Low viscosity liquid dosage forms
AssigneeElan Pharma International Limited
InventorsTuula Ryde, Niels Ryde, H. William Bosch, John D. Pruitt, Christian F. Wertz
Life of this patent
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Abstract
The present invention relates to liquid dosage forms of nanoparticulate active agents having very low viscosities.
Claims82
A low viscosity liquid dosage form comprising:
- (a) particles of at least one active agent;
- (b) at least one surface stabilizer;
- and
- (c) at least one pharmaceutically acceptable excipient, carrier, or a combination thereof,
- wherein:
- (i) the active agent particles have an effective average particle size of less than about 2 microns and (ii) the dosage form has a viscosity of less than about 2000 mPa·s at a shear rate of 0.1 (1/s).
A method of improving a conventional solid dosage form of an active agent comprising:
- (a) identifying a conventional solid dosage form of an active agent having at least one undesirable trait, wherein the undesirable trait is selected from the group consisting of poor dose uniformity, low dose loading, large size, poor bioavailability, slow onset of activity;
- poor active agent retention in blood and tumors, significant fed-fasted variability;
- and
- (b) formulating the active agent into a low viscosity liquid dosage form comprising:
- (i) particles of at least one active agent;
- (ii) at least one surface stabilizer;
- and
- (iii) at least one pharmaceutically acceptable excipient, carrier, or a combination thereof,
- wherein:
- (1) the active agent particles have an effective average particle size of less than about 2 microns and (2) the dosage form has a viscosity of less than about 2000 mPa·s at a shear rate of 0.1 (1/s).
A method of improving a conventional liquid dosage form of an active agent comprising:
- (a) identifying a conventional solid dosage form of an active agent having at least one undesirable trait, wherein the undesirable trait is selected from the group consisting of high viscosity, poor taste, grittiness, poor bioavailability, slow onset of activity, presence of thickening agents, poor dose loading, poor performance characteristics for oral, intravenous, subcutaneous, or intramuscular injection, presence of organic solvents, presence of a pH extreme, poor active agent retention in blood and tumors, significant fed-fasted variability, high dose volume, poor suitability for parenteral administration, and an inability to be sterile filtered;
- and
- (b) formulating the active agent into a low viscosity liquid dosage form comprising:
- (i) particles of at least one active agent;
- (ii) at least one surface stabilizer;
- and
- (iii) at least one pharmaceutically acceptable excipient, carrier, or a combination thereof,
- wherein:
- (1) the active agent particles have an effective average particle size of less than about 2 microns and (2) the dosage form has a viscosity of less than about 2000 mPa·s at a shear rate of 0.1 (1/s).
A method of making a liquid dosage form comprising contacting particles of at least one active agent with at least one surface stabilizer and at least one pharmaceutically acceptable excipient, carrier, or a combination thereof for a time and under conditions sufficient to provide a nanoparticulate composition of the active agent, wherein:
- (a) the active agent particles have an effective average particle size of less than about 2 microns;
- and
- (b) the liquid dosage form has a viscosity of less than about 2000 mPa·s at a shear rate of 0.1 (1/s).
A method of treating a subject in need with a liquid dosage form of a nanoparticulate active agent comprising administering to the subject an effective amount of a liquid dosage form comprising:
- (a) particles of at least one active agent;
- (b) at least one surface stabilizer;
- and
- (c) at least one pharmaceutically acceptable excipient, carrier, or a combination thereof,
- wherein:
- (i) the active agent particles have an effective average particle size of less than about 2 microns and (ii) the liquid dosage form has a viscosity of less than about 2000 mPa·s at a shear rate of 0.1 (1/s).
Dependencies are inferred from the claim text.