[Prolonged action preparation of cefaclor].
This study was conducted to develop a prolonged action preparation of cefaclor (CCL) which can offer, with the twice-a-day administration, as much effectiveness as its conventional preparation (Kefral capsule) with the 3 times-a-day administration. Absorption site of CCL in gastrointestinal tract, preparation form (enteric coated granules) which slowly release CCL, dissolution property of the form, and mixed ratio of the form and rapid release form (nonenteric coated granules) were studied and complex granules consisting of 40% of nonenteric coated granules and 60% of enteric coated granules which dissolve at pH 6 were chosen as a prolonged action preparation of CCL. Bactericidal activity of the prolonged action preparation (S6472) was confirmed to be the same as that of the conventional preparation by comparative viable cell count study in which concentrations of CCL simulated to plasma concentrations following the administration of S6472 at the dosage of 375 mg b.i.d. and the conventional preparation at the dosage of 250 mg t.i.d. were used. From the above, S6472 is considered to be a prolonged action preparation of CCL which serve our purpose. Since S6472 can be given with the twice-a-day administration, its daytime administration is not necessary. Therefore, S6472 is considered to be much useful preparation for the patients.
D000328:Adult; D000818:Animals; D002433:Cefaclor / Q000008:administration & dosage / Q000378:metabolism* / Q000494:pharmacology; D002506:Cephalexin / Q000031:analogs & derivatives*; D003692:Delayed-Action Preparations; D004352:Drug Resistance, Microbial; D004926:Escherichia coli / Q000187:drug effects; D006801:Humans; D007408:Intestinal Absorption; D008297:Male; D008875:Middle Aged; D051381:Rats; D013211:Staphylococcus aureus / Q000187:drug effects
D003692:Delayed-Action Preparations; D002433:Cefaclor; D002506:Cephalexin