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
✍ Scribed by Ronald Gust; Gunther Bernhardt; Thilo Spruß; Rudolf Krauser; Marion Koch; Helmut Schönenberger; Kurt-Heinz Bauer; Sabine Schertl; Zhi Lu
- Publisher
- John Wiley and Sons
- Year
- 1995
- Tongue
- English
- Weight
- 960 KB
- Volume
- 328
- Category
- Article
- ISSN
- 0365-6233
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✦ Synopsis
The development of a galenical formulation for poorly water soluble dichloroplatinum(I1) complexes suitable for the parenteral administration in cancer chemotherapy is described. The procedure, which we elaborated for [(+)-1,2-bis(4-fluorophenyI)ethyle- nediamine]dichloroplatinum(II) (rac-4F-PtClz), is based on the reaction of a soluble diaquaplatinum(I1) 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 ruc-4F-PtCl2, 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.