Extended release formulations of erythromycin derivatives

• Main Authors: CRAMPTON SHERI L, HUI HO-WAH, GUSTAVSON LINDA E, SEMLA SUSAN J, AL-RAZZAK LAMAN A, MILMAN NELLY
• Format: Patent
• Language: English; Slovak
• Published: 02.08.2013
• Subjects: HUMAN NECESSITIES; HYGIENE; MEDICAL OR VETERINARY SCIENCE; PREPARATIONS FOR MEDICAL, DENTAL, OR TOILET PURPOSES; SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS ORMEDICINAL PREPARATIONS

Disclosed is a pharmaceutical composition for oral administration in form of a tablet with extended release of clarithromycine in the gastrointestinal environment. The composition comprises clarithromycine and a pharmaceutically acceptable, hydrophilic, water soluble polymer that is hydroxypropylmethyl cellulose 2208 containing 19 % to 24 % of metoxyle, 7 % to 12 % of hydroxypropoxyle having 80 to 120 mPa.s viscosity, as 2 % water solution and having a such particle size that 100 % of the particles passes through the sieve with sieve mesh 595 micro m (30 mesh), more than 99 % of the particles passes through the sieve with sieve 400 micro m (40 mesh) and more than 90 % of the particles passes through the sieve with sieve 149 micro m (100 mesh). The tablet formulation comprises 500 mg of clarithromycine and 200 mg of polymer, 260 mg lactose monohydrate, 30 mg of talc USP and 10 mg of magnesium stearate. It is obtainable by wet process. The formulation releases clarithromycine in such a way, that after the single dose of 500 mg the area below the curve plasma concentration - time 0 - infinity is 15.0 + 6.5 ug.h/ml, the maximum concentration in the plasma is achieved after 5.0 + 1.7 hours after administration of the dose and maximum concentration in the plasma is 1.19 + 0.6 ug.h/ml. Further there is described use of the formulation for preparation of a medicine for bacterial infection treatment of mammals. Disclosed is a pharmaceutical composition for oral administration in form of a tablet with extended release of clarithromycine in the gastrointestinal environment. The composition comprises clarithromycine and a pharmaceutically acceptable, hydrophilic, water soluble polymer that is hydroxypropylmethyl cellulose 2208 containing 19 % to 24 % of metoxyle, 7 % to 12 % of hydroxypropoxyle having 80 to 120 mPa.s viscosity, as 2 % water solution and having a such particle size that 100 % of the particles passes through the sieve with sieve mesh 595 micro m (30 mesh), more than 99 % of the particles passes through the sieve with sieve 400 micro m (40 mesh) and more than 90 % of the particles passes through the sieve with sieve 149 micro m (100 mesh). The tablet formulation comprises 500 mg of clarithromycine and 200 mg of polymer, 260 mg lactose monohydrate, 30 mg of talc USP and 10 mg of magnesium stearate. It is obtainable by wet process. The formulation releases clarithromycine in such a way, that after the single dose of 500 mg the area below the curve plasma concentration - time 0 - infinity is 15.0 + 6.5 ug.h/ml, the maximum concentration in the plasma is achieved after 5.0 + 1.7 hours after administration of the dose and maximum concentration in the plasma is 1.19 + 0.6 ug.h/ml. Further there is described use of the formulation for preparation of a medicine for bacterial infection treatment of mammals.