Development of a parenterally administrable hydrosol preparation of the ''third generation platinum complex'' [(+/-)-1,2-bis(4-fluorophenyl)ethylenediamine]dichloroplatinum(II) .1. Preparation and studies on the stability and antitumor activity

被引：9

作者：

Gust, R ^{[1
]}

Bernhardt, G ^{[1
]}

Spruss, T ^{[1
]}

Krauser, R ^{[1
]}

Koch, M ^{[1
]}

Schoenenberger, H ^{[1
]}

Bauer, KH ^{[1
]}

Schertl, S ^{[1
]}

Lu, Z ^{[1
]}

机构：

[1] UNIV FREIBURG,INST PHARM,FREIBURGER MAT FORSCHUNGSZENTRUM,LEHRSTUHL PHARMAZEUT TECHNOL,D-79104 FREIBURG,GERMANY

来源：

ARCHIV DER PHARMAZIE | 1995年 / 328卷 / 09期

关键词：

Pt-complex solubilization; hydrosol breast cancer inhibiting properties;

D O I：

10.1002/ardp.19953280904

中图分类号：

R914 [药物化学];

学科分类号：

100701 ;

摘要：

The development of a galenical formulation for poorly water soluble dichloroplatinum(II) complexes suitable for the parenteral administration in cancer chemotherapy is described. The procedure, which we elaborated for [(+/-)-1,2-bis(4-fluorophenyl)ethlenediamine]dichloroplatinum(II) (rac-4F-PtCl2), is based on the reaction of a soluble diaquaplatinum(II) salt with sodium chloride in water in the presence of pluronic F 68 as stabilizer and results in a sufficiently stable colloidal solution (i.e. hydrosol). In contrast to the poorly water soluble synthetic rac-4F-PtCl2, which was ineffective towards the hormone sensitive MXT-M-3.2 breast cancer of the mouse, its hydros of formulation proved to be highly active and was very well tolerated.

引用

页码：645 / 653

页数：9

共 22 条

[1]

ANDREWS PA, 1991, PLATINUM AND OTHER METAL COORDINATION COMPOUNDS IN CANCER CHEMOTHERAPY, P151

[2]

BEDNARSKI PJ, 1994, DRUG METAB DISPOS, V22, P419

[3] DIAMINE LIGAND RELEASE FROM THE CISPLATIN ANALOG [MESO-1,2-BIS(2,6-DICHLORO-4-HYDROXYPHENYL)ETHYLENEDIAMINE]DICHLOROPLATINUM(II) IN CELL-CULTURE MEDIUM [J].