[Pharmacokinetic study of implantable gentamycin preparations. I. Antibiotic pharmacokinetics in the implantation area and an evaluation of the prolonged effect of the preparations].
Gentamicin pharmacokinetics was studied in the zone of subcutaneous implantation to rats of Septopal, a dosage form based on polymethylmethacrylate stable in vivo (4.5 mg of the antibiotic) and of preparations based on biodegradable polymers such as monocarboxycellulose, alginic acid, nonmodified and modified collagens (1 and 5 mg of the antibiotic). A three-phase pattern of gentamicin level changing in the implantation zone was observed: (1) rapid increasing and decreasing of the antibiotic concentration, (2) stabilization of the gentamicin content at a practically constant level and (3) slow lowering of the antibiotic level in the tissue. Comparison of the areas under the concentration/time curves showed that the modified collagen, alginic acid and monocarboxycellulose had the highest prolongation effect among the biodegradable polymers. Their use in the compositions provided during the first hours after the implantation the antibiotic concentrations in the administration site equal to tens micrograms per 1 g of the tissue. After that during 14 days the concentration of gentamicin in the implantation zone maintained at the level higher than its MIC for the main pathogens of wound infections.
Nazarov
A D
AD
Firsov
A A
AA
Navashin
P S
PS
Fomina
I P
IP
Rudenko
T G
TG
D000042:Absorption; D000818:Animals; D001673:Biodegradation, Environmental; D001682:Biological Availability; D003692:Delayed-Action Preparations; D004337:Drug Carriers; D004343:Drug Implants; D005839:Gentamicins / Q000008:administration & dosage / Q000493:pharmacokinetics*; D008297:Male; D011108:Polymers / Q000493:pharmacokinetics; D051381:Rats; D013997:Time Factors
D003692:Delayed-Action Preparations; D004337:Drug Carriers; D004343:Drug Implants; D005839:Gentamicins; D011108:Polymers
Farmakokineticheskoe izuchenie implantiruemykh preparatov gentamitsina. I. Farmakokinetika antibiotikov v zone implantatsii i otsenka prolongiruiushchego éffekta preparatov.