US 6,713,089 B1Granted

Quick release pharmaceutical compositions of drug substances

AssigneeNycomed Danmark A/S

InventorsPoul Bertelsen, Niels Gjørløv Hansen, Hermann Ruckendorfer, Shigeru Itai

Life of this patent

Estimating the term…

Loading patent…

Abstract

The present invention relates to an oral modified release pharmaceutical composition for the administration of a therapeutically and/or prophylactically effective amount of an active substance (a drug substance), to obtain a relatively fast or quick onset of the therapeutic and/or prophylactic effect. The drug substances contained in a modified release pharmaceutical composition according to the invention are suitably a drug substance which has a pKa value below about 5, such as in a range of from about 4 to about 5. The composition is based on a powder comprising a therapeutically and/or prophylactically active substance and has such a particle size that: when the powder is subjected to a sieve analysis, then at least about 90% w/w of the particles pass through a 180 micron sieve, and when the powder is contacted with an aqueous medium to form a particulate composition, which as such a particle size that when the particulate composition is subjected to a sieve analysis, then at least about 50% w/w of the particles passes through a 180 micron sieve. Further more, the composition, when tested in accordance with the dissolution method (I) defines herein, employing 0.07 HCl as dissolution medium, release at least about 50% w/w of the active substance within the first 20 minutes of the test.

Claims66

Dependent claims

A quick release pharmaceutical composition for oral administration comprising a therapeutically and/or prophylactically active substance and at least one pharmaceutically acceptable excipient, said active substance being defined by one of features i) or ii):

i) the active substance has a solubility which does not exceed 0.1% w/v in 0.1 N hydrochloric acid at room temperature;
ii) the active substance has a pKa value which does not exceed 5.5,
wherein the quick release pharmaceutical composition is in the form of a particulate composition or being based on a particulate composition, the particulate composition contains the active substance in contact with an alkaline substance and further comprises one of features iii) or iv):
iii) the particulate composition is based on a powder comprising the therapeutically and/or prophylactically active substance, wherein said powder has a particle size such that when the powder is subjected to a sieve analysis, then at least 90% w/w of the particles pass through sieve 180 μm, and wherein when the powder is being contacted with an aqueous medium to form a particulate composition, the particle size of the particulate composition when subjected to a sieve analysis, is such that at least 50% w/w of the particles pass through sieve 180 μm;
iv) the particulate composition is obtained by contacting a powder that comprises the therapeutically and/or prophylactically active substance and has a particle size such that when the powder is subjected to a sieve analysis then at least 90% w/w of the particles pass through sieve 180 μm with an aqueous medium in such a manner that the mean particle size of the particles of the particulate composition is not greater than 100% larger than the mean particle size of the powder before being contacted with the aqueous medium,
and wherein the quick release pharmaceutical composition, when tested in accordance with the dissolution method I defined herein employing 0.07 N hydrochloric acid as dissolution medium, dissolves at least 50% w/w of the active substance within the first 20 minutes of the test.

3 more elements

A method for treatment and/or prophylaxis of acute pain and/or mild or moderate pain comprising administering to a patient an effective amount of a therapeutically and/or prophylactically active substance in the form of a quick release composition, said active substance being defined by one of features i) or ii):

i) the active substance has a solubility which does not exceed 0.1% w/v in 0.1 N hydrochloric acid at room temperature;
ii) the active substance has a pKa value which does not exceed 5.5,
and wherein the quick release pharmaceutical composition is in the form of a particulate composition or being based on a particulate composition, the particulate composition contains the active substance in contact with an alkaline substance and further has one of features iii) or iv):
iii) the particulate composition is based on a powder comprising the therapeutically and/or prophylactically active substance, wherein said powder has a particle size such that when the powder is subjected to a sieve analysis, at least 90% w/w of the particles pass through sieve 180 μm, and wherein when the powder is being contacted with an aqueous medium to form a particulate composition, the particle size of the particulate composition, when subjected to a sieve analysis, is such that at least 50% w/w of the particles pass through sieve 180 μm;
iv) the particulate composition is in the form of a particulate composition or being based on a particulate composition which is obtained by contacting a powder that comprises the therapeutically and/or prophylactically active substance and has a particle size such that when the powder is subjected to a sieve analysis then at least 90% w/w of the particles pass through sieve 180 μm with an aqueous medium in a manner such that the mean particle size of the particles of the particulate composition is not greater than 100% larger than the mean particle size of the powder before being contacted with the aqueous medium,
and wherein the quick release pharmaceutical composition, when tested in accordance with the dissolution method I defined herein employing 0.07 N hydrochloric acid as dissolution medium, dissolves at least 50% w/w of the active substance within the first 20 minutes of the test.

3 more elements

A method for fast relief of acute pain comprising administering to a patient in need thereof an effective amount of a therapeutically and/or prophylactically active substance in the form of a quick release composition, said active substance being defined by one of features i) or ii):

i) the active substance has a solubility which does not exceed 0.1% w/v in 0.1 N hydrochloric acid at room temperature;
ii) the active substance has a pKa value which does not exceed 5.5,
and wherein the quick release pharmaceutical composition is in the form of a particulate composition or being based on a particulate composition, the particulate composition contains the active substance in contact with an alkaline substance and further has one of features iii) or iv):
iii) the particulate composition is based on a powder comprising the therapeutically and/or prophylactically active substance, wherein said powder has a particle size such that when the powder is subjected to a sieve analysis, at least 90% w/w of the particles pass through sieve 180 μm, and wherein when the powder is being contacted with an aqueous medium to form a particulate composition, the particle size of the particulate composition, when subjected to a sieve analysis, is such that at least 50% w/w of the particles pass through sieve 180 μm;
iv) the particulate composition is in the form of a particulate composition or being based on a particulate composition which is obtained by contacting a powder that comprises the therapeutically and/or prophylactically active substance and has a particle size such that when the powder is subjected to a sieve analysis then at least 90% w/w of the particles pass through sieve 180 μm with an aqueous medium in such a manner that the mean particle size of the particles of the particulate composition is not greater than 100% larger than the mean particle size of the powder before being contacted with the aqueous medium,
and wherein the quick release pharmaceutical composition, when tested in accordance with the dissolution method I defined herein employing 0.07 N hydrochloric acid as dissolution medium, dissolves at least 50% w/w of the active substance within the first 20 minutes of the test.

3 more elements

Dependencies are inferred from the claim text.