As the results of laboratory investigation with a new cephalosporin C derivative, Cephalexin (CEX), the following conculsions were obtained.
1)
In vitro antibacterial activity: CEX has a broad spectrum activity against gram positive and gram negative species of standard test organisms. The minimal inhibitory concentration of CEX against 80 strains of coagulase positive staphylococcus aureus isolated from otorrhoea was distributed over range of≤0.19-to≥100mcg/ml, with a peak being observed particullary at 6.25mcg/ml. Further, in 24 strains of streptococcus hemolyticus and diplococcus pneumoniae CEX inhibited their growth from≤0.19 to 25mcg/ml. while, that of CEX inhibited in most of the an agar cultures of gram negative bacteria, except pseudomonas aeruginosa and aerobacter aerogenes, against which the MIC of CEX ranged from 0.78-to≥100mcg/ml.
2) Concentration in blood: The blood level of CEX in healthy adults who were given 500mg of CEX orally reached maximum of 14.5mcg/ml 2 hours after the administration. Even at 6 hours after oral administration clinically effetcive serum CEX concentration of 1.04mcg/ml was still demonstrable.
3) Urinary excretion: The CEX was excreted in urine with high concentration until 6 hours and about 81.3 per cent recovered from urine up to 8 hours after oral administration in healthy adults.
4) Concentration in tissues: At 2 hours after a single oral dose 500mg, the concentration in the tissues of palatine tonsilla was 1.2mcg/g as against 9.3mcg/ml in the serum, and the concentration in the tissues of mucous membrane of maxillary sinus was 2.4mcg/g as compared with 8.3mcg/ml in the serum.
5) Clinical results: CEX was given orally in 38 cases with typical infection in the field of otorhinolaryngology. As a result, there were 16 “Excellent” responses, 17 “Good” responses, 5 “Fair” responses. CEX (Syncl) was effective in 33 cases, 87 per cent.
6) Side effect: The comparative examination of liver, electrocyte and audiogram before and after the admistration showed no significant disturbances, and CEX showed no side effect at all in administration.
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