Formulation and Evaluation of Irinotecan Suppository for Rectal Administration.
- Author:
Haiyang FENG
1
;
Yuping ZHU
;
Dechuan LI
Author Information
1. Colorectal Surgery, Zhejiang Cancer Hospital, Hangzhou 310-022, China. dchuanli@sina.com
- Publication Type:Original Article
- Keywords:
Irinotecan;
Oral;
Rectal;
Pharmacokinetics;
HPLC
- MeSH:
Administration, Rectal*;
Biological Availability;
Chromatography, High Pressure Liquid;
Fluorescence;
Pharmacokinetics;
Plasma;
Rabbits
- From:Biomolecules & Therapeutics
2014;22(1):78-81
- CountryRepublic of Korea
- Language:English
-
Abstract:
Irinotecan suppository was prepared using the moulding method with a homogeneous blend. A sensitive and specific fluorescence method was developed and validated for the determination of irinotecan in plasma using HPLC. The pharmacokinetics of intravenous administered and rectal administered in rabbits was investigated. Following a single intravenous dose of irinotecan (50 mg/kg), the plasma irinotecan concentration demonstrated a bi-exponential decay, with a rapid decline over 15 min. C(max), t(1/2), AUC(0-30h) and AUC(0-infinity) were 16.1 +/- 2.7 g/ml, 7.6 +/- 1.2 h, 71.3 +/- 8.8 microg.h/ml and 82.3 +/- 9.5 microg.h/ml, respectively. Following rectal administration of 100 mg/kg irinotecan, the plasma irinotecan concentration reached a peak of 5.3 +/- 2.5 microg/ml at 4 h. The AUC(0-30h) and AUC(0-infinity) were 32.2 +/- 6.2 microg.h/ml and 41.6 +/- 7.2 microg.h/ml, respectively. It representing ~50.6% of the absolute bioavailability.
