DE3319304A1 - MEDICINAL PRODUCTS WITH ANTINEOPLASTIC EFFECT - Google Patents

Description

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The invention relates to drugs with antineoplastic Effect that as active ingredient component (a) at least one Polyfluoroalcohol of the general formula I

CHF ₀ - (CF ₀ ) - CH _n OH (I)

Z 2 η 2

TO in which η has the value 3, 5, '7 or 9, and optionally contain cholesterol as component (b).

The medicaments of the invention preferably contain at least two and in particular at least three polyfluoroalcohols of the general formula I and cholesterol. The relative proportions of the three polyfluorinated alcohols in the preferred medicaments of the invention can be in a relatively wide range, for example from 12 parts of dodecafluoroheptanol (formula I, η = 5), 1 part of octafluoropentanol (formula I, η = 3) and 1 part of hexadecafluorononanol (Formula I, η = 7) to 1 part of dodecafluorohexanol, 1 part of octafluoropentanol and 12 parts of hexadecafluorononanol.

The relative proportions of polyfluorinated alcohol and cholesterol can range from 10: 1 to 1: 10 lie.

The medicaments of the invention can also be lipophilic Carrier, preferably sesame oil, included. However, similar substances can also be used. All Substances of the medicaments of the invention are known.

The examples illustrate the invention. 35

- 4 - 'Example

3 g of octafluoropentanol, 5 g of dodecafluoroheptanol and 7.5 g of hexadecafluorononanol are dissolved in 150 g of sesame oil. The solution obtained is mixed with 2.5 g of cholesterol while briefly heating to 35 to 40 ^{° C.}

Example 2

100 g sesame oil. are with 2.5 g of dodecafluoroheptanol, 2.5 g Hexadecafluorononanol, 5 g octafluoropentanol and 4 g cholesterol offset. The mixture is stirred until all of the ingredients are completely dissolved.

15 'Example 3

174 g of sesame oil are mixed with the following ingredients:

Dodecafluoroheptanol (I, n = 5) 12g

Hexadecafluorononal (I, η = 7) 4g

Octafluoropentanol (I, η = 3) 4g

Cholesterol 6 g

The mixture is stirred until all of the ingredients are dissolved. The resulting solution is in 0.2 ml, 0.3 ml and 0.5 ml filled ampoules which are sterilized by heating.

Example 4 '■

Example 1 is repeated, but an additional 2 g of eicosafluorundecanol (I, η = 9) are added.

Example5

Example 1 is repeated, but the hexadecafluorononanol replaced by an equal amount of octafluoropentanol.

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Examples

Example 3 is repeated, but without adding cholesterol.

With the drug prepared according to Example 3, the acute toxicity, subacute toxicity and chronic toxicity certainly.

Acute toxicity:

When subcutaneous "administration of doses above 0.5 ml to mice with a body weight of 30 g shows sleep as the only symptom. The animals wake up after a few hours without normal Sign up. The same phenomenon occurs in rats at doses above 1.5 ml per 100 g of body weight.

Subacute toxicity:

When administered subcutaneously in an amount of 0.3 ml / day during 5 days within the 1st week and for three consecutive ■ No toxic symptoms were observed in mice with a body weight of 30 g after several weeks. There aren't any determine pathological changes in the killed animals.

Chronic toxicity:

Mice with a body weight of 30 g are subcutaneously 0.2 ml / Day given three times a week for three consecutive months. The animals did not show any abnormal reactions versus the control group. There were no pathological changes in the killed animals either.

. The same results are observed with subcutaneous administration of 0.4 ml per 100 g of body weight to rats. Even with oral Administration to mice and rats by means of a catheter in one Amounts of 0.2 ml / day or 0.4 ml / 100 g body weight / day (in rats) for a longer period of time cannot

toxic symptoms are observed. Furthermore, no toxic symptoms can be observed when using the drug is added to the feed in a concentration of 1%. However, the animals are less fond of this food than Feed without the drug.

The results reported above show that according to Example 3 manufactured drug is practically non-toxic.

From E. Revici, Research in Physiopathology, Van Nostrand, Princeton, 1961, is familiar with the concept of anabolic-catabolic dualism. The medicaments of the invention and in particular the medicament produced according to Example 3 show a very beneficial effect on injuries. The medicines thus show a catabolic effect. This effect is clearly evident in the healing of wounds and burns. A marked difference in the effect was observed in experimentally produced cancer, depending on whether the Tumors are anabolic or catabolic in nature. In anabolic tumors, the drugs of the invention delay the death of the Animals. For catabolic tumors with necrosis, accumulation of fluid (ascites) and cell loss (cell pycnosis) the drugs show a clearly beneficial effect.

Patients with catabolic tumors were treated according to Example 3 Prepared drugs are given intramuscularly at a dose of 2 to 3 ml. It turned out to be a clearly favorable one Effect. The suffering was alleviated or for several hours

canceled. The remedy thus has a galliative effect. 30th

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Claims (11)

vossius · vossius: -t-au: c * hn: ef? ·: Η eunemann · rauh PATENTANWÄLTE OO 1 Π Ο Γι / Jo ι yj υ 4 SIEB ERTSTR AS SE 4.-8ΟΟΟ MÜNCHEN 86 · PHONE: (O89) 47 4Ο75 CABLE: B EN ZOLPATENT MÖNCHEN -TELEX 5-29 45 3 VOPAT D uZ: S 446 (Vo / kä) Case: 1915 V ALPHATIME Ltd. Company Inc. F.C.N.s.r.l. "Medicines with antineoplastic effects". Claims 1. Medicines with antineoplastic effects, characterized by a content of at least one polyfluoro alcohol of the general formula I ' CHF ₀ - (CF ₀ ) -CH ₀ OH. (I) 2 2 η 2 in which η has the value 3, 5, 7 or 9. 2. Medicament according to claim 1, characterized by an additional content of cholesterol. 3. Medicament according to claim 1 or 2, characterized by a content of at least two polyfluoroalcohols of the general formula I.
'' 4. Medicament according to claim 1 or 2, characterized by a content of at least three polyfluoroalcohols of the general formula I. 5. Medicament according to claim 1 or 2, characterized by a content of three polyfluoroalcohols of the general formula I in an amount ratio of 12: 1: 1 to 1:12: 1 up to 1: 1:12 - ^L copy ^J r ·: ·· ^: · '·· _ ' ₂ 'ί' ~ 331930Α-1 6. Medicament according to claim 2, characterized by a content of at least one polyfluoroalcohol and cholesterol in a quantity ratio of 10: 1 to 1:10. 7. Medicament according to claim 1 or 2, characterized by an additional content of a lipophilic solvent. .8th. Medicament according to claim 7, characterized in that the lipophilic solvent is sesame oil. 9. Medicament according to claim 4 and 8, characterized by a content of 6 parts by weight of dodecafluoroheptanol (formula I, η = 5), 2 parts by weight of hexadecafluorononanol (formula I, η 1), 2 parts by weight of octafluoropentanol (formula I, η = 3) _f 3 Parts by weight of cholesterol and 87 parts by weight of sesame oil. 10. Medicament according to one of claims 1 to 9, characterized characterized in that they are in the form of oral administration. 11. Medicament according to one of claims 1 to 9, characterized in that it is used in parenteral administration form. L J