Ocular Penetration and Clinical Evaluation of Ceftezole for Ocular Infections

Summary

Intraocular penetration of Ceftezole (CTZ) was investigated in rabbit eye. The peak of aqueous humor level, 1.36 ug/ml, attained at one hour after intramuscular injection of 50mg/kg CTZ, and decreased rapidly to 2 hours. Aqueous/serum ratio in one hour was 7.4%.

After intravenous injection of 50mg/kg, the peak of aqueous level, 2.8ug/ml, revealled at 1/2 hour. The aqueous/serum ratio was 11.79%.

Compared with those of Cefazolin (CEZ), aqueous humor level of CTZ was seemd to be higher than that of CEZ. However, CEZ showed higher value of blood concentration.

Intramuscular or intravenous injections of 1.0g CTZ one or two daily revealled good effects on ocular infections, such as hordeolum, dacryocystitis, keratitis and endophthalmitis. No severe side ffects like allergic reactions were observed, and no abnormal finding in hepatic and renal tests were recognized.

Ceftezole (CTZ) has been synthesized as an analogous compound of Cefazolin (CEZ). It is a new member of the Cephalosporin group and is under development in the research laboratories of the Chugai Pharmaceutical Co. Ltd.

CTZ has a wide antibacterial spectrum for both gram positive and negative bacteria as in the case of CEZ. It possesses bactericidal action and sows antibacterial acitivity toward gram negative bacteria which are especially susceptible to Cephalosporin drugs.

The results of basic research on this drugs were repor- ted at the 14th Interscience Conference on Antimicrobial Agent and Chemotherapy in San Francisco in 1974.

We have studied on ocular penetration and clinical experiments for ophthalmic use of CTZ, and report these results as follows.