Modified release pharmaceutical formulation comprising amoxycillin

A modified release pharmaceutical formulation comprising about 2000 mg of amoxycillin in an immediate release phase and a slow release phase;

• the immediate release phase comprising a first part of amoxycillin formulated with one or more pharmaceutically acceptable excipients which allows for immediate release of the first part of amoxycillin, and
• the slow release phase comprising a second part of amoxycillin formulated with one or more release modifying pharmaceutically acceptable excipients,
• wherein the ratio of amoxycillin in the immediate and slow release phase is from 3:1 to 1:3,
• such that the formulation has an in vitro dissolution profile wherein 45 to 65% of the amoxycillin content is dissolved within 30 min, measured in <711> dissolution test, Apparatus 2, USP 23, 1995, at 37.0±0.5° C., using 900 mL of deionised water and a paddle speed of 75 rpm.

A modified release formulation comprising about 2000 mg of amoxycillin in an immediate release phase and a slow release phase;

• the immediate release phase comprising a first part of amoxycillin formulated with one or more pharmaceutically acceptable excipients which allows for immediate release of the first part of amoxycillin, and
• the slow release phase comprising a second part of amoxycillin formulated with one or more release modifying pharmaceutically acceptable excipients,
• wherein the ratio of amoxycillin in the immediate and slow release phase is from 3:1 to 1:3,
• such that the amoxycillin has an in vitro dissolution profile wherein 45 to 65% of the amoxycillin content is dissolved within 30 minutes;
• 50 to 75% of the amoxycillin content is dissolved within 60 minutes;
• 55 to 85% of the amoxycillin content is dissolved within 120 minutes;
• 70 to 95% of the amoxycillin content is dissolved within 180 minutes;
• and 70 to 100% of the amoxycillin content is dissolved within 240 minutes, measured in the <711> dissolution test, Apparatus 2, USP 23, 1995, at 37.0±0.5° C., using 900 mL of deionised water and a paddle speed of 75 rpm.

A modified release pharmaceutical formulation comprising about 2000 mg of amoxycillin in an immediate release phase and a slow release phase;

• the immediate release phase comprising a first part of amoxycillin formulated with one or more pharmaceutically acceptable excipients which allows for immediate release of the first part of amoxycillin, and
• the slow release phase comprising a second part of amoxycillin formulated with one or mare release modifying pharmaceutically acceptable excipients,
• wherein the ratio of amoxycillin in the immediate and slow release phase is from 3:1 to 1:3,
• such that the formulation provides a mean Cmax of amoxycillin of at least 16 μg/mL, an AUC value of amoxycillin which is at least 80% of that of the same amount if taken as an immediate release formulation, and a mean plasma concentration of amoxycillin of at least 4 μg/mL for at least 4.2 hours.

A modified release formulation comprising about 2000 mg of amoxycillin in an immediate release phase and a slow release phase;

• the immediate release phase comprising a first part of amoxycillin formulated with one or more pharmaceutically acceptable excipients which allows for immediate release of the first part of amoxycillin, and
• the slow release phase comprising a second part of amoxycillin formulated with one or more release modifying pharmaceutically acceptable excipients,
• wherein the ratio of amoxycillin in the immediate and slow release phase is from 3:1 to 1:3,
• such that the amoxycillin provides a mean Cmax of amoxycillin of about 17.4 μg/mL, an AUC value of amoxycillin which is at least 74.9% of that of the same amount if taken as an immediate release formulation over the same dosage regimen interval, and a mean plasma concentration of amoxycillin of at least 4 μg/mL for about 6 hours.