[Pharmacokinetics of N4-behenoyl-1-beta-D-arabinofuranosylcytosine after intraperitoneal administration].
The patients with cartinomatous peritonitis were treated with the intraperitoneal administration (ip) of N4-behenoyl-1-beta-D-arabinofuranosylcytosineine (BH-AC: analogue of Ara-C), and the pharmacokinetics of BH-AC ip was studied. The following results were obtained (1) Immediately after ip administration, the concentration of BH-AC in ascites became as high as 10(6) ng/ml. At 24 hours following BH-AC ip, 10(4) ng/ml of BH-AC was detected in ascites. (2) Immediately after ip administration the concentration of Ara-C derived from BH-AC in ascites became as high as 10(3) ng/ml. At 24 hours, more than 10 ng/ml of Ara-C was detected in the ascites. (3) Ara-U in ascites was detected also soon after BH-AC ip was performed. Accordingly, it is expected that deaminase may be present in ascites. (4) As compared with in ascites, Ara-C in plasma showed very low level (less than 1 ng/ml). These findings indicate that BH-AC is suitable drug for intraperitoneal administration, because BH-AC revealed low peritoneal and high plasma clearances.
Noda
T
T
Dept. of Obstetrics and Gynecology, Nara Medical University.
Oku
M
M
Kiyozuka
Y
Y
Maruyama
M
M
Adachi
S
S
Akada
S
S
Okamura
Y
Y
Ichijo
M
M
D000368:Aged; D000970:Antineoplastic Agents / Q000008:administration & dosage / Q000493:pharmacokinetics*; D001202:Ascitic Fluid / Q000378:metabolism; D003536:Cystadenocarcinoma / Q000188:drug therapy / Q000378:metabolism; D003561:Cytarabine / Q000008:administration & dosage / Q000031:analogs & derivatives* / Q000493:pharmacokinetics; D005260:Female; D006801:Humans; D007263:Infusions, Parenteral; D008875:Middle Aged; D010051:Ovarian Neoplasms / Q000188:drug therapy / Q000378:metabolism; D010538:Peritonitis / Q000188:drug therapy / Q000378:metabolism; D014594:Uterine Neoplasms / Q000188:drug therapy / Q000378:metabolism
D000970:Antineoplastic Agents; D003561:Cytarabine; C015019:enocitabine