JPH11158066A - Pharmaceutical product containing ibuprofen - Google Patents

Abstract

PROBLEM TO BE SOLVED: To obtain a preparation including only ibuprofen and acetaminophen as active ingredients by formulating in a preferable proportion in order to satisfy both potentiation of the analgesic effect of ibuprofen and relief of the gastrointestinal disorder. SOLUTION: This invention relates to the pharmaceutical product is obtained by formulating 1 pt.wt. of ibuprofen with 0.40-0.60 pts.wt., preferably 0.40-0.50 pts.wt., of acetaminophen, includes only ibuprofen and acetaminophen as active ingredients and satisfies both potentiation of the analgesic effect of ibuprofen and relief of the gastrointestinal disorder.

Description

DETAILED DESCRIPTION OF THE INVENTION

[0001]

The present invention relates to ibuprofen (ibup
rofen).

[0002]

BACKGROUND OF THE INVENTION Ibuprofen has antipyretic, analgesic and anti-inflammatory effects and is currently a non-steroidal antipyretic analgesic used worldwide. Since it is easy to cause side effects such as discomfort and stomach pain, for the purpose of enhancing the analgesic effect itself of ibuprofen, or for the purpose of reducing its gastrointestinal disorders,
Attempts have been made to blend them with various medicinal ingredients. For example, a combination preparation of an antipyretic analgesic based on an aniline derivative such as ibuprofen and busetin (Japanese Patent Publication No. 64-8602), a pharmaceutical composition comprising a combination of ibuprofen and an acetaminophen in an amount less than the analgesic amount (Japanese Patent Laid-Open No. 59-1984). No. 104315), a pharmaceutical composition containing ibuprofen and caffeine (Japanese Patent Publication No. 1-24131), ibuprofen,
A compounding agent of acetaminophen and a magnesium-based antacid (JP-A-5-148139) and a compounding agent of ibuprofen and tranexamic acid (JP-A-9-48728)
Publication).

On the other hand, acetaminophen is widely used as a highly safe antipyretic analgesic, and attempts have been made to mix it with ibuprofen as mentioned in the above prior art. However, in order to satisfy both the enhancement of the analgesic effect of ibuprofen and the reduction of gastrointestinal disorders, a formulation containing only ibuprofen and acetaminophen as medicinal ingredients and combining them in a preferable ratio has not yet been found. It has not been.

[0004]

SUMMARY OF THE INVENTION An object of the present invention is to provide a pharmaceutical composition containing only ibuprofen and acetaminophen in order to satisfy both the analgesic effect of ibuprofen and the reduction of gastrointestinal disorders. It is an object of the present invention to provide a preparation containing both components as a component and blending them in a preferable ratio. The present inventors have made various studies on the combination of ibuprofen and acetaminophen, and found that by combining both at a specific ratio, the analgesic effect of ibuprofen can be enhanced and gastrointestinal disorders can be reduced at the same time. After further studies, the present invention was completed.

[0005]

DETAILED DESCRIPTION OF THE PREFERRED EMBODIMENTS As a specific embodiment of the present invention, 1) only ibuprofen and acetaminophen are contained as active ingredients, and 0.40-0 acetaminophen is added to 1 part by weight of ibuprofen. .60 parts by weight; and 2) 0.40 to 0.50 parts by weight of acetaminophen as described in 1) above.

[0006] The above-mentioned medicinal ingredient means an active ingredient contained in a drug, and specific examples of the active ingredient include, for example, Japanese Pharmaceutical Collection, October 1997 edition of Pharmaceutical Pharmaceutical Co., Ltd. ) In the Japanese syllabary index or the alphabetical index. The pharmaceutical preparation of the present invention contains only ibuprofen and acetaminophen as active ingredients. The ibuprofen in the above is a substance having a chemical name of 2- (4-isobutylphenyl) propionic acid, and is a medicinal ingredient listed in the “13th Revised Japanese Pharmacopoeia” (hereinafter referred to as “the Pharmacopoeia”) and the like. . The acetaminophen in the above is a substance having a chemical name of N- (4-hydroxyphenyl) acetamide, and is a medicinal ingredient listed in a pharmacopeia or the like.

The pharmaceutical preparation of the present invention contains only ibuprofen and acetaminophen as the active ingredients, and the ratio of both is 0.40 to 0.60% by weight of acetaminophen per 1 part by weight of ibuprofen. Of acetaminophen in 0.40 parts by weight.
More preferably, a composition containing 0.50 parts by weight is used. By mixing ibuprofen and acetaminophen at the above ratio, the analgesic effect of ibuprofen can be enhanced and gastrointestinal disorders can be reduced at the same time.

The above-mentioned pharmaceutical preparations include tablets, granules, powders, hard capsules, soft capsules, troches,
Solid preparations and liquid preparations suitable for oral administration, such as syrups and oral suspensions. The pharmaceutical preparation of the present invention can contain, in addition to ibuprofen and acetaminophen described above, formulation additives suitable for the pharmaceutical preparation. The pharmaceutical additive refers to an additive usually used for producing a pharmaceutical of the dosage form mentioned in the above pharmaceutical preparation, and includes, for example, the Pharmacopoeia and the “Drug Encyclopedia” (Yakuji Nippo, Jan. 1994). Excipients listed on March 14)
Tablets, granules, powders, hard capsules, soft capsules, troches, syrups, oral suspensions, and the like are selected from binders, disintegrants, lubricants, coating agents, and the like. Specific substances of the pharmaceutical additives include starch, corn starch, crystalline cellulose, lactose, sucrose, glucose, mannitol, sorbitol, xylitol, glycerin, gelatin, agar, gum arabic, hydroxypropylcellulose, low-substituted hydroxypropylcellulose , Methylcellulose, carboxymethylcellulose, polyvinylpyrrolidone, carboxymethylcellulose sodium, carboxymethylcellulose calcium, magnesium stearate, talc,
Hydrogenated vegetable oils, macrogol, bentonite, hectorite, tragacanth, sodium alginate and the like. Pharmaceutical preparations of the present invention include, for example, tablets, granules, powders, hard capsules, soft capsules,
It can be produced according to the method for producing troches, syrups and oral suspensions.

The pharmaceutical preparation of the present invention is effective for relieving headache, toothache, post-extraction pain, sore throat, arthralgia, neuralgia, back pain, muscle pain, menstrual pain, etc., and fever relief during fever. The pharmaceutical preparation of the present invention is usually orally administered once or several times a day, but the amount of ibuprofen in the pharmaceutical preparation of the present invention is 10% when the dose of ibuprofen is adult.
0-1000 mg / day, preferably 200-800 mg
/ Day, more preferably about 300 to 600 mg / day. The dose of ibuprofen can be appropriately increased or decreased depending on the age, weight, and symptoms of the patient, including the child. In addition, the amount of acetaminophen in the pharmaceutical preparation of the present invention ranges from 0.40 to 0.1 to 1 part by weight of ibuprofen depending on the amount of ibuprofen.
60 parts by weight, preferably 0.40 to 0.50 parts by weight. Hereinafter, the present invention will be described in more detail based on Test Examples and Examples, but the present invention is not limited to these exemplifications.

Test Example 1 Analgesic effect test by acetic acid writhing method <Test method> A test drug suspended in a 1% gum arabic solution in groups of 6 to 12 mice at a rate of 0.1 ml / 10 g body weight was used. Orally after 30 minutes, 0.6% acetic acid was added to 0.1%.
It was intraperitoneally administered at a rate of 1 ml / 10 g body weight. afterwards,
The number of rises for 20 minutes was measured, and the inhibition ratio with respect to the control group to which only a 1% gum arabic solution was administered was calculated. Based on this, the ED ₅₀ value was obtained. The ED ₅₀ value is Litchfield
& Calculated by the Wilcoxon method, and the results are shown in Table 1.
Table 1 shows the Gaddum formula (Pharmacology, Oxford Univers
ED ₅₀ value calculated from the above-mentioned information is also shown.

[0011]

[Table 1]

<Results> According to Table 1, 0.43 and 0.5 parts of acetaminophen were added to 1 part by weight of ibuprofen.
When 0 parts by weight are blended, the theoretical value of Gaddum is about 1.5 to 2
An analgesic activity twice as strong was observed, indicating that the compounding ratio exhibited an excellent analgesic enhancing effect.

Test Example 2 Inhibitory effect on stomach damage <Test method> A test drug was orally administered to 4 to 6 rats per group, and after 3.5 hours, 1.0% pontamine sky blue 1
ml was administered intravenously. 30 minutes after that, the stomach is removed and 5
After fixing with% formalin, it was opened along the greater curvature. The sum of the lengths of the disorders (erosions) was determined for each individual, and the sum was used as the degree of gastric damage. The results are shown in Tables 2 and 3.

[0014]

[Table 2]

[0015]

[Table 3]

<Results> According to Tables 2 and 3, when 0.43 and 0.50 parts by weight of acetaminophen were added to 1 part by weight of ibuprofen, the degree of gastric damage was about 1/2 that of the case of ibuprofen alone. It can be seen that the compounding ratio shows an excellent gastric disorder-suppressing action at this ratio.

Example 1 Formulation example per tablet (134 mg in total): 75 mg of ibuprofen, 32.5 mg of acetaminophen, 16.15 g of corn starch, 7.00 mg of low-substituted hydroxypropylcellulose and 3.35 mg of starch The granulation scale is set to 6000 tablets (804 g), and granulation is performed using a vertical granulator. The obtained granules were sized by a spid mill and dried by a ventilated box drier to obtain sized powders, which were compression molded to produce tablets.

Example 2 Capsule Formulation in 1 capsule (total amount 150 mg): 75 mg of ibuprofen, 37.5 m of acetaminophen
g, 37.5 mg of corn starch For the above formulation, a capsule was prepared according to a known method described in the General Rules for Pharmaceutical Preparations. Example 3 Formulation in one package of granules (total amount: 440 mg): 75 mg of ibuprofen, 32.5 mg of acetaminophen, lactose 3
1.00 mg, crystalline cellulose 30 mg, gum arabic
About 5 mg of the above-mentioned formulation, a granule was produced according to a known method described in the general rules of preparations in Japanese Pharmacopoeia.

[0019]

According to the present invention, a pharmacologically active ingredient is obtained by blending 0.40 to 0.60 part by weight, more preferably 0.40 to 0.50 part by weight, of acetaminophen with respect to 1 part by weight of ibuprofen. Thus, it is possible to provide a pharmaceutical preparation containing only ibuprofen and acetaminophen and satisfying both the analgesic effect of ibuprofen and the reduction of gastrointestinal disorders.

Claims (2)

[Claims] 1. Ibuprofen 1 containing only ibuprofen and acetaminophen as medicinal ingredients
Acetaminophen was added in an amount of 0.40 to 0.4 parts by weight based on parts by weight.
A pharmaceutical preparation containing 60 parts by weight. 2. Acetaminophen in an amount of 0.40 to 0.1.
The pharmaceutical preparation according to claim 1, which is blended in an amount of 50 parts by weight.