US2020009218A1PendingUtilityA1

Oral pharmaceutical composition

69
Assignee: SUBLIMITY THERAPEUTICS LTDPriority: Apr 4, 2007Filed: Jul 11, 2019Published: Jan 9, 2020
Est. expiryApr 4, 2027(~0.7 yrs left)· nominal 20-yr term from priority
Inventors:Ivan Coulter
A61P 43/00A61P 37/06A61P 37/04A61P 37/00A61P 3/10A61P 31/00A61P 3/00A61P 25/28A61P 1/12A61P 1/00A61P 19/02A61P 1/10A61P 1/04A61K 35/741A61K 9/5057A61K 9/5015A61K 38/28A61K 9/0053A61K 31/439A61K 31/635A61K 2039/55583A61K 31/436A61K 45/06A61K 9/5042A61K 38/13A61K 9/5026A61K 9/5047A61K 9/5073A61K 39/0005A61K 9/50A61K 9/5089
69
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References
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Claims

Abstract

An oral composition comprising minicapsules wherein the minicapsules comprise one or more therapeutic prophylactic substances in a liquid, semi-liquid, or solid core. The minicapsules have release profiles to release the substance in an active form at one or more sites along the gastro-intestinal tract to maximise absorption and/or therapeutic efficiency.

Claims

exact text as granted — not AI-modified
1 - 91 . (canceled) 
     
     
         92 . A method for the treatment of inflammatory bowel disease, wherein the method comprises administering to a patient in need thereof a therapeutically effective amount of an oral composition comprising minicapsules wherein the minicapsules comprise an active pharmaceutical in a liquid, semi-solid, or solid core, the minicapsules having release profiles to release the active pharmaceutical in an active form at one or more sites along the gastrointestinal tract; wherein the active pharmaceutical is selected from:
 an immunosuppressant;   a hydroxylase inhibitor or   a combination thereof.   
     
     
         93 . The method of  claim 92 , wherein the inflammatory bowel disease is selected from ulcerative colitis or Crohn's disease. 
     
     
         94 . The method of  claim 92 , wherein the active pharmaceutical is a hydroxylase inhibitor. 
     
     
         95 . The method of  claim 94 , wherein the hydroxylase inhibitor is selected from a propyl hydroxylase inhibitor or an asparaginyl hydroxylase inhibitor. 
     
     
         96 . The method of  claim 94  wherein the active pharmaceutical is DMOG. 
     
     
         97 . The method of  claim 92  wherein the active pharmaceutical is hydralazine. 
     
     
         98 . The method of  claim 92  wherein the active pharmaceutical is FG4095. 
     
     
         99 . The method of  claim 92 , wherein the minicapsules further comprise an excipient selected from an excipient to maximize permeability of the active pharmaceutical compound(s) in the colon, an excipient to maximize solubility of the active pharmaceutical compound(s) in the colon, and combinations thereof. 
     
     
         100 . The method of  claim 92  wherein the minicapsules comprise a gelling agent encapsulating the active pharmaceutical. 
     
     
         101 . The method of  claim 92  wherein the active pharmaceutical is an immunosuppressant and the minicapsules are minicapsules in which the immunosuppressant is as a solubilised formulation encapsulated with a gelling agent and have the characteristics of minicapsules obtained by a process utilising surface tension of different solutions and comprising ejecting through a nozzle having a single orifice a hydrophobic solution or suspension and a solution comprising a gelling agent, to form into a spherical form and fall into a cooling air flow or into a cooling or hardening solution whereby the gelling agent is gelled and encapsulates the hydrophobic suspension or solution. 
     
     
         102 . The method of  claim 92  wherein the minicapsules comprise a gelling agent encapsulating solubilised active and are coated to target release to the ileum and/or the colon. 
     
     
         103 . The method of  claim 92  wherein the active is as a hydrophobic solution. 
     
     
         104 . The method of  claim 92  wherein the minicapsules comprise an emulsion comprising a gelling agent which emulsion is in extruded, gelled and dried form. 
     
     
         105 . The method of  claim 104  wherein the active pharmaceutical is an immunosuppressant and the immunosuppressant is solubilised in a hydrophobic solution and the minicapsules comprise gelatin as a gelling agent. 
     
     
         106 . The method of  claim 105  wherein the minicapsules further comprise a hydroxylase inhibitor. 
     
     
         107 . The method of  claim 92  wherein the active pharmaceutical is protected from the environment of the upper gastrointestinal tract. 
     
     
         108 . The method of  claim 92  wherein the active pharmaceutical is selected from: an immunosuppressant in combination with cyclosporin A or tacrolimus; tacrolimus or cyclosporin in combination with an antioxidant or nuclear factor kappa B inhibitor; and tacrolimus, sirolimus or cyclosporin in combination with mycophenolate motefil and/or other immunomodulators. 
     
     
         109 . The method of  claim 92  wherein the active pharmaceutical is in a solubilised liquid, semi-liquid or solid form. 
     
     
         110 . The method of  claim 92  wherein the minicapsules comprise a gelling agent encapsulating the core. 
     
     
         111 . The method of  claim 92 , wherein the minicapsules are coated to target release to the colon. 
     
     
         112 . The method of  claim 92  wherein the minicapsules comprise a gelling agent encapsulating the core and are coated with a coating selected from a modified release coating, and a controlled release coating comprising a material selected from acrylic-, methacrylic-, and ethylcellulose-based polymers and combinations thereof. 
     
     
         113 . The method of  claim 92 , wherein the active pharmaceutical is an immunosuppressant selected from cyclosporin and tacrolimus and the minicapsules further comprise another immunosuppressant, or wherein the active pharmaceutical is an immunosuppressant and the minicapsules further comprise a nuclear factor kappa B activator. 
     
     
         114 . The method of  claim 92  wherein the active pharmaceutical is an immunosuppressant and wherein the minicapsule comprises an extruded and gelled emulsion which comprises the immunosuppressant and a medium chain triglyceride, the minicapsule having a coating comprising a pH independent polymer. 
     
     
         115 . The method of  claim 114  wherein the coating comprises ethylcellulose. 
     
     
         116 . The method of  claim 92  wherein the active pharmaceutical is an immunosuppressant and is in a solubilised liquid, semi-liquid or solid form. 
     
     
         117 . The method of  claim 116  wherein the immunosuppressant is solubilised in a hydrophobic solution. 
     
     
         118 . The method of  claim 92 , wherein the release is a pH-independent release. 
     
     
         119 . The method of  claim 92  wherein the active pharmaceutical is protected from the environment of the upper gastrointestinal tract but allows abrupt and/or sustained release into the proximal colon. 
     
     
         120 . The method of  claim 92  wherein the active pharmaceutical is an immunosuppressant selected from cyclosporin A, tacrolimus or sirolimus. 
     
     
         121 . The method of  claim 92  wherein the active pharmaceutical is cyclosporin A. 
     
     
         122 . The method of  claim 92  wherein the minicapsules comprise a gelling agent encapsulating solubilised immunosuppressant and are coated to permit targeted release in the colon. 
     
     
         123 . The method of  claim 122 , wherein the immunosuppressant is cyclosporin or tacrolimus. 
     
     
         124 . The method of  claim 122  wherein the minicapsules are coated to permit targeted release in the colon and the ileum. 
     
     
         125 . The method of  claim 92 , wherein a modified release coating is applied to the minicapsule the modified release being said release in the colon. 
     
     
         126 . The method of  claim 125 , wherein the modified release coating or modified outer shell layer comprises a polymeric material that is sensitive to one or more of pH, time, thickness, erosion, and bacterial breakdown. 
     
     
         127 . The method of  claim 92 , wherein the minicapsules comprise an emulsion comprising a gelling agent which emulsion is in extruded and gelled form, the minicapsules comprising a polymeric material that is sensitive to one or more of pH, time, thickness, erosion, and bacterial breakdown. 
     
     
         128 . The method of  claim 127 , wherein a coating comprises the polymeric material, the material being selected from the group consisting of acrylic-, methacrylic-, and ethylcellulose-based polymers and combinations thereof. 
     
     
         129 . The method of  claim 127 , wherein the emulsion is in extruded, gelled and dried form. 
     
     
         130 . A method for the treatment of a disease of the colon, wherein the method comprises administering to a patient in need thereof a therapeutically effective amount of an oral composition comprising minicapsules wherein the minicapsules comprise an active pharmaceutical in a liquid, semi-solid, or solid core, the minicapsules having release profiles to release the active pharmaceutical in an active form at one or more sites along the gastrointestinal tract; wherein the active pharmaceutical is selected from:
 an immunosuppressant;   a hydroxylase inhibitor or   a combination thereof.   
     
     
         131 . A method of  claim 130  wherein the disease of the intestine is selected from Crohn's disease, ulcerative colitis, colorectal cancer, Irritable Bowel Syndrome, constipation, diarrhoea and celiac disease. 
     
     
         132 . The method of  claim 130  wherein the minicapsules comprise a gelling agent encapsulating the active pharmaceutical. 
     
     
         133 . The method of  claim 130  wherein the minicapsules comprise an emulsion comprising a gelling agent which emulsion is in extruded, gelled and dried form. 
     
     
         134 . The method of  claim 130  wherein the active pharmaceutical is an immunosuppressant and the immunosuppressant is solubilised in a hydrophobic solution and the minicapsules comprise gelatin as a gelling agent. 
     
     
         135 . The method of  claim 130 , wherein the minicapsules are coated to target release to the colon. 
     
     
         136 . The method of  claim 130  wherein the minicapsules comprise a gelling agent encapsulating the core and are coated with a coating selected from a modified release coating, and a controlled release coating comprising a material selected from acrylic-, methacrylic-, and ethylcellulose-based polymers and combinations thereof. 
     
     
         137 . The method of  claim 130  wherein the active pharmaceutical is an immunosuppressant and wherein the minicapsule comprises an extruded and gelled emulsion which comprises the immunosuppressant and a medium chain triglyceride, the minicapsule having a coating comprising a pH independent polymer. 
     
     
         138 . The method of  claim 137  wherein the coating comprises ethylcellulose. 
     
     
         139 . The method of  claim 130  wherein the active pharmaceutical is an immunosuppressant and the immunosuppressant is solubilised in a hydrophobic solution. 
     
     
         140 . The method of  claim 130  wherein the active pharmaceutical is cyclosporin A.

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