JPS60215624A - Antiphlogistic analgesic - Google Patents

Abstract

PURPOSE:An antiphlogistic analgesic showing excellent effects more on chronic ache of neuralgia, rheumatism, arthritis, etc. than cute inflammation, having almost no side effect even by long-period administration, comprising an ester of linoleic acid and a lower alcohol as an active ingredient. CONSTITUTION:An antiphlogistic analgesic comprising an ester of linoleic acid and a lower alcohol as an active ingredient. 2-4C alcohol is fittest as the lower alcohol used in the esterification. Although the ester has mild action, alleviates gradually an ache and a pain of the affected part, and is effective for chronic ache of neuralgia, rheumatism, etc. Mechanism of manifestation of medicinal effect is considered that the ester is integrated instead of arachidonic acid of a constituent component of phospholipid of cell membrane by long-period administration, and metabolic products (e.g., PG, leukotriene, thromboxane, etc.) of arachidonic acid is reduced.

Description

[Detailed description of the invention] Industrial applications The present invention relates to anti-inflammatory analgesics.

More specifically, it provides an anti-inflammatory analgesic that has almost no Ilj effect even when taken for a long period of time, and the first effect is easing and I/i, but it gradually relieves pain and stiffness in the affected area and has a curative effect. be.

BACKGROUND OF THE INVENTION Conventionally, various anti-inflammatory analgesics have been used for neuralgia, rheumatism, arthritis, etc.

All of these are often accompanied by side effects such as severe stiffness and disability.
Long-term use was a hardship for patients.

On the other hand, oil containing a high amount of linoleic acid is extracted from the seeds of safflower and is used as an edible oil. It is also known that linoleic acid has the effect of reducing cholesterol in the body.

Purpose of the Invention The present inventors focused on the cholesterol-reducing effect of linoleic acid and conducted various studies.
Rheumatism/arthritis.

The present invention was achieved based on the knowledge that this drug is particularly effective against chronic pain.

That is, the gist of the present invention is an anti-inflammatory analgesic agent containing an ester of linoleic acid with a lower alcohol as an active ingredient.

Means to solve Zhenpeng point The present invention will be explained in detail below.

The method for producing linoleic acid lower alcohol ester in the present invention is not particularly limited, but even if oleic acid is about /!
H, saturated fatty acids (approx.
Distillation is performed at 3θ°C and about 2 Torr to obtain a mixed fatty acid ester. Next, the urea adduct obtained by the so-called urea adduct method, in which urea is weighted and diluted with ethanol, is separated from the solution, the jetanol is evaporated, and the MA is washed with water.
The desired ester of linoleic acid with a lower alcohol can be obtained by distillation. If necessary, the steps after the silver-based adduct method can be repeated for purification to further improve purity.Also, after saponifying safflower oil with sodium hydrate,
The above-mentioned urea attack method can also be used after hydrolyzing with dilute sulfuric acid or sulfuric acid and then distilling.

Furthermore, the above-mentioned linoleic ester can also be obtained by other conventional methods such as chromatography and solvent fractionation. In addition to the above-mentioned safflower oil, the raw material oils and fats include soybean oil, walnut oil, sunflower oil, etc. Although oils and fats can be used, safflower oil is most suitable due to its linoleic acid content and size.

As for the manufacturing method, the above-mentioned transesterification method is most suitable from the viewpoint of product stability.

The lower alcohol used in the esterification of linoleic acid in the present invention is optimally one having a carbon number of - to Z.

If the purity of the ester of linoleic acid with a low fatty alcohol is usually 1 or more, preferably 23% or more, more preferably 11 or more, but less than 90%, the present invention is sufficient. It is difficult to delay the purpose of The above-mentioned 9 degrees refers to the content (weighted %) of linoleic acid in the fatty acid composition when the product is hydrolyzed.

In order to prevent oxidation of the ester of linoleic acid with a lower alcohol, it is preferable to add vitamin E to the ester in an amount of about 0.0% to 1%.

The medicament according to the invention is preferably administered at 1 to 10 doses.

The dosage is determined depending on the patient's age, health condition, body weight, etc., but in general, for an adult weighing Δ-o kg, it is preferably administered at 3-30 f/day. Yes, these are divided into 3 to 3 doses every 7 days. When administered orally, powders are commonly used.

It can be in any dosage form such as capsules.

In addition, a suitable carrier that does not impair the drug's efficacy can also be used.

Effects of the Invention The anti-inflammatory chihogan/ka of the drug according to the present invention is more effective against chronic inflammation and pain than acute inflammation.

The pain and stiffness in the affected area are alleviated by administration of Choruruj.

Although the mechanism of this medicinal effect is not clear, long-term administration incorporates esters of linoleic acid with lower alcohols instead of arachidonic acid, which is a component of phospholipids in cell membranes, and as a result, arachidonic acid metabolites (e.g. This is thought to be due to a decrease in prostaglandins, leukotrienes, thromboxane, etc.).

EXAMPLES The present invention will be explained in more detail with reference to examples below, but the present invention is not limited to examples of one hop or less that do not exceed the gist thereof.

Example/ (Suppressive effect on adjuvant arthritis, therapeutic efficacy test) Male Wistar rats (evening age) were purchased as animals, and -
For the weekly study, those in good health were used.

The method involves using Mycobact θ- suspended in liquid paraffin.
rium butyricum 0.6 my/0
, 7 ml was administered subcutaneously to Ishisa's limbs. On the day of administration, body weight, non-treated foot edema volume, and systemic symptoms were measured, and rats with arthritis were selected and grouped. After that, ethyl linoleate (purity 5'!%) according to the present invention was added to θ, J
, /, 397 to 9. Control system, indomethacin-2+
++y/kg and ibuprofen/j W/k
g was administered continuously for 7θ days at 7 days/time to examine the effect on edema. Edema $ was calculated as follows.

X/θ0 The result-! 1ζ, ethyl linoleate 397 to 9 was found to acutely suppress the floaters caused by arthritis.

Also, linol ethyl, / 0.3, / , 3 t
/kg edema suppression was found to be dose-dependent.

No pre-effects due to administration of Mapζ were observed.

The characteristics are shown in Table 7.

Claims (1)

[Claims] (1) An anti-inflammatory analgesic whose active ingredient is an ester of linoleic acid with a lower alcohol.