Rapidly bioavailable tablet and capsule formulations of diclofenac
AssigneeKowa Pharmaeuticals America, Inc.
InventorsGiorgio Reiner, Alberto Reiner
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Abstract
The present invention relates to excipients for the production of rapidly bioavailable solid oral dosage forms of diclofenac. In particular, the invention relates to the use of excipients that promote the bioavailability of such formulations, including alkaline buffering agents, gas forming excipients, hygroscopic excipients, water soluble diluents, wetting agents, and particular pharmaceutically acceptable salts.
Claims62
1) A method of treating acute pain comprising orally administering diclofenac potassium in an intact rapidly bioavailable tablet or capsule dosage form characterized by (i) a disintegration time of less than about 15 minutes when tested according to USP 28 <701>, (ii) a tmax of from about 5 to about 30 minutes, and (iii) a Cmax of from about 1500 to about 2500 ng/ml, wherein said dosage form comprises an excipient base comprising means for generating a gaseous and alkaline environment for said diclofenac potassium when orally ingested into the stomach.
17) A method of treating acute pain comprising orally administering diclofenac potassium in an intact rapidly bioavailable tablet or capsule dosage form characterized by (i) a tmax of from about 5 to about 30 minutes, and (iii) a Cmax of from about 1700 to about 2300 ng/ml, wherein said dosage form comprises an excipient base comprising means for generating a gaseous and alkaline environment for said diclofenac potassium when orally ingested into the stomach.
31) A method of treating acute pain comprising orally administering diclofenac potassium in an intact rapidly bioavailable tablet or capsule dosage form characterized by (i) a disintegration time of less than about 15 minutes when tested according to USP 28 <701>, (ii) a tmax of from about 5 to about 30 minutes, and (iii) a Cmax of from about 1500 to about 2500 ng/ml, wherein said dosage form comprises from about 7 to about 20 wt. % of a hygroscopic excipient that absorbs greater than 1 wt. % moisture when maintained in a humidity chamber at 80% RH and 25 degrees Celcius for 24 hours.
38) A method of treating acute pain comprising orally administering diclofenac potassium in an intact rapidly bioavailable tablet or capsule dosage form characterized by (i) a disintegration time of less than about 15 minutes when tested according to USP 28 <701>, (ii) a tmax of from about 5 to about 30 minutes, and (iii) a Cmax of from about 1500 to about 2500 ng/ml, wherein said dosage form has a hygroscopicity of greater than about 1 wt. % water absorption within a twenty four hour period in a humidity chamber maintained at 80% RH.
44) A method of treating acute pain comprising orally administering diclofenac potassium in an intact rapidly bioavailable tablet or capsule dosage form characterized by (i) a disintegration time of less than about 15 minutes when tested according to USP 28 <701>, (ii) a tmax of from about 5 to about 30 minutes, and (iii) a Cmax of from about 1500 to about 2500 ng/ml, wherein said dosage form comprises at least 20 wt. % of excipients that are freely soluble in water.
51) A method of treating acute pain comprising orally administering diclofenac potassium in an intact rapidly bioavailable tablet or capsule dosage form characterized by (i) a disintegration time of less than about 15 minutes when tested according to USP 28 <701>, (ii) a tmax of from about 5 to about 30 minutes, and (iii) a Cmax of from about 1500 to about 2500 ng/ml, wherein said dosage form comprises a wetting agent.
59) A method of treating acute pain comprising orally administering diclofenac potassium in an intact rapidly bioavailable tablet or capsule dosage form characterized by (i) a disintegration time of less than about 15 minutes when tested according to USP 28 <701>, (ii) a tmax of from about 5 to about 30 minutes, and (iii) a Cmax of from about 1500 to about 2500 ng/ml, wherein said dosage form comprises from about 30 to about 80 wt. % of a hygroscopic diluent and a freely soluble diluent at a weight ratio of from about 1:20 to about 5:1.
Dependencies are inferred from the claim text.