JPH0959149A - Anti-inflammatory analgesic composition - Google Patents

Abstract

PROBLEM TO BE SOLVED: To obtain an antiphlogostic and analgesic composition having enhanced analgesic actions. SOLUTION: This antiphlogistic and analgesic composition comprises oxaprozin and ibuprofen or acetaminophen as active ingredients. The blending ratio (weight ratio) of the oxaprozin : ibuprofen or acetaminophen is (1:0.1) to (1:10), preferably (1:0.25) to (1:5) and, as necessary, an adjuvant agent, a carrier, an excipient, a binder, a disintegrating agent, a lubricant, a buffer agent, a preservative, a perfume, a coloring matter, a flavoring agent, etc., are suitably blended and prepared as a peroral administration agent such as a tablet, a granule, a powder, a capsule or a solution. The daily dose thereof for an adult is 300-1600mg, expressed in terms of the active ingredients and perorally administered once or several times. Since the composition manifests effects on diseases in respiratory organs including cold syndrome, it is useful as a medicine for the cold. Since the effects are obtained in a low dose, adverse effects can be reduced.

Description

Detailed Description of the Invention

[0001]

This invention relates to anti-inflammatory and analgesic compositions with enhanced analgesic activity.

[0002]

Oxaprozin is widely used as an anti-inflammatory and analgesic drug, but its action is relatively weak and it is difficult to obtain a sufficient effect on respiratory diseases. On the other hand, the analgesics ibuprofen and acetaminophen are effective against respiratory diseases such as cold syndrome, but side effects are strong, and there is a problem in prescribing an amount that can sufficiently expect a therapeutic effect.

[0003]

DISCLOSURE OF THE INVENTION An object of the present invention is to provide an anti-inflammatory analgesic composition having an enhanced analgesic effect.

[0004]

Means for Solving the Problems The present inventors have studied for the purpose of enhancing the analgesic action. As a result, the analgesic action was enhanced by combining oxaprozin with the analgesic drug ibuprofen or acetaminophen. It was found that an anti-inflammatory analgesic composition was obtained, and the present invention was completed.

The present invention is an anti-inflammatory and analgesic composition containing oxaprozin as an active ingredient and ibuprofen or acetaminophen.

The blending ratio (weight ratio) of oxaprozin: ibuprofen or acetaminophen is 1: 0.1-
It is 1:10, preferably 1: 0.25 to 1: 5.

That is, the present invention includes the following inventions.

(1) An anti-inflammatory analgesic composition containing oxaprozin as an active ingredient and ibuprofen or acetaminophen (2) An anti-inflammatory analgesic composition containing oxaprozin and ibuprofen as active ingredients (3) Oxaprozin: The anti-inflammatory analgesic composition according to the above (2), wherein the compounding ratio (weight ratio) of ibuprofen is 1: 0.1 to 1:10. (4) The compounding ratio (weight ratio) of oxaprozin: ibuprofen is 1: 0.25-. The anti-inflammatory analgesic composition according to (2) above, which is 1: 5. (5) The anti-inflammatory analgesic composition containing oxaprozin and acetaminophen as active ingredients. (6) The compounding ratio (weight ratio) of oxaprozin: acetaminophen is 1. The anti-inflammatory analgesic composition according to the above (5), wherein the ratio is 0.1 to 1:10. (7) The compounding ratio (weight ratio) of oxaprozin: acetaminophen is 1: 0.25 to 1. 5 a is the (5) anti-inflammatory composition.

The antipyretic and analgesic composition of the present invention can be orally administered to an adult in an amount of 300 to 1600 mg as an active ingredient once or in several divided doses per day.
This dose can be appropriately adjusted depending on the age, weight, and medical condition.

If necessary, an antitussive drug, an anti-inflammatory enzyme drug, a sympathomimetic drug, an anti-inflammatory drug, a drowsiness preventive drug, a vitamin drug, a crude drug, an antacid drug and the like may be appropriately mixed. .

Furthermore, the anti-inflammatory and analgesic composition of the present invention is used as an oral dosage form such as tablets, granules, powders, capsules and solutions. These preparations can be prepared by a conventional method. The carrier used for preparation of the preparation includes excipients such as lactose, starch, sugar, mannitol, crystalline cellulose, hydroxypropyl cellulose, hydroxypropylmethyl cellulose, gelatin, PVP.
There are binders such as calcium carboxymethyl cellulose, disintegrants such as low-substituted hydroxypropyl cellulose, magnesium stearate, hydrogenated castor oil, lubricants such as talc, and other solubilizers as necessary.
Buffers, preservatives, fragrances, dyes, flavoring agents and the like can be used.

[0012]

INDUSTRIAL APPLICABILITY The anti-inflammatory and analgesic composition of the present invention has an enhanced analgesic effect as compared with the case where oxaprozin, ibuprofen or acetaminophen are used alone, and is effective against respiratory diseases such as cold syndrome. Since it has an effect, it can be used as a cold medicine. Moreover, since the effect is obtained at a low dose, side effects can be reduced.

[0013]

EXAMPLES The present invention will be described in more detail with reference to Examples and Test Examples. Example 1 The following components and amounts were weighed and uniformly mixed, and then the obtained mixed powder was filled in No. 2 hard capsules in an amount of 200 mg each to obtain 5000 capsules. Oxaprozin 400 g Ibuprofen 450 g Lactose 100 g Microcrystalline cellulose 40 g Magnesium stearate 10 g.

Example 2 The following components and amounts were weighed and uniformly mixed, and then the obtained mixed powder was filled in a No. 2 hard capsule in an amount of 200 mg to obtain 6000 capsules. Oxaprozin 400 g Ibuprofen 450 g Lysozyme chloride 90 g (potency) Lactose 170 g Microcrystalline cellulose 80 g Magnesium stearate 10 g.

Example 3 The following components and amounts were weighed and uniformly mixed, and the resulting mixed powder was tableted by a direct compression method to give a tablet weight of 200 mg to obtain 10,000 tablets. Oxaprozin 400 g Acetaminophen 900 g Ambroxol hydrochloride 45 g Lysozyme chloride 90 g (potency) Lactose 300 g Low-substituted hydroxypropyl cellulose 245 g Magnesium stearate 10 g Hardened castor oil 10 g.

Example 4 The following components and amounts were weighed and uniformly mixed, and 7,000 300 mg tablets were obtained according to Example 3. Oxaprozin 600 g Ibuprofen 450 g Dihydrocodeine phosphate 24 g Mequitazine 6 g Ambroxol hydrochloride 45 g Lysozyme chloride 90 g (potency) dl-methylephedrine hydrochloride 60 g Lactose 400 g Microcrystalline cellulose 395 g Magnesium stearate 15 g Hardened castor oil 15 g.

Example 5 The following components and amounts were weighed and uniformly mixed, and 7,000 300 mg tablets were obtained according to Example 3. Oxaprozin 400 g Ibuprofen 225 g Acetaminophen 450 g Noscapine 48 g Dihydrocodeine phosphate 24 g Mequitazine 6 g Ambroxol hydrochloride 45 g Lysozyme chloride 90 g (potency) Trimethoquinol hydrochloride 6 g Anhydrous caffeine 75 g Vitamin B ₁ Nitrate salt 8 g Lactose B ₂ Vitamin B ₂ Cellulose 339 g Magnesium stearate 15 g Hardened castor oil 15 g.

Test Example 1 [Analgesic effect in mice (acetic acid writ
hing method)] A group of 10 4-week-old male ddY mice was used, and Koster was used.
Et al. (Koster R., Anderson M. and De Beer EJ, F
ed.Proc., Vol. 18, p. 412 (1958)), 30 minutes after oral administration of each drug shown in Table 1, 0.7% acetic acid was intraperitoneally administered to 0.1 ml / 10 g of acetic acid. Administration 10
After 10 minutes, the writhing number was measured for 10 minutes. A 5% gum arabic solution was orally administered to the control group, and the same measurement was performed. The results are shown in Table 1.

[0019]

[Table 1]

As shown in Table 1, the efficacy of the combination of oxaprozin and acetaminophen was about 1.60 times, and the efficacy of the combination of oxaprozin and ibuprofen was about 1.97 times, as compared with the case of oxaprozine alone.

Test Example 2 [Analgesic effect in rats (Randall
and Selitto method)] A group of 4 to 12-week-old male Wistar rats was used.
It examined using algesymeter (Ugo Basile).

A carrageenin aqueous solution was subcutaneously injected into the footpad of the right hind leg twice at 1 hour intervals, and 2 hours after that, each drug shown in Table 2 was orally administered, and every 1 hour until 4 hours, left (normal foot) ) The pain threshold of the right (inflamed foot) hind limb was measured. A 5% gum arabic solution was orally administered to the control group, and the same measurement was performed. The results are shown in Table 2.

[0023]

[Table 2]

As shown in Table 2, the combination of oxaprozin and acetaminophen increased the potency by about 1.61 times, and the combination of oxaprozin and ibuprofen increased by about 2.49 times as compared with the case of oxaprozin alone. It was

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Claims (1)

[Claims] 1. An anti-inflammatory analgesic composition comprising the following (a) and (b) as active ingredients. (a) Oxaprozin (b) Ibuprofen or acetaminophen