Claims for Patent: 9,107,822

Summary for Patent: 9,107,822

Title:	Water-in oil type emulsion for treating a disease of the eye
Abstract:	The invention relates to a composition for administering with a sustained release kinetic a therapeutically effective amount of a therapeutic agent to a subject in need thereof for treating diseases or conditions of the eye, wherein the composition is an water-in-oil type emulsion comprising an oil phase, a lipophilic surfactant dissolved in the oil phase, an aqueous phase dispersed in the oil phase, a hydrophilic therapeutic agent dissolved in the aqueous dispersed phase, and wherein the composition is intraocularly injectable, wherein the composition has a density lower than 1. The invention also relates to a pharmaceutical composition or to a medicament comprising the composition of the invention, and to a method for treating a condition or disease of the eye comprising administering a therapeutic amount of the composition of the invention. The invention also relates to a device comprising the composition of the invention.
Inventor(s):	Lallemand; Frederic (Fresnes, FR), Garrigue; Jean-Sebastien (Verrieres-le-Buisson, FR), Philips; Betty (Antony, FR)
Assignee:	SANTEN SAS (Evry, FR)
Application Number:	13/820,456
Patent Claims:	1. A composition comprising a water-in-oil emulsion comprising an oil phase, a lipophilic surfactant dissolved in the oil phase, an aqueous phase dispersed in the oil phase, a hydrophilic therapeutic agent dissolved in the aqueous dispersed phase, and wherein the composition: has a density lower than the density of water; has a viscosity ranging from 25 to 10 000 mPas at 20.degree. C.; has droplets of water ranging from 20 nm to 600 nm; and is formulated for intraocular injection. 2. The composition of claim 1, wherein the composition has a density ranging from 0.91 to 0.97 g/cm.sup.3. 3. The composition of claim 1, wherein the oil phase comprises at least one triglyceride, monoglyceride, diglyceride, vegetable oil, or mineral oil. 4. The composition of claim 3, further defined as comprising a medium chain or long chain triglyceride. 5. The composition of claim 1, wherein the lipophilic surfactant comprises at least one sorbitan ester, bentonite, glycerol monostearate, or propylene glycol monolaurate. 6. The composition of claim 5, further defined as comprising sorbitan stearate, sorbitan laurate, or sorbitan monopalmitate. 7. The composition of claim 1, wherein the aqueous phase is present in an amount ranging from 0.1 to less than 50% in weight to the total weight of the composition. 8. The composition of claim 7, wherein the aqueous phase is present in an amount ranging from 0.5 to 15% w/w. 9. The composition of claim 8, wherein the aqueous phase is present in an amount ranging from 2 to 10% w/w. 10. The composition of claim 1, wherein the hydrophilic therapeutic agent is a monoclonal antibody (full or fragment Fab), an anti-angiogenic molecule, a ROCK (Rho-kinases) inhibitor, a protein, WNT3A protein, a growth factor, a siRNA, an oligonucleotide, an iron chelating molecule, an anti-inflammatory molecule, an antibiotic, or a cortico-steroid. 11. The composition of claim 10, wherein the hydrophilic therapeutic agent is ranibizumab, bevacizumab trastuzumab, cituximab, rituximab, pegaptanib, fasudil, anti-CD160 S-HLA-G, epithelium growth factors (EGF), anti-EGF, TGF (Transforming growth factor), siRNA anti-arginase, miRNA, antisense DNA, antisense RNA, deferiprone, salicylaldehyde isonicotinoyl hydrazone, epigallocatechin gallate, linezolide, clavulamic acid, macrolide, or dexamethasone including its hydrophilic derivatives. 12. The composition of claim 1, further comprising a lipophilic therapeutic agent dissolved in the oil phase, the lipophilic therapeutic agent further defined as comprising cyclosporine A lutein, alpha-tocopherol, and/or dexamethasone palmitate. 13. The composition of claim 1, further comprising viscosity modifying agents, pH buffering agents, and/or osmolality modifying agents. 14. The composition of claim 13, further defined as comprising at least one of a hydrogel of sodium hyaluronate, carbopol gel, hydroxyethyl cellulose, dextran, carboxymethyl cellulose, PEG, polyvinyl alcohol, collagen; phosphate, citrate, tris, histidine, or acetate buffer; NaCl, KCl, CaCl.sub.2, glycerol, mannitol, alpha-trehalose and/or propylene glycol. 15. The composition of claim 1, further comprising one or more pharmaceutically acceptable excipient.

Details for Patent 9,107,822

Applicant	Tradename	Biologic Ingredient	Dosage Form	BLA	Approval Date	Patent No.	Expiredate
Genentech, Inc.	RITUXAN	rituximab	Injection	103705	11/26/1997		2030-09-03
Idec Pharmaceuticals Corp.	RITUXAN	rituximab	Injection	103737	02/19/2002		2030-09-03
Genentech, Inc.	HERCEPTIN	trastuzumab	For Injection	103792	09/25/1998		2030-09-03
Genentech, Inc.	HERCEPTIN	trastuzumab	For Injection	103792	02/10/2017		2030-09-03
Genentech, Inc.	AVASTIN	bevacizumab	Injection	125085	02/26/2004		2030-09-03
Genentech, Inc.	LUCENTIS	ranibizumab	Injection	125156	06/30/2006		2030-09-03