JP2007137896A - Ibuprofen-containing pharmaceutical preparation - Google Patents

Abstract

<P>PROBLEM TO BE SOLVED: To provide a preparation in which only ibuprofen and acetoaminofen are contained as the effective ingredients and are formulated in a suitable ratio to achieve both an enhanced analgesic activity of ibuprofen and the reduction of the gastrointestinal dysfunction effect. <P>SOLUTION: The pharmaceutical preparation contains only ibuprofen and acetoaminofen as the effective ingredients by mixing 0.40-0.60 pt.wt., more preferably 0.40-0.50 pt.wt. of acetoaminofen to 1 pt.wt. of ibuprofen and has both an enhanced analgesic activity of ibuprofen and a reduced gastrointestinal dysfunction effect. <P>COPYRIGHT: (C)2007,JPO&INPIT

Description

  The present invention relates to a novel pharmaceutical formulation containing ibuprofen.

  Ibuprofen has antipyretic, analgesic and anti-inflammatory effects and is a non-steroidal antipyretic analgesic currently used around the world, but it has a relatively mild analgesic effect and stomach discomfort, stomach pain, etc. In order to increase the analgesic effect of ibuprofen itself, or to reduce its gastrointestinal disorders, attempts have been made to combine it with various medicinal ingredients.

  For example, a pharmaceutical composition comprising a combination of an aniline derivative antipyretic analgesic agent such as ibuprofen and busetine (Japanese Patent Publication No. 64-8602 (Patent Document 1)), a combination of ibuprofen and an amount of acetaminophen less than the analgesic amount ( JP-A-59-104315 (Patent Document 2)), ibuprofen and caffeine-containing pharmaceutical composition (Japanese Patent Publication No. 1-24131 (Patent Document 3)), ibuprofen, acetaminophen and magnesium-based antacid A compounding agent (JP-A-5-148139 (Patent Document 4)) and a compounding agent of ibuprofen and tranexamic acid (JP-A-9-48728 (Patent Document 5)) have been proposed.

On the other hand, acetaminophen is widely used as a highly safe antipyretic analgesic, and as mentioned in the above prior art, blending with ibuprofen has been attempted. However, in order to satisfy both the enhancement of analgesic effect of ibuprofen and the reduction of gastrointestinal disorders, a formulation containing only ibuprofen and acetaminophen as medicinal ingredients and containing them in a desirable ratio has not yet been found. It has not been.
Japanese Patent Publication No. 64-8602 JP 59-104315 A Japanese Patent Publication No. 1-24131 JP-A-5-148139 Japanese Patent Laid-Open No. 9-48728

  An object of the present invention is to provide a preparation containing only ibuprofen and acetaminophen as a medicinal component and blending them in a desirable ratio in order to satisfy both the enhancement of analgesic effect of ibuprofen and the reduction of gastrointestinal disorders. There is.

  As a result of various studies on the combination of ibuprofen and acetaminophen, the present inventors have found that by combining both at a specific ratio, the analgesic effect of ibuprofen can be enhanced and gastrointestinal disorders can be reduced. Further studies were made to complete the present invention.

  That is, the pharmaceutical preparation of the present invention is a pharmaceutical preparation containing only ibuprofen and acetaminophen as medicinal ingredients, and 0.40 to 0.60 parts by weight of acetaminophen per 1 part by weight of ibuprofen. . The pharmaceutical preparation may contain 0.40 to 0.50 parts by weight of acetaminophen.

  In the present invention, by adding 0.40 to 0.60 parts by weight, more preferably 0.40 to 0.50 parts by weight of acetaminophen to 1 part by weight of ibuprofen, It is possible to provide a pharmaceutical preparation that contains only aminophene and satisfies both the enhancement of the analgesic effect of ibuprofen and the reduction of gastrointestinal disorders.

Specific embodiments of the present invention include:
1) A pharmaceutical preparation containing only ibuprofen and acetaminophen as medicinal ingredients, and 0.40 to 0.60 parts by weight of acetaminophen per 1 part by weight of ibuprofen; and 2) 0 of acetaminophen Examples include the pharmaceutical preparation according to the above 1) containing 40 to 0.50 parts by weight.

  The medicinal ingredient in the above means an active ingredient contained in a pharmaceutical product. Specific examples of the active ingredient include, for example, the October 1997 edition of the Japan Pharmaceutical Collection of Pharmaceuticals (published by Yakuho Hokpo). Substances listed in the ten-tone index or alphabet index are listed. The pharmaceutical preparation of the present invention contains only ibuprofen and acetaminophen as medicinal 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 “13th revised Japanese Pharmacopeia” (hereinafter referred to as “Pharmacopeia”) and the like. .

  Acetaminophen in the above is a substance having the chemical name of N- (4-hydroxyphenyl) acetamide, and is a medicinal ingredient listed in the pharmacopoeia.

  The pharmaceutical preparation of the present invention contains only ibuprofen and acetaminophen as medicinal ingredients, and the ratio of both is 0.40 to 0.60 part by weight of acetaminophen with respect to 1 part by weight of ibuprofen. What mix | blended 0.40-0.50 weight part of acetaminophen is more preferable. By blending ibuprofen and acetaminophen at this ratio, the analgesic effect of ibuprofen can be enhanced and gastrointestinal disorders can be reduced.

  The above-mentioned pharmaceutical preparations mean solid preparations and liquids suitable for oral administration such as tablets, granules, powders, hard capsules, soft capsules, troches, syrups and oral suspensions.

  The pharmaceutical formulation of the present invention can contain formulation additives suitable for the above pharmaceutical formulation, in addition to the above-mentioned ibuprofen and acetaminophen. The formulation additive refers to an additive that is usually used for producing a pharmaceutical product of the dosage form mentioned in the above pharmaceutical formulation. For example, the Pharmacopoeia and the “Pharmaceutical Additives Encyclopedia” (Pharmaceutical Daily, 11994) Issued on May 14) from tablets, granules, powders, hard capsules, soft capsules, troches, syrups and oral from excipients, binders, disintegrants, lubricants, coatings, etc. Those suitable for suspending agents are selected.

  Specific substances of the formulation additive include starch, corn starch, crystalline cellulose, lactose, sucrose, glucose, mannitol, sorbitol, xylitol, glycerin, gelatin, agar, gum arabic, hydroxypropylcellulose, low-substituted hydroxypropylcellulose. , Methylcellulose, carboxymethylcellulose, polyvinylpyrrolidone, sodium carboxymethylcellulose, carboxymethylcellulose calcium, magnesium stearate, talc, hydrogenated vegetable oil, macrogol, bentonite, hectorite, tragacanth and sodium alginate.

  The pharmaceutical preparation of the present invention can be produced, for example, according to the method for producing tablets, granules, powders, hard capsules, soft capsules, troches, syrups and oral suspensions described in the pharmacopoeia.

  The pharmaceutical preparation of the present invention is effective for analgesia such as headache, toothache, post-extraction pain, sore throat, joint pain, neuralgia, low back pain, muscle pain, menstrual pain, antipyretic during fever, and the like. The pharmaceutical preparation of the present invention is usually orally administered in 1 to several times a day, and the amount of ibuprofen in the pharmaceutical preparation of the present invention is 100 to 1000 mg / day when the dose of ibuprofen is an adult. Preferably, it is blended so as to be about 200 to 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 children. The amount of acetaminophen in the pharmaceutical preparation of the present invention is 0.40 to 0.60 parts by weight, preferably 0.40 to 0.50, based on 1 part by weight of ibuprofen, depending on the amount of ibuprofen. Part by weight is blended.

  The pharmaceutical preparation of the present invention is effective for analgesia such as headache, toothache, post-extraction pain, sore throat, joint pain, neuralgia, low back pain, muscle pain, menstrual pain, antipyretic during fever, and the like.

  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 examples.

Test Example 1 Analgesic effect test by acetic acid rising method <Test method> Oral administration of test drug suspended in 1% gum arabic solution at a rate of 0.1 ml / 10 g body weight to 6 to 12 mice per group 30 minutes later, 0.6% acetic acid was intraperitoneally administered at a rate of 0.1 ml / 10 g body weight. Thereafter, the number of risings for 20 minutes was measured, the inhibition rate relative to the control group administered with only 1% gum arabic solution was calculated, and the ED ₅₀ value was determined based on this. The ED ₅₀ value was calculated by the Litchfield & Wilcoxon method, and the results are shown in Table 1. Table 1 also shows theoretical values of ED ₅₀ values calculated from Gaddum's formula (Pharmacology, Oxford University Press, London, 1953).

  <Results> From Table 1, when 0.43 and 0.50 parts by weight of acetaminophen are blended with 1 part by weight of ibuprofen, the analgesic activity is about 1.5 to 2 times stronger than the theoretical value of Gaddum. It can be seen that the compounding ratio shows an excellent analgesic enhancing action.

Test Example 2 Stomach Disorder Suppressing Action <Test Method> The test drug was orally administered to 4 to 6 rats of 1 group, and 1 ml of 1.0% pontamsky blue was intravenously administered 3.5 hours later. Thirty minutes later, the stomach was removed, fixed with 5% formalin, and then opened along the large heel. The sum of the length of erosion (erosion) was calculated for each individual and used as the degree of gastric dysfunction. The results are shown in Tables 2 and 3.

  <Results> From Tables 2 and 3, when 0.43 and 0.50 parts by weight of acetaminophen are blended with 1 part by weight of ibuprofen, the degree of gastric damage is close to about 1/2 that of ibuprofen alone, It can be seen that the compounding ratio shows an excellent gastric disorder inhibitory action.

Example 1
Formulation example in one tablet (total amount 134 mg): ibuprofen 75 mg, acetaminophen 32.5 mg, corn starch 16.15 g, low-substituted hydroxypropylcellulose 7.00 mg and starch 3.35 mg
About the said prescription, a granulation scale is set to 6000 tablets (804g), and it granulates with a vertical granulator. The obtained granule was sized with a spidmill and then dried with a ventilated box dryer to obtain a sized powder, which was compression-molded to produce a tablet.

Example 2
Formulation in one capsule (total amount 150 mg): ibuprofen 75 mg, acetaminophen 37.5 mg, corn starch 37.5 mg
About the said prescription, the capsule was manufactured in accordance with the well-known method of a pharmacopoeia general rule description.

Example 3
Formulation in one capsule (total amount 440 mg): ibuprofen 75 mg, acetaminophen 32.5 mg, lactose 300 mg, crystalline cellulose 30 mg, gum arabic 2.5 mg
About the said prescription, the granule was manufactured in accordance with the well-known method of a pharmacopoeia general rule description.

Claims (2)

  A pharmaceutical preparation containing only ibuprofen and acetaminophen as medicinal ingredients, and containing 0.40 to 0.60 parts by weight of acetaminophen to 1 part by weight of ibuprofen.   The pharmaceutical formulation of Claim 1 which mix | blended 0.40-0.50 weight part of acetaminophen.