PHARMACEUTICAL PREPARATIONS FOR THE THERAPY OF TUMORS CONTAINING COLCHICINE AS THE ACTIVE PRINCIPLE AND METHODS FOR THE USE OF THE SAME

Abstract: Pharmaceutical preparation for the therapy of tumors containing from 1.3 to 4.9 mg of colchicine and from 5 to 54 mg of 7 % aqueous acetic acid solution for each 10 ml of ethyl alcohol. The preparation so obtained is administered in subliminar dosages and, preferably, by translingual route.

Description: Descripti on / "Pharmaceutical preparations for the therapy of tumors containing colchicine as the active principle and methods for the use of the same ' ' . The present invention refers to pharmaceutical products for the therapy of tumors and, in particular, to two preparations containing colchicine as the active principle 5 Colchicine is an alkaloid extracted from "Colchicum a tumnalis". Its use is known in biology for the preparation of chromosomic paper and in medicine as anti- uric in the therapy of gout. It is also known that colchicine has the property of interfering in karyokinesis 10 inhibiting the formation of mitotic fusus and therefore preventing the cell division. Owing to this property colchicine has been utilized, substantially in the sperimental phase, for the treatment of Hodgkin's disease ( lymphogranuloma malignant). This therapeutic application, 15 carried out via intravenous injection and with remarkable dosages, did not give appreciable results and. above all, it showed itself variable in its effects and potentially ( dangerous owing to colchicine toxicity when _t is administered at high levels. 20 The object of the present invention is to provide preparations, containing colchicine as the active principle, effectively utilizable within the limits of the highest security in the therapy of human tumors, and to describe methods for such preparations. Such object is achieved, according to a first embodiment of the invention, with a preparation containing colchicine, at least 70% ethyl alcohol and a 7% aqueous acetic acid solution in the following proportions: from 1.3 to 4.9 mg of colchicine and from 5 to 54 mg of acetic acid aqueous solution for 10 ml of ethyl alcohol. Preferably, the colchicine utilized has a pharmacological purity index of 100 and the ethyl alcol has a content of 99.8%. In a second embodiment of the invention it is foreseen that the preparation contains colchicine dissolved in apyrogenic distilled water in an amount of 1.3-4.9 mg in 250 ml. The exact proportions of the components of the preparation are fixed from time to time according to the specific applicative requirements, that is in relation to the patient body weight, the histopathological type of the neoplasia to be cured and the general conditions of the emunctory organs and of the hematochemical parameters of permissibility. The preparation according to the first embodiment is obtained without particular precaution, but observing the usual cautions for the pharmaceutical preparations dissolving at room temperature colchicine in ethyl alcol and then adding the acid acetic aqueous solution. Similarly, the preparation according to the second embodiment is obtained dissolving at room temperature colchicine in apyrogenic distilled water. The method according to the invention foresees that the preparations so obtained are administered in subliminar dosages, that is lower than the limit dosages to which colchicine has its main pharmacological effect. At such dosages colchicine has the property to cause an explosion of mitosis of potentially blastic cells, stopping their karyokinesis in pre-metaphase, accelerating their prophase and stopping in pre-metaphase the inverse transcriptase. Further, when the preparation is utilized according to the first embodiment, it is preferable that the administration is effected by translingual route, so that the drug is subtracted to the hepatic circulation that would alter or reduce the effect: As indicative form, and not in any way in limitative sense, an effective dosage may be as follow: - attack phase: 10 ml every 10th days for three times - consolidation and mantainance phase: 9 drops every day for one year. Regarding the use of the preparation according to the second form of embodiment, the preparation is best administered by intravenous injection in slow drops, that is at 30-40 drops/minute.

Claims: Claims 1. Pharmaceutical preparation for the therapy of tumors, containing colchicine as the active principle, characterized by the fact that it contains the following substances: - colchicine, - at least 70% ethyl alcohol, and - about 7% aqueous acetic acid solution, in the following proportions: - from 1.3 to 4.9 mg of colchicine and - from 5 to 54 mg of aqueous acetic acid solution in 10 ml of ethyl alcol. 2. Pharmaceutical preparation according to claim 1, characterized by the fact chat colchicine has a pharmacological purity index of about 100 and ethyl alcol has a concentration of about 99.8%. 3. Pharmaceutial preparation for the therapy of tumors containing colchicine as the active principle, cha acterized by the facr that colchicine is dissolved in apyrogenic distilled water in concentration of 1.3-4.S mg in 250 ml. 4. Method of use of the preparation according to claims 1, 2 or 3, characterized by the fact that the preparation is administered in subliminar doses. 5. Method according to claim 4 for the use of the preparation according to claim 1 or 2, characterized by the fact that the preparation is administered by translingual route. 6. Method according to claim 4 for the use of the preparation according to claim 3, characterized by the fact that the preparation is administered intravenously in slow drops.

Inventors: BONURA GIORGIO, SANTOLIQUIDO GAETANO, BONURA, GIORGIO, SANTOLIQUIDO, GAETANO
Applicants: BONURA GIORGIO, SANTOLIQUIDO GAETANO, BONURA, GIORGIO, SANTOLIQUIDO, GAETANO
Application year: 1992
Main classification: A61K47
IPC codes: A61K9, A61K31, A61K47