The platinum complex [meso-1,2-bis(2,6-dichloro-4-hydroxyphenyl)- ethylenediamine]dichloroplatinum(II),K, was tested for its antitumor activity on hormone-sensitive tumor models under peroral administration. The resorption from the gastrointestinal tract was proved by determining the estrogenic effect of K in a dose/activity study using the immature-mouse uterine weight test. In comparison to the subcutaneous injection, a tenfold peroral dose was administered to achieve identical effects. By peroral treatment of the hormone-sensitive MXT(M3.2) mammary carcinoma of the mouse with K an almost complete inhibition of the tumor growth was obtained. This effect was superior to that of subcutaneously applied cisplatin and significantly better than that obtained by perorally administered ligand L at an equimolar dose, indicating that the antitumor effect is caused by the intact complex K and not by the liberated ligand L. The strong antitumor activity of perorally applied K was also demonstrated on the hormone-sensitive Noble Nb-R prostatic carcinoma of the rat. Histological examinations showed that the platinum complex K did not cause cisplatin-like kidney damage or irritations of gastric or intestinal mucosa when given perorally.
Common pharmaceutical excipients and compounds were dried either by a simple convection method or by a combined convection and microwave method in a static bed or by a combined microwave and vacuum method in a mixed bed. A simple placebo granulation was dried by an exclusive vacuum method and by a combined microwave and vacuum method in a mixed bed. The results were compared.
Practically all low molecular weight surfactants show hemolytic activities. Aside of this serious disadvantage .almost all low molecular weight solubilizers cause considerable side effects, particularly during or alter parented application. Polymeric surfactants, however, usually show no or only very little hemolytic effects. They therefore are supposed not to be able to penetrate neither into cellular or erythrocyte walls nor into phospholipid bilayers, resp.,similar bilayer membranes due to their large molecular size. Therefore no decay of biological bilayers should be expected with polymeric surfactants. The only phannaceuticdly widely used polymeric surfactants are at the moment polyoxyethylene-polyoxypropylene block copolymers (poloxamers 0, Pluronics" and Pluriols@). Unfortunately they have only poor solubility capacities.In order to find better solubilizing polymeric surfactants, some water soluble dextran fatty acid estem (Ref. 1) were synthesized and tested with respect to their solubilisation capacity and hemolytic activity.Usually the hemolytic activity is tested by standard methods using puxified animal or human erythrocyte suspensions. As erythrocytes also contain a relatively high amount of lactose dehydrogenase (LDH), we studied the suitability of the highly sensitive, and in the medical diagnostic well known LDH test, as a supplemental hemolytic detennination method (Ref. 2). The advantage of this test is, that there is no need of the time consuming purification and standardization as it is required with the erythrocytes' suspension. It can be perfonned with original blood and without costly preparations at all.The synthesized dextran fatty acid esters proved themselves as very little hemolytic and, compared with the polyoxyethylene-polyoxypmpylene block copolymers, they show improved solubilisation capacities.
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