Claims for Patent: 9,173,944

Summary for Patent: 9,173,944

Title:	Formulation suitable for stabilizing proteins, which is free of mammalian excipients
Abstract:	A formulation free of protein which stabilizes pharmaceutical active proteins, peptides, or mixtures thereof in large scale production processes comprising a mixture of a hydrophilic polymer and a non-ionic detergent, and a mixture of a polyalcohol and a sugar. In some embodiments the polyalcohol is absent.
Inventor(s):	Taylor; Harold Victor (Frankfurt am Main, DE), Mander; Gerd J. (Frankfurt am Main, DE), Burger; Markus (Frankfurt am Main, DE)
Assignee:	MERZ PHARMA GmbH & CO. KGaA (Frankfurt am Main, DE)
Application Number:	13/878,629
Patent Claims:	1. A formulation free of proteins comprising, (a) a hydrophilic polymer; (b) a sugar; (c) a non-ionic detergent; and (d) a polyalcohol, wherein the weight ratio of polyalcohol to sugar is from 2:1 to 5:1 (wt-%), wherein the weight ratio between the hydrophilic polymer and the non-ionic detergent is from 18:1 to 22:1 (wt-%), and wherein the non-ionic detergent is present in said formulation in an amount between 0.2 and 0.01 mg/g. 2. A formulation free of proteins comprising, (a) a hydrophilic polymer; (b) a sugar; and (c) a non-ionic detergent, wherein the weight ratio between the hydrophilic polymer and the non-ionic detergent is from 2:1 to 30:1 (wt-%), and wherein the non-ionic detergent is present in the formulation in an amount between 0.2 and 0.01 mg/g, and wherein no polyalcohol is present. 3. The formulation of claim 1, wherein the hydrophilic polymer is selected from the group consisting of hyaluronic acid, polyvinylpyrollidone (PVP), copolymers of N-vinylpyrollidone, a cellulose derivative, Polyethyleneglycol (PEG), PEG/PPG block copolymers, homo- and copolymers of acrylic and methacrylic acid, polyurethanes, polyvinyl alcohol, polyvinylethers, maleic anhydride based copolymers, polyesters, vinylamines, polyethyleneimines, polyethyleneoxides, poly(carboxylic acids), polyamides, polyanhydrides, polyphosphazenes, and mixtures thereof. 4. The formulation of claim 1, wherein the polyalcohol is selected from the group consisting of mannitol, inositol, lactilol, isomalt, xylitol, erythritol, sorbitol, and mixtures thereof. 5. The formulation of claim 1, wherein the sugar is selected from the group consisting of monosaccharides, disaccharides, polysaccharides, and mixtures thereof. 6. The formulation of claim 1, which is in the form of a composition further comprising a pharmaceutically active peptide, a protein or a mixture thereof. 7. The composition of claim 6, which is lyophilized. 8. The composition of claim 6, wherein said pharmaceutically active protein is selected from the group consisting of toxins, chondroitin, elastin, actin, myosin, aprotinin, growth hormone, growth hormone releasing factor, parathyroid hormone, thyroid stimulating hormone, lipoproteins (LDL, IDL, VLDL, VHDL, HDL), apolipoproteins (ApoA-1, ApoA-II, ApoA-IV, ApoC-I, ApoC-II, ApoC-III, ApoD, ApoE), .alpha.-1 Antitrypsin, insulin, proinsulin, follicle stimulating hormone, calcitonin, oxytocin, vasopressin, leuprolide acetate, somatostatin, luteinizing hormone, glucagons, clotting factors, anti-clotting factors, plasminogen activator, human macrophage inflammatory protein, vascular endothelin growth factor (VEGF), rheumatoid factors, Done derived neurotrophic factor (BDNF), nerve growth factor-.beta. (NGF-.beta.), platelet-derived growth factor (PDGF), fibroblast growth factor (FGF), epidermal growth factor (EGF), transforming growth factor (TGF-.beta.1, TGF-.beta.2, TGF-.beta.3, TGE-.beta.4, TGE-.beta.5), erythropoietin, interleukins (IL-1 to IL-10), bone morphogenic protein (BMP) parathyroid hormone, DNAse, cationic ferritin, interferon .alpha., interferon .beta., interferon .gamma., and mixtures thereof. 9. The composition of claim 6, wherein the pharmaceutically active protein is selected from the group consisting of Botulinum toxin, diphtheria toxin, tetanus toxin and mixtures thereof. 10. The composition of claim 9, which comprises botulinum toxin, hyaluronic acid, mannitol, sucrose, polysorbate 80 and, optionally, water for injection. 11. The composition of claim 6, which is comprised in a medicament, a cosmetic product, a cosmeceutical product or a diagnostic product. 12. An injectable solution comprising the composition of claim 11. 13. A kit comprising, (a) one or more containers comprising the composition of claim 6; and (b) instructions for use of the composition. 14. A method for stabilizing pharmaceutically active proteins, peptides, or mixtures thereof, comprising admixing such pharmaceutically active protein, peptide, or a mixture thereof, with the formulation of claim 1. 15. The kit of claim 13, further comprising a container of a pharmaceutically acceptable sterile solvent selected from the group consisting of water for injection, isotonic salt solution, Ringer's solution, pH-buffered solution, an aqueous solution of 5% glucose, and mixtures thereof.

Details for Patent 9,173,944

Applicant	Tradename	Biologic Ingredient	Dosage Form	BLA	Approval Date	Patent No.	Expiredate
Bayer Healthcare Pharmaceuticals Inc.	TRASYLOL	aprotinin	Injection	020304	12/29/1993		2030-10-12
Nps Pharmaceuticals, Inc.	NATPARA	parathyroid hormone	For Injection	125511	01/23/2015		2030-10-12