shoukri RA, Ahmed IS, Shamma RN. In vitro and in vivo evaluation of nimesulide lyophilized orally disintegrating tablets. Eur J Pharm Biopharm 2009;73:162-71.

Talele Swati G, Harak Yogesh, Bakliwal Akshada A, N CG. Formulation and evaluation of mouth dissolving film of almotriptan malate. J Pharm BioSci 2015;3:42-52.

Alladi A, Damodharan N. Formulation, taste masking and evaluation of almotriptan oral disintegrating tablets. Int J Pharm Sci Res 2012;3:3940-6.

Gowtham G, Reddy GR, Sathyanarayana R, Pandey V. Formulation and evaluation of almotriptan tablets. Res J Pharm Technol 2011;4:533-6.

Fonte P, Reis S, Sarmento B. Facts and evidences on the lyophilization of polymeric nanoparticles for drug delivery. J Control Rel 2016;225:75-86.

Korsmeyer RW, Gurny R, Doelker E, Buri P, Peppas NA. Mechanisms of solute release from porous hydrophilic polymers. Int J Pharm 1983;15:25-35.

Thombre AGaC JR. Biopolymers for controlled drug delivery. Encyclopedia of Pharmaceutical Technology. ed. Swarbrick JaB JC. Vol. 2. New York: Marcel Dekker, Inc; 1990.

Nicolazzo JA, Reed BL, Finnin BC. Buccal penetration enhancers-how do they really work? J Control Rel 2005;105:1-15.

Şenel S, Hıncal AA. Drug permeation enhancement via buccal route: possibilities and limitations. J Control Rel 2001; 72:133-44.

Kuno Y, Kojima M, Ando S, Nakagami H. Evaluation of rapidly disintegrating tablets manufactured by phase transition of sugar alcohols. J Control Rel 2005;105:16-22.



How to Cite

Kassem, A. A., and G. S. Labib. “FLASH DISSOLVING SUBLINGUAL ALMOTRIPTAN MALATE LYOTABS FOR MANAGEMENT OF MIGRAINE”. International Journal of Pharmacy and Pharmaceutical Sciences, vol. 9, no. 1, Jan. 2017, pp. 125-31, doi:10.22159/ijpps.2017v9i1.15489.



Original Article(s)