A SLOW-RELEASE METHOTREXATE FORMULATION FOR INTRATHECAL CHEMOTHERAPY

被引：18

作者：

CHATELUT, E ^{[1
]}

KIM, T ^{[1
]}

KIM, S ^{[1
]}

机构：

[1] UNIV CALIF SAN DIEGO,CTR CANC,LA JOLLA,CA 92103

来源：

CANCER CHEMOTHERAPY AND PHARMACOLOGY | 1993年 / 32卷 / 03期

关键词：

D O I：

10.1007/BF00685832

中图分类号：

R73 [肿瘤学];

学科分类号：

100214 ;

摘要：

Optimal anticancer treatment with cell cycle phase-specific antimetabolites requires a sustained maintenance of cytotoxic drug levels. However, drugs that can be administered intrathecally have short half-lives in cerebrospinal fluid (CSF) and require repeated administrations by lumbar punctures, which are painful and inconvenient. Implantable pumps are expensive and require surgery. In a rat model, a lipid-based formulation of methotrexate (Depo/methotrexate) was tested for extended maintenance of therapeutic CSF concentration after a single injection. The half-life of methotrexate in CSF after an intracisternal injection of Depo/methotrexate was 5.4 days compared to 0.30 days for unencapsulated methotrexate. This 18-fold increase in methotrexate half-life may make Depo/methotrexate useful for intrathecal chemotherapy of neoplastic meningitis.

引用

页码：179 / 182

页数：4

共 14 条

[1] HIGH-PERFORMANCE LIQUID-CHROMATOGRAPHIC DETERMINATION OF METHOTREXATE IN PLASMA [J].