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1. (WO2018089570) PHARMACEUTICAL FORMULATION FOR SUBLINGUAL OR BUCCAL DELIVERY OF EPINEPHRINE

Pub. No.:    WO/2018/089570    International Application No.:    PCT/US2017/060761
Publication Date: Fri May 18 01:59:59 CEST 2018 International Filing Date: Fri Nov 10 00:59:59 CET 2017
IPC: A61K 31/137
Applicants: IONO PHARMA, LLC
Inventors: ALMOAZEN, Hassan
HAYNES, Lindsay
Title: PHARMACEUTICAL FORMULATION FOR SUBLINGUAL OR BUCCAL DELIVERY OF EPINEPHRINE
Abstract:
The present invention relates to a pharmaceutical composition for the treatment of anaphylaxis formulated for rapid delivery, in one embodiment, the delivery vehicle is a rapidly dissolvmg film. The films contain an epinephrine or a novel epinephrine pro-drag for fee rapid treatment of anaphylaxis in a patient. This invention relates to pharmaceutical compositions made by modifying the physicoehemieal properties of epinephrine in order to enhance its permeability through biological membranes (sublingual and buccal membranes). Several prodrugs of epinephrine are shown by modifying the two hydroxyl (phenolic) groups in positions 3 and 4 on the benzene ring, by chemically reacting the two groups with several acid moieties to form an ester bond with different alkyl chains. The addition of an alkyl group will enhance the lipophilicity of epinephrine (increase log P) and will consequently increase its permeability through the biological membranes (sublingual and buccal tissues in the oral cavity).