JP2003277258A - Agent for treating migraine - Google Patents

Abstract

<P>PROBLEM TO BE SOLVED: To provide an agent for preventing or treating migraine having an excellent effect with high safety. <P>SOLUTION: The agent for preventing or treating migraine contains ibuprofen and caffeine compounds as the effective ingredients. The agent is capable of reducing migraine and also reducing nausea, vomitting and excessive sensitivities against lights and sounds which occur simultaneously together with migraine. <P>COPYRIGHT: (C)2004,JPO

Description

Detailed Description of the Invention

[0001]

TECHNICAL FIELD The present invention relates to a preventive or therapeutic agent for migraine.

[0002]

2. Description of the Related Art Migraine is a headache in which the frontal region of the head is aching, and 40% of it is not only on one side but on both sides. The frequency is recurring once to twice a month, often once a week, which lasts for 4 to 72 hours. As an incidental symptom, there are some people who are hypersensitive to light and sound in addition to nausea and vomiting. In addition, before the migraine occurs, some people have a precursory phenomenon such as a bright scotoma. It is said that about 8% of Japanese people have migraine,
A few percent of them go to a medical facility for the treatment, but the other half take over-the-counter medicine (OTC), and the rest, who do neither, endure too painful. It is said.

Mechanisms and causes of migraine include vascular theory, neurological theory, trigeminal vascular theory, etc., which have not yet been confirmed. However, blood flow in the skull is changed in any theory. Is recognized. Therefore, in Japan, zolmitriptan preparations having intracranial vasoconstriction, sumatriptan succinate preparations, or ergotamine tartrate and anhydrous caffeine preparations exist as agents with "migraine" efficacy. .

In the United States, "Exce" containing acetaminophen, aspirin and caffeine as active ingredients.
din Migraine "(Bristo1-Myers) or" Advil Migraine "(Whiteha11-R) containing ibuprofen as an active ingredient.
obins) and "Mortrin Migraine Pain Caplets" (Nc
Neil Consumer Co., Ltd.) is marketed as a non-prescription drug with the effect / effect of “migraine”. In Japan, ibuprofen, acetaminophen, etc., which are marketed as over-the-counter drugs, are also indicated as “migraine”. Although it is not present, it is used for migraine because it has the effect of "headache".

However, zolmitriptan preparations and the like have a problem that side effects on the circulatory system, such as angina and myocardial infarction, may be exacerbated, and when ibuprofen or acetaminophen is used alone. However, the current situation is that a sufficient therapeutic effect has not been obtained for persons with severe migraine.

[0006]

DISCLOSURE OF THE INVENTION An object of the present invention is to provide a drug which exhibits excellent effects in the prevention or treatment of migraine and is highly safe.

[0007]

Means for Solving the Problems As a result of intensive studies in view of such actual circumstances, the present inventors have found that when a combination of ibuprofen, an antipyretic analgesic, and caffeine is used,
It was found that it has a remarkable therapeutic effect on migraine as compared with the case where ibuprofen is used alone, and is useful as a preventive or therapeutic agent for migraine.

That is, the present invention provides a prophylactic or therapeutic agent for migraine, which contains ibuprofen and caffeine as active ingredients.

[0009]

DETAILED DESCRIPTION OF THE INVENTION Ibuprofen, ie 2-
(4-isobutylphenyl) propionic acid is used for rheumatoid arthritis, arthralgia and arthritis, neuralgia and neuritis, back and back pain, cervical arm syndrome, uterine adnexitis, dysmenorrhea, erythema (erythema nodosum, erythema multiforme erythema). , Centrifugal erythema), etc., anti-inflammatory / analgesic after surgery and trauma, and antipyretic / analgesic of acute upper respiratory tract inflammation (including acute upper respiratory tract inflammation with acute bronchitis) It is a drug. The ibuprofen of the present invention is 2- (4-
It may be a salt of isobutylphenyl) propionic acid, for example, a salt with an amino acid such as sodium, potassium, magnesium, calcium, ammonium, methylglucamine, or lysine.

Examples of the caffeines of the present invention include caffeine, anhydrous caffeine, sodium benzoate caffeine, caffeine hydrochloride, caffeine citrate, etc. Among them, anhydrous caffeine is preferable.

The drug of the present invention is used in combination with the above-mentioned ibuprofen and caffeine, and, as shown in the Examples below, remarkably suppresses migraine compared to the case where ibuprofen is administered alone. Exert the effect of. Therefore, the drug of the present invention is effective in preventing or treating migraine.

The use form of ibuprofen and caffeine in the preventive or therapeutic agent for migraine of the present invention is not particularly limited. That is, ibuprofen and caffeine are mixed with a pharmaceutically acceptable diluent, excipient, etc. into a single preparation, or both drugs are separately formulated into a set (kit). But it's okay.
When the two drugs are prepared in different formulations, they may have different dosage forms.

The preventive or therapeutic agent for migraine of the present invention can be made into pharmaceutical preparations of various dosage forms according to the usage, and examples of such dosage forms include powders, granules, fine granules, tablets,
Capsules, liquids, syrups and the like can be mentioned. Further, it may be in the form of sustained-release preparation with controlled release of the components.

These preparations are pharmaceutically acceptable excipients, disintegrating agents, binders, lubricants, diluents, buffers, stabilizers, solubilizing agents, etc., which are pharmaceutically acceptable depending on the dosage form. It can be manufactured according to a conventional method by appropriately mixing, diluting or dissolving it with the pharmaceutical additive of. For example, a powder may be prepared by thoroughly mixing active ingredients (ibuprofen and caffeine) with appropriate excipients, lubricants and the like, if necessary, and tablets and granules may be prepared by lactose, sucrose, Grapes, sugars such as mannitol,
Excipients such as crystalline cellulose; binders such as gelatin, sodium alginate, hydroxypropylmethylcellulose, polyvinylpyrrolidone, carboxymethylcellulose; disintegrants such as carboxymethylcellulose calcium, low-substituted hydroxypropylcellulose, calcium carbonate; magnesium stearate, hardening A hydrogenated vegetable oil such as castor oil, a lubricant such as talc, etc. may be added as necessary, and the mixture may be prepared according to a conventional method. Further, the tablets may be coated as necessary to form film-coated tablets, sugar-coated tablets and the like.

In addition, the prophylactic or therapeutic agent for migraine of the present invention may contain other medicinal components as long as it does not affect the preventive or therapeutic effect of migraine. From the viewpoint of immediate effect and the like, it is preferable to add an antacid such as magnesium hydroxide, magnesium oxide, magnesium aluminometasilicate, or magnesium carbonate.

The content of ibuprofen and caffeine in the agent for preventing or treating migraine of the present invention may be appropriately selected depending on the preparation.
50% by weight, 10-30% by weight for caffeine
Is preferable, and it is preferable to add 20 to 70 parts by weight of caffeine to 100 parts by weight of ibuprofen.

The dosage of the preventive or therapeutic agent for migraine of the present invention is appropriately selected according to the type and symptom of migraine, but for ibuprofen, it is 50 to 60 per day.
0 mg, preferably 100 to 350 mg, and for caffeines, it is preferable to administer 20 to 400 mg, preferably 40 to 250 mg per day in one to several divided doses per day.

[0018]

[Example] Example 1 The film-coated tablets shown in Table 1 below were produced.

[0019]

[Table 1]

Five volunteers who had mild migraine about twice a month took two preparations of Table 1 once each during migraine, and when the pain disappeared within 1 hour, it was considered effective. As a result, with the product of the present invention, the pain disappeared within 1 hour for all volunteers, but with the comparative product, only 4 people answered that the pain disappeared within 1 hour. In addition, 4 out of 5 people answered that the product of the present invention seemed to have slightly shorter time until pain disappeared.

[0021]

The preventive or therapeutic agent for migraine of the present invention can alleviate migraine and its associated nausea, vomiting, and hypersensitivity to light and sound.

   ─────────────────────────────────────────────────── ─── Continued front page    (72) Inventor Muneshi Otaki             3-17-1-703 Nishinohara, Inzai City, Chiba Prefecture F-term (reference) 4C086 AA01 AA02 CB07 MA02 MA52                       NA14 ZA08 ZC75                 4C206 AA01 AA02 DA24 MA02 MA05                       MA72 NA14 ZA08 ZC75

Claims (3)

[Claims] 1. A preventive or therapeutic agent for migraine comprising ibuprofen and caffeines as active ingredients. 2. The preventive or therapeutic agent for migraine according to claim 1, which contains 20 to 70 parts by weight of caffeine with respect to 100 parts by weight of ibuprofen. 3. The method according to claim 1, further comprising an antacid.
The preventive or therapeutic agent for migraine described.