SOLID PHARMACEUTICAL COMPOSITION COMPRISING TELITHROMYCIN

摘要

#CMT# #/CMT# Solid pharmaceutical composition (A), comprises telithromycin (I) (0.1-80 wt.%) or its acid addition salts as an active ingredient and a diluting agent (II) (10-50 wt.%) having plastic behavior. #CMT#ACTIVITY : #/CMT# Antibacterial. #CMT#MECHANISM OF ACTION : #/CMT# None given. #CMT#USE : #/CMT# (A) is used as an antibiotic, for treating bacterial infections. #CMT#ADVANTAGE : #/CMT# The tablet containing (A) is in reduced size and it can be swallowed orally. The process of preparing (A) is cost effective and it has improved mechanical properties. #CMT#ORGANIC CHEMISTRY : #/CMT# Preferred Composition: (A) further comprises a binding agent (2.5-3.5 (preferably 2.8-3) wt.%), a disintegrating agent (3-8 (3.5-6) wt.%) and a lubricating agent (0.6-1 wt.%). (A) comprises (I) (50-80 (preferably 60-70) wt.%) and a diluting agent (20-30 wt.%). Preferred Components: The disintegrating agent is sodium croscarmellose (preferred), crospovidone and/or sodium carboxymethylamine. The lubricating agent is magnesium stearate (claimed) and/or micronized stearic acid. #CMT#POLYMERS : #/CMT# Preferred Components: (II) is microcrystalline cellulose, present at 20-30 wt.%. The binding agent is Povidone K25 (RTM: Polyvinyl pyrrolidone) and/or Povidone K30 (RTM: Polyvinyl pyrrolidone) (both preferred), copovidone and/or hydroxypropyl cellulose. #CMT#ADMINISTRATION : #/CMT# Administration of (A) is 50-600 (preferably 300) mg is oral in the form of a tablet or a film-coated tablet, where the film-coating material comprises a component of hypromellose, polyethylene glycol, titanium dioxide, talc, yellow iron oxide and/or red iron oxide (claimed). #CMT#EXAMPLE : #/CMT# Typical pharmaceutical composition comprises (in %): telithromycin (65.2); cellulose microcrystalline (25.1); sodium croscarmellose (3.91); Povidone K25 (RTM: Polyvinyl pyrrolidone) (2.93); magnesium stearate (0.65); hypromellose 6 cP (1.62); polyethylene glycol 8000 (0.07); titanium dioxide (0.34); talc (0.12); yellow iron oxide (0.05); and iron red oxide (0.01).