JP2000080034A - Composition for cold - Google Patents
Composition for coldInfo
- Publication number
- JP2000080034A JP2000080034A JP10247905A JP24790598A JP2000080034A JP 2000080034 A JP2000080034 A JP 2000080034A JP 10247905 A JP10247905 A JP 10247905A JP 24790598 A JP24790598 A JP 24790598A JP 2000080034 A JP2000080034 A JP 2000080034A
- Authority
- JP
- Japan
- Prior art keywords
- cold
- composition
- salts
- ambroxol
- naproxen
- Prior art date
- Legal status (The legal status is an assumption and is not a legal conclusion. Google has not performed a legal analysis and makes no representation as to the accuracy of the status listed.)
- Pending
Links
- 239000000203 mixture Substances 0.000 title claims abstract description 14
- 150000003839 salts Chemical class 0.000 claims abstract description 15
- CMWTZPSULFXXJA-UHFFFAOYSA-N Naproxen Natural products C1=C(C(C)C(O)=O)C=CC2=CC(OC)=CC=C21 CMWTZPSULFXXJA-UHFFFAOYSA-N 0.000 claims abstract description 8
- 229960002009 naproxen Drugs 0.000 claims abstract description 8
- CMWTZPSULFXXJA-VIFPVBQESA-N naproxen Chemical compound C1=C([C@H](C)C(O)=O)C=CC2=CC(OC)=CC=C21 CMWTZPSULFXXJA-VIFPVBQESA-N 0.000 claims abstract description 8
- DKYWVDODHFEZIM-UHFFFAOYSA-N ketoprofen Chemical compound OC(=O)C(C)C1=CC=CC(C(=O)C=2C=CC=CC=2)=C1 DKYWVDODHFEZIM-UHFFFAOYSA-N 0.000 claims abstract description 7
- 229960000991 ketoprofen Drugs 0.000 claims abstract description 7
- PXWLVJLKJGVOKE-UHFFFAOYSA-N propyphenazone Chemical compound O=C1C(C(C)C)=C(C)N(C)N1C1=CC=CC=C1 PXWLVJLKJGVOKE-UHFFFAOYSA-N 0.000 claims abstract description 7
- 229960002189 propyphenazone Drugs 0.000 claims abstract description 7
- 229960005174 ambroxol Drugs 0.000 claims abstract description 6
- 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 claims abstract description 6
- OJGDCBLYJGHCIH-UHFFFAOYSA-N bromhexine Chemical compound C1CCCCC1N(C)CC1=CC(Br)=CC(Br)=C1N OJGDCBLYJGHCIH-UHFFFAOYSA-N 0.000 claims abstract description 6
- 229960003870 bromhexine Drugs 0.000 claims abstract description 6
- DCOPUUMXTXDBNB-UHFFFAOYSA-N diclofenac Chemical compound OC(=O)CC1=CC=CC=C1NC1=C(Cl)C=CC=C1Cl DCOPUUMXTXDBNB-UHFFFAOYSA-N 0.000 claims abstract description 6
- 229960001259 diclofenac Drugs 0.000 claims abstract description 6
- 208000024891 symptom Diseases 0.000 abstract description 10
- 206010011224 Cough Diseases 0.000 abstract description 7
- 208000011580 syndromic disease Diseases 0.000 abstract description 6
- 230000000694 effects Effects 0.000 abstract description 3
- 238000002156 mixing Methods 0.000 abstract description 2
- HQKMJHAJHXVSDF-UHFFFAOYSA-L magnesium stearate Chemical compound [Mg+2].CCCCCCCCCCCCCCCCCC([O-])=O.CCCCCCCCCCCCCCCCCC([O-])=O HQKMJHAJHXVSDF-UHFFFAOYSA-L 0.000 description 8
- -1 chewables Substances 0.000 description 6
- 238000002360 preparation method Methods 0.000 description 6
- 239000003755 preservative agent Substances 0.000 description 6
- 239000003814 drug Substances 0.000 description 5
- 229940079593 drug Drugs 0.000 description 5
- 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 4
- 239000004359 castor oil Substances 0.000 description 4
- 235000019438 castor oil Nutrition 0.000 description 4
- HFBYLYCMISIEMM-FFHNEAJVSA-N dihydrocodeine phosphate Chemical compound OP(O)(O)=O.C([C@H]1[C@H](N(CC[C@@]112)C)C3)C[C@H](O)[C@@H]1OC1=C2C3=CC=C1OC HFBYLYCMISIEMM-FFHNEAJVSA-N 0.000 description 4
- 239000000796 flavoring agent Substances 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
- 239000008187 granular material Substances 0.000 description 4
- 239000008101 lactose Substances 0.000 description 4
- 235000019359 magnesium stearate Nutrition 0.000 description 4
- 230000002335 preservative effect Effects 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
- 102000016943 Muramidase Human genes 0.000 description 3
- 108010014251 Muramidase Proteins 0.000 description 3
- 108010062010 N-Acetylmuramoyl-L-alanine Amidase Proteins 0.000 description 3
- 229930006000 Sucrose Natural products 0.000 description 3
- 239000004480 active ingredient Substances 0.000 description 3
- 229960000985 ambroxol hydrochloride Drugs 0.000 description 3
- 230000000954 anitussive effect Effects 0.000 description 3
- 235000014113 dietary fatty acids Nutrition 0.000 description 3
- 229960000920 dihydrocodeine Drugs 0.000 description 3
- 239000003172 expectorant agent Substances 0.000 description 3
- 230000003419 expectorant effect Effects 0.000 description 3
- 229940066493 expectorants Drugs 0.000 description 3
- 239000000194 fatty acid Substances 0.000 description 3
- 229930195729 fatty acid Natural products 0.000 description 3
- 235000019634 flavors Nutrition 0.000 description 3
- 235000003599 food sweetener Nutrition 0.000 description 3
- 229960000274 lysozyme Drugs 0.000 description 3
- 239000004325 lysozyme Substances 0.000 description 3
- 235000010335 lysozyme Nutrition 0.000 description 3
- 239000002904 solvent Substances 0.000 description 3
- 239000005720 sucrose Substances 0.000 description 3
- 239000003765 sweetening agent Substances 0.000 description 3
- 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 2
- 101000879758 Homo sapiens Sjoegren syndrome nuclear autoantigen 1 Proteins 0.000 description 2
- HOKDBMAJZXIPGC-UHFFFAOYSA-N Mequitazine Chemical compound C12=CC=CC=C2SC2=CC=CC=C2N1CC1C(CC2)CCN2C1 HOKDBMAJZXIPGC-UHFFFAOYSA-N 0.000 description 2
- 229920000168 Microcrystalline cellulose Polymers 0.000 description 2
- 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 2
- 102100037330 Sjoegren syndrome nuclear autoantigen 1 Human genes 0.000 description 2
- 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 2
- 229960001948 caffeine Drugs 0.000 description 2
- RYYVLZVUVIJVGH-UHFFFAOYSA-N caffeine Chemical compound CN1C(=O)N(C)C(=O)C2=C1N=CN2C RYYVLZVUVIJVGH-UHFFFAOYSA-N 0.000 description 2
- 239000002775 capsule Substances 0.000 description 2
- 239000003795 chemical substances by application Substances 0.000 description 2
- 239000007788 liquid Substances 0.000 description 2
- 229940031703 low substituted hydroxypropyl cellulose Drugs 0.000 description 2
- 229960005042 mequitazine Drugs 0.000 description 2
- 238000000034 method Methods 0.000 description 2
- 235000019813 microcrystalline cellulose Nutrition 0.000 description 2
- 239000008108 microcrystalline cellulose Substances 0.000 description 2
- 229940016286 microcrystalline cellulose Drugs 0.000 description 2
- PLPRGLOFPNJOTN-UHFFFAOYSA-N narcotine Natural products COc1ccc2C(OC(=O)c2c1OC)C3Cc4c(CN3C)cc5OCOc5c4OC PLPRGLOFPNJOTN-UHFFFAOYSA-N 0.000 description 2
- 229940021182 non-steroidal anti-inflammatory drug Drugs 0.000 description 2
- 229960004708 noscapine Drugs 0.000 description 2
- 239000008363 phosphate buffer Substances 0.000 description 2
- 239000000049 pigment Substances 0.000 description 2
- 239000000843 powder Substances 0.000 description 2
- 239000008213 purified water Substances 0.000 description 2
- 239000006188 syrup Substances 0.000 description 2
- 235000020357 syrup Nutrition 0.000 description 2
- 239000003826 tablet Substances 0.000 description 2
- ZFXYFBGIUFBOJW-UHFFFAOYSA-N theophylline Chemical compound O=C1N(C)C(=O)N(C)C2=C1NC=N2 ZFXYFBGIUFBOJW-UHFFFAOYSA-N 0.000 description 2
- UIERGBJEBXXIGO-UHFFFAOYSA-N thiamine mononitrate Chemical compound [O-][N+]([O-])=O.CC1=C(CCO)SC=[N+]1CC1=CN=C(C)N=C1N UIERGBJEBXXIGO-UHFFFAOYSA-N 0.000 description 2
- XLYOFNOQVPJJNP-UHFFFAOYSA-N water Chemical compound O XLYOFNOQVPJJNP-UHFFFAOYSA-N 0.000 description 2
- 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
- 229920002153 Hydroxypropyl cellulose Polymers 0.000 description 1
- 229930195725 Mannitol Natural products 0.000 description 1
- 241001465754 Metazoa Species 0.000 description 1
- 229920003171 Poly (ethylene oxide) Polymers 0.000 description 1
- 229920002675 Polyoxyl Polymers 0.000 description 1
- 241000700159 Rattus Species 0.000 description 1
- 229920002472 Starch Polymers 0.000 description 1
- NTCYWJCEOILKNG-ROLPUNSJSA-N [(1r,2s)-1-hydroxy-1-phenylpropan-2-yl]-dimethylazanium;chloride Chemical compound Cl.CN(C)[C@@H](C)[C@H](O)C1=CC=CC=C1 NTCYWJCEOILKNG-ROLPUNSJSA-N 0.000 description 1
- YKTSYUJCYHOUJP-UHFFFAOYSA-N [O--].[Al+3].[Al+3].[O-][Si]([O-])([O-])[O-] Chemical compound [O--].[Al+3].[Al+3].[O-][Si]([O-])([O-])[O-] YKTSYUJCYHOUJP-UHFFFAOYSA-N 0.000 description 1
- 239000002253 acid Substances 0.000 description 1
- WMGSQTMJHBYJMQ-UHFFFAOYSA-N aluminum;magnesium;silicate Chemical compound [Mg+2].[Al+3].[O-][Si]([O-])([O-])[O-] WMGSQTMJHBYJMQ-UHFFFAOYSA-N 0.000 description 1
- 229940069428 antacid Drugs 0.000 description 1
- 239000003159 antacid agent Substances 0.000 description 1
- 230000003266 anti-allergic effect Effects 0.000 description 1
- 229940124599 anti-inflammatory drug Drugs 0.000 description 1
- 230000003110 anti-inflammatory effect Effects 0.000 description 1
- 239000000043 antiallergic agent Substances 0.000 description 1
- 229940065524 anticholinergics inhalants for obstructive airway diseases Drugs 0.000 description 1
- 239000000739 antihistaminic agent Substances 0.000 description 1
- 229940125715 antihistaminic agent Drugs 0.000 description 1
- 239000003434 antitussive agent Substances 0.000 description 1
- 229940124584 antitussives Drugs 0.000 description 1
- 239000007864 aqueous solution Substances 0.000 description 1
- 239000011230 binding agent Substances 0.000 description 1
- 230000037396 body weight Effects 0.000 description 1
- 229960002335 bromhexine hydrochloride Drugs 0.000 description 1
- 206010006451 bronchitis Diseases 0.000 description 1
- 229940124630 bronchodilator Drugs 0.000 description 1
- 239000000168 bronchodilator agent Substances 0.000 description 1
- 239000000872 buffer Substances 0.000 description 1
- 239000006172 buffering agent Substances 0.000 description 1
- 229960000456 carbinoxamine maleate Drugs 0.000 description 1
- GVNWHCVWDRNXAZ-BTJKTKAUSA-N carbinoxamine maleate Chemical compound OC(=O)\C=C/C(O)=O.C=1C=CC=NC=1C(OCCN(C)C)C1=CC=C(Cl)C=C1 GVNWHCVWDRNXAZ-BTJKTKAUSA-N 0.000 description 1
- 229940084030 carboxymethylcellulose calcium Drugs 0.000 description 1
- 239000000969 carrier Substances 0.000 description 1
- 239000001913 cellulose Substances 0.000 description 1
- 229920002678 cellulose Polymers 0.000 description 1
- 235000010980 cellulose Nutrition 0.000 description 1
- 239000000812 cholinergic antagonist Substances 0.000 description 1
- 239000007979 citrate buffer Substances 0.000 description 1
- 229940124579 cold medicine Drugs 0.000 description 1
- 238000007796 conventional method Methods 0.000 description 1
- 230000003247 decreasing effect Effects 0.000 description 1
- 229960001193 diclofenac sodium Drugs 0.000 description 1
- 238000007907 direct compression Methods 0.000 description 1
- 229940073563 dl- methylephedrine hydrochloride Drugs 0.000 description 1
- DLNKOYKMWOXYQA-UHFFFAOYSA-N dl-pseudophenylpropanolamine Natural products CC(N)C(O)C1=CC=CC=C1 DLNKOYKMWOXYQA-UHFFFAOYSA-N 0.000 description 1
- 230000000210 effect on cough Effects 0.000 description 1
- 229940088598 enzyme Drugs 0.000 description 1
- 150000002148 esters Chemical class 0.000 description 1
- YRSGDLIATOURQO-UHFFFAOYSA-N ethyl 4-acetyl-5-oxohexanoate Chemical compound CCOC(=O)CCC(C(C)=O)C(C)=O YRSGDLIATOURQO-UHFFFAOYSA-N 0.000 description 1
- 239000006260 foam Substances 0.000 description 1
- 239000004088 foaming agent Substances 0.000 description 1
- 235000013355 food flavoring agent Nutrition 0.000 description 1
- 238000009472 formulation Methods 0.000 description 1
- 239000003205 fragrance Substances 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
- 150000002334 glycols Chemical class 0.000 description 1
- 239000001863 hydroxypropyl cellulose Substances 0.000 description 1
- 235000010977 hydroxypropyl cellulose Nutrition 0.000 description 1
- 239000001866 hydroxypropyl methyl cellulose Substances 0.000 description 1
- 235000010979 hydroxypropyl methyl cellulose Nutrition 0.000 description 1
- 229920003088 hydroxypropyl methyl cellulose Polymers 0.000 description 1
- UFVKGYZPFZQRLF-UHFFFAOYSA-N hydroxypropyl methyl cellulose Chemical compound OC1C(O)C(OC)OC(CO)C1OC1C(O)C(O)C(OC2C(C(O)C(OC3C(C(O)C(O)C(CO)O3)O)C(CO)O2)O)C(CO)O1 UFVKGYZPFZQRLF-UHFFFAOYSA-N 0.000 description 1
- 230000002401 inhibitory effect Effects 0.000 description 1
- 239000000314 lubricant Substances 0.000 description 1
- ZLNQQNXFFQJAID-UHFFFAOYSA-L magnesium carbonate Chemical compound [Mg+2].[O-]C([O-])=O ZLNQQNXFFQJAID-UHFFFAOYSA-L 0.000 description 1
- 239000001095 magnesium carbonate Substances 0.000 description 1
- 229910000021 magnesium carbonate Inorganic materials 0.000 description 1
- 239000000395 magnesium oxide Substances 0.000 description 1
- CPLXHLVBOLITMK-UHFFFAOYSA-N magnesium oxide Inorganic materials [Mg]=O CPLXHLVBOLITMK-UHFFFAOYSA-N 0.000 description 1
- 239000000391 magnesium silicate Substances 0.000 description 1
- 229910052919 magnesium silicate Inorganic materials 0.000 description 1
- 235000019792 magnesium silicate Nutrition 0.000 description 1
- AXZKOIWUVFPNLO-UHFFFAOYSA-N magnesium;oxygen(2-) Chemical compound [O-2].[Mg+2] AXZKOIWUVFPNLO-UHFFFAOYSA-N 0.000 description 1
- ZADYMNAVLSWLEQ-UHFFFAOYSA-N magnesium;oxygen(2-);silicon(4+) Chemical compound [O-2].[O-2].[O-2].[Mg+2].[Si+4] ZADYMNAVLSWLEQ-UHFFFAOYSA-N 0.000 description 1
- 239000000594 mannitol Substances 0.000 description 1
- 235000010355 mannitol Nutrition 0.000 description 1
- 150000007522 mineralic acids Chemical class 0.000 description 1
- 239000011812 mixed powder Substances 0.000 description 1
- 201000009240 nasopharyngitis Diseases 0.000 description 1
- QIQXTHQIDYTFRH-UHFFFAOYSA-N octadecanoic acid Chemical compound CCCCCCCCCCCCCCCCCC(O)=O QIQXTHQIDYTFRH-UHFFFAOYSA-N 0.000 description 1
- 239000006186 oral dosage form Substances 0.000 description 1
- 150000007524 organic acids Chemical class 0.000 description 1
- 239000003002 pH adjusting agent Substances 0.000 description 1
- 230000007170 pathology Effects 0.000 description 1
- 239000000546 pharmaceutical excipient Substances 0.000 description 1
- DLNKOYKMWOXYQA-APPZFPTMSA-N phenylpropanolamine Chemical compound C[C@@H](N)[C@H](O)C1=CC=CC=C1 DLNKOYKMWOXYQA-APPZFPTMSA-N 0.000 description 1
- 229960000395 phenylpropanolamine Drugs 0.000 description 1
- 229920002503 polyoxyethylene-polyoxypropylene Polymers 0.000 description 1
- JGMJQSFLQWGYMQ-UHFFFAOYSA-M sodium;2,6-dichloro-n-phenylaniline;acetate Chemical compound [Na+].CC([O-])=O.ClC1=CC=CC(Cl)=C1NC1=CC=CC=C1 JGMJQSFLQWGYMQ-UHFFFAOYSA-M 0.000 description 1
- 239000000243 solution Substances 0.000 description 1
- 241000894007 species Species 0.000 description 1
- 239000008107 starch Substances 0.000 description 1
- 235000019698 starch Nutrition 0.000 description 1
- 239000000021 stimulant Substances 0.000 description 1
- 235000000346 sugar Nutrition 0.000 description 1
- 230000001629 suppression Effects 0.000 description 1
- 239000004094 surface-active agent Substances 0.000 description 1
- 238000002636 symptomatic treatment Methods 0.000 description 1
- 239000000454 talc Substances 0.000 description 1
- 229910052623 talc Inorganic materials 0.000 description 1
- 238000010998 test method Methods 0.000 description 1
- 229960000278 theophylline Drugs 0.000 description 1
- 239000002562 thickening agent Substances 0.000 description 1
- 239000011782 vitamin Substances 0.000 description 1
- 229930003231 vitamin Natural products 0.000 description 1
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- 229940088594 vitamin Drugs 0.000 description 1
Abstract
Description
【０００１】[0001]
【産業上の利用分野】本発明は、風邪症候群による諸症
状のうち咳嗽に対する効果が増強された風邪用組成物に
関する。BACKGROUND OF THE INVENTION 1. Field of the Invention The present invention relates to a composition for colds having an enhanced effect on cough among various symptoms caused by cold syndrome.
【０００２】[0002]
【従来の技術】風邪症候群の治療は、個々の風邪症状の
改善を目的とする対症療法が中心となっており、風邪症
候群の諸症状を如何に早く除去或いは軽減するかが治療
上の重要なポイントとなっている。2. Description of the Related Art The treatment of the cold syndrome is centered on symptomatic treatment for the purpose of improving individual cold symptoms, and it is important how to eliminate or reduce various symptoms of the cold syndrome as soon as possible. Points.
【０００３】従来、多種の風邪用組成物が知られている
が、何れも風邪症候群による咳嗽症状に対する効果が充
分でないため、充分満足できる効果が得られていなかっ
た。[0003] Conventionally, various types of compositions for cold have been known, but none of them have been sufficiently effective for cough symptoms caused by cold syndrome, and thus have not been able to obtain sufficiently satisfactory effects.
【０００４】ナプロキセン、ジクロフェナク、ケトプロ
フェン及びイソプロピルアンチピリンは、抗炎症薬とし
て用いられており、ブロムヘキシン及びアンブロキソー
ルは去痰薬として用いられている。[0004] Naproxen, diclofenac, ketoprofen and isopropylantipyrine have been used as anti-inflammatory drugs, and bromhexine and ambroxol have been used as expectorants.
【０００５】[0005]
【発明が解決しようとする課題】本発明の目的は、鎮咳
作用の高い風邪用組成物を提供することである。SUMMARY OF THE INVENTION An object of the present invention is to provide a composition for colds having a high antitussive effect.
【０００６】[0006]
【課題を解決するための手段】本発明者らは、風邪症候
群の諸症状のうち咳嗽症状の除去あるいは軽減をはかる
ことを目的とし研究した結果、有効成分としてある種の
非ステロイド性抗炎症薬及びある種の去痰薬の配合する
ことにより、目的を達成することができることを見いだ
し、本発明を完成した。DISCLOSURE OF THE INVENTION The present inventors have studied for the purpose of eliminating or alleviating coughing symptoms among various symptoms of cold syndrome, and as a result, have found that certain nonsteroidal anti-inflammatory drugs as active ingredients It has been found that the purpose can be achieved by blending certain expectorants, and the present invention has been completed.
【０００７】すなわち、本発明は有効成分として（Ａ）
ナプロキセン、ジクロフェナク、ケトプロフェン、イソ
プロピルアンチピリン及びそれらの塩類から選ばれる１
種又は２種以上及び（Ｂ）ブロムヘキシン、アンブロキ
ソール及びそれらの塩類から選ばれる１種又は２種以上
を配合することにより、風邪等による咳嗽症状の軽減・
除去に対し劇的な効果がある風邪用組成物である。That is, the present invention provides (A)
1 selected from naproxen, diclofenac, ketoprofen, isopropylantipyrine and salts thereof
Combination of one or more species or two or more and (B) one or more selected from bromhexine, ambroxol and salts thereof, to reduce cough symptoms due to colds and the like
It is a cold composition that has a dramatic effect on removal.
【０００８】本発明の風邪用組成物は、上記の有効成分
の他に必要に応じて他の非ステロイド性抗炎症薬や去痰
薬、消炎酵素薬類、気管支拡張薬、中枢神経興奮薬、鎮
咳薬、抗ヒスタミン薬または抗アレルギー薬、抗コリン
薬、ビタミン類、制酸薬、生薬等を適宜に配合しても良
い。[0008] In addition to the above-mentioned active ingredients, the composition for colds of the present invention may contain other non-steroidal anti-inflammatory drugs, expectorants, anti-inflammatory enzymes, bronchodilators, central nervous stimulants, antitussives, if necessary. Drugs, antihistamines or antiallergics, anticholinergics, vitamins, antacids, crude drugs, etc. may be appropriately compounded.
【０００９】なお、これらは単独または相互に混合して
用いることができ、例えば、医薬品製造指針（１９９５
年版・薬業時報社）に収載されているかぜ薬基準等に準
拠して配合することができる。[0009] These can be used alone or in admixture with each other.
It can be compounded according to the cold medicine standards and the like listed in Yakuhin Higashihosha (Year Edition).
【００１０】本発明の風邪用組成物は、１回ないし数回
に分けて経口投与することができる。投与量は年齢、体
重、病状により適宜増減することができる。The composition for colds of the present invention can be administered orally in one or several divided doses. The dose can be appropriately increased or decreased depending on the age, body weight and medical condition.
【００１１】それぞれの有効成分の配合量は、成人に対
して１日当たり、ナプロキセンまたはその塩類は１５０
〜６００ｍｇがよく、ジクロフェナクまたはその塩類は
１２.５〜１００ｍｇがよく、ケトプロフェンまたはそ
の塩類は５０〜１５０ｍｇがよく、イソプロピルアンチ
ピリンまたはその塩類は２００〜４００ｍｇがよい。ブ
ロムヘキシンまたはその塩類は６〜２４ｍｇがよく、ア
ンブロキソールまたはその塩類は２２．５〜７５ｍｇが
よい。[0011] The amount of each active ingredient to be used per day for an adult is 150 mg of naproxen or a salt thereof.
６００600 mg is good, diclofenac or its salt is 12.5-100 mg, ketoprofen or its salt is 50-150 mg, and isopropylantipyrine or its salt is 200-400 mg. Bromhexine or a salt thereof is preferably 6 to 24 mg, and ambroxol or a salt thereof is preferably 22.5 to 75 mg.
【００１２】本発明の風邪用組成物は、錠剤、カプセル
剤、顆粒剤、細粒剤、粉剤、チュアブル剤、発泡剤、ド
ロップ剤、口中溶解剤、ドライシロップ剤、内服液剤等
の経口投与形態の製剤として用いる。The composition for colds of the present invention can be used in the form of oral dosage forms such as tablets, capsules, granules, fine granules, powders, chewables, foams, drops, dissolving agents in the mouth, dry syrups, and oral liquids. Use as a formulation.
【００１３】これらの製剤は、常法により調製すること
ができる。錠剤、カプセル剤、顆粒剤、細粒剤、粉剤、
チュアブル剤、発泡剤、ドロップ剤、口中溶解剤及びド
ライシロップ剤においては製剤の調製に使用する担体と
しては、乳糖、デンプン、砂糖、マンニトール、結晶セ
ルロースなどの賦形剤、ヒドロキシプロピルセルロー
ス、ヒドロキシプロピルメチルセルロース、ゼラチン、
ＰＶＰなどの結合剤、カルボキシメチルセルロースカル
シウム、低置換度ヒドロキシプロピルセルロースなどの
崩壊剤、ステアリン酸マグネシウム、硬化ヒマシ油、タ
ルクなどの滑沢剤があり、この他必要に応じて溶解補助
剤、緩衝剤、保存剤、香料、色素、矯味剤等を使用する
ことができる。また、内服液剤においては製剤の調製に
使用する担体としては、ショ糖脂肪酸エステル類、ステ
アリン酸ポリオキシル類、ポリオキシエチレンポリオキ
シプロピレングリコール類、ポリオキシエチレンモノ脂
肪酸エステル類等の界面活性剤、合成ケイ酸アルミニウ
ム、ケイ酸マグネシウム、炭酸マグネシウム、酸化マグ
ネシウム、メタケイ酸アルミン酸マグネシウム等の増粘
剤、クエン酸緩衝液、リン酸緩衝液等の有機酸系・無機
酸系のｐＨ調整剤があり、この他必要に応じて溶解補助
剤、緩衝剤、保存剤、香料、色素、甘味剤等を使用する
ことができる。These preparations can be prepared by a conventional method. Tablets, capsules, granules, fine granules, powders,
In chewables, foaming agents, drops, mouth solubilizers and dry syrups, carriers used for preparation of preparations include lactose, starch, sugar, mannitol, excipients such as crystalline cellulose, hydroxypropylcellulose, hydroxypropylmethylcellulose. ,gelatin,
There are binders such as PVP, disintegrators such as carboxymethylcellulose calcium and low-substituted hydroxypropylcellulose, lubricants such as magnesium stearate, hydrogenated castor oil, and talc, and other solubilizing agents and buffering agents as necessary. , Preservatives, flavors, pigments, flavoring agents and the like can be used. In addition, in the oral liquid preparation, the carrier used for the preparation of the preparation includes sucrose fatty acid esters, polyoxyl stearate, polyoxyethylene polyoxypropylene glycols, surfactants such as polyoxyethylene monofatty acid esters, and synthetic agents. There are thickeners such as aluminum silicate, magnesium silicate, magnesium carbonate, magnesium oxide and magnesium aluminate metasilicate, and pH adjusters for organic acid and inorganic acid such as citrate buffer and phosphate buffer. In addition, if necessary, a solubilizing agent, a buffer, a preservative, a flavor, a pigment, a sweetener, and the like can be used.
【００１４】[0014]
【発明の効果】本発明の風邪用組成物は、（Ａ）ナプロ
キセン、ジクロフェナク、ケトプロフェン、イソプロピ
ルアンチピリン及びそれらの塩類から選ばれる１種又は
２種以上及び（Ｂ）ブロムヘキシン、アンブロキソール
及びそれらの塩類から選ばれる１種又は２種以上を配合
することにより、咳嗽症状に対し、強い鎮咳作用を有す
る組成物を提供することが可能となった。The cold composition of the present invention comprises (A) one or more selected from naproxen, diclofenac, ketoprofen, isopropylantipyrine and salts thereof, and (B) bromhexine, ambroxol and their salts. By combining one or more selected from salts, it has become possible to provide a composition having a strong antitussive action against cough symptoms.
【００１５】[0015]
【実施例】以下、実施例及び試験例を挙げ本発明をさら
に詳しく説明するが、本発明は下記の例に限定されるも
のではない。The present invention will be described in more detail with reference to the following examples and test examples, but the present invention is not limited to the following examples.
【００１６】実施例１ 下記の各成分の分量を秤量し、均一に混合した後、得ら
れた混合粉末を直打法により１錠重量１００ｍｇになる
ように打錠し、錠剤４０００個を得た。Example 1 The following components were weighed and uniformly mixed, and then the resulting mixed powder was tableted by a direct compression method to a weight of 100 mg per tablet to obtain 4000 tablets. .
【００１７】 ケトプロフェン １５０ｇ マレイン酸カルビノキサミン ７.５ｇ リン酸ジヒドロコデイン ２４ｇ 塩酸アンブロキソール ４５ｇ 塩化リゾチーム ９０ｇ（力価） 乳糖 ３５ｇ 低置換度ヒドロキシプロピルセルロース ２５.５ｇ ステアリン酸マグネシウム １５ｇ 硬化ヒマシ油 ８ｇ。Ketoprofen 150 g Carbinoxamine maleate 7.5 g Dihydrocodeine phosphate 24 g Ambroxol hydrochloride 45 g Lysozyme chloride 90 g (titer) Lactose 35 g Low substituted hydroxypropylcellulose 25.5 g Magnesium stearate 15 g Hardened castor oil 8 g.
【００１８】実施例２ 下記の各成分の分量を秤量し、均一に混合した後、実施
例１に準拠し２００ｍｇの錠剤９０００個を得た。Example 2 The following components were weighed and uniformly mixed, and 9000 tablets of 200 mg were obtained according to Example 1.
【００１９】 ジクロフェナクナトリウム ７５ｇ ノスカピン ４８ｇ リン酸ジヒドロコデイン ２４ｇ メキタジン ６ｇ 塩酸ブロムヘキシン １２ｇ 塩化リゾチーム ９０ｇ（力価） 乳糖 ７７５ｇ 微結晶セルロース ７５０ｇ ステアリン酸マグネシウム １０ｇ 硬化ヒマシ油 １０ｇ。Diclofenac sodium 75 g Noscapine 48 g Dihydrocodeine phosphate 24 g Mequitadine 6 g Bromhexine hydrochloride 12 g Lysozyme chloride 90 g (titer) Lactose 775 g Microcrystalline cellulose 750 g Magnesium stearate 10 g Hardened castor oil 10 g
【００２０】実施例３ 下記の各成分の分量を秤量し、均一に混合した後、実施
例１に準拠し２００ｍｇの錠剤９０００個を得た。Example 3 The following components were weighed and uniformly mixed, and 9000 tablets of 200 mg were obtained according to Example 1.
【００２１】 ナプロキセン ６００ｇ ノスカピン ４８ｇ リン酸ジヒドロコデイン ２４ｇ メキタジン ６ｇ 塩酸アンブロキソール ４５ｇ フェニルプロパノールアミン ６０ｇ テオフィリン １５０ｇ 塩化リゾチーム ９０ｇ（力価） 無水カフェイン ７５ｇ ビタミンＢ1硝酸塩 ８ｇ ビタミンＢ2 ４ｇ 乳糖 ３５０ｇ 微結晶セルロース ３２０ｇ ステアリン酸マグネシウム １０ｇ 硬化ヒマシ油 １０ｇ。[0021] Naproxen 600g noscapine 48g phosphoric acid dihydrocodeine 24g mequitazine 6g ambroxol hydrochloride 45g phenylpropanolamine 60g theophylline 150g Lysozyme chloride 90 g (potency) of anhydrous caffeine 75g Vitamin B 1 nitrate 8g vitamin B 2 4g Lactose 350g Microcrystalline cellulose 320g Magnesium stearate 10 g Hardened castor oil 10 g.
【００２２】実施例４ ｐＨ調整剤(リン酸緩衝液)を溶解した水溶液に、防腐
剤，甘味剤，香料を加え完全に溶解し、その溶液にショ
糖脂肪酸エステルを均一に分散した後、ナプロキセン及
びその他の薬剤を加え溶解させた後、精製水を加えて全
量を１０００ｍｌにして製した。Example 4 Preservatives, sweeteners and flavors were added to an aqueous solution in which a pH adjuster (phosphate buffer) was dissolved and completely dissolved, and the sucrose fatty acid ester was uniformly dispersed in the solution. Then, after adding and dissolving other drugs, purified water was added to make the total volume 1000 ml.
【００２３】 ナプロキセン イソプロピルアンチピリン ３００ｇ リン酸ジヒドロコデイン ２４ｇ メキタジン ６ｇ ｄｌ−塩酸メチルエフェドリン ６０ｇ 塩酸アンブロキソール ４５ｇ 無水カフェイン ７５ｇ ビタミンＢ1硝酸塩 ８ｇ ビタミンＢ2 ４ｇ ショ糖脂肪酸エステル １５ｇ 甘味剤 適 量 防腐剤 適 量 香料 適 量。Naproxen Isopropylantipyrine 300 g Dihydrocodeine phosphate 24 g Mequitazine 6 g dl-methylephedrine hydrochloride 60 g Ambroxol hydrochloride 45 g Anhydrous caffeine 75 g Vitamin B 1 nitrate 8 g Vitamin B 2 4 g Sucrose fatty acid ester 15 g Sweetener Preservative Preservative Preservative Fragrance appropriate amount.
【００２４】試験例１ 〔咳嗽症状に対する作用〕 《試験方法》宮田ら（和漢医薬学会誌；7,215,1990）の
方法を参考にして、ｄｄＹ系雄性ラットを用い、大気に
亜硫酸ガスを２．０％混合し、その気体中に５秒間暴露
して急性気管支炎病態を惹起し、発生した咳嗽反応の１
分間の回数の抑制の有無を指標に評価した。Test Example 1 [Action for Cough Symptoms] << Test Method >> Referring to the method of Miyata et al. %, And exposed to the gas for 5 seconds to cause acute bronchitis pathology.
The presence or absence of suppression of the number of minutes was evaluated as an index.
【００２５】比較した薬剤は、表１に示す１４群であ
り、各群（５匹）とも気体暴露３０分前に薬剤３ｍｌを
経口投与した。なお、コントロール群には、精製水３ｍ
ｌを与えた。The compared drugs were 14 groups shown in Table 1. Each group (5 animals) was orally administered 3 ml of the drug 30 minutes before gas exposure. The control group had 3 m of purified water.
l.
【００２６】[0026]
【表１】 [Table 1]
【００２７】《結果》結果を表２に示す。ｄｄＹ系雄性
ラットによる咳嗽反応に対する抑制作用は、Ａ〜Ｈ群に
優れた効果があることが証明された。<< Results >> The results are shown in Table 2. It was proved that the group A to H had an excellent inhibitory effect on the coughing reaction by male ddY rats.
【００２８】[0028]
【表２】 [Table 2]
【００２９】[0029]
フロントページの続き Ｆターム(参考） 4C086 AA01 AA02 BC36 MA02 MA04 MA08 MA09 MA10 NA14 ZA63 ZB33 4C206 AA01 AA02 DA23 DA25 FA29 FA31 FA33 MA02 MA03 MA04 MA14 NA14 ZA63 ZB33 Continued on the front page F term (reference) 4C086 AA01 AA02 BC36 MA02 MA04 MA08 MA09 MA10 NA14 ZA63 ZB33 4C206 AA01 AA02 DA23 DA25 FA29 FA31 FA33 MA02 MA03 MA04 MA14 NA14 ZA63 ZB33
Claims (1)
トプロフェン、イソプロピルアンチピリン及びそれらの
塩類から選ばれる１種又は２種以上及び（Ｂ）ブロムヘ
キシン、アンブロキソール及びそれらの塩類から選ばれ
る１種又は２種以上を配合する風邪用組成物。(1) one or more selected from (A) naproxen, diclofenac, ketoprofen, isopropylantipyrine and salts thereof, and (B) one or two selected from bromhexine, ambroxol and salts thereof A composition for a cold comprising the above.
Priority Applications (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| JP10247905A JP2000080034A (en) | 1998-09-02 | 1998-09-02 | Composition for cold |
Applications Claiming Priority (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| JP10247905A JP2000080034A (en) | 1998-09-02 | 1998-09-02 | Composition for cold |
Publications (1)
| Publication Number | Publication Date |
|---|---|
| JP2000080034A true JP2000080034A (en) | 2000-03-21 |
Family
ID=17170312
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP10247905A Pending JP2000080034A (en) | 1998-09-02 | 1998-09-02 | Composition for cold |
Country Status (1)
| Country | Link |
|---|---|
| JP (1) | JP2000080034A (en) |
Cited By (5)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| WO2003061642A1 (en) * | 2002-01-25 | 2003-07-31 | Boehringer Ingelheim Pharma Gmbh & Co Kg | Use of ambroxol in the treatment of chronic pains, cerebral excitotoxicity-related disorders and cardiac arrhythmias |
| WO2005007146A1 (en) * | 2003-07-16 | 2005-01-27 | Boehringer Ingelheim International Gmbh | Ambroxol for treating chronic nociceptive pains |
| JP2009513551A (en) * | 2003-07-16 | 2009-04-02 | ベーリンガー インゲルハイム インターナショナル ゲゼルシャフト ミット ベシュレンクテル ハフツング | Ambroxol for the treatment of acute pain |
| DE102011111944A1 (en) * | 2011-08-29 | 2013-02-28 | Richard A. Huthmacher | Use of diclofenac for the prevention and treatment of influenza infections as well as disease symptoms caused by influenza infections |
| JP2018076306A (en) * | 2016-10-31 | 2018-05-17 | エスエス製薬株式会社 | Cold remedy |
-
1998
- 1998-09-02 JP JP10247905A patent/JP2000080034A/en active Pending
Cited By (9)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| WO2003061642A1 (en) * | 2002-01-25 | 2003-07-31 | Boehringer Ingelheim Pharma Gmbh & Co Kg | Use of ambroxol in the treatment of chronic pains, cerebral excitotoxicity-related disorders and cardiac arrhythmias |
| JP2005526713A (en) * | 2002-01-25 | 2005-09-08 | ベーリンガー インゲルハイム ファルマ ゲゼルシャフト ミット ベシュレンクテル ハフツング ウント コンパニー コマンディトゲゼルシャフト | Use of ambroxol for the treatment of chronic pain, excitotoxic brain disorders and cardiac arrhythmias |
| WO2005007146A1 (en) * | 2003-07-16 | 2005-01-27 | Boehringer Ingelheim International Gmbh | Ambroxol for treating chronic nociceptive pains |
| JP2009513550A (en) * | 2003-07-16 | 2009-04-02 | ベーリンガー インゲルハイム インターナショナル ゲゼルシャフト ミット ベシュレンクテル ハフツング | Ambroxol for the treatment of chronic nociceptive pain |
| JP2009513551A (en) * | 2003-07-16 | 2009-04-02 | ベーリンガー インゲルハイム インターナショナル ゲゼルシャフト ミット ベシュレンクテル ハフツング | Ambroxol for the treatment of acute pain |
| DE102011111944A1 (en) * | 2011-08-29 | 2013-02-28 | Richard A. Huthmacher | Use of diclofenac for the prevention and treatment of influenza infections as well as disease symptoms caused by influenza infections |
| WO2013030058A1 (en) | 2011-08-29 | 2013-03-07 | Huthmacher Richard A | Use of diclofenac |
| JP2018076306A (en) * | 2016-10-31 | 2018-05-17 | エスエス製薬株式会社 | Cold remedy |
| JP7163014B2 (en) | 2016-10-31 | 2022-10-31 | エスエス製薬株式会社 | cold medicine |
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