JPS62145015A - Anti-inflammatory agent - Google Patents

Abstract

PURPOSE:To provide an anti-inflammatory agent containing sialic acid as an active component. CONSTITUTION:The objective anti-inflammatory agent contains sialic acid, especially N-acetylneuraminic acid as an active component. Sialic acid is rich in placenta extract and is an important component of an animal polysaccharide. It can be administered by oral administration, injection or external application in the form of tablet, pill, suspension, emulsion, suppository, injection, ointment, etc. Dose, 10-2,000mg/kg daily, preferably 100-1,000mg/kg daily.

Description

DETAILED DESCRIPTION OF THE INVENTION Field of Industrial Application The present invention relates to a novel anti-inflammatory agent, and more particularly to an anti-inflammatory agent containing sialic acid, particularly N-acetylneuraminic acid, as an active ingredient.

Technical background and prior art Mammalian placenta extracts contain various pharmacologically active ingredients, and are therefore incorporated into pharmaceuticals, cosmetics, and the like. This placenta extract is known to contain many amino acids, vitamins, inorganic components, alkaline phosphatase, deoxyribonucleic acid, neutral Ctt ketosteroids, etc., although it varies depending on the type of animal. There is.

Purpose of the Invention The present inventors have spent many years researching the pharmacological activity and active ingredients of placenta extract, especially bovine placenta extract, and have now discovered that the placenta extract contains sialic acid and N.
-We discovered that it is contained in the form of acetylneuraminic acid, focused on this sialic acid, and conducted various studies on its pharmacological activities. As a result, they discovered that sialic acid has an excellent anti-inflammatory effect and completed the present invention.

That is, the present invention provides an anti-inflammatory agent containing sialic acid, particularly N-acetylneuraminic acid, as an active ingredient.

Structure of the Invention and Effects Sialic acid, which is an active ingredient in the anti-inflammatory agent of the present invention, was found to be contained in Gracenta extract, but this sialic acid is an acyl derivative of neuraminic acid. It is known to be an important component of many animal polysaccharides, and one of its main types, N-acetylneuraminic acid, is commercially available as a reagent.

Although the present invention includes any sialic acid, N-acedelneuraminic acid is particularly preferably used as an active ingredient.

According to experiments conducted by the present inventors, sialic acid (N-acetylneuraminic acid) exhibits the following pharmacological and biochemical actions.

(+) Anti-inflammatory effect Commercially available N-acetylneuraminic acid was used to test its inhibitory effect on carrageenan-induced edema in rats. Note that aspirin was used as the target drug.

(i) Experiment 1 Method - Wistar male rats (body weight 130-1629.1 Group 7
The mice were kept indoors (temperature: 23±1° C., humidity: 55±5%) and raised for one week with solid feed (CE-2, manufactured by Nippon Clear Co., Ltd.) and drinking water. Add N-acetylneuraminic acid (SEA) 30.100.300.500 liters to this and 000w9/9 gud buffer (pH 6,4).
[Good N,ll, Biochemistry (11i
ochcmisLry), 5.467-47 G(
(1966)] was injected subcutaneously. Next, 0.1 ml of 1% carrageenan saline solution was injected into the right hind paw of the animal to induce carrageenan edema. Edema was observed for 30 minutes to 24 hours after the injection.

Results: The edema rates obtained are shown in the attached Figure 1. Furthermore, the edema suppression rate of N-acetylneuraminic acid (SIA) was calculated from the edema rate as shown in Table 1 below.

Table 1 (Suppression rate %) (1
1) Experiment 2 In order to compare the effects of sialic acid and aspirin, rats were given 300. o/&y and as a control aspirin 1 o o mg/kg in Gud buffer (pH 6
, 4) was injected subcutaneously, and edema was induced with carrageenan.

The edema rate is shown in Figure 2. The edema suppression rate was calculated from the edema rate as shown in Table 2 below.

Table 2 (Inhibition rate %) As is clear from the above results, N-acetylneuraminic acid 300
It showed a considerable edema suppression rate at m9/kft or higher, and also showed a longer duration of action than aspirin.

2. Acutely toxic ddY male mice (body weight 22~aoy, 10 mice per group) were injected with N-acedelneuraminic acid 100.300.1000 and 5000 μg/9 gud buffer (pl-16,4
) solution was injected subcutaneously, and! Observe general symptoms for a week and also for 24 hours after administration using a modified Irwin method [
P sychopharmacology
-cologia), 1,3. 2 2 2~2
5 7 (+ 9 6 8) (Accordingly, behavioral symptoms were observed. As a result, there were no cases of death due to the effects of Dso is 500'mg/kg or more,
It is found that toxicity is extremely low and safe.

The anti-inflammatory agent of the present invention can be used in any form of administration, including oral administration, injection, and external administration, and can be used in common pharmaceutical preparations, such as tablets, emulsions, solutions, suspensions, emulsions, granules, capsules,
Various dosage forms such as suppositories, injections, and ointments are employed.

These preparations are manufactured by conventional methods using commonly used excipients and diluents such as fillers, thickeners, binders, wetting agents, disintegrants, and lubricants. Note that the anti-inflammatory agent of the present invention may be appropriately blended with other known anti-inflammatory active drugs.

The dose of sialic acid, which is the active ingredient in the anti-inflammatory agent of the present invention, varies somewhat depending on the age and weight of the child, as well as the severity of symptoms, but usually, in an adult human, I O ~
2000mg/kg/day, preferably I 00-100
It is used at a dosage of 0 mg/kg/day.

Next, the anti-inflammatory agent of the present invention will be explained in more detail with reference to Examples.
20 (1119″Dry starch 20011g Magnesium stearate 5019 in 1 tablet by conventional method”)
A tablet having the following composition is prepared.

Example 2 Injection Components Dosage N-acetylneuraminic acid 10011g Gud buffer Total 100011f2 An injection having the above composition is prepared by a conventional method.

Example 3 Ointment (0/W type) Asari Ichibu□ Dose Liquid paraffin 9.00% by weight Stearic acid 4.00 Setanol
3.00 Boxoxyethylene sorbitan monostearate (20EO) 0.50 Noricon resin 0.50 N-acedelneuraminic acid 3.00 Propylene glycol 18.00” Medyl paraoxybenzoate 0
．． 20 Ayacol LC-Wax 3.00
Purified water 58.50 An ointment having the above composition is prepared by a conventional method.

[Brief explanation of drawings]

Figure 1 is a graph showing the edema-suppressing activity (anti-inflammatory activity) of N-acedelneuraminic acid against carrageenan-induced edema;
FIG. 2 is a graph showing the anti-carrageenan-induced edema activity of N-acedelneuraminic acid and control aspirin. C-1 Contrage

Claims (2)

[Claims] (1) An anti-inflammatory agent characterized by containing sialic acid as an active ingredient. (2) The anti-inflammatory agent according to item 1 above, wherein the sialic acid is N-acetylneuraminic acid.