Fast Dissolving Oral Thin Film Drug Delivery Systems Consist of Ergotamine Tartrate and Caffeine Anhydrous

Abstract

Background: Ergotamine tartrate (ET), a serotonin 5-HT1 receptor agonist, is an antimigraine drug. Due to high first-pass metabolism, ET shows a very low bioavailability in oral administrations (<1%). Caffeine (CA) increases the rate and extent of water solubility of ET. The present study intended to investigate the possibility of developing ET fast dissolving thin films for the fast drug dissolution in the oral cavity, and thus bypassing first pass metabolism for providing quick onset of action of the drug. Methods: The films (ET and CA) were prepared according to solvent casting method, separately. Low viscosity grade of hydroxylpropyl methylcellulose (HPMC E-15) was employed in preparation as a film forming polymer. Propylene glycol was the plasticizer used. All the films were evaluated for their thickness, weight variations, folding endurance, surface pH, disintegration, drug content, DSC, in-vitro drug release, and ex-vivo permeation. Results: The best polymer drug ratio in ET/CA films was 1:20 (E 2) and 1:4 (C 2), respectively. The films E 2 and C 2 showed 9.9, 3.2 mg weight, 74, 45 µm thickness, 120.66, up to 300 folding endurance and 0.38, 0.52 mg/cm 2 drug content, respectively. The DSC showed no stable characteristic for ET and CA in the drug loaded films and revealed amorphous form. The results showed that ET films prepared had faster release and CA films had slower release (p<o.o5). Both films (ET and CA) exhibited good mucoadhesion properties and shorter retention time (36-150 s). Conclusion: The formulations were found to be a suitable candidate for the development of oral thin films for migraine therapy.

Evaluation and characterization of orally disintegrating films loaded donepezil hydrochloride for Alzheimer’s disease

“…The In vitro release test was conducted for three parallels and protected from light and heat during the studies. In vitro release values were calculated with the aid of the predetermined donepezil HCl standard calibration curve equation [26,27].…”

Development and in vitro Characterization of Gastroretentive Formulations as Calcium Pectinate Hydrogel Pellets of Pregabalin by Ionotropic Gelation Method

“…Samples were filtered through 0.45 µm membrane filters, and released PG amounts were determined by a validated HPLC method. 36 Release results in pH 1.2 HCl buffer were applied to the computer program in order to determine the kinetic model of the release from the selected hydrogel pellets containing PG. Whether formulations are compatible with Zero-Order, First-Order, Korsmeyer-Peppas, or Higuchi kinetic models were determined by mathematical operations and formulas.…”

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“…It is retained at the site of application and rapidly releases the active agent for local and/or systemic absorption. [21][22][23][24][25][26][27][28][29]…”