Carboxyalkylcellulose esters for administration of poorly soluble pharmaceutically active agents
OwnerMichael Shelton, Jessica Posey-Dowty +5inventors
InventorsMichael Shelton, Jessica Posey-Dowty, Kevin Edgar, Larry Lingerfelt, Sandra Klein, Shane Kirk, Jennifer Dressman
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Abstract
Disclosed herein are pharmaceutical compositions comprising carboxyalkylcellulose esters for delivery of pharmaceutically active substances having low solubility in a medium such as water, an acidic aqueous buffer, a neutral aqueous buffer, or a basic aqueous buffer. Also disclosed are methods for making pharmaceutical compositions and methods of administering the compositions.
Claims35
A pharmaceutical composition comprising:
- at least one pharmaceutically active agent having low solubility in a medium, and
- at least one carboxyalkylcellulose ester comprising an anhydroglucose repeat unit having the structure:
- wherein:
- R1-R6 are each independently selected from —OH, —OC(O)(alkyl), and —O(CH2)xC(O)OH, and pharmaceutically acceptable salts, wherein x ranges from 1-3,
- a degree of substitution per anhydroglucose of —OH ranges from 0.1 to 0.7,
- a degree of substitution per anhydroglucose of —OC(O)(alkyl) ranges from 0.1 to 2.7, and
- a degree of substitution per anhydroglucose of —O(CH2)xC(O)OH ranges from 0.2 to 0.75.
A composition comprising:
- at least one pharmaceutically active agent, and
- at least one carboxyalkylcellulose ester comprising an anhydroglucose repeat unit having the structure:
- wherein:
- R1-R6 are each independently selected from —OH, —OC(O)(alkyl), and —O(CH2)xC(O)OH, and pharmaceutically acceptable salts, wherein x ranges from 1-3,
- a degree of substitution per anhydroglucose of —OH ranges from 0.1 to 0.7,
- a degree of substitution per anhydroglucose of —OC(O)(alkyl) ranges from 0.1 to 2.7, and
- a degree of substitution per anhydroglucose of —O(CH2)xC(O)OH ranges from 0.2 to 0.75,
- wherein the composition is in the form of a solid dispersion.
A pharmaceutical composition comprising:
- at least one pharmaceutically active agent, wherein at least 10,000 mL of water is required to dissolve 1 g of the agent, and
- at least one carboxyalkylcellulose ester comprising an anhydroglucose repeat unit having the structure:
- wherein:
- R1-R6 are each independently selected from —OH, —OC(O)(alkyl), and —O(CH2)xC(O)OH, and pharmaceutically acceptable salts, wherein x ranges from 1-3,
- a degree of substitution per anhydroglucose of —OH ranges from 0.1 to 0.7,
- a degree of substitution per anhydroglucose of —OC(O)(alkyl) ranges from 0.1 to 2.7, and
- a degree of substitution per anhydroglucose of —O(CH2)xC(O)OH ranges from 0.2 to 0.75.
A method of treating a mammal in need thereof with a pharmaceutical composition, comprising:
- administering to the mammal in need of treatment the pharmaceutical composition comprising:
- a therapeutically effective amount of at least one poorly soluble pharmaceutically active agent, and
- at least one carboxyalkylcellulose ester comprising an anhydroglucose repeat unit having the structure:
- wherein:
- R1-R6 are each independently selected from —OH, —O—C(O)(alkyl), and —O(CH2)xC(O)OH, and pharmaceutically acceptable salts, wherein x ranges from 1-3,
- a degree of substitution per anhydroglucose of —OH ranges from 0.1 to 0.7,
- a degree of substitution per anhydroglucose of —OC(O)(alkyl) ranges from 0.1 to 2.7, and
- a degree of substitution per anhydroglucose of —O(CH2)xC(O)OH ranges from 0.2to 0.75.
A pharmaceutical composition comprising:
- at least one pharmaceutically active agent having low solubility in a medium, and
- at least one carboxyalkylcellulose ester comprising an anhydroglucose repeat unit having the structure:
- wherein:
- R1-R6 are each independently selected from —OH, —OC(O)(alkyl), and —O(CH2)xC(O)OH, O−A+, and —O(CH2)xC(O)O−A+, wherein x ranges from 1-3, and A+ is a counter ion,
- a degree of substitution per anhydroglucose of —OH and O−A+ ranges from 0.1 to 0.7,
- a degree of substitution per anhydroglucose of —OC(O)(alkyl) ranges from 0.1 to 2.7, and
- a degree of substitution per anhydroglucose of —O(CH2)xC(O)OH and —O(CH2)x(O)O−A+ ranges from 0.2 to 0.75.
Dependencies are inferred from the claim text.