JPS591414A - Medicine containing at least one kind of polyfluorinated alcohol - Google Patents

Abstract

(57) [Summary] This bulletin contains application data before electronic filing, so abstract data is not recorded.

Description

[Detailed Description of the Invention] The present invention uses (aJ formula (υ: 0HF2f OF2'') n oH2on as an active ingredient)
CI) (wherein n is 6,5,7 or 9) and optionally (b) cholesterol.

Preferably, the medicament of the invention has at least two compounds of formula (I)
Contains refluorinated alcohol and cholesterol. It is more effective to use 6 types of poly7-oleated alcohols of formula (1) ((a) component a) and a drug containing cholesterol (component (b)) in addition to these.0 In preferred medicaments of the invention, the relative proportions of the 6 polyfluorinated alcohols may vary within a wide range, for example 12 parts by weight of dodecafluoroheptatool, the compound with n = 5 in formula (I). (the same applies hereinafter), in formula (I), n=
1 part of octafluoropentanol, which is a compound of 6 compounds, and 1 part of hexadecafluorononanol, which is a compound of n = 7 in formula (I), to 1 part of dodecafluorotetrahebutanol, 1 part of octafluoropentanol, and 1 part of hexadecafluorononanol, which is a compound of n = 7 in formula (I). It may vary within a range of up to 12 parts of alcohol.

The relative ratio between components (a) and (b) is 1o:1
It may vary within the range of ~1:10.

The medicament of the invention may further contain a lipophilic carrier such as sesame oil or similar substances.

All components of the medicament of the invention are well known and commercially available.

The medicament of the present invention will be explained in more detail with reference to Examples below.

Example 1 1509 of sesame oil, 69 of octa7/I/oropentanol, 5 of dodecafluoropentanol and 7.5
9 of hexadecafluorononanol was dissolved. 2.59 cholesterol was added to the solution while briefly warming at 65-4000 Example 2 1009 sesame oil had 2.59 dodecafluor gastric hepta7
2.59 g of hexadecafluorononanol and 5 g of octafluoropentanol and 4 g of cholesterol were added with stirring until completely dissolved.

Example 6 The following ingredients were added to 174 g of sesame oil with stirring until completely dissolved.

Dodecafluoroy-'flnor (Formula ■ x where n = 5
) f2g hexadecafluorononanol (1 mn
= 7) 49 octafluoro U pentanol (Imn = 5) 4 g Cholesterol
xthfals), 0,3oc 7thiar and 0
．． Distributed into 5cc 7thiars. Those 7 thials were sterilized by heating. Example 4 A medicament of the present invention was prepared in the same manner as in Example 1, except that 2 g of eicosafluoroundecanol (n-9 in formula (I)) was further added. did.

Example 5 A medicament of the present invention was prepared in the same manner as in Example 1, except that the same amount of octafluoropentanol was used in place of hexadecafluorononanol.

Example 6 A medicament of the present invention was prepared in the same manner as in Example 3 except that cholesterol was not used. The medicament obtained in Example 6 was examined for acute toxicity, acute toxicity, and chronic toxicity.

Acute toxicity: A similar phenomenon occurred when a mouse weighing 60 g was subcutaneously injected with a dose exceeding 5 ca.

Subacute toxicity: Subcutaneous route number trowel 1 to mice weighing 2'50 g.
When Nippon QJca wrinkles were administered for 5 days a week for 6 consecutive weeks, no symptoms of toxicity or any pathological changes were observed in the animals after they were killed.

Chronic toxicity: Subcutaneous injection was administered to mice weighing 30 g at a dose of 2 cc per day, 6 times a week for 6 consecutive months.
The treated animals did not show any abnormal reactions compared to the controls, nor were any pathological changes observed in the animals after they were killed. It was also obtained when 0.4 cc was administered. 0.2cc/day for horses, mice, and rats (or 0.2cc/day for horses, mice, and rats).
In the case of rats, when the drug was orally administered to children weighing 4oc/1009 using a catheter for an extended period of time, no toxic symptoms were observed. Furthermore, when 1% of the drug of the present invention was added to the diet of animals undergoing administration, the animals clearly resisted eating the food containing the additive, but no symptoms of toxicity were observed. Therefore, it is clear that the medicine of the present invention has no toxicity in practical use.Pharmacological considerationsThe concepts of dual assimilation/anabolic dualism and the related definitions described below are based on the theory of physiology written by R. Research in Phys
iopathy), Pan Nostrand (V
Noatland), Flinstone, 19
It is extensively explained from the perspective of both animal and human experiments in 61. However, the novelty of the present invention does not depend on the correctness of the theory stated in the paper.

The medicament of the invention and in particular the medicament of Example 6 above exhibits a very favorable anti-disorder effect, ie a catabolic effect. The effect is clearly visible in the treatment of wounds and burns. In the case of experimental cancers, clear differences in efficacy have been noted depending on whether the tumor is anabolic or catabolic. In fact, in the case of anabolic tumors, the medicament of the present invention only delays the death of the animal, whereas in the case of catabolic tumors with necrosis, fluid retention, and pycnotic cells, the same drug according to the present invention of medicines had a substantial beneficial effect.

Clinical studies: In the treatment of patients suffering from catabolic tumors, the medicament of the invention can also be administered by intramuscular injection of 2 to 3 cc (thus eliminating or reducing suffering for several hours). O, which clearly had a favorable effect

Claims (1)

[Claims] 1. As an active ingredient (a) formula (■): o) rF2-f-oy2+n0H20H (I) (in the formula,
n is 6.5.7 or 9) A medicament having antitumor activity containing at least one type of Rifluoro V alcohol. 2. The medicine according to claim 1, wherein the active ingredient further contains (b) cholesterol as an ingredient. 6. The medicament according to Patent M*, scope 1 or 2, wherein the component (a) contains at least two types of polyfluoroalcohols of formula (1). 4. The medicament according to claim 1 or 2, wherein the component (a) contains at least six types of polyfluoroalcohols of formula (I). 5 Six types of boria/I/oro alcohols of formula (I) are 1
A medicament according to claim 1 or 2, wherein the medicament is present in a ratio varying in the range from 2:1:1 to 1:12:1 to 1:1;12. 6. The ratio between component (a) and component (b) is 10:1 to 1.
: 10. The medicament according to claim 1 or 2, further comprising a lipophilic solvent. 8. The medicament according to claim 1 or 2, wherein the lipophilic solvent is present as sesame oil.0 96 parts by weight of dodecafluorohebutanol (n=5 in formula (I)), hexadecafluoro 7nanol (B=7 in formula (I)), 2 parts by weight of octafluoropentanol (n=31.
The medicament according to claim 2, comprising 3 parts by weight of cholesterol and 87 parts by weight of sesame oil. 10. The medicament according to claim 1, 2 or 9, which is in a dosage form suitable for oral administration. 11. The medicament according to claim 1, 2 or 9, which is in a dosage form suitable for parenteral administration.