Jelvehgari, Mitra, et al. Pharmaceutical sciences, 2015, 21(2), 102-110.
In order to improve the oral bioavailability of ergotamine tartrate (ET), a rapidly dissolving oral ET/CA film delivery system was developed in this work, considering that caffeine (CA) can increase the speed and degree of water solubility of ET.
· Preparation of ET/CA Film
Rapidly dissolving films (ET and CA) were successfully prepared by solvent casting using low viscosity grade hydroxypropyl methylcellulose (HPMC E-15) as film-forming polymer and propylene glycol as plasticizer. The optimal drug/polymer ratios in ET/CA films were 1:20 (E2) and 1:4 (C2), respectively. The weights of E2 and C2 films were 9.9 and 3.2 mg, respectively, the thicknesses were 74 and 45 μm, respectively, the folding endurances were 120.66 and up to 300 times, and the drug contents were 0.38 and 0.52 mg/cm2, respectively.
· Performance of ET/CA Film
The average disintegration time of the optimized film was within 26-165 s, and the release was 59.09-101.34% within 2 h. The film was non-irritating, had good film properties, and showed sufficient mucoadhesion potential before the drug was absorbed from the formulation. In addition, it was demonstrated that the combination of ET and CA film for oral delivery can treat migraine, avoiding the disadvantages of the oral route.