WO1997000072A1 - Composition anti-inflammatoire/analgesique - Google Patents
Composition anti-inflammatoire/analgesique Download PDFInfo
- Publication number
- WO1997000072A1 WO1997000072A1 PCT/JP1996/001614 JP9601614W WO9700072A1 WO 1997000072 A1 WO1997000072 A1 WO 1997000072A1 JP 9601614 W JP9601614 W JP 9601614W WO 9700072 A1 WO9700072 A1 WO 9700072A1
- Authority
- WO
- WIPO (PCT)
- Prior art keywords
- ibuprofen
- acetaminophen
- inflammatory
- composition according
- inflammatory analgesic
- Prior art date
Links
- 230000000202 analgesic effect Effects 0.000 title claims abstract description 28
- 239000000203 mixture Substances 0.000 title claims abstract description 27
- 230000003110 anti-inflammatory effect Effects 0.000 title claims abstract description 22
- RZVAJINKPMORJF-UHFFFAOYSA-N Acetaminophen Chemical compound CC(=O)NC1=CC=C(O)C=C1 RZVAJINKPMORJF-UHFFFAOYSA-N 0.000 claims abstract description 34
- HEFNNWSXXWATRW-UHFFFAOYSA-N Ibuprofen Chemical compound CC(C)CC1=CC=C(C(C)C(O)=O)C=C1 HEFNNWSXXWATRW-UHFFFAOYSA-N 0.000 claims abstract description 19
- 229960001680 ibuprofen Drugs 0.000 claims abstract description 19
- 229960005489 paracetamol Drugs 0.000 claims abstract description 17
- 208000023504 respiratory system disease Diseases 0.000 claims abstract description 11
- 229960002739 oxaprozin Drugs 0.000 claims abstract description 9
- OFPXSFXSNFPTHF-UHFFFAOYSA-N oxaprozin Chemical compound O1C(CCC(=O)O)=NC(C=2C=CC=CC=2)=C1C1=CC=CC=C1 OFPXSFXSNFPTHF-UHFFFAOYSA-N 0.000 claims abstract description 9
- 239000004480 active ingredient Substances 0.000 claims abstract description 7
- 208000011580 syndromic disease Diseases 0.000 claims abstract description 4
- 238000000034 method Methods 0.000 claims description 10
- 238000013329 compounding Methods 0.000 claims description 5
- 201000009240 nasopharyngitis Diseases 0.000 claims description 3
- 229940124579 cold medicine Drugs 0.000 claims description 2
- BCHZICNRHXRCHY-UHFFFAOYSA-N 2h-oxazine Chemical compound N1OC=CC=C1 BCHZICNRHXRCHY-UHFFFAOYSA-N 0.000 claims 1
- QTBSBXVTEAMEQO-UHFFFAOYSA-N Acetic acid Chemical compound CC(O)=O QTBSBXVTEAMEQO-UHFFFAOYSA-N 0.000 description 12
- HQKMJHAJHXVSDF-UHFFFAOYSA-L magnesium stearate Chemical compound [Mg+2].CCCCCCCCCCCCCCCCCC([O-])=O.CCCCCCCCCCCCCCCCCC([O-])=O HQKMJHAJHXVSDF-UHFFFAOYSA-L 0.000 description 12
- 239000003814 drug Substances 0.000 description 6
- 229940079593 drug Drugs 0.000 description 6
- 235000019359 magnesium stearate Nutrition 0.000 description 6
- GUBGYTABKSRVRQ-QKKXKWKRSA-N Lactose Natural products OC[C@H]1O[C@@H](O[C@H]2[C@H](O)[C@@H](O)C(O)O[C@@H]2CO)[C@H](O)[C@@H](O)[C@H]1O GUBGYTABKSRVRQ-QKKXKWKRSA-N 0.000 description 5
- 239000008101 lactose Substances 0.000 description 5
- 239000003826 tablet Substances 0.000 description 5
- 229920000168 Microcrystalline cellulose Polymers 0.000 description 4
- 102000016943 Muramidase Human genes 0.000 description 4
- 108010014251 Muramidase Proteins 0.000 description 4
- 241000699670 Mus sp. Species 0.000 description 4
- 108010062010 N-Acetylmuramoyl-L-alanine Amidase Proteins 0.000 description 4
- 239000004359 castor oil Substances 0.000 description 4
- 235000019438 castor oil Nutrition 0.000 description 4
- 239000001913 cellulose Substances 0.000 description 4
- 235000010980 cellulose Nutrition 0.000 description 4
- 229920002678 cellulose Polymers 0.000 description 4
- 230000000694 effects Effects 0.000 description 4
- ZEMPKEQAKRGZGQ-XOQCFJPHSA-N glycerol triricinoleate Natural products CCCCCC[C@@H](O)CC=CCCCCCCCC(=O)OC[C@@H](COC(=O)CCCCCCCC=CC[C@@H](O)CCCCCC)OC(=O)CCCCCCCC=CC[C@H](O)CCCCCC ZEMPKEQAKRGZGQ-XOQCFJPHSA-N 0.000 description 4
- 229960000274 lysozyme Drugs 0.000 description 4
- 239000004325 lysozyme Substances 0.000 description 4
- 235000010335 lysozyme Nutrition 0.000 description 4
- 235000019813 microcrystalline cellulose Nutrition 0.000 description 4
- 239000008108 microcrystalline cellulose Substances 0.000 description 4
- 229940016286 microcrystalline cellulose Drugs 0.000 description 4
- QNVKOSLOVOTXKF-UHFFFAOYSA-N 4-[(2-amino-3,5-dibromophenyl)methylamino]cyclohexan-1-ol;hydron;chloride Chemical compound Cl.NC1=C(Br)C=C(Br)C=C1CNC1CCC(O)CC1 QNVKOSLOVOTXKF-UHFFFAOYSA-N 0.000 description 3
- VEXZGXHMUGYJMC-UHFFFAOYSA-M Chloride anion Chemical compound [Cl-] VEXZGXHMUGYJMC-UHFFFAOYSA-M 0.000 description 3
- 229960000985 ambroxol hydrochloride Drugs 0.000 description 3
- 229940121363 anti-inflammatory agent Drugs 0.000 description 3
- 239000002260 anti-inflammatory agent Substances 0.000 description 3
- 239000002775 capsule Substances 0.000 description 3
- 239000011812 mixed powder Substances 0.000 description 3
- 239000008194 pharmaceutical composition Substances 0.000 description 3
- 238000002360 preparation method Methods 0.000 description 3
- 230000002195 synergetic effect Effects 0.000 description 3
- 238000005303 weighing Methods 0.000 description 3
- 229920000084 Gum arabic Polymers 0.000 description 2
- 229910019142 PO4 Inorganic materials 0.000 description 2
- 241000978776 Senegalia senegal Species 0.000 description 2
- 239000000150 Sympathomimetic Substances 0.000 description 2
- 239000000205 acacia gum Substances 0.000 description 2
- 235000010489 acacia gum Nutrition 0.000 description 2
- 239000000730 antalgic agent Substances 0.000 description 2
- 239000007864 aqueous solution Substances 0.000 description 2
- 210000002683 foot Anatomy 0.000 description 2
- 239000007902 hard capsule Substances 0.000 description 2
- -1 hydroxypropyl Chemical group 0.000 description 2
- 239000010452 phosphate Substances 0.000 description 2
- NBIIXXVUZAFLBC-UHFFFAOYSA-K phosphate Chemical compound [O-]P([O-])([O-])=O NBIIXXVUZAFLBC-UHFFFAOYSA-K 0.000 description 2
- 239000000243 solution Substances 0.000 description 2
- 230000001975 sympathomimetic effect Effects 0.000 description 2
- 239000011782 vitamin Substances 0.000 description 2
- 229930003231 vitamin Natural products 0.000 description 2
- 235000013343 vitamin Nutrition 0.000 description 2
- 229940088594 vitamin Drugs 0.000 description 2
- AKNNEGZIBPJZJG-MSOLQXFVSA-N (-)-noscapine Chemical compound CN1CCC2=CC=3OCOC=3C(OC)=C2[C@@H]1[C@@H]1C2=CC=C(OC)C(OC)=C2C(=O)O1 AKNNEGZIBPJZJG-MSOLQXFVSA-N 0.000 description 1
- UHSXRTHJCJGEKG-UQKRIMTDSA-N (1s)-1-[(3,4,5-trimethoxyphenyl)methyl]-1,2,3,4-tetrahydroisoquinolin-2-ium-6,7-diol;chloride Chemical compound Cl.COC1=C(OC)C(OC)=CC(C[C@H]2C3=CC(O)=C(O)C=C3CCN2)=C1 UHSXRTHJCJGEKG-UQKRIMTDSA-N 0.000 description 1
- 241001535291 Analges Species 0.000 description 1
- OYPRJOBELJOOCE-UHFFFAOYSA-N Calcium Chemical compound [Ca] OYPRJOBELJOOCE-UHFFFAOYSA-N 0.000 description 1
- VTYYLEPIZMXCLO-UHFFFAOYSA-L Calcium carbonate Chemical class [Ca+2].[O-]C([O-])=O VTYYLEPIZMXCLO-UHFFFAOYSA-L 0.000 description 1
- FBPFZTCFMRRESA-KVTDHHQDSA-N D-Mannitol Chemical compound OC[C@@H](O)[C@@H](O)[C@H](O)[C@H](O)CO FBPFZTCFMRRESA-KVTDHHQDSA-N 0.000 description 1
- 108090000790 Enzymes Proteins 0.000 description 1
- 102000004190 Enzymes Human genes 0.000 description 1
- 108010010803 Gelatin Proteins 0.000 description 1
- VEXZGXHMUGYJMC-UHFFFAOYSA-N Hydrochloric acid Chemical compound Cl VEXZGXHMUGYJMC-UHFFFAOYSA-N 0.000 description 1
- 229920002153 Hydroxypropyl cellulose Polymers 0.000 description 1
- 229930195725 Mannitol Natural products 0.000 description 1
- HOKDBMAJZXIPGC-UHFFFAOYSA-N Mequitazine Chemical compound C12=CC=CC=C2SC2=CC=CC=C2N1CC1C(CC2)CCN2C1 HOKDBMAJZXIPGC-UHFFFAOYSA-N 0.000 description 1
- 229910002651 NO3 Inorganic materials 0.000 description 1
- 208000000114 Pain Threshold Diseases 0.000 description 1
- 241000700159 Rattus Species 0.000 description 1
- 241000700157 Rattus norvegicus Species 0.000 description 1
- AUNGANRZJHBGPY-SCRDCRAPSA-N Riboflavin Chemical compound OC[C@@H](O)[C@@H](O)[C@@H](O)CN1C=2C=C(C)C(C)=CC=2N=C2C1=NC(=O)NC2=O AUNGANRZJHBGPY-SCRDCRAPSA-N 0.000 description 1
- 206010041349 Somnolence Diseases 0.000 description 1
- 229920002472 Starch Polymers 0.000 description 1
- GUGOEEXESWIERI-UHFFFAOYSA-N Terfenadine Chemical compound C1=CC(C(C)(C)C)=CC=C1C(O)CCCN1CCC(C(O)(C=2C=CC=CC=2)C=2C=CC=CC=2)CC1 GUGOEEXESWIERI-UHFFFAOYSA-N 0.000 description 1
- AKNNEGZIBPJZJG-UHFFFAOYSA-N alpha-noscapine Natural products CN1CCC2=CC=3OCOC=3C(OC)=C2C1C1C2=CC=C(OC)C(OC)=C2C(=O)O1 AKNNEGZIBPJZJG-UHFFFAOYSA-N 0.000 description 1
- 229960005174 ambroxol Drugs 0.000 description 1
- JBDGDEWWOUBZPM-XYPYZODXSA-N ambroxol Chemical compound NC1=C(Br)C=C(Br)C=C1CN[C@@H]1CC[C@@H](O)CC1 JBDGDEWWOUBZPM-XYPYZODXSA-N 0.000 description 1
- 229940035676 analgesics Drugs 0.000 description 1
- 230000000954 anitussive effect Effects 0.000 description 1
- 229940069428 antacid Drugs 0.000 description 1
- 239000003159 antacid agent Substances 0.000 description 1
- 230000001458 anti-acid effect Effects 0.000 description 1
- 230000001387 anti-histamine Effects 0.000 description 1
- 239000000739 antihistaminic agent Substances 0.000 description 1
- 229940124584 antitussives Drugs 0.000 description 1
- 239000011230 binding agent Substances 0.000 description 1
- 229960001948 caffeine Drugs 0.000 description 1
- RYYVLZVUVIJVGH-UHFFFAOYSA-N caffeine Chemical compound CN1C(=O)N(C)C(=O)C2=C1N=CN2C RYYVLZVUVIJVGH-UHFFFAOYSA-N 0.000 description 1
- 229910052791 calcium Inorganic materials 0.000 description 1
- 239000011575 calcium Substances 0.000 description 1
- 239000000969 carrier Substances 0.000 description 1
- 238000007796 conventional method Methods 0.000 description 1
- ZZVUWRFHKOJYTH-UHFFFAOYSA-N diphenhydramine Chemical compound C=1C=CC=CC=1C(OCCN(C)C)C1=CC=CC=C1 ZZVUWRFHKOJYTH-UHFFFAOYSA-N 0.000 description 1
- 238000007907 direct compression Methods 0.000 description 1
- 239000007884 disintegrant Substances 0.000 description 1
- 239000000975 dye Substances 0.000 description 1
- 230000002708 enhancing effect Effects 0.000 description 1
- 229940088598 enzyme Drugs 0.000 description 1
- 239000000796 flavoring agent Substances 0.000 description 1
- 235000013355 food flavoring agent Nutrition 0.000 description 1
- 238000009472 formulation Methods 0.000 description 1
- 229920000159 gelatin Polymers 0.000 description 1
- 239000008273 gelatin Substances 0.000 description 1
- 235000019322 gelatine Nutrition 0.000 description 1
- 235000011852 gelatine desserts Nutrition 0.000 description 1
- 239000008187 granular material Substances 0.000 description 1
- 210000000548 hind-foot Anatomy 0.000 description 1
- 125000002887 hydroxy group Chemical group [H]O* 0.000 description 1
- 239000001863 hydroxypropyl cellulose Substances 0.000 description 1
- 235000010977 hydroxypropyl cellulose Nutrition 0.000 description 1
- 239000004615 ingredient Substances 0.000 description 1
- 239000003112 inhibitor Substances 0.000 description 1
- 108010027678 lagenin Proteins 0.000 description 1
- 229940031703 low substituted hydroxypropyl cellulose Drugs 0.000 description 1
- 210000003141 lower extremity Anatomy 0.000 description 1
- 239000000314 lubricant Substances 0.000 description 1
- 239000000594 mannitol Substances 0.000 description 1
- 235000010355 mannitol Nutrition 0.000 description 1
- 238000005259 measurement Methods 0.000 description 1
- 229960005042 mequitazine Drugs 0.000 description 1
- PLPRGLOFPNJOTN-UHFFFAOYSA-N narcotine Natural products COc1ccc2C(OC(=O)c2c1OC)C3Cc4c(CN3C)cc5OCOc5c4OC PLPRGLOFPNJOTN-UHFFFAOYSA-N 0.000 description 1
- 229960004708 noscapine Drugs 0.000 description 1
- 230000037040 pain threshold Effects 0.000 description 1
- 239000000546 pharmaceutical excipient Substances 0.000 description 1
- 239000000843 powder Substances 0.000 description 1
- 125000001436 propyl group Chemical group [H]C([*])([H])C([H])([H])C([H])([H])[H] 0.000 description 1
- 239000008107 starch Substances 0.000 description 1
- 235000019698 starch Nutrition 0.000 description 1
- 235000000346 sugar Nutrition 0.000 description 1
- 239000000454 talc Substances 0.000 description 1
- 229910052623 talc Inorganic materials 0.000 description 1
- 150000003722 vitamin derivatives Chemical class 0.000 description 1
Classifications
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K31/00—Medicinal preparations containing organic active ingredients
- A61K31/33—Heterocyclic compounds
- A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
- A61K31/41—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with two or more ring hetero atoms, at least one of which being nitrogen, e.g. tetrazole
- A61K31/42—Oxazoles
Definitions
- the present invention relates to an anti-inflammatory analgesic composition having enhanced analgesic activity.
- Oxaprozin is widely used as an anti-inflammatory analgesic, but its action is relatively weak, and it is said that it is difficult to obtain a sufficient effect on respiratory diseases.
- the analgesics ibuprofen and acetaminophen are effective for respiratory diseases such as common cold syndrome. Had a problem.
- U.S. Pat. No. 4,552,8999 describes a pharmaceutical composition for treating respiratory diseases such as common cold, which contains anti-inflammatory agents such as ibuprofen and oxabrogine. I have.
- the pharmaceutical composition produces a synergistic effect by combining an anti-inflammatory agent with a sympathomimetic stimulant, an antihistamine, and the like, and does not suggest a synergistic effect due to the combination of the anti-inflammatory agents.
- a pharmaceutical composition containing oxaboxazin and ibubrofen or acetoaminophen Disclosure of the invention
- An object of the present invention is to provide an anti-inflammatory analgesic having an enhanced analgesic effect.
- the present inventors have conducted studies with the aim of enhancing the analgesic effect.
- the combination of oxaprozin with the analgesic agent ibuprofen or acetaminophen provides an anti-inflammatory analgesic with enhanced analgesic action. This has led to the completion of the present invention.
- the present invention includes the following inventions.
- An anti-inflammatory analgesic composition comprising oxasuboral gin and ibubrofen as active ingredients.
- composition according to (2) wherein the mixing ratio (weight ratio) of oxabrozin: ibuprofen is 1: 0.1 to 1:10.
- composition according to (2), wherein the mixing ratio (weight ratio) of oxabrozin: ibuprofen is 0.25 to 1: 5.
- An anti-inflammatory analgesic composition containing oxasubatin and acetoaminophen as active ingredients.
- composition according to (5), wherein the compounding ratio (heavy Mit) of oxaprozin: acetaminophen is 1: 0.1 to 1: 1.
- composition according to the above (5), wherein the mixing ratio (weight ratio) of oxabrozine: acetaminophen is from 1: 0.25 to 1: 5.
- a method for treating a respiratory disease which comprises administering the anti-inflammatory analgesic composition according to the above (1) to a patient with a respiratory disease.
- the mixing ratio (weight ratio) of oxabrozine: ibubrofen or acetoaminophen is usually 1: 0.1-1: 10, preferably 1: 0.25: L: 5.
- the anti-inflammatory analgesic composition of the present invention can usually be orally administered to an adult at 300 to 1600 mg per day as an active ingredient in one or several divided doses. This dose can be appropriately adjusted depending on the age, weight, and medical condition.
- an auxiliary drug such as an antitussive, an anti-inflammatory enzyme, a sympathomimetic, an anti-inflammatory, a drowsiness inhibitor, a vitamin, a crude drug, or an antacid may be appropriately added.
- the anti-inflammatory analgesic composition of the present invention is used as a formulation for oral administration such as tablets, granules, powders, capsules and solutions. These preparations can be prepared by a conventional method.
- Carriers used in the preparation of preparations include excipients such as lactose, starch, sugar, mannitol, crystalline cellulose, binders such as hydroxypropylcellulose, hydroxypropyl xymethylcellulose, gelatin, PVP, There are disintegrants such as calcium cellulose cellulose and low-substituted hydroxypropylcellulose, and lubricants such as magnesium stearate, hydrogenated castor oil, and talc. Dyes, flavoring agents and the like can be used.
- No. 2 hard capsule was filled in 200 mg each to obtain 5000 capsules.
- the obtained mixed powder was filled into No. 2 hard capsules in an amount of 20 mg each to obtain 6000 capsules.
- the anti-inflammatory analgesic composition of the present invention has an enhanced analgesic effect as compared to a case where (a) oxabrozine or (b) ibuprofen or acetaminophen is used alone, and includes a power syndrome and the like. Since it has an effect on respiratory diseases, it can be used as a cold remedy. In addition, since a synergistic effect is observed, the effect can be obtained at a low dose, thereby reducing side effects.
Landscapes
- Health & Medical Sciences (AREA)
- Chemical & Material Sciences (AREA)
- Medicinal Chemistry (AREA)
- Pharmacology & Pharmacy (AREA)
- Epidemiology (AREA)
- Life Sciences & Earth Sciences (AREA)
- Animal Behavior & Ethology (AREA)
- General Health & Medical Sciences (AREA)
- Public Health (AREA)
- Veterinary Medicine (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
Abstract
Composition anti-inflammatoire/analgésique qui comporte en tant qu'ingrédients actifs (a) de l'oxaprozine et (b) de l'ibuprofène ou de l'acétaminophène. Comparée aux cas où soit (a) l'oxaprozine, soit (b) l'ibuprofène ou l'acétaminophène est employé seul, la présente composition présente un effet analgésique amélioré et est efficace contre les maladies du système respiratoire telles que le syndrome de refroidissement, ce qui permet de l'utiliser en tant que remède contre le rhume.
Priority Applications (1)
Application Number | Priority Date | Filing Date | Title |
---|---|---|---|
AU60160/96A AU6016096A (en) | 1995-06-16 | 1996-06-13 | Anti-inflammatory/analgetic composition |
Applications Claiming Priority (2)
Application Number | Priority Date | Filing Date | Title |
---|---|---|---|
JP14982195 | 1995-06-16 | ||
JP7/149821 | 1995-06-16 |
Publications (1)
Publication Number | Publication Date |
---|---|
WO1997000072A1 true WO1997000072A1 (fr) | 1997-01-03 |
Family
ID=15483440
Family Applications (1)
Application Number | Title | Priority Date | Filing Date |
---|---|---|---|
PCT/JP1996/001614 WO1997000072A1 (fr) | 1995-06-16 | 1996-06-13 | Composition anti-inflammatoire/analgesique |
Country Status (2)
Country | Link |
---|---|
AU (1) | AU6016096A (fr) |
WO (1) | WO1997000072A1 (fr) |
Cited By (1)
Publication number | Priority date | Publication date | Assignee | Title |
---|---|---|---|---|
KR20010089913A (ko) * | 2000-03-13 | 2001-10-17 | 류영선 | 무공해 완구신소재 및 그 제조공법 |
-
1996
- 1996-06-13 WO PCT/JP1996/001614 patent/WO1997000072A1/fr active Application Filing
- 1996-06-13 AU AU60160/96A patent/AU6016096A/en not_active Abandoned
Non-Patent Citations (2)
Title |
---|
BY THE PHARMACIST SOCIETY OF OSAKA HOSPITAL, "Drug Handbook (5th Edit.)", YAKUGYO JIHOSHA CO., LTD., 5 February 1995, p. 126-127, 108-109, 94-95. * |
THE MERCK INDEX, Eleventh Edition (1989) p. 6880, 4811, 39. * |
Cited By (1)
Publication number | Priority date | Publication date | Assignee | Title |
---|---|---|---|---|
KR20010089913A (ko) * | 2000-03-13 | 2001-10-17 | 류영선 | 무공해 완구신소재 및 그 제조공법 |
Also Published As
Publication number | Publication date |
---|---|
AU6016096A (en) | 1997-01-15 |
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