Enhancement of absorption of drugs from gastrointestinal tract using choline ester salts
AssigneeMerck & Co., Inc.
InventorsJose Alexander, Joseph A. Fix
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Abstract
Choline ester salts are used as drug absorption enhancing agents for orally and rectally administered drugs.
Claims3
A method of enhancing the rate of gastrointestinal absorption of an orally or rectally administred drug, comprising administering a dosage form capable of being orally or rectally absorbed, said dosage form comprising a therapeutically effective dosage amount of a poorly absorbed .beta.-lactam antibiotic drug selected from the group consisting of cefoxitin, N-formamidinyltheinamycin, ampicillin, azlocillin, bacampicillin, carbenicillin, cefaclor, cefadroxil, cefamandole, cefatrizine, cefazoline, cefonicid, cefaperazone, ceforanide, cefotaxime, cefotiam, cefroxadine, cefsulodin, ceftazidime, ceftriaxone, ceftizoxime, cephalexin, cephaloglycin, cephaloridine, cephradine, cyclacillin, cloxacillin, dicloxacillin, floxacillin, hetacillin, methicillin, nafcillin, oxacillin, sarmoxacillin, sarpicillin, talampicillin, ticaricillin, penicillin G., penicillin V., pivampicillin. piperacillin, pirbenicillin and a choline ester absorption enhancing agent of the formula :
- [(CH.sub.3).sub.3 N.sup.+ CH.sub.2 CH.sub.2 OR]X.sup.-
- wherein R is saturated acyl (C.sub.2 -C.sub.20), acyl(C.sub.2 -C.sub.20) with 1 to 6 double bonds, hydroxyacyl(C.sub.2 -C.sub.20) with 1 to 3 hydroxy groups, ketoacyl(C.sub.4 -C.sub.20), unsaturated hydroxycacyl(C.sub.5 -C.sub.20) or carbalkoxyacyl(C.sub.5 -C.sub.20), or carboxy acyl(C.sub.4 -C.sub.20) and X- is a pharmaceutically acceptable counterion.
Dependencies are inferred from the claim text.