著者

井藤 達也 高岡 和夫 竹本 功 秦 温信 井上 勝一 佐々木 健太郎 平野 剛 井関 健 菅原 満 宮崎 勝巳

出版者

The Japanese Society of Clinical Pharmacology and Therapeutics

雑誌

臨床薬理 (ISSN:03881601)

巻号頁・発行日

vol.33, no.2, pp.47-52, 2002-03-31 (Released:2010-06-28)

参考文献数

13

---

The purpose of this study was to evaluate the distribution of CPT-11 and its active metabolite, SN-38, in pleural and pericardial fluid after intravenous administration.Two patients with lung cancer were treated with intravenous CPT-11 (60 mg/m2) on days 1, 8, and 15. The CPT-11 was detected in the pleural fluid 1.5 hr after the begining of intravenous infusion, and the level reached the maximum 24 hrs later. Similarly, the active metabolite SN-38 was detected in the pleural fluid 1.5 hr after the begining of intravenous infusion, and SN-38 concentration in the pleural fluid was almost as high as that in plasma 24 hrs later. These results suggest that intravenously administered CPT-11 may penetrate the thoracic cavity and may be metabolized to SN-38 there. The proportions of maximum concentrations of CPT-11 and SN-38 in the pleural fluid to the corresponding plasma levels were 20.4% and 28.5%, respectively. In addition, the AUCs of the lactone form SN-38 were much lower than those of the carboxyl form in the pleural fluid.CPT-11, SN-38 and SN-38 glucronide showed similar pharmacokinetics in the pericardium as that in plasma.

著者

井藤 達也

出版者

一般社団法人日本医療薬学会

雑誌

医療薬学 (ISSN:1346342X)

巻号頁・発行日

vol.28, no.6, pp.511-520, 2002-12-10 (Released:2011-03-04)

参考文献数

26

被引用文献数

1 2

---

The purpose of this study was to evaluate the distribution of CPT-11 and its active metabolite, SN-38, in both pleural and pericardial fluid after intravenous administration.Two patients with lung cancer were intravenously treated with 60mg/m2 CPT-11 on days 1, 8, and 15. The CPT-11 was detected in the pleural fluid 1.5 hrs after the start of intravenous infusion, and its level reached a maximum 24 hrs later. Similarly, the active metabolite SN-38 was detected in the pleural fluid 1.5 hrs after the start of intravenous infusion. In addition, the SN-38 concentration in the pleural fluid was almost as high as that in the plasma 24 hrs later. These results suggest that intravenously administered CPT-11 may penetrate into the thoracic cavity and therefore be metabolized into SN-38 there. The maximum concentrations of CPT-11 and SN-38 in the pleural fluid to the corresponding plasma levels were 20. 4 % and 28. 5%, respectively. In addition, the AUCs of the lactone form of SN-38 were much lower than that of the carboxyl form in the pleural fluid.CPT-11, SN-38 and SN-38 glucronide all showed similar pharmacokinetics in the pericardium to that in plasma.