Radio-sensitizing agent for treatment of cancer

 

(57) Abstract:

The invention relates to medicine, in particular to cancer, and can be used in radiation therapy of malignant tumors. The invention lies in the fact that radio-sensitizing substance includes 8-Bromley and the solvent, the solvent used polyoxyethylenesorbitan monolead, or polyoxyethylenesorbitan stearate, or polyoxyethylenesorbitan monolaurate, or polyoxyethylenesorbitan monopalmitate, or polyoxyethylenesorbitan the monostearate, or polyoxyethylenesorbitan tristearate, it further comprises methylcellulose, calcium stearate or magnesium and starch in the proposed ratio of ingredients. The invention provides a high clinical effect due to improvement in the absorbability of the drug in the body and increase its resistance and the possibility of pre-production and long-term storage.

The invention relates to medicine, in particular to cancer, and can be used in radiation therapy of malignant tumors.

Known radio-sensitizing substance used in Oncology, containing m, N - bucillamine applications due to its high toxicity.

Known means, having a radio-sensitizing effect on hypoxic tumor cells in radiation therapy of malignant tumors containing ester of succinic acid, see patent of Russian Federation N 2052991 class A 61 K 31/41 from 15.08.1984.

Succinic acid, although low-toxic, but its radio-sensitizing effect is not confirmed in the clinical setting. The effect is only on hypoxic tumor cells, which is rare. The drug is intravenously in an amount corresponding to the number of sessions of radiation therapy (25-30), which is associated with an additional detrimental effect on the body and therefore not always feasible.

Known radio-sensitizing substances containing compounds intorimidazole, see , for example, U.S. patent N 5304654 class C 07 D 233/91 from 19.04.1994.

Such compounds have high toxicity, exposure is carried out exclusively in cells under hypoxia, with the introduction of the drug is necessary to create and maintain the desired threshold substance concentration in the tumor tissue, which is very difficult. Connection intorimidazole, in particular metronidazole, use the STW for treatment of malignant tumors of different histogenesis and localization, containing an aqueous solution of 8-brancoveanu. This drug is easily tolerated when used in effective dosages. The introduction of the drug not tied rigidly to the time of radiation therapy, see , for example, L. P. Vartanyan and others, "effectiveness of the derivative of caffeine with radiation and chemotherapy of brain neoplasms" Actual problems of experimental and clinical pharmacology", materials of all-Russian scientific conference with international participation, St. Petersburg, 1999, S. 37, 38 (reference copy attached).

This substance is taken as a prototype of the present invention.

The disadvantage of this substance is relatively low clinical effect due to poor solubility of 8-brancoveanu in water and biological environments of the body. Water-insoluble particles of the drug have a very large range of sizes: from dust to glibtoolize. Particles tend to stick together and enlargement of their size. This leads to poor absorption of the drug in the body and, ultimately, his lack of effectiveness. In addition, the drug starts to collapse already in the oral cavity, which reduces its effectiveness; substance very nesticle or sometimes even impossible in real clinical conditions.

The present invention laid the task of creating a radio-sensitizing substances for the treatment of cancer, which would have a high clinical effect due to improvement in the absorbability of the drug in the body and increase its resistance, ensuring the possibility of pre-production and long-term storage.

According to the invention this problem is solved due to the fact that radio-sensitizing agent for the treatment of cancer includes 8-Bromley and the solvent, the solvent used polyoxyethylenesorbitan monooleate, or polyoxyethylenesorbitan stearate, or polyoxyethylenesorbitan monolaurate, or polyoxyethylenesorbitan monopalmitate, or polyoxyethylenesorbitan the monostearate, or polyoxyethylenesorbitan tristearate, it further comprises methylcellulose, calcium stearate or magnesium and starch in the following ratio of ingredients, wt.%:

8-bromophen - 75-96

the methylcellulose and 0.5-2

calcium stearate or magnesium - 0,5-1

starch - 2,5-20

polyoxyethylenesorbitan monooleate, or polyoxyethylenesorbitan stearate, or polyoxyethylenesorbitan monolaurate, or polyoxy is at - 0,5-2

The applicant has not identified any decision that is identical to the claimed invention, which allows to make a conclusion about its compliance with the criterion of "novelty".

Thanks to the implementation of the invention radio-sensitizing substance becomes important new properties, consisting in the fact that the particles of the drug are approximately the same size, which makes them uniform emulsification and flow in the body.

Also prevents the adhesion and aggregation of the particles. In addition, the drug becomes bioavailable not before it enters the stomach and small intestine. This 8-Bromley transitions in emulsified condition and is significantly better absorbed.

The drug can be manufactured in the form of pills, which can be stored for at least two years. When released tablets in the biological environment of the body it intensively absorbs water and evenly breaks up after a desired time (15-40 min) shallow well suction fragments.

These circumstances determine, according to the applicant, the proposed technical solutions to the criterion of "inventive step".

Clinical tests conducted at the Medical radilova M I., 1927, R., diagnosis: primary multiple cancer of the skin of the right forearm, right submandibular region, the ear area on the right. Applied the stated radio-sensitizing substance in tablet form in the following ratio of ingredients, wt.%:

8-bromophen - 80

methylcellulose - 0,5

calcium stearate and 0.5

starch - 18,5

polyoxyethylenesorbitan the monostearate and 0.5

The drug is administered at a dosage of 0.5 g twice a day for 8 days during radiotherapy to 4 Grams a day to the total focal dose (SOD) - 20 G, followed by 5 Grams to SOD - 40 Gr.

Thanks to effective radiosensibility were excluded surgical and hemiauchenia.

Achieved remission, which continues during the period of observation.

Example 2. Patient Pozdnyakov C. S., 1934, R., diagnosis: primary multiple cancer upper and lower thirds of the esophagus. Applied radio-sensitizing substance in tablet form in the following ratio of ingredients, wt.%:

8-bromophen - 88

methylcellulose - 1,5

calcium stearate - 0,8

starch - 8,2

polyoxyethylenesorbitan monooleate - 1,5

Radiation therapy according to the scheme given in example 1.

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Example 3. Patient Kornilova, A. I., 1936, R., diagnosis: malignant fibrous histiocytoma soft tissues of the back. Used the drug in tablet form in the following ratio of ingredients, wt.%:

8-bromophen - 96

methylcellulose - 0,5

magnesium stearate and 0.5

starch - 2,5

polyoxyethylenesorbitan monopalmitate - 0,5

Radiation therapy to 4 Grams a day until COD is 24 Gy, followed by 5 Grams to COD - 44 Gr.

Additionally chemotherapy: cisplatin 150 mg 2 times. Achieved reduction of tumor size, improvement in overall health.

Conducted long-term tests showed that in most cases the most effective in the claimed range is the ratio of ingredients, similar to those given in example 2. These pharmaceutically acceptable compounds polyethylenimine almost equivalent.

The drug is made in the conditions of pharmaceutical production of well-known, readily available components, which confirms the conformity of the invention, the criterion of "industrial applicability".

Radio-sensitizing agent for the treatment of cancer, including 8-Bromley and solvent, otlecheylard, or polyoxyethylenesorbitan monolaurate, or polyoxyethylenesorbitan monopalmitate, or polyoxyethylenesorbitan the monostearate, or polyoxyethylenesorbitan tristearate, it further comprises methylcellulose, calcium stearate or magnesium and starch in the following ratio of ingredients, wt.%:

8-Bromophen - 75 - 96

The methylcellulose and 0.5 - 2

Calcium stearate or magnesium - 0,5 - 1

Starch - 2,5 - 20

Polyoxyethylenesorbitan monooleate, or polyoxyethylenesorbitan stearate, or polyoxyethylenesorbitan monopalmitate, or polyoxyethylenesorbitan the monostearate, or polyoxyethylenesorbitan tristearate - 0,5 - 2

 

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