JP2001172175A - Composition for the cold - Google Patents
Composition for the coldInfo
- Publication number
- JP2001172175A JP2001172175A JP35455199A JP35455199A JP2001172175A JP 2001172175 A JP2001172175 A JP 2001172175A JP 35455199 A JP35455199 A JP 35455199A JP 35455199 A JP35455199 A JP 35455199A JP 2001172175 A JP2001172175 A JP 2001172175A
- Authority
- JP
- Japan
- Prior art keywords
- cold
- composition
- salt
- loxoprofen
- drug
- 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.)
- Withdrawn
Links
- 239000000203 mixture Substances 0.000 title claims abstract description 13
- 150000003839 salts Chemical class 0.000 claims abstract description 11
- 229960002373 loxoprofen Drugs 0.000 claims abstract description 10
- BAZQYVYVKYOAGO-UHFFFAOYSA-M loxoprofen sodium hydrate Chemical compound O.O.[Na+].C1=CC(C(C([O-])=O)C)=CC=C1CC1C(=O)CCC1 BAZQYVYVKYOAGO-UHFFFAOYSA-M 0.000 claims abstract description 10
- 239000003172 expectorant agent Substances 0.000 claims abstract description 6
- 230000003419 expectorant effect Effects 0.000 claims abstract description 6
- 229960005174 ambroxol Drugs 0.000 claims description 4
- 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 description 4
- OJGDCBLYJGHCIH-UHFFFAOYSA-N bromhexine Chemical group C1CCCCC1N(C)CC1=CC(Br)=CC(Br)=C1N OJGDCBLYJGHCIH-UHFFFAOYSA-N 0.000 claims description 3
- 229960003870 bromhexine Drugs 0.000 claims description 3
- 208000011580 syndromic disease Diseases 0.000 abstract description 5
- 230000000294 tussive effect Effects 0.000 abstract 1
- 206010011224 Cough Diseases 0.000 description 12
- 229940079593 drug Drugs 0.000 description 10
- 239000003814 drug Substances 0.000 description 10
- HQKMJHAJHXVSDF-UHFFFAOYSA-L magnesium stearate Chemical compound [Mg+2].CCCCCCCCCCCCCCCCCC([O-])=O.CCCCCCCCCCCCCCCCCC([O-])=O HQKMJHAJHXVSDF-UHFFFAOYSA-L 0.000 description 8
- 208000024891 symptom Diseases 0.000 description 8
- -1 chewables Substances 0.000 description 6
- 238000002360 preparation method Methods 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
- 230000000694 effects Effects 0.000 description 5
- YKPUWZUDDOIDPM-SOFGYWHQSA-N capsaicin Chemical compound COC1=CC(CNC(=O)CCCC\C=C\C(C)C)=CC=C1O YKPUWZUDDOIDPM-SOFGYWHQSA-N 0.000 description 4
- 239000004359 castor oil Substances 0.000 description 4
- 235000019438 castor oil Nutrition 0.000 description 4
- 235000014113 dietary fatty acids Nutrition 0.000 description 4
- 229960000920 dihydrocodeine Drugs 0.000 description 4
- RBOXVHNMENFORY-DNJOTXNNSA-N dihydrocodeine Chemical compound C([C@H]1[C@H](N(CC[C@@]112)C)C3)C[C@H](O)[C@@H]1OC1=C2C3=CC=C1OC RBOXVHNMENFORY-DNJOTXNNSA-N 0.000 description 4
- 239000000194 fatty acid Substances 0.000 description 4
- 229930195729 fatty acid Natural products 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
- 235000019359 magnesium stearate Nutrition 0.000 description 4
- 239000003755 preservative agent Substances 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
- 229960000985 ambroxol hydrochloride Drugs 0.000 description 3
- 238000006243 chemical reaction Methods 0.000 description 3
- 235000019634 flavors Nutrition 0.000 description 3
- 235000003599 food sweetener Nutrition 0.000 description 3
- 239000008101 lactose Substances 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
- 230000002335 preservative effect Effects 0.000 description 3
- 239000008213 purified water Substances 0.000 description 3
- 239000005720 sucrose Substances 0.000 description 3
- 230000001629 suppression Effects 0.000 description 3
- 239000003765 sweetening agent Substances 0.000 description 3
- 238000012360 testing method Methods 0.000 description 3
- XLYOFNOQVPJJNP-UHFFFAOYSA-N water Chemical compound O XLYOFNOQVPJJNP-UHFFFAOYSA-N 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
- 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
- NIXOWILDQLNWCW-UHFFFAOYSA-N acrylic acid group Chemical group C(C=C)(=O)O NIXOWILDQLNWCW-UHFFFAOYSA-N 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
- 229960002504 capsaicin Drugs 0.000 description 2
- 235000017663 capsaicin Nutrition 0.000 description 2
- 229940066493 expectorants Drugs 0.000 description 2
- 238000009472 formulation Methods 0.000 description 2
- 239000008187 granular material Substances 0.000 description 2
- 238000011597 hartley guinea pig Methods 0.000 description 2
- 239000007788 liquid Substances 0.000 description 2
- 229940031703 low substituted hydroxypropyl 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
- 239000000820 nonprescription drug Substances 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
- 239000000243 solution 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
- VTYYLEPIZMXCLO-UHFFFAOYSA-L Calcium carbonate Chemical class [Ca+2].[O-]C([O-])=O VTYYLEPIZMXCLO-UHFFFAOYSA-L 0.000 description 1
- 241000700198 Cavia Species 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
- 229920002153 Hydroxypropyl cellulose Polymers 0.000 description 1
- 229930195725 Mannitol Natural products 0.000 description 1
- 241001465754 Metazoa Species 0.000 description 1
- 229920000168 Microcrystalline cellulose Polymers 0.000 description 1
- CMWTZPSULFXXJA-UHFFFAOYSA-N Naproxen Natural products C1=C(C(C)C(O)=O)C=CC2=CC(OC)=CC=C21 CMWTZPSULFXXJA-UHFFFAOYSA-N 0.000 description 1
- 229920003171 Poly (ethylene oxide) Polymers 0.000 description 1
- 229920002675 Polyoxyl Polymers 0.000 description 1
- 206010036790 Productive cough Diseases 0.000 description 1
- 206010037660 Pyrexia 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
- 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
- WMGSQTMJHBYJMQ-UHFFFAOYSA-N aluminum;magnesium;silicate Chemical compound [Mg+2].[Al+3].[O-][Si]([O-])([O-])[O-] WMGSQTMJHBYJMQ-UHFFFAOYSA-N 0.000 description 1
- 239000002269 analeptic agent Substances 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
- 230000003266 anti-allergic effect Effects 0.000 description 1
- 230000001078 anti-cholinergic effect Effects 0.000 description 1
- 230000001387 anti-histamine Effects 0.000 description 1
- 230000003110 anti-inflammatory effect Effects 0.000 description 1
- 239000000739 antihistaminic agent Substances 0.000 description 1
- 229940124584 antitussives Drugs 0.000 description 1
- 239000007864 aqueous solution Substances 0.000 description 1
- 208000006673 asthma Diseases 0.000 description 1
- 239000011230 binding agent Substances 0.000 description 1
- 229960002335 bromhexine hydrochloride Drugs 0.000 description 1
- 229940124630 bronchodilator Drugs 0.000 description 1
- 239000000872 buffer Substances 0.000 description 1
- 239000002775 capsule 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
- 239000003795 chemical substances by application Substances 0.000 description 1
- 230000001886 ciliary effect Effects 0.000 description 1
- 239000007979 citrate buffer Substances 0.000 description 1
- 230000000052 comparative effect Effects 0.000 description 1
- 238000013329 compounding Methods 0.000 description 1
- 238000007796 conventional method Methods 0.000 description 1
- 238000011161 development Methods 0.000 description 1
- PCHPORCSPXIHLZ-UHFFFAOYSA-N diphenhydramine hydrochloride Chemical compound [Cl-].C=1C=CC=CC=1C(OCC[NH+](C)C)C1=CC=CC=C1 PCHPORCSPXIHLZ-UHFFFAOYSA-N 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
- 239000003651 drinking water Substances 0.000 description 1
- 235000020188 drinking water Nutrition 0.000 description 1
- 230000008030 elimination Effects 0.000 description 1
- 238000003379 elimination reaction Methods 0.000 description 1
- 229940088598 enzyme Drugs 0.000 description 1
- WHWZLSFABNNENI-UHFFFAOYSA-N epinastine Chemical compound C1C2=CC=CC=C2C2CN=C(N)N2C2=CC=CC=C21 WHWZLSFABNNENI-UHFFFAOYSA-N 0.000 description 1
- 229960002548 epinastine hydrochloride Drugs 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
- 238000011156 evaluation Methods 0.000 description 1
- 238000002474 experimental method Methods 0.000 description 1
- 239000012530 fluid Substances 0.000 description 1
- 239000004088 foaming agent Substances 0.000 description 1
- 235000013355 food flavoring agent Nutrition 0.000 description 1
- XGVJWXAYKUHDOO-UHFFFAOYSA-N galanthidine Natural products C1CN2CC3=CC=4OCOC=4C=C3C3C2C1=CC(O)C3O XGVJWXAYKUHDOO-UHFFFAOYSA-N 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
- 235000015110 jellies Nutrition 0.000 description 1
- 229960003630 ketotifen fumarate Drugs 0.000 description 1
- YNQQEYBLVYAWNX-WLHGVMLRSA-N ketotifen fumarate Chemical compound OC(=O)\C=C\C(O)=O.C1CN(C)CCC1=C1C2=CC=CC=C2CC(=O)C2=C1C=CS2 YNQQEYBLVYAWNX-WLHGVMLRSA-N 0.000 description 1
- 239000000314 lubricant Substances 0.000 description 1
- XGVJWXAYKUHDOO-DANNLKNASA-N lycorine Chemical compound C1CN2CC3=CC=4OCOC=4C=C3[C@H]3[C@H]2C1=C[C@H](O)[C@H]3O XGVJWXAYKUHDOO-DANNLKNASA-N 0.000 description 1
- KQAOMBGKIWRWNA-UHFFFAOYSA-N lycorine Natural products OC1C=C2CCN3C2C(C1O)c4cc5OCOc5cc34 KQAOMBGKIWRWNA-UHFFFAOYSA-N 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
- 238000000034 method Methods 0.000 description 1
- 235000019813 microcrystalline cellulose Nutrition 0.000 description 1
- 239000008108 microcrystalline cellulose Substances 0.000 description 1
- 229940016286 microcrystalline cellulose Drugs 0.000 description 1
- 150000007522 mineralic acids Chemical class 0.000 description 1
- 239000011812 mixed powder Substances 0.000 description 1
- 210000004400 mucous membrane Anatomy 0.000 description 1
- 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 description 1
- 229960002009 naproxen Drugs 0.000 description 1
- 239000006199 nebulizer Substances 0.000 description 1
- 239000000041 non-steroidal anti-inflammatory agent Substances 0.000 description 1
- 229940021182 non-steroidal anti-inflammatory drug Drugs 0.000 description 1
- QIQXTHQIDYTFRH-UHFFFAOYSA-N octadecanoic acid Chemical compound CCCCCCCCCCCCCCCCCC(O)=O QIQXTHQIDYTFRH-UHFFFAOYSA-N 0.000 description 1
- 150000007524 organic acids Chemical class 0.000 description 1
- 239000003002 pH adjusting agent Substances 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
- 239000000843 powder Substances 0.000 description 1
- 239000001397 quillaja saponaria molina bark Substances 0.000 description 1
- 230000011514 reflex Effects 0.000 description 1
- 210000002345 respiratory system Anatomy 0.000 description 1
- 239000000837 restrainer Substances 0.000 description 1
- 229930182490 saponin Natural products 0.000 description 1
- 150000007949 saponins Chemical class 0.000 description 1
- 230000028327 secretion Effects 0.000 description 1
- 239000007787 solid Substances 0.000 description 1
- 239000002904 solvent Substances 0.000 description 1
- 208000024794 sputum Diseases 0.000 description 1
- 210000003802 sputum Anatomy 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
- 239000004094 surface-active agent Substances 0.000 description 1
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- 239000003826 tablet Substances 0.000 description 1
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- 239000011782 vitamin Substances 0.000 description 1
- 229930003231 vitamin Natural products 0.000 description 1
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Landscapes
- Acyclic And Carbocyclic Compounds In Medicinal Compositions (AREA)
Abstract
Description
【0001】[0001]
【産業上の利用分野】本発明は、風邪による諸症状のう
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 coughing among various symptoms caused by colds.
【0002】[0002]
【従来の技術】風邪症候群は、発熱、痛み、各粘膜の腫
脹等をもたらし、実際の日常生活に大きな障害と社会経
済上の損失を与えている。2. Description of the Related Art The cold syndrome causes fever, pain, swelling of mucous membranes, etc., and causes serious obstacles to actual daily life and social and economic losses.
【0003】風邪の諸症状を除去或いは軽減するかが現
実の治療上の重要なポイントとなっている。殊に、一般
用医薬品(OTC)の分野においては、如何に効果的に
風邪の諸症状を除去等するかが薬剤(風邪用組成物)開
発のポイントとなっている。[0003] Eliminating or alleviating the symptoms of colds is an important therapeutic point. In particular, in the field of over-the-counter medicines (OTC), how to effectively eliminate various symptoms of colds, etc., has become a point of drug (cold composition) development.
【0004】[0004]
【発明が解決しようとする課題】本発明の目的は、咳嗽
症状の除去あるいは軽減された風邪用組成物を提供する
ことにある。SUMMARY OF THE INVENTION It is an object of the present invention to provide a composition for colds in which cough symptoms are eliminated or reduced.
【0005】[0005]
【課題を解決するための手段】本発明者らは、上記目的
を達成するべく研究を重ねた結果、去痰薬にロキソプロ
フェンを配合することにより、咳嗽症状の除去・軽減に
対し劇的な効果があることを見いだし、発明を完成し
た。Means for Solving the Problems As a result of repeated studies to achieve the above object, the present inventors have found that the addition of loxoprofen to expectorants has a dramatic effect on the elimination and reduction of cough symptoms. He found something and completed the invention.
【0006】すなわち、本発明は、去痰薬、および、ロ
キソプロフェンまたはその塩類を配合することを特徴と
する風邪用組成物である。[0006] That is, the present invention is a cold composition comprising an expectorant and loxoprofen or a salt thereof.
【0007】本発明において去痰薬とは、風邪症候群、
喘息等の際に呼吸器から分泌される過剰な粘性の気道液
に対して、分泌を止めるかまたは粘度を下げるかまたは
気道の線毛運動を促進するか等の作用により、喀痰を抑
える薬剤をいい、例えば、ブロムヘキシン、アンブロキ
ソール、リコリン、サポニンなどを挙げることができ
る。In the present invention, expectorants include cold syndrome,
For drugs with excessive viscous airway fluid secreted from the respiratory tract during asthma, etc., drugs that suppress sputum by acting to stop secretion, reduce viscosity, or promote airway ciliary movement, etc. For example, bromhexine, ambroxol, lycorine, saponin and the like can be mentioned.
【0008】咳嗽症状の除去・軽減の点で優れた配合量
は、それぞれ成人に対して1日当たり、ロキソプロフェ
ンまたはその塩類は15〜225mgがよく、好ましく
は30〜200mgがよく、ブロムヘキシンまたはその
塩類は3〜30mgがよく、好ましくは6〜24mgが
よく、アンブロキソールまたはその塩類は15〜75m
gがよく、好ましくは22.5〜50mgがよい。[0008] The amount of loxoprofen or a salt thereof is preferably 15 to 225 mg, preferably 30 to 200 mg, and more preferably 30 to 200 mg, and bromhexine or a salt thereof per day for adults. The amount is preferably 3 to 30 mg, more preferably 6 to 24 mg, and the amount of ambroxol or a salt thereof is 15 to 75 m.
g is good, and preferably 22.5 to 50 mg.
【0009】咳嗽症状の除去・軽減の点で優れた配合比
は、それぞれ成人に対して1日当たり、ロキソプロフェ
ンまたはその塩類1重量部に対し、ブロムヘキシンまた
はその塩類は0.01〜2重量部がよく、好ましくは
0.03〜0.8重量部がよく、アンブロキソールまた
はその塩類は0.06〜5重量部がよく、好ましくは
0.12〜1.7重量部がよい。An excellent compounding ratio in terms of eliminating and reducing cough symptoms is that loxoprofen or a salt thereof is preferably 1 to 1 part by weight of bromohexine or a salt thereof in an amount of 0.01 to 2 parts by weight per day for an adult. The amount is preferably 0.03 to 0.8 parts by weight, and the amount of ambroxol or a salt thereof is preferably 0.06 to 5 parts by weight, more preferably 0.12 to 1.7 parts by weight.
【0010】本発明の風邪用組成物は、必要に応じて非
ステロイド性抗炎症薬、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
配合しても良い。[0010] The cold composition of the present invention may contain a nonsteroidal anti-inflammatory drug, an anti-inflammatory enzyme drug, a bronchodilator,
A central nervous system stimulant, an antitussive, an antihistamine or an antiallergic, an anticholinergic, a vitamin, an antacid, a crude drug and the like may be added.
【0011】本発明の風邪用組成物は、剤型として錠
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、ゼリー剤、内服液剤等の経口投与形態の製剤として
用いる。The composition for a cold of the present invention may be in the form of tablets, capsules, granules, fine granules, powders, chewables, foaming agents, drops, dissolving agents in the mouth, dry syrups, jellies, oral liquids. And so on.
【0012】これらの製剤は、常法により調製すること
ができる。固形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。These preparations can be prepared by a conventional method. In solid preparations, carriers used for preparation of the preparation 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, and lubricants such as magnesium stearate, hydrogenated castor oil, and talc. , Preservatives, flavors, pigments, flavoring agents and the like can be used.
【0013】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。[0013] In the oral liquid preparation, the carrier used for preparing the preparation includes surfactants such as sucrose fatty acid esters, polyoxyl stearate, polyoxyethylene polyoxypropylene glycols and polyoxyethylene mono fatty acid esters; There are thickeners such as synthetic aluminum silicate, magnesium silicate, magnesium carbonate, magnesium oxide and magnesium aluminate metasilicate, and organic acid and inorganic acid pH adjusters such as citrate buffer and phosphate buffer. In addition, if necessary, a solubilizer, a buffer, a preservative, a flavor, a pigment, a sweetener, and the like can be used.
【0014】[0014]
【発明の効果】本発明は、咳嗽反応に対する作用が著し
く改善された結果、風邪症候群に対して著しく有用な薬
剤を提供することができた。According to the present invention, the effect on the cough reaction is remarkably improved, and as a result, a drug which is extremely useful for the cold syndrome can be provided.
【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、錠剤を得た。 ロキソプロフェンナトリウム 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。Example 1 The following components were weighed and uniformly mixed, and the resulting mixed powder was tableted by a direct compression method to a tablet weight of 100 mg to obtain tablets. Loxoprofen sodium 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.
【0017】実施例2 下記の各成分を秤量し均一に混合した後、実施例1に準
拠し200mgの錠剤を得た。 ロキソプロフェンナトリウム 180g ノスカピン 48g リン酸ジヒドロコデイン 24g 塩酸ブロムヘキシン 12g 塩化リゾチーム 90g(力価) 乳糖 720g 微結晶セルロース 700g ステアリン酸マグネシウム 13g 硬化ヒマシ油 13g。Example 2 The following components were weighed and uniformly mixed, and a tablet of 200 mg was obtained according to Example 1. Loxoprofen sodium 180 g noscapine 48 g dihydrocodeine phosphate 24 g bromhexine hydrochloride 12 g lysozyme chloride 90 g (titer) lactose 720 g microcrystalline cellulose 700 g magnesium stearate 13 g hardened castor oil 13 g.
【0018】実施例3 下記の各成分を秤量し均一に混合した後、実施例1に準
拠し200mgの錠剤を得た。 ロキソプロフェンナトリウム 150g ノスカピン 48g リン酸ジヒドロコデイン 24g フマル酸ケトチフェン 2g 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 150g 微結晶セルロース 150g ステアリン酸マグネシウム 22g 硬化ヒマシ油 22g。Example 3 The following components were weighed and uniformly mixed, and a tablet of 200 mg was obtained according to Example 1. Loxoprofen sodium 150 g Noscapine 48 g Dihydrocodeine phosphate 24 g Ketotifen fumarate 2 g Ambroxol hydrochloride 45 g Phenylpropanolamine 60 g Theophylline 150 g Lysozyme chloride 90 g (Titer) Anhydrous caffeine 75 g Vitamin B 1 nitrate 8 g Vitamin B 2 4 g Milk sugar Magnesium stearate 22 g Hardened castor oil 22 g.
【0019】実施例4 pH調整剤(リン酸緩衝液pH4.5)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。 ロキソプロフェンナトリウム 100g リン酸ジヒドロコデイン 24g 塩酸エピナスチン 20g 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。Example 4 A preservative, a sweetener, and a flavor are added to an aqueous solution in which a pH adjuster (phosphate buffer, pH 4.5) is dissolved, and the solution is completely dissolved. The sucrose fatty acid ester is uniformly dispersed in the solution. Thereafter, naproxen and other drugs were added and dissolved, and purified water was added to make the total amount to 1000 ml. Loxoprofen sodium 100 g dihydrocodeine phosphate 24 g epinastine hydrochloride 20 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 suitable amount preservative suitable amount .
【0020】試験例〔配合製剤の咳嗽症状に対する作
用〕 体重300〜400gのHartley系モルモットを
用い、室温24±1℃の環境下で飼料及び飲料水を自由
摂取させて予備飼育後に実験に供した。無麻酔のモルモ
ットをbody plethysmograph内に入
れた。body plethysmographは、頭
部と体部の二つの透明なアクリル製の円筒状box(約
1.2L)及び上下二つのゴム膜で覆ったアクリル製n
eck restrainerから構成されている。K
ohrogiらの方法(J.Clin.Invest.
82,2063〜2068(1988))に従い、容器
の全面上部からcapsaicinを超音波ネブライザ
ーTUR−3200,日本光電)により2分間噴霧し
(2.2mL/min)、咳の発現の有無,咳反射の強
さ及び頻度を調べた。咳嗽音をマイクロフォンで確認す
るとともに、密閉した体部用boxの内圧の変化をfl
ow meter(MEP−1100,日本光電)を介
してペンレコーダー上に記録した。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。なお、室
温は25℃に設定した。Test Example [Effects of Combination Formulation on Cough Symptoms] Using a Hartley guinea pig weighing 300 to 400 g, feed and drinking water were freely taken under an environment of room temperature 24 ± 1 ° C., and preliminarily reared and subjected to experiments. . Anesthetized guinea pigs were placed in a body plethysmograph. The body plethysmograph consists of two transparent acrylic cylindrical boxes (about 1.2 L) of the head and body, and an acrylic n covered with two upper and lower rubber films.
It consists of an eck restrainer. K
ohlogi et al. (J. Clin. Invest.
82, 2063-2068 (1988)), capsaicin is sprayed from the top of the entire surface of the container with an ultrasonic nebulizer (TUR-3200, Nippon Koden) for 2 minutes (2.2 mL / min), the presence or absence of coughing, cough reflex The strength and frequency were examined. The coughing sound was confirmed with a microphone, and the change in the internal pressure of the sealed body box was measured by fl.
Recording was performed on a pen recorder via an ow meter (MEP-1100, Nihon Kohden). The evaluation was made based on the presence or absence of suppression of the number of 1-minute cough reactions that occurred. The room temperature was set at 25 ° C.
【0021】比較した薬剤は、表1に示した処方を精製
水50mLに溶解したものを用いた。1群5匹で試験
し、各群ともcapsaicin暴露30分前に薬剤3
mLを経口投与した。(コントロール群は、精製水3m
Lを与えた。)As a comparative drug, one prepared by dissolving the formulation shown in Table 1 in 50 mL of purified water was used. Each group consisted of 5 animals, and each group was treated with drug 3 30 minutes before exposure to capsaicin.
mL was administered orally. (Control group is 3m of purified water
L was given. )
【0022】[0022]
【表1】 結果を表2に示す。Hartley系モルモットによる
咳嗽反応に対する抑制作用の程度はA,B群が優ってお
り、これらの群の薬剤に優れた効果があることが証明さ
れた。[Table 1] Table 2 shows the results. Groups A and B are superior in the degree of suppression of coughing reaction by Hartley guinea pigs, and it has been proved that drugs in these groups have excellent effects.
【0023】[0023]
【表2】試験結果 〔咳嗽症状の回数とコントロール群に対す
る抑制率〕 [Table 2] Test results [Number of cough symptoms and suppression rate for control group]
Claims (2)
その塩類を配合することを特徴とする風邪用組成物。1. A cold composition comprising an expectorant and loxoprofen or a salt thereof.
類、または、アンブロキソールもしくはその塩類である
請求項1記載の風邪用組成物。2. The composition according to claim 1, wherein the expectorant is bromhexine or a salt thereof, or ambroxol or a salt thereof.
Priority Applications (1)
Application Number | Priority Date | Filing Date | Title |
---|---|---|---|
JP35455199A JP2001172175A (en) | 1999-12-14 | 1999-12-14 | Composition for the cold |
Applications Claiming Priority (1)
Application Number | Priority Date | Filing Date | Title |
---|---|---|---|
JP35455199A JP2001172175A (en) | 1999-12-14 | 1999-12-14 | Composition for the cold |
Publications (1)
Publication Number | Publication Date |
---|---|
JP2001172175A true JP2001172175A (en) | 2001-06-26 |
Family
ID=18438322
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Application Number | Title | Priority Date | Filing Date |
---|---|---|---|
JP35455199A Withdrawn JP2001172175A (en) | 1999-12-14 | 1999-12-14 | Composition for the cold |
Country Status (1)
Country | Link |
---|---|
JP (1) | JP2001172175A (en) |
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