PHARMACEUTICAL COMPOSITION FOR PARENTERAL ADMINISTRATION OF IDEBENONE
The invention describes use of an injectable form of Idebenone, suitable for intravenous injection or infusion. The proposed formulation is an oil-in-water emulsion, where Idebenone is associated with the oil droplets.
1 . A sterile pharmaceutical composition for parenteral administration of Idebenone, said composition comprises an oil-in-water emulsion, stabilized with pharmaceutically acceptable surfactants and stabilizers, in which Idebenone is dissolved in a water-immiscible oil phase.
2 . A composition as set forth in claim 1 wherein said oil phase is comprised of pharmaceutically acceptable long chain triglycerides.
3 . A composition as set forth in claim 1 wherein said oil phase is comprised of pharmaceutically acceptable medium chain triglycerides.
4 . A composition as set forth in claim 1 wherein said oil phase is comprised of pharmaceutically acceptable acetylated monoglycerides or diglycerides.
5 . A composition as set forth in claim 1 wherein said oil phase is comprised of mixture of long chain triglycerides and acetylated monoglycerides or diglycerides.
6 . A composition as set forth in claim 1 wherein said oil phase is comprised of mixture of long chain triglycerides and medium chain triglycerides with omega-3-acid triglycerides (fish oil).
7 . A composition as set forth in claim 1 wherein said oil phase may additionally be comprised of fatty acids
8 . A composition as set forth in claim 1 further comprising pharmaceutically acceptable stabilizers, selected from group of natural or synthetic phospholipids.
9 . A stabilizer as set forth in claim 8 , wherein said phospholipid is phosphatidylcholine, phosphatidylethanolamine or a mixture thereof.
10 . A stabilizer as set forth in claim 8 , wherein said phospholipid is soy lecithin or egg lecithin.
11 . A stabilizer as set forth in claim 8 , wherein said phospholipid is hydrogenated lecithin.
12 . A stabilizer as set forth in claim 8 , wherein said phospholipid is synthetic phospholipid.
13 . A stabilizer as set forth in claim 12 , wherein said synthetic phosphatidylcholine contains PEG moiety.
14 . A composition as set forth in claim 1 which may additionally contain pharmaceutically acceptable non-ionic surfactants or anionic surfactants.
15 . A composition as set forth in claim 14 wherein said non-ionic surfactant is selected from a group of polyethoxylated esters or ethers of fatty acids, fatty alcohols or sorbitane or fatty acid esters of sugars and polyols.
16 . A composition as set forth in claim 14 wherein said anionic surfactant is selected from a group of sodium oleate, sodium stearate or sodium deoxycholate.
17 . A composition as set forth in claim 15 wherein said surfactant is polyoxyethylene sorbitan fatty acid ester.
18 . A composition as set forth in claim 15 wherein said surfactant is polyethoxylated castor oil.
19 . A composition as set forth in claim 15 wherein said surfactant is polyethoxylated (4-hydroxy)stearic acid Solutol® HS-15.
20 . A composition as set forth in claim 15 wherein said surfactant is PEG stearate or PEG distearate.
21 . A composition as set forth in claim 15 wherein said surfactant is polyoxyethylene alkylether.
22 . A composition as set forth in claim 15 wherein said surfactant is d-alpha tocopheryl polyethylene glycol 1000 succinate (Vitamin E TPGS).
23 . A composition as set forth in claim 15 wherein said surfactant is p-(isooctyl)polyoxyethylene phenolformaldehyde polymer (Tyloxapol®).
24 . A composition as set forth in claim 15 wherein said surfactant is Poloxamer.
25 . A composition as set forth in claim 1 , comprised of 0.05-2.5% of idebenone, 5-60% of the oil phase, 0.1-10% of phospholipid stabilizer, 0-10% of the surfactant and 20-90% of the aqueous phase.
26 . A composition as set forth in claim 25 , intended for parenteral administration, non-diluted or diluted via intravenous injection or intravenous infusion.
27 . A composition as set forth in claim 25 , sterilized by sterile filtration.
28 . A composition as set forth in claim 25 , sterilized by moist heat sterilization.
29 . A composition as set forth in claim 25 , sterilized by gamma-irradiation.
30 . A composition as set forth in claim 25 , sterilized by electron beam sterilization.