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Development of a Parenterally Administrable Hydrosol Preparation of the “Third Generation Platinum Complex” [(±)‐1,2‐Bis(4‐fluorophenyl)ethylenediamine]dichloroplatinum(II). Part 1. Preparation and Studies on the Stability and Antitumor Activity
Author(s) -
Gust Ronald,
Bernhardt Gunther,
Spruß Thilo,
Krauser Rudolf,
Koch Marion,
Schönenberger Helmut,
Bauer KurtHeinz,
Schertl Sabine,
Lu Zhi
Publication year - 1995
Publication title -
archiv der pharmazie
Language(s) - English
Resource type - Journals
SCImago Journal Rank - 0.468
H-Index - 61
eISSN - 1521-4184
pISSN - 0365-6233
DOI - 10.1002/ardp.19953280904
Subject(s) - ethylenediamine , hydrosol , chemistry , poloxamer , platinum , nuclear chemistry , organic chemistry , catalysis , polymer , copolymer
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)ethylenediamine]dichloroplatinum(II) ( rac ‐4F‐PtCl 2 ), 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‐PtCl 2 , which was ineffective towards the hormone sensitive MXT‐M‐3.2 breast cancer of the mouse, its hydrosol formulation proved to be highly active and was very well tolerated.