Pharmacokinetic and immunosuppressive effects of tacrolimus-loaded biodegradable microspheres

Autor: Takeji Uno, Yoshiaki Kawashima, Hideo Kawarasaki, Koh-ichi Sakamoto, Li Xiao-Kang, Hirofumi Takenaka, Hiromitsu Yamamoto, Hisakuni Hashimoto, Yasunori Miyamoto
Rok vydání: 2004
Předmět:
Zdroj: Liver Transplantation. 10:392-396
ISSN: 1527-6473
1527-6465
Popis: The objective of this study was to characterize the pharmacokinetics and immunosuppression of a tacrolimus-loaded biodegradable microsphere (TLBM) in rats. We prepared TLBM. DA/Slc rats were given TLBM at a dose of 1.6 mg/kg (n = 9), 2.4 mg/kg (n = 5), or 7.2 mg/kg (n = 7) tacrolimus contents by a single subcutaneous administration to achieve sustained release over a long period. DA/Slc rats were given TLBM by a single subcutaneous administration at a dose of 4.8 mg/kg (n = 6) tacrolimus contents to clarify the main site of TLBM uptake in the organs. In the rat liver transplantation model, the recipients were given TLBM at a dose of 0.16 mg/kg (n = 5), 2.4 mg/kg (n = 4), or 4.8 mg/kg (n = 5) tacrolimus contents by a single subcutaneous administration on the first day after operation. Overall survival days were compared. Continuous flat parallel concentration profiles were significant for 10 days from the first day after a single subcutaneous administration of TLBM (P
Databáze: OpenAIRE