US2012058178A1PendingUtilityA1

Liposome Composition

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Assignee: KIKUCHI HIROSHIPriority: Mar 30, 2009Filed: Mar 30, 2010Published: Mar 8, 2012
Est. expiryMar 30, 2029(~2.7 yrs left)· nominal 20-yr term from priority
Inventors:Hiroshi KikuchiKenji HyodoHiroshi Ishihara
A61P 35/00A61K 31/357A61K 9/1277A61K 9/1278A61K 9/127A61K 47/02A61K 9/1271A61K 47/18
49
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Claims

Abstract

The present invention provides a novel liposome composition containing eribulin or its pharmacologically permissible salt, and its method of manufacture.

Claims

exact text as granted — not AI-modified
What is claimed is: 
     
         1 . A liposome composition containing liposome, and containing an active compound in the liposome internal phase, wherein the active compound is eribulin or its pharmacologically permissible salt. 
     
     
         2 . The liposome composition according to  claim 1 , wherein the liposome composition is in solid or liquid form. 
     
     
         3 . The liposome composition according to  claim 1 , wherein the liposome internal phase further contains ammonium salt. 
     
     
         4 . The liposome composition according to  claim 3 , wherein the concentration of said ammonium salt is 10 mM or higher. 
     
     
         5 . The liposome composition according to  claim 1 , wherein the liposome internal phase further contains salt, acid, base and/or amino acid. 
     
     
         6 . The liposome composition according to  claim 5 , wherein the concentration of said salt is 1 to 300 mM. 
     
     
         7 . The liposome composition according to  claim 5 , wherein the concentration of said acid is 1 to 300 mM. 
     
     
         8 . The liposome composition according to  claim 5 , wherein the concentration of said amino acid is 1 to 300 mM. 
     
     
         9 . The liposome composition according to  claim 5 , wherein the concentration of said base is 1 to 300 mM. 
     
     
         10 . The liposome composition according to  claim 1 , wherein the concentration of said active compound is 0.01 to 300 mg/mL. 
     
     
         11 . The liposome composition according to  claim 1 , wherein said active compound is eribulin mesylate. 
     
     
         12 . The liposome composition according to  claim 1 , wherein the liposome internal phase further contains ammonium sulfate, citric acid, and an active compound. 
     
     
         13 . The liposome composition according to  claim 1 , wherein the liposome external phase contains sugar, electrolyte, and/or amino acid. 
     
     
         14 . The liposome composition according to  claim 13 , wherein the liposome external phase contains sugar, electrolyte, and amino acid. 
     
     
         15 . The liposome composition according to  claim 13 , wherein the concentration of said sugar is 2 to 20%. 
     
     
         16 . The liposome composition according to  claim 13 , wherein the concentration of said amino acid is 1 to 300 mM. 
     
     
         17 . The liposome composition according to  claim 13 , wherein the liposome external phase contains sucrose or sodium chloride, and histidine. 
     
     
         18 . The liposome composition according to  claim 1 , wherein said liposome internal phase does not substantially contain cyclodextrin. 
     
     
         19 . The liposome composition according to  claim 1 , wherein the liposome contains hydrogenated phosphatidylcholine. 
     
     
         20 . The liposome composition according to  claims 1 , wherein the liposome contains cholesterol. 
     
     
         21 . The liposome composition according to  claim 1 , wherein the liposome contains methoxypolyethylene glycol condensate. 
     
     
         22 . The liposome composition according to  claim 21 , wherein said methoxypolyethylene glycol condensate is distearoylphosphatidyl ethanolamino polyethylene glycol condensate. 
     
     
         23 . The liposome composition according to  claim 1 , wherein the liposome contains hydrogenated phosphatidylcholine, cholesterol, and distearoylphosphatidyl ethanolamino polyethylene glycol condensate. 
     
     
         24 . The liposome composition according to  claim 23 , which contains 10 to 80% of said hydrogenated phosphatidylcholine, 1 to 60% of said cholesterol, and 0 to 50% of said distearoylphosphatidyl ethanolamino polyethylene glycol condensate. 
     
     
         25 . The liposome composition according to  claim 1 , wherein the liposome contains hydrogenated soy phosphatidylcholine, cholesterol, and polyethylene glycol 2000-phosphatidylethanolamine. 
     
     
         26 . A method of manufacture of the liposome composition according to  claim 1 , including:
 a step in which a liposome dispersion liquid containing liposome is provided;   a step in which said liposome dispersion liquid is mixed with said active compound; and   a step in which said active compound is introduced into the liposome internal phase of said liposome dispersion liquid.   
     
     
         27 . The method according to  claim 26 , wherein said liposome dispersion liquid does not substantially contain ammonium salt in the liposome external phase. 
     
     
         28 . The method according to  claim 26 , wherein the pH of the liposome external phase of said liposome dispersion liquid is 3 to 10. 
     
     
         29 . The method according to  claim 28 , wherein the pH of the liposome external phase of said liposome dispersion liquid is 7 to 10. 
     
     
         30 . The method according to  claim 28 , wherein said pH is the pH of the liposome external phase of said liposome dispersion liquid in the step in which said liposome dispersion liquid and said active compound are mixed. 
     
     
         31 . The method according to  claim 26 , wherein
 the step in which said liposome dispersion liquid is provided includes: a step in which a liposome preparatory solution is provided that contains liposome and that contains ammonium salt in the liposome internal phase and liposome external phase; and   a step in which the liposome external phase of said liposome preparatory solution is substituted or diluted.   
     
     
         32 . The method according to  claim 31 , wherein the step in which said liposome external phase is substituted or diluted is a step in which the pH of the liposome external phase is made higher than the pH of the liposome internal phase. 
     
     
         33 . The method according to  claim 31 , wherein the step in which said liposome external phase is substituted or diluted is a step in which the difference between the pH of the liposome internal phase and the pH of the liposome external phase is 1 to 5. 
     
     
         34 . The method according to  claim 26 , wherein the pH of said liposome internal phase is 3 to 9. 
     
     
         35 . The method according to  claim 26 , wherein the pH of said liposome internal phase is 4 to 9. 
     
     
         36 . The method according to  claim 26 , wherein the pH of said liposome internal phase is 5 to 8. 
     
     
         37 . The method according to  claim 26 , wherein the liposome external phase is a solution that contains electrolyte in the step in which said active compound is introduced. 
     
     
         38 . The method according to  claim 26 , wherein said liposome dispersion liquid does not substantially contain cyclodextrin. 
     
     
         39 . The method according to  claim 26 , which further contains a step in which the pH of the liposome external phase is neutralized.

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