1978 Volume 26 Issue Supplement2 Pages 371-382
Fundamental and clinical examinations were carried out on newly developed antibiotic, PC-904, and the following results were obtained;
1) Antibacterial effect
Against 976 strains isolated recently from various clinical materials (Staphylococcus aureus 81, Sal-monella 33, Shigella 47, Citrobacter freundii 63, E. coli 81, Erwinia herbicola 11, Klebsiella aerogenes 81, Enterobacter aerogenes 43, Enterobacter cloacae 42, Serratia marcescens 161, Proteus vulgaris 26, Proteus mirabilis 51, Proteus rettgeri 22, Proteus inconstans 17, Proteus morganii 42, Aeromonashydrophila 23, Vibrio parahaemolyticus 24, Pseudomonas aeruginosa 128) and 23 standard strainswhich were kept in our department, each MIC when PC-904 or Sulbenicillin (SBPC) were applied wasdetermined, then these MICs were compared each other.
In general, the antibacterial effect of PC-904 was as same as or a few times as powerful as that of SBPC.
2) Drug concentration in organs of rats
The drug concentration in organs of male rats (Wistar) after the intramuscular injection of 20 mg/kg of PC-904 was the highest in the liver, then in the kidneys, lungs and serum in order.
3) Serum concentration
2g of PC-904 diluted in 500ml of 5% glucose solution were drip infused for 2 hours into 3 chronic bronchitis patients whose renal functions were normal, then serum concentrations of PC-904 were measured. The peak levels were from 59 to 126 μg/ml at the end of infusion and it was from 15 to 30 μg/ml at 2 hours after and from 4.2 to 9.0μg/ml at 6 hours after the completion of infusion.
The half life of serum concentration revealed to be from 0.5 to 0.8 hours.
4) Diffusion of PC-904 into sputum and its concentration
When 2g of PC-904 were i. v. drip infused for 2 hours into 2 chronic bronchitis patients characte-rized by purulent sputa, the peak drug concentrations in sputa were from 0.06 to 0.62μg/ml, whichwas from 0.05 to 1.05% of the maximal serum levels.
5) Clinical application
The effects of PC-904 (from 2 to 4g per day) on 15 respiratory tract infections (9bronchopneumonia, 4 chronic bronchitis, 1 chronic panbronchiolitis, 1 pyothorax), 2 urinary tract infections and 1 cholecy-stitis were considered excellent in 5, good in 7, fair in 5 and poor in 1 case.
Among them, skin rashes were noted in 2 cases, but they were recovered quickly after withdrawalof the drug in one case and in the other one drug administration was continued without additionaltroubles.
