Antiphlogistic lysine salts of acemetacin - stable, of good solubility and giving solns. of physiological pH

摘要

Lysine-(1-(p-chlorobenzoyl)-5-methoxy -2-methyl-3-indole)- acetoxy acetates (I) are new, and are pharmaceuticals, esp. antiphlogistics for the treatment of rheumatic diseases. Suitable doses for oral and rectal use are 1-10 mg/kg and/or intramuscular application 0.5-10 mg/kg. The doses are administered 1-5 times daily. The water solubility of (I) is ca. 30 times that of the corresp. lysin salt of indometacin and therefore its solns. can be more concentrated and dose volume is reduced. The aq. solns. are of physiological pH. (I) are very stable and are more effective than the corresp. indometacin salts. (I) dissolve rapidly in water, esp. if they have been lyophilised, e.g. freeze dried. (I) are easily disposed of biologically. When administered orally (I) have a considerably longer half-life in blood than the free acid (acemetacin).