[The studies on distributions of cefsulodin and cefotiam to human aqueous humor and cornea].

ABSTRACT

Distributions of cefsulodin (CFS) and cefotiam (CTM), new parenteral cephalosporins, to human aqueous humor and cornea were studied in comparison with those of sulbenicillin (SBPC) and cefazolin (CEZ), and pharmacokinetic analysis was made by theory of compartment model, to obtain the following results. 1. Maximum aqueous humor levels of CFS and CTM were noticed at 2.5 hours after the start of 1 g CFS or CTM administration by 30 minute intravenous drip infusion, with the levels of 3.6 micrograms/ml and 4.2 micrograms/ml respectively. On the other hand, in case of 5 g SBPC or 2 g CEZ administration maximum aqueous humor levels were 12.5 micrograms/ml and 5.2 micrograms/ml respectively. 2. The ratios of maximum aqueous humor level to plasma level of the same time in CFS, CTM, SBPC and CEZ were 15.0, 16.8, 6.4% and 5.5%. Distribution of CFS or CTM was 2 to 3 times better than that of SBPC or CEZ. 3. From the result of pharmacokinetic analysis, ratios of aqueous humor to plasma levels in area under curves (AUC) of CFS, CTM, SBPC and CEZ were 25.6, 29.9, 16.4% and 7.9% respectively. Maximum aqueous humor levels of CFS, CTM, SBPC and CEZ were 2.9, 3.6, 11.4 micrograms/ml and 4.3 micrograms/ml and biological half life of gamma-phase were 2.57, 2.31, 2.77 hours and 2.24 hours respectively. 4. Cornea levels of CFS or CTM at one hour after the start of 1 g CFS or CTM administration by 30 minutes intravenous drip infusion were 2.9 micrograms/g and 5.2 micrograms/g, and their ratios to plasma level were 7.5% or 14.3% respectively. In case of 5 g SBPC or 2 g CEZ administration, the cornea levels were 26.7 micrograms/g and 5.0 micrograms/g, and the ratios were 9.4% and 3.4% respectively. 5. From the above, the distribution of CFS or CTM to human aqueous humor and cornea is better than that of SBPC or CEZ, and it is considered that clinical usefulness of both CFS and CTM by parenteral administration is expected in intraocular infections.