Bacampicillin

Bacampicillin is an orally active semi-synthetic aminopenicillin derivative, prodrug and bactericide that is readily inactivated by β-lactamases. Bacampicillin is hydrolyzed by carboxylester hydrolases and non-specific esterases in the gastrointestinal wall and plasma to form Ampicillin (HY-B0522), and produces higher levels of Ampicillin in rodents in vivo. Bacampicillin exhibits bactericidal activity against Gram-positive and Gram-negative bacteria. Bacampicillin can be used in studies related to bacterial infections^[1][2]. In Vitro:Bacampicillin (10-20 μg/mL; 30 min) is stable in synthetic gastric juice (pH 1.2) and phosphate buffer (pH 7.4), but undergoes extensive hydrolysis to Ampicillin (HY-B0522) in the presence of 10% human or rat serum after 30 min incubation at 37°C, with rat serum driving more complete hydrolysis than human serum^[1].
Bacampicillin (100 μg/mL; up to 30 min) undergoes rapid first-order hydrolysis to Ampicillin in heparinized human blood, human plasma, and canine plasma at 37°C, with the fastest hydrolysis observed in human blood^[1]. In Vivo:Bacampicillin (20 mg/kg; p.o.; single dose) has a 3.7-fold higher bioavailability than equimolar Ampicillin in male SPF-grade Sprague-Dawley rats^[1].
Bacampicillin (135 mg/kg; p.o.; single dose) produces significantly higher and longer-lasting interstitial fluid Ampicillin levels in female SPF-grade Sprague-Dawley rats with subcutaneous tissue cages compared to equimolar doses of Ampicillin^[1].
Bacampicillin (135 mg/kg; p.o.; single dose) produces ampicillin concentrations in the kidney and liver tissues of female SPF-grade Sprague-Dawley rats that are 3 to 4 times those of equimolar ampicillin^[1].
Bacampicillin (20 mg/kg; p.o.; single dose) exhibits 3-fold higher bioavailability than equimolar ampicillin in female beagle dogs^[1].
Bacampicillin (p.o.; single dose) exhibits potent activity against a variety of bacterial infections in female NMRI mice, with better efficacy than Ampicillin^[1].