Comparative Bioavailability of Oral Ampicillin Suspension, Pivampicillin Hydrochloride Salt (Capsule), Pivampicillin Pamoate Salt (Suspension) and Pivampicillin Probenecid Salt (Tablet) in Man
Ampicillin, although being absorbed from the gastrointestinal tract, has the drawback of not being absorbed completely. Comparisons of the plasma levels following intramuscular and oral administration revealed that after parenteral application the plasma level is 2 – 3 times that achieved by oral administration (5,8). Thus methods have been sought to improve the absorption of ampicillin. Several authors have found that ampicillin potassium was absorbed more readily than ampicillin-trihydrate, i.e. approximately 50 vs. 30% (1,4,6). Later it could be demonstrated that the pivaloyloxy-methyl ester of ampicillin (generic name: pivampicillin) yielded nearly the same antimicrobial activity in the plasma after oral administration as compared to the intramuscular route (2,3). Following oral administration pivampicillin is rapidly hydrolyzed to ampicillin (Figure 1) and 60 to 70% of the administered compound are recovered as ampicillin in the urine within 6 hours. When administered as a powder, pivampicillin is present in the form of the crystalline hydrochloride salt. Because this salt possesses a strongly bitter taste, however, it is unsuitable for pediatric use. Therefore several pediatricians asked for a more suitable preparation for the pediatric use (7).
KeywordsBitter Taste Relative Availability Urinary Recovery Hydrochloride Salt Intramuscular Route
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