Drug – bio-affecting and body treating compositions – Preparations characterized by special physical form – Tablets – lozenges – or pills
Patent
1996-07-25
1997-11-11
Page, Thurman K.
Drug, bio-affecting and body treating compositions
Preparations characterized by special physical form
Tablets, lozenges, or pills
424472, 424480, A61K 924
Patent
active
056861095
DESCRIPTION:
BRIEF SUMMARY
This application is an 35USC 31L of PCT/JP94/0231 filed Dec. 2, 1994.
TECHNICAL FIELD
This invention relates to an antipyretic analgesic composition containing ibuprofen and isopropylantipyrine and producing excellent antipyretic and analgesic effects and, more particularly, to three-layer tablets and dry coated tablets, which are utilized in the field of medicine.
BACKGROUND ART
Ibuprofen (2-(4-isobutylphenyl)propionic acid) is a nonsteroid antiinflammatory agent and has excellent antiinflammatory, analgesic and antipyretic activities. It is widely used also in the form of over-the-counter drugs containing it alone or in combination with one or more other active ingredients.
On the other hand, isopropylantipyrine (4-isopropyl-2,3-dimethyl-1-phenyl-3-pyrazolin-5-one) is an antipyretic analgesic of the pyrazolone type. It is used not only as such but also in combination with one or more other analgesic, antipyretic and/or antiinflammatory agents, such as phenacetin, bromodiethylacetylurea, butylisopropylurea, ephedrine, acetaminophen, ethenzamide, caffeine, etc.
However, no mixture composition comprising ibuprofen and isopropylantipyrine is known.
For developing an antipyretic analgesic agent as a drug, in particular as an over-the-counter drug which is freely available for consumers, a preparation is required with which the manifestation of adverse effects is slight and satisfactory antipyretic and analgesic effects can be obtained.
However, ibuprofen causes such adverse effects as gastrointestinal disorders, for example nausea, vomiting, anorexia, pyrosis and the like.
Isopropylantipyrine also has its drawback in that it causes similar gastrointestinal disorders although such disorders are less in degree as compared with ibuprofen.
DISCLOSURE OF THE INVENTION
As a result of intensive investigations made by the present inventors in an attempt to solve the problem mentioned above, it has now been found that when ibuprofen (hereinafter sometimes referred to as "IBP") and isopropylantipyrine (hereinafter sometimes referred to as "IPA") are used combinedly, markedly increased antipyretic and analgesic effects are produced as compared with the cases where IBP and IPA are used each alone separately, with the result that gastrointestinal disorders and other adverse effects can be mitigated.
The proportion of ibuprofen to isopropylantipyrine in the mixture composition of this invention is preferably in the range of 5:1 to 1:5, more preferably in the range of 3:1 to 1:3, on the weight basis.
Preferred examples of said proportion, on the weight basis, of IBP to IPA are thus 5:1, 4:1, 3:1, 2:1, 3:2, 1:1, 2:3, 1:2, 1:3, 1:4, 1:5, and so on.
For use as an over-the-counter drug in Japan, for instance, the mixture composition of this invention contains IBP and IPA in such a proportion as mentioned above, with the maximum daily dose of either of them being taken as 450 mg.
The mixture composition of this invention can be prepared by admixing one or more of the additives mentioned below, each in an appropriate amount, with ibuprofen and isopropylantipyrine. It can then be made up into any of the dosage forms suited for oral administration, for example tablets, hard capsules, soft capsules, powders, granules, fine granules, solutions, syrups and the like, by a per se known method, for example by one of the methods described in the 12th edition of Japanese Pharmacopeia, General rules for preparations.
The additives to be used in dosage form production includes, for example, excipients (e.g. lactose, corn starch, light anhydrous silicic acid, microcrystalline cellulose, etc.), binders (e.g. methylcellulose, carboxymethylcellulose, hydroxypropylcellulose, hydroxypropylmethylcellulose, polyvinylpyrrolidone, etc.), disintegrators (e.g. carboxymethylcellulose calcium, carboxymethylcellulose sodium, low substituted hydroxypropylcellulose, etc.), lubricants (e.g. magnesium stearate, talc, etc.), sweetening agents (e.g. sucrose, D-sorbitol, saccharin sodium, etc.), preservatives (e.g. sodium benzoate, parabens, etc.), thick
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Fujitsu Takashi
Ikebe Isao
Yoneda Kikuko
Fujisawa Pharmaceutical Co. Ltd.
Page Thurman K.
Sikha Murthy
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