Antitumor agent

 

(57) Abstract:

The invention relates to anticancer remedies to treat some cancers: leukemia, adenocarcinoma, cervical cancer, melanoma, sarcoma, carcinoma Lewis, hepatoma and other diseases. Antitumor agent comprises a connection plate CIS-diamminedichloroplatinum /IV/ number 10 - 25%, sodium bicarbonate in the amount of 25 to 55% and the sodium alginate in the number of 40 - 60%. Antitumor agent containing CIS-diamminedichloroplatinum /IV/ has activity in oral administration, the lack of nephrotoxicity, the growth inhibition of metastasis, high breadth of therapeutic action, a wide range of therapeutic action. table 2.

The invention relates to medicine, in particular to a tool with a broad spectrum of antitumor activity.

Known antitumor agent cisplatin, which is derived from CIS-diamminedichloroplatinum /II/ /I/. It is used in medical practice in the treatment of malignant tumors of the ovary and ovarian cancer, cervical cancer, bladder, when blockallocator cancer of the head and neck osteosarcoma. the I in tumors, not enough inhibits the growth of metastases.

The present invention was to eliminate the above disadvantages.

Problem solved by creating applied oral anticancer drug based on CIS-dihydroxydiphenylsulfone /IV/, /so-called oxiplatin, sodium alginate and sodium bicarbonate, taken in the following proportions: CIS-diamminedichloroplatinum /IV/-10-25% sodium bicarbonate-25-55% sodium alginate 40 60%

Bicarbonate plays the following role.

1. Is baking powder tablets. When hit in the stomach in the acidic environment of gastric juice produces carbon dioxide.

2. Neutralization of the acidic environment of gastric juice by dissolving tablet prevents substitution of hydroxyl groups oxiplatin on chlorosilane education tetrachloride.

3. The formation of sodium chloride when interacting with hydrochloric acid sodium bicarbonate contributes to the stabilization of chlorine ions in CIS-diamminedichloroplatinum platinum /IV/.

The choice of sodium alginate as a filler associated with its high binding properties, and that its interaction with the salt kilosegment tetravalent platinum with high antitumor activity is a yellow crystalline substance, the solubility of which in water is 0.3% compared with cisplatin is significantly less toxic drug. In particular, when administered intravenously into the body does not show nephrotoxicity and in the range of optimal therapeutic doses of up to the maximum tolerated ranges from 10-40 mg/kg up to 100-120 mg/kg, respectively, whereas the cisplatin this range significantly already, and equals 2-4 mg/kg to 10 mg/kg

As can be seen from the table. 1 oxaliplatin inhibits the development of metastases, whereas cisplatin in some cases stimulates their growth.

Antitumor agent is a tablet, the active principle of which is oxaliplatin /NH3Cl/2/OH/2Pt, as baking powder is sodium bicarbonate, and as the binder component aldehyde sodium. The tablet is obtained by mixing all ingredients. The composition of the tablets varies within the following limits: oxaliplatin 10-25% sodium bicarbonate 25-55% sodium alginate 40-60% of the Total weight of the tablet is 0.35 to 0.60, Content oxiplatin was determined based on the required treatment dose, the content of sodium bicarbonate was determined on the one hand, the speed and completeness of dissolution of the tablet in rabbia in the tablet of sodium alginate is determined by its strength, as the upper need not exceed its mass.

The mixture of the composition is thoroughly crushed and mixed in a ball mill to obtain a powder of uniform composition. About the homogeneity of the product was judged on the basis of the analysis of the content of platinum in two parallel samples taken from five points selected according to the method of the envelope. The thus prepared mixture of alloy preformed in the usual way.

Example. 100 g oxiplatin, 200 g of sodium bicarbonate and 300 g of sodium alginate was dispersively and stirred until smooth in a ball mill. About the homogeneity of the obtained powder was judged by the results of the analysis of the content of platinum in two parallel samples taken from five occuapancy according to the method of the envelope. The thus prepared mixture of alloy preformed conventional method. 600 g of a mixture in the tabletting received 95-100 tablets, each of which weighs 0,600, the Content of platinum in the tablet 9,50,3%

Antitumor activity was tested on linear mice with various transplantable tumors. The tablet was ground into powder and with food oral introduced into the body of the mouse. therapeutic effect was evaluated by the percentage inhibition of growth /SRW/ solid what you are given in table. 2.

From the data table. 2 shows that the claimed anti-cancer agent has significant advantages over cisplatin.

1. It is active when administered orally in the body.

2. A distinct lack of nephrotoxicity.

3. Has more pronounced than that of cisplatin, growth inhibition of metastasis, which is due to the fact that it is concentrated in the tissues of tumors.

4. More powerful than cisplatin, range of therapeutic action.

5. Is greater than that of cisplatin, breadth of therapeutic effect.

Antitumor agent based on CIS-diaminononane platinum, characterized in that it as platinum compounds contains CIS-diaminedichloroplatinum IV, sodium bicarbonate and sodium alginate in the following ratio, wt.

CIS-diaminedichloroplatinum IV 10 25

Sodium bicarbonate 25 55

Sodium alginate 40 601

 

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