JP2894955B2 - Ibuprofen preparation - Google Patents

Description

DETAILED DESCRIPTION OF THE INVENTION

[0001]

The present invention relates to an ibuprofen preparation comprising ibuprofen and aminoacetic acid.

[0002]

2. Description of the Related Art Many antipyretic analgesics are known, and among them, salicylic acid derivative drugs such as aspirin, aniline derivative drugs such as acetaminophen, and pyrazolone derivative drugs such as antipyrine are often used. I have. Also, for the purpose of improving the antipyretic analgesic effect, combination preparations combining these three derivatives are widely used. A recently developed phenylpropionic acid derivative drug ibuprofen has been widely used as a nonsteroidal antipyretic analgesic because of its excellent antipyretic analgesic activity. However, ibuprofen, similarly to salicylic acid derivative drugs, has a drawback that when administered orally, it tends to cause gastrointestinal disorders such as gastric discomfort and gastric pain. For the purpose of reducing these side effects, from the viewpoint of reducing the dose of ibuprofen,
An aniline derivative-based antipyretic analgesic with less gastrointestinal disorders may be compounded (Japanese Patent Publication No. 1-8602, Japanese Patent Publication No. 41608/1994).
No. 1), caffeine having an action to enhance the antipyretic and analgesic effect of ibuprofen is blended (Japanese Patent Publication No. 1-24131)
No.) and other attempts have been made. On the other hand, in order to directly reduce side effects, it has been proposed to use an antacid and / or a mucosal coating agent in combination (Japanese Patent Laid-Open No. 63-198620).
issue). However, an antipyretic analgesic containing such a drug cannot always satisfy both enhancement of the antipyretic analgesic effect and reduction of gastrointestinal disorders at the same time.

[0003]

SUMMARY OF THE INVENTION An object of the present invention is to provide a highly safe ibuprofen preparation in which the antipyretic and analgesic effect of ibuprofen is enhanced and the gastrointestinal damage of ibuprofen is reduced.

[0004]

Means for Solving the Problems The present inventors have made intensive studies to achieve the above-mentioned object, and as a result, surprisingly, ibuprofen was added to ibuprofen by adding aminoacetic acid known as an antacid to ibuprofen. It has been found that the antipyretic and analgesic effect of the compound is further improved. This has the unexpected effect of requiring less ibuprofen to achieve the same antipyretic analgesic effect.
At the same time, since gastrointestinal disorders can be reduced by the antacid action inherent to aminoacetic acid and the like, it has been found that by combining aminoacetic acid with ibuprofen, a highly effective and safe preparation can be obtained. It was completed. That is, the present invention provides an ibuprofen preparation comprising ibuprofen and an aminoacetic acid in an amount that enhances the antipyretic analgesic effect of ibuprofen.

[0005] The ibuprofen preparation of the present invention is an antipyretic analgesic or cold remedy containing ibuprofen and aminoacetic acid as described above. Examples of ibuprofen used in the present invention include 2- (4-isobutylphenyl) propionic acid or a pharmaceutically acceptable salt thereof. Usually, the amount of ibuprofen in the preparation according to the present invention is 100 to 1000 mg / day, preferably 200 to 600 mg / day for an adult, which can be administered once or several times. The dose can be appropriately increased or decreased depending on the age, weight, and symptoms of the patient. The amount of aminoacetic acid is preferably 1 to 100 parts by weight, more preferably 1 to 20 parts by weight, based on 10 parts by weight of ibuprofen. When the amount is less than 1 part by weight, the antipyretic analgesic effect is not improved and gastrointestinal disorders are not reduced.

[0006] ibuprofen formulations of the present invention, bromovalerylurea, sedative hypnotics such allylisopropylacetylurea, sodium benzoate caffeine, anhydrous caffeine, central stimulant such as caffeine, vitamin B ₁ and its derivatives and their Vitamins such as salts, vitamin B ₂ and its derivatives and their salts, vitamin C and its derivatives and their salts, hesperidin and its derivatives and their salts, magnesium silicate, synthetic aluminum silicate, synthetic hydrotalcite, Magnesium oxide, aluminum glycinate, aluminum hydroxide gel, dried aluminum hydroxide gel, mixed dried gel of aluminum hydroxide and magnesium carbonate, co-precipitated product of aluminum hydroxide and sodium hydrogen carbonate, aluminum hydroxide and calcium carbonate Pharmaceutical ingredients such as coprecipitated product of calcium / magnesium carbonate, coprecipitated product of magnesium hydroxide / potassium aluminum sulfate, and antacids such as magnesium carbonate and magnesium aluminate metasilicate can be appropriately blended. Further additives include, for example, lactose,
Excipients such as crystalline cellulose, hydroxypropylmethylcellulose, binders such as carboxymethylcellulose,
There are disintegrating agents such as methylcellulose and polysorbate 80, and lubricating agents such as magnesium stearate and polyethylene glycol. In addition, flavors, coloring agents, and flavoring agents can be used as needed.

The ibuprofen preparation of the present invention is used in various dosage forms such as tablets, effervescent tablets, granules, fine granules, powders, troches, syrups, dispersants, hard capsules and soft capsules. These preparations can be prepared by a conventional method.
At that time, in addition to the above-mentioned components, conventional additives according to the preparation can be used.

[0008]

The ibuprofen preparation of the present invention is a preparation excellent in efficacy and safety in which the antipyretic analgesic action of ibuprofen is further improved by adding aminoacetic acid, and at the same time, gastrointestinal disorders are reduced. This is due to the unexpected effect that the addition of aminoacetic acid enhances the antipyretic and analgesic effect of ibuprofen. Next, experimental examples and examples will be shown to specifically show the effects of the present invention. The present invention is not limited by these experimental examples and examples.

Experimental Example 1 (Analgesic Action) Drug suspended in a 3% aqueous solution of gum arabic in male mice (body weight 23 to 28 g) fasted for 18 hours [1] Ibuprofen 30 mg / kg, 2) Ibuprofen 30 mg / kg and amino acid Acetic acid 3
mg / kg, 3) Ibuprofen 30 mg / kg and aminoacetic acid 10 mg / k
g, 4) Ibuprofen 30 mg / kg and aminoacetic acid 30 mg / kg, 5)
30 mg / kg of ibuprofen and 60 mg / kg of aminoacetic acid, 6) 30 mg / kg of ibuprofen and 100 mg / kg of aminoacetic acid, 7) 30 mg / kg of ibuprofen and 300 mg / kg of aminoacetic acid] were administered by oral gavage. Thirty minutes later, a 0.6% acetic acid aqueous solution was intraperitoneally administered, and five minutes thereafter, the number of writhing occurrences for 15 minutes was counted. 3% gum arabic was administered as a control, and the rate of suppression of the rising of the drug group with respect to the number of risings was calculated according to the following formula. The results are shown in FIG.

(Equation 1) As is clear from FIG. 1, it can be seen that the addition of aminoacetic acid to ibuprofen enhances the analgesic effect as compared to ibuprofen alone.

Experimental Example 2 (Gastrointestinal disorder inhibitory action) Male rats (body weight 160-180) fasted for 18 hours
g) Drug suspended in 3% gum arabic aqueous solution [1) Ibuprofen 450 mg / kg and amino acetic acid 150 mg / kg, 2) Ibuprofen 450 mg / kg and amino acetic acid 225 mg / kg, 3) Ibuprofen 450 mg / kg and amino acetic acid 300 mg / kg, 4) Ibuprofen 45
0 mg / kg and aminoacetic acid 450 mg / kg, 5) ibuprofen 450 mg / kg
kg and aminoacetic acid 900 mg / kg] were administered by gavage. Four hours later, the stomach was removed and cut longitudinally along the Great Bay.
% Formalin. Using the stomach specimen, the area of the ulcer was measured with an image riser. As a control, ibuprofen was administered at 450 mg / kg, and the ulcer inhibition rate of the drug group with respect to the ulcer area was calculated by the following formula. The results are shown in FIG.

(Equation 2) As is clear from FIG. 2, it is found that the gastric mucosal damage caused by the administration of ibuprofen can be suppressed by adding aminoacetic acid to ibuprofen. The following are formulation examples.

Example 1 Tablet (1 tablet) Ibuprofen 150 mg aminoacetic acid 75 mg anhydrous caffeine 50 mg crystalline cellulose 50 mg hydroxypropylcellulose 10 mg magnesium stearate 5 mg The above ingredients are tableted by a conventional method.

Example 2 Effervescent tablets (in one tablet) Ibuprofen 150 mg Aminoacetic acid 100 mg Ascorbic acid 150 mg Sodium bicarbonate 400 mg Citric acid 600 mg The above components are tableted by a conventional method.

Example 3 Granules (in one package) Ibuprofen 100 mg aminoacetic acid 75 mg dried aluminum hydroxide gel 100 mg crystalline cellulose 50 mg hydroxypropylcellulose 10 mg The above ingredients were extruded, granulated by a granulation method, dried and sized.
Obtain granules.

Example 4 Hard Capsules (in One Capsule) Ibuprofen 100 mg Aspirin 100 mg Aminoacetic Acid 100 mg Corn Starch 20 mg Hardened Oil 20 mg Hard capsules are obtained from the above components by a conventional method.

Example 5 Soft Capsules (In One Capsule) Ibuprofen 100 mg Aminoacetic Acid 100 mg Safflower Fatty Acid 100 mg Tocopherol 5 mg Hard capsules are obtained from the above components by a conventional method.

[0016]

[Brief description of the drawings]

FIG. 1 is a graph showing the analgesic action enhancing effect of the preparation of the present invention.

FIG. 2 is a graph showing the gastrointestinal disorder suppressing effect of the preparation of the present invention.

Claims (2)

(57) [Claims] 1. An ibuprofen preparation comprising ibuprofen and an aminoacetic acid in an amount that enhances the antipyretic and analgesic action of ibuprofen. 2. The preparation according to claim 1, wherein 1 to 100 parts by weight of aminoacetic acid is mixed with 10 parts by weight of ibuprofen.