Composition comprising amoxicillin and potassium clavulanate
AssigneeBeecham Pharmaceuticals (Pte) Limited
InventorsKevin H. Storm, Creighton P. Conley, John A. Roush
Life of this patent
Estimating the term…
Abstract
Bacterial infections may be treated using a high dosage regimen of amoxicillin and potassium clavulanate. Preferably, the dosage is provided by a bilayer tablet.
Claims133
A composition comprising amoxicillin and potassium clavulanate, the composition being in a solid form and comprising a first release phase and a second release phase;
- the first release phase comprising potassium clavulanate and a first amount of the amoxicillin;
- the second release phase comprising a second amount of the amoxicillin-, said second amount of amoxicillin being a pharmaceutically acceptable soluble salt of amoxicillin, and at least one pharmaceutically acceptable organic acid which are admixed, as solids, in intimate contact at a ratio of from about 20:1 to about 1:2.
A composition in solid dosage form comprising amoxicillin and potassium clavulanate in a weight ratio of amoxicillin to potassium clavulanate from about 2:1 to about 20:1, the amount of amoxicillin is in the range of about 1950 to about 2550 mg;
- and the dosage regimen interval is about 12 hours,
- such that the amount of amoxicillin released over thirty minutes is in the range about 45% to about 65% of the total amoxicillin content, over sixty minutes is in the range about 50% to about 75% of the total amoxicillin content, over two hours is in the range about 55-% to about 85% of the total amoxicillin content, over 180 minutes is in the range about 70-% to about 95% of the total amoxicillin content and over 240 minutes is in the range about 70% to about 100% of the total amoxicillin content, as tested by the USP Dissolution Test, Apparatus 2, method at 37 degrees C., a paddle speed of 75 rpm and in 900 ml deionized water, over a period of 8 hours;
- and which provides a mean maximum plasma concentration (Cmax) that is at least 12 micrograms/ml and a mean time that the plasma concentration exceeds 4 micrograms/ml for at least 4.4 hours, when tested in a group of at least 7 healthy humans, based on blood sampling at half hourly intervals for the first two hours and thereafter at hourly intervals.
A composition in solid dosage form comprising amoxicillin and potassium clavulanate, such that the amount of amoxicillin is about 2000 mg and comprising a first release phase and a second release phase;
- the first release phase comprising potassium clavulanate and a first portion of the amoxicillin;
- the second release phase comprising a second portion of amoxicillin, which is a pharmaceutically acceptable soluble salt of amoxicillin, and at least one pharmaceutically acceptable organic acid which are admixed in intimate contact at a ratio of from about 20:1 to about 1:2;
- such that the weight ratio of amoxicillin to potassium clavulanate is from about 2:1 to about 20:1, and the solid dosage is administered at a regimen interval of about 12 hours, and
- wherein the solid dosage is such that the amount of amoxicillin released over thirty minutes is in the range about 45% to about 65% of the total amoxicillin content, over sixty minutes is in the range about 50% to about 75% of the total amoxicillin content, over two hours is in the range about 55-% to about 85% of the total amoxicillin content, over 180 minutes is in the range about 70-% to about 95% of the total amoxicillin content and over 240 minutes is in the range about 70% to about 100% of the total amoxicillin content, as tested by the USP Dissolution Test, Apparatus 2, method at 37 degrees C., a paddle speed of 75 rpm and in 900 ml deionized water, over a period of 8 hours;
- and which provides a mean maximum plasma concentration (Cmax) that is at least 12 micrograms/ml and a mean time that the plasma concentration exceeds 4 micrograms/ml for at least 4.4 hours, when tested in a group of at least 7 healthy humans, based on blood sampling at half hourly intervals for the first two hours and thereafter at hourly intervals.
Dependencies are inferred from the claim text.