US2018243210A1PendingUtilityA1

Method for treating intestinal fibrosis

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Assignee: SIGMOID PHARMA LTDPriority: Feb 21, 2013Filed: May 1, 2018Published: Aug 30, 2018
Est. expiryFeb 21, 2033(~6.6 yrs left)· nominal 20-yr term from priority
Inventors:Ivan CoulterVincenzo Aversa
A61P 43/00A61K 31/223A61K 31/58A61K 9/1641A61K 9/0053A61K 9/1623A61K 9/1652A61K 9/1617A61K 9/4891A61K 9/5042A61K 9/1658A61K 9/4808A61P 1/00A61K 9/5036A61K 9/1611A61K 9/1694A61K 9/50A61K 31/502A61K 31/56A61K 38/13A61P 1/04A61K 9/16A61K 2300/00
55
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Claims

Abstract

A method for treating intestinal fibrosis in a subject, comprising enterally administering a steroid to the subject. The steroid may be in a multiple minibead formulation.

Claims

exact text as granted — not AI-modified
We claim: 
     
         1 . An oral steroid formulation, the formulation being a multiple minibead formulation wherein the minibeads comprise a water-soluble polymer matrix in which a steroid is distributed, wherein the steroid is distributed in the polymer matrix in any of the following forms:
 a) as a solution in the polymer matrix;   b) dissolved in a disperse phase;   c) as particles dispersed in a disperse phase;   d) dissolved in the aqueous phase of a water-in-oil or water-in-wax emulsion dispersed in the polymer matrix.   
     
     
         2 . The formulation according to  claim 1 , wherein the steroid is a steroid susceptible to first pass metabolism. 
     
     
         3 . The formulation according to  claim 2 , wherein the steroid susceptible to first pass metabolism is selected from budesonide, flunisolide, fluticasone proprionate, rimexolone, butixocort, tixocortol and beclomethasone and the salts and esters, thereof. 
     
     
         4 . The formulation according to  claim 2  wherein the steroid is budesonide, or an ester thereof. 
     
     
         5 . The formulation according to  claim 1 , wherein the steroid is dissolved in a disperse phase. 
     
     
         6 . The formulation according to  claim 1 , wherein the composition comprises a dispersed phase distributed within the matrix. 
     
     
         7 . The formulation according to  claim 6 , wherein the dispersed phase comprises an oil. 
     
     
         8 . The formulation according to  claim 5 , wherein the dispersed phase comprises olive oil, sesame oil, coconut oil, palm kernel oil, medium chain triglycerides, linoleoyl macrogolglycerides (polyoxylglycerides), caprylocaproyl macrogolglycerides and caprylic/capric triglycerides, 2-(2-ethoxyethoxy)ethanol, poly(ethylene glycol) or a combination thereof. 
     
     
         9 . The formulation according to  claim 5 , wherein the dispersed phase comprises at least one surfactant. 
     
     
         10 . The formulation according to  claim 5 , wherein the disperse phase comprises a liquid or a wax which has a melting temperature of no more than 37° C. 
     
     
         11 . The formulation according to  claim 10 , wherein the liquid or wax comprises a macrogol ester. 
     
     
         12 . The formulation according to  claim 11 , wherein the macrogol ester is selected from macrogol 25 cetostearyl ether, macrogol 6 cetostearyl ether, macrogol glycerol ricinoleate 35, macrogol-glycerol hydroxystearate 40 or macrogol-15-hydroxystearate. 
     
     
         13 . The formulation according to  claim 12 , wherein the macrogol ester is macrogol-15-hydroxystearate. 
     
     
         14 . The formulation according to  claim 5 , wherein the disperse phase comprises a liquid or a wax which is solid or semi-solid at ambient temperature. 
     
     
         15 . The formulation according to  claim 14 , wherein the liquid or wax comprises a macrogol ester. 
     
     
         16 . The formulation according to  claim 15 , wherein the macrogol ester is selected from macrogol 25 cetostearyl ether, macrogol 6 cetostearyl ether, macrogol glycerol ricinoleate 35, macrogol-glycerol hydroxystearate 40 or macrogol-15-hydroxystearate. 
     
     
         17 . The formulation according to  claim 16 , wherein the macrogol ester is macrogol-15-hydroxystearate 
     
     
         18 . The formulation according to  claim 10  wherein the liquid or wax comprises a medium chain triglyceride. 
     
     
         19 . The formulation according to  claim 1 , which is adapted to release:
 the steroid at least in the colon; or   the steroid at least in the ileum; or   the steroid at least in the jejunum; or   the steroid at least in the duodenum.   
     
     
         20 . The formulation according to  claim 1 , which is an immediate release formulation. 
     
     
         21 . The formulation according to  claim 1 , which is a controlled release formulation, the steroid being in solution in the formulation. 
     
     
         22 . The formulation according to  claim 1 , wherein the minibeads comprise a coating. 
     
     
         23 . The formulation according to  claim 22 , wherein the coating is a controlled release coating. 
     
     
         24 . The formulation according to  claim 22 , wherein the coating is adapted to release the steroid in the colon. 
     
     
         25 . The formulation according to  claim 22 , wherein the coating comprises a polymeric material. 
     
     
         26 . The formulation according to  claim 25 , wherein the polymeric material comprises methacrylic acid co-polymers, ammonio methacrylate co-polymers, polysaccharides, ethylcellulose, methacrylic acid, methyl acrylate, methyl methacrylate, hydroxypropyl methylcellulose, cellulose acetate phthalate, cellulose acetate succinate, cellulose hydrogen phthalate, cellulose acetate trimellitate, hydroxypropyl-methylcellulose phthalate, hydroxypropyl methylcellulose acetate succinate, starch acetate phthalate, amylose acetate phthalate, polyvinyl acetate phthalate, polyvinyl butyrate phthalate or a combination thereof. 
     
     
         27 . The formulation according to  claim 1 , wherein the minibeads are seamless minibeads that comprise the water-soluble polymer matrix and, dispersed in the matrix, a disperse phase comprising materials selected from hydrophobic and amphiphilic materials, and combinations thereof, the steroid being included in the dispersed phase. 
     
     
         28 . The formulation according to  claim 1 , wherein the polymer comprises or consists of gelatin or another thermotropic hydrogel-forming polymer, or a combination thereof. 
     
     
         29 . The formulation according to  claim 1 , wherein the composition further comprises one, two or three of active agents (a), (b) and (c) below:
 (a) an immunosuppressant;   (b) a promoter of the expression or activity of hypoxia-inducible factor;   (c) another anti-fibrotic agent.   
     
     
         30 . The formulation according to  claim 28 , wherein the composition comprises a promoter of the expression or activity of hypoxia-inducible factor selected from hydroxylase inhibitors. 
     
     
         31 . The formulation according to  claim 1 , wherein the formulation further comprises at least one of the following active agent(s), cyclosporin A, DMOG, hydralazine, FG-4497, FG4095, AGN-2979, metirosine, 3-iodotyrosine, aquayamycin, bulbocapnine, oudenone, TM 6008, TM 6089, siRNAs against hydroxylases, antisense therapeutics against hydroxylases, caspase inhibitors, peroxisome proliferator-activated receptor-g (PPAR-g) agonists, pioglitazone, TGF-b blockers, colchicines, relaxin, adiponectin, endothelin A, angiotensin receptor blockers, cannabinoids, agents altering the MMP-TIMP balance, a wound healing agent, Ilodecakin and Mannose-6-Phosphate.

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