US2019381131A1PendingUtilityA1

Formulations

58
Assignee: SUBLIMITY THERAPEUTICS LTDPriority: Nov 8, 2013Filed: Jul 2, 2019Published: Dec 19, 2019
Est. expiryNov 8, 2033(~7.3 yrs left)· nominal 20-yr term from priority
Inventors:Ivan CoulterVincenzo AversaMónica Torres RosaBernard Francis Mcdonald
A61P 43/00A61P 37/06A61P 35/00A61P 29/00A61P 1/00A61P 15/08A61P 1/04A61K 9/5036A61K 9/0053A61K 9/5073A61K 9/4858A61K 9/4866A61K 38/13A61K 47/14A61K 47/36A61K 47/20A61K 9/5047A61K 9/5089A61K 9/1658A61K 31/635A61K 31/502A61K 47/42A61K 31/196A61K 47/10A61K 9/5026
58
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Claims

Abstract

The present invention relates to a formulation comprising a pharmaceutically active ingredient and a coating. The invention also relates to the use of the formulation in the treatment and prevention of disorders of the gastrointestinal tract. Also disclosed are methods for preparing the formulations.

Claims

exact text as granted — not AI-modified
What is claimed is: 
     
         1 . A pharmaceutical formulation comprising a population of minibeads presented in a unit dosage form for oral administration, said minibeads each comprising a core and a first coating, wherein:
 the population comprises minibeads having a largest cross sectional dimension of from about 0.5 mm to about 2.5 mm;   the core is in the form of a solid colloid, the colloid comprising a continuous phase and a disperse phase;   the continuous phase comprises a gelatin matrix, the matrix comprising an anionic surfactant and optionally a plasticiser selected from glycerin, a polyol, polyethylene glycol, triethyl citrate or a mixture thereof;   the disperse phase is a hydrophobic phase that comprises cyclosporin A in solution and a non-ionic surfactant;   the first coating comprises at least 50% by weight of the first coating of one or more film-forming polymers and optionally, in addition to film-forming polymer(s), one or more other components other than film-forming polymers;   the one or more film-forming polymers present in the first coating are one or more water soluble cellulose ethers selected from the group consisting of hydroxyethyl cellulose, hydroxypropyl cellulose, hydroxyethyl methylcellulose and hydroxypropylmethyl cellulose and combinations thereof, provided that hydroxypropylmethyl cellulose is at least one of the film-forming polymers;   the first coating is present in an amount corresponding to a weight gain due to the coating of from 9% to 15% by weight of the core.   
     
     
         2 . A pharmaceutical formulation of  claim 1 , wherein the first coating is present in an amount corresponding to a weight gain due to the coating of from 10% to 15% by weight of the core. 
     
     
         3 . A pharmaceutical formulation of  claim 1 , wherein the minibeads further comprise a second coating and the second coating comprises a single polymer being a delayed release pH independent polymer. 
     
     
         4 . The pharmaceutical formulation of  claim 3 , wherein the second coating is in contact with the first coating comprising a water-soluble cellulose ether. 
     
     
         5 . The pharmaceutical formulation of  claim 3 , wherein the second coating is present in an amount corresponding to a weight gain due to the second coating of from 2% to 40%. 
     
     
         6 . The pharmaceutical formulation of  claim 3 , wherein the delayed release pH independent polymer is water-soluble or water-permeable in an aqueous medium with a pH greater than 6.5. 
     
     
         7 . The pharmaceutical formulation of  claim 3 , wherein the delayed release pH independent polymer comprises ethyl cellulose. 
     
     
         8 . A pharmaceutical formulation of  claim 1 , wherein the anionic surfactant is at least one surfactant selected from fatty acid salts and bile salts. 
     
     
         9 . A pharmaceutical formulation of  claim 1 , wherein the anionic surfactant is an alkyl sulphate salt. 
     
     
         10 . A pharmaceutical formulation of  claim 1 , wherein the anionic surfactant is sodium dodecyl sulphate. 
     
     
         11 . A pharmaceutical formulation of  claim 1 , wherein the disperse phase comprises a medium chain mono- di- or triglyceride, a polyethoxylated castor oil and 2-(ethoxyethoxy)ethanol. 
     
     
         12 . A pharmaceutical formulation of  claim 11 , wherein the medium chain mono-di- or triglyceride is a medium chain triglyceride. 
     
     
         13 . A pharmaceutical formulation of  claim 1 , wherein the non-ionic surfactant is selected from sorbitan-based surfactants, PEG-fatty acids, glyceryl fatty acids and poloxamers. 
     
     
         14 . A pharmaceutical formulation of  claim 1 , wherein the non-ionic surfactant is polyethoxylated castor oil. 
     
     
         15 . A pharmaceutical formulation of  claim 1 , wherein the disperse phase comprises a solvent. 
     
     
         16 . A pharmaceutical formulation of  claim 15 , wherein the solvent is 2-(ethoxyethoxy)ethanol. 
     
     
         17 . A minibead for oral administration, said minibead comprising a core and a single coating, wherein:
 the minibead has a largest cross sectional dimension of from about 0.5 mm to about 2.5 mm;   the core is in the form of a solid colloid, the colloid comprising a continuous phase and a disperse phase;   the continuous phase comprises a gelatin matrix, the matrix comprising an anionic surfactant and optionally a plasticiser selected from glycerin, a polyol, polyethylene glycol, triethyl citrate or a mixture thereof;   the disperse phase is a hydrophobic phase that comprises cyclosporin A in solution and a non-ionic surfactant;   the coating comprises at least 50% by weight of the coating of one or more film-forming polymers and optionally, in addition to film-forming polymer(s), one or more other components other than film-forming polymers;   the one or more film-forming polymers present in the coating are one or more water soluble cellulose ethers selected from the group consisting of hydroxyethyl cellulose, hydroxypropyl cellulose, hydroxyethyl methylcellulose and hydroxypropylmethyl cellulose and combinations thereof, provided that hydroxypropylmethyl cellulose is at least one of the film-forming polymers;   the coating is present in an amount corresponding to a weight gain due to the coating of from 9% to 15% by weight of the core.   
     
     
         18 . The minibead of  claim 17 , wherein the coating is present in an amount corresponding to a weight gain due to the coating of from 10% to 15% by weight of the core. 
     
     
         19 . A pharmaceutical formulation of  claim 17 , wherein the minibeads further comprise a second coating and the second coating comprises a single polymer being a delayed release pH independent polymer. 
     
     
         20 . The pharmaceutical formulation of  claim 19 , wherein the second coating is in contact with the first coating comprising a water-soluble cellulose ether. 
     
     
         21 . The pharmaceutical formulation of  claim 19 , wherein the second coating is present in an amount corresponding to a weight gain due to the second coating of from 2% to 40%. 
     
     
         22 . The pharmaceutical formulation of  claim 19 , wherein the delayed release pH independent polymer is water-soluble or water-permeable in an aqueous medium with a pH greater than 6.5. 
     
     
         23 . The pharmaceutical formulation of  claim 19 , wherein the delayed release pH independent polymer comprises ethyl cellulose. 
     
     
         24 . The minibead of  claim 17 , wherein the anionic surfactant is at least one surfactant selected from fatty acid salts and bile salts. 
     
     
         25 . The minibead of  claim 17 , wherein the anionic surfactant is an alkyl sulphate salt. 
     
     
         26 . The minibead of  claim 17 , wherein the anionic surfactant is sodium dodecyl sulphate. 
     
     
         27 . The minibead of  claim 17 , wherein the disperse phase comprises a medium chain mono- di- or triglyceride, a polyethoxylated castor oil and 2-(ethoxyethoxy)ethanol. 
     
     
         28 . The minibead of  claim 27 , wherein the medium chain mono- di- or triglyceride is a medium chain triglyceride. 
     
     
         29 . The minibead of  claim 17 , wherein the non-ionic surfactant is selected from sorbitan-based surfactants, PEG-fatty acids, glyceryl fatty acids and poloxamers. 
     
     
         30 . The minibead of  claim 17 , wherein the non-ionic surfactant is polyethoxylated castor oil. 
     
     
         31 . The minibead of  claim 17 , wherein the disperse phase comprises a solvent. 
     
     
         32 . The minibead of  claim 31 , wherein the solvent is 2-(ethoxyethoxy)ethanol. 
     
     
         33 . The pharmaceutical formulation of  claim 1 , wherein the coating comprises at least 60% by weight of the coating of one or more film-forming polymers. 
     
     
         34 . The pharmaceutical formulation of  claim 1 , wherein the coating comprises from 50% to 90% by weight of the coating of one or more film-forming polymers. 
     
     
         35 . The pharmaceutical formulation of  claim 1 , wherein the coating comprises from 60% to 80% by weight of the coating of one or more film-forming polymers. 
     
     
         36 . The minibead of  claim 17 , wherein the coating comprises at least 60% by weight of the coating of one or more film-forming polymers. 
     
     
         37 . The minibead of  claim 17 , wherein the coating comprises from 50% to 90% by weight of the coating of one or more film-forming polymers. 
     
     
         38 . The minibead of  claim 17 , wherein the coating comprises from 60% to 80% by weight of the coating of one or more film-forming polymers.

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