JP2000256186A - Composition for pharyngeal disease - Google Patents
Composition for pharyngeal diseaseInfo
- Publication number
- JP2000256186A JP2000256186A JP11058239A JP5823999A JP2000256186A JP 2000256186 A JP2000256186 A JP 2000256186A JP 11058239 A JP11058239 A JP 11058239A JP 5823999 A JP5823999 A JP 5823999A JP 2000256186 A JP2000256186 A JP 2000256186A
- Authority
- JP
- Japan
- Prior art keywords
- composition
- pharyngeal
- quaternary ammonium
- ammonium salt
- cetylpyridinium chloride
- 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- Withdrawn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 24
- 208000023668 Pharyngeal disease Diseases 0.000 title claims abstract description 20
- 208000033420 disorder of pharynx Diseases 0.000 title abstract description 5
- PEDCQBHIVMGVHV-UHFFFAOYSA-N Glycerine Chemical compound OCC(O)CO PEDCQBHIVMGVHV-UHFFFAOYSA-N 0.000 claims abstract description 29
- 235000019410 glycyrrhizin Nutrition 0.000 claims abstract description 20
- XLYOFNOQVPJJNP-UHFFFAOYSA-N water Substances O XLYOFNOQVPJJNP-UHFFFAOYSA-N 0.000 claims abstract description 20
- 230000000844 anti-bacterial effect Effects 0.000 claims abstract description 16
- 150000003242 quaternary ammonium salts Chemical class 0.000 claims abstract description 15
- 229960001927 cetylpyridinium chloride Drugs 0.000 claims abstract description 13
- YMKDRGPMQRFJGP-UHFFFAOYSA-M cetylpyridinium chloride Chemical compound [Cl-].CCCCCCCCCCCCCCCC[N+]1=CC=CC=C1 YMKDRGPMQRFJGP-UHFFFAOYSA-M 0.000 claims abstract description 13
- 229960004949 glycyrrhizic acid Drugs 0.000 claims abstract description 12
- LPLVUJXQOOQHMX-QWBHMCJMSA-N glycyrrhizinic acid Chemical compound O([C@@H]1[C@@H](O)[C@H](O)[C@H](O[C@@H]1O[C@@H]1C([C@H]2[C@]([C@@H]3[C@@]([C@@]4(CC[C@@]5(C)CC[C@@](C)(C[C@H]5C4=CC3=O)C(O)=O)C)(C)CC2)(C)CC1)(C)C)C(O)=O)[C@@H]1O[C@H](C(O)=O)[C@@H](O)[C@H](O)[C@H]1O LPLVUJXQOOQHMX-QWBHMCJMSA-N 0.000 claims abstract description 12
- 150000003839 salts Chemical class 0.000 claims abstract description 8
- BIVBRWYINDPWKA-VLQRKCJKSA-L Glycyrrhizinate dipotassium Chemical compound [K+].[K+].O([C@@H]1[C@@H](O)[C@H](O)[C@H](O[C@@H]1O[C@H]1CC[C@]2(C)[C@H]3C(=O)C=C4[C@@H]5C[C@](C)(CC[C@@]5(CC[C@@]4(C)[C@]3(C)CC[C@H]2C1(C)C)C)C(O)=O)C([O-])=O)[C@@H]1O[C@H](C([O-])=O)[C@@H](O)[C@H](O)[C@H]1O BIVBRWYINDPWKA-VLQRKCJKSA-L 0.000 claims description 13
- 229940101029 dipotassium glycyrrhizinate Drugs 0.000 claims description 13
- 235000011187 glycerol Nutrition 0.000 claims description 13
- VTAJIXDZFCRWBR-UHFFFAOYSA-N Licoricesaponin B2 Natural products C1C(C2C(C3(CCC4(C)CCC(C)(CC4C3=CC2)C(O)=O)C)(C)CC2)(C)C2C(C)(C)CC1OC1OC(C(O)=O)C(O)C(O)C1OC1OC(C(O)=O)C(O)C(O)C1O VTAJIXDZFCRWBR-UHFFFAOYSA-N 0.000 claims description 11
- LPLVUJXQOOQHMX-UHFFFAOYSA-N glycyrrhetinic acid glycoside Natural products C1CC(C2C(C3(CCC4(C)CCC(C)(CC4C3=CC2=O)C(O)=O)C)(C)CC2)(C)C2C(C)(C)C1OC1OC(C(O)=O)C(O)C(O)C1OC1OC(C(O)=O)C(O)C(O)C1O LPLVUJXQOOQHMX-UHFFFAOYSA-N 0.000 claims description 11
- 239000001685 glycyrrhizic acid Substances 0.000 claims description 11
- UYRUBYNTXSDKQT-UHFFFAOYSA-N glycyrrhizic acid Natural products CC1(C)C(CCC2(C)C1CCC3(C)C2C(=O)C=C4C5CC(C)(CCC5(C)CCC34C)C(=O)O)OC6OC(C(O)C(O)C6OC7OC(O)C(O)C(O)C7C(=O)O)C(=O)O UYRUBYNTXSDKQT-UHFFFAOYSA-N 0.000 claims description 11
- 238000002360 preparation method Methods 0.000 claims description 10
- 229940069445 licorice extract Drugs 0.000 claims description 3
- KPQJOKRSYYJJEL-VLQRKCJKSA-K [Na+].[Na+].CC1(C)[C@H](CC[C@@]2(C)[C@H]1CC[C@]1(C)[C@@H]2C(=O)C=C2[C@@H]3C[C@](C)(CC[C@]3(C)CC[C@@]12C)C([O-])=O)O[C@H]1O[C@@H]([C@@H](O)[C@H](O)[C@H]1O[C@@H]1O[C@@H]([C@@H](O)[C@H](O)[C@H]1O)C([O-])=O)C([O-])=O Chemical compound [Na+].[Na+].CC1(C)[C@H](CC[C@@]2(C)[C@H]1CC[C@]1(C)[C@@H]2C(=O)C=C2[C@@H]3C[C@](C)(CC[C@]3(C)CC[C@@]12C)C([O-])=O)O[C@H]1O[C@@H]([C@@H](O)[C@H](O)[C@H]1O[C@@H]1O[C@@H]([C@@H](O)[C@H](O)[C@H]1O)C([O-])=O)C([O-])=O KPQJOKRSYYJJEL-VLQRKCJKSA-K 0.000 claims description 2
- SPPIIOPGDLITJE-VLQRKCJKSA-N diazanium;(2s,3s,4s,5r,6s)-6-[[(3s,4ar,6ar,6bs,8as,11s,12ar,14ar,14bs)-11-carboxylato-4,4,6a,6b,8a,11,14b-heptamethyl-14-oxo-2,3,4a,5,6,7,8,9,10,12,12a,14a-dodecahydro-1h-picen-3-yl]oxy]-5-[(2r,3r,4s,5s,6s)-6-carboxy-3,4,5-trihydroxyoxan-2-yl]oxy-3,4-dihy Chemical compound N.N.O([C@@H]1[C@@H](O)[C@H](O)[C@H](O[C@@H]1O[C@H]1CC[C@]2(C)[C@H]3C(=O)C=C4[C@@H]5C[C@](C)(CC[C@@]5(CC[C@@]4(C)[C@]3(C)CC[C@H]2C1(C)C)C)C(O)=O)C(O)=O)[C@@H]1O[C@H](C(O)=O)[C@@H](O)[C@H](O)[C@H]1O SPPIIOPGDLITJE-VLQRKCJKSA-N 0.000 claims description 2
- 238000013329 compounding Methods 0.000 claims 2
- 238000001556 precipitation Methods 0.000 abstract description 3
- 238000009472 formulation Methods 0.000 abstract 2
- LFQSCWFLJHTTHZ-UHFFFAOYSA-N Ethanol Chemical compound CCO LFQSCWFLJHTTHZ-UHFFFAOYSA-N 0.000 description 16
- 239000000243 solution Substances 0.000 description 9
- 230000000052 comparative effect Effects 0.000 description 8
- 239000008213 purified water Substances 0.000 description 8
- 239000002244 precipitate Substances 0.000 description 4
- DNIAPMSPPWPWGF-UHFFFAOYSA-N Propylene glycol Chemical compound CC(O)CO DNIAPMSPPWPWGF-UHFFFAOYSA-N 0.000 description 3
- HEMHJVSKTPXQMS-UHFFFAOYSA-M Sodium hydroxide Chemical compound [OH-].[Na+] HEMHJVSKTPXQMS-UHFFFAOYSA-M 0.000 description 3
- 239000003795 chemical substances by application Substances 0.000 description 3
- KRKNYBCHXYNGOX-UHFFFAOYSA-N citric acid Chemical compound OC(=O)CC(O)(C(O)=O)CC(O)=O KRKNYBCHXYNGOX-UHFFFAOYSA-N 0.000 description 3
- 238000007796 conventional method Methods 0.000 description 3
- 229940079593 drug Drugs 0.000 description 3
- 239000003814 drug Substances 0.000 description 3
- 238000002156 mixing Methods 0.000 description 3
- 239000007921 spray Substances 0.000 description 3
- PUPZLCDOIYMWBV-UHFFFAOYSA-N (+/-)-1,3-Butanediol Chemical compound CC(O)CCO PUPZLCDOIYMWBV-UHFFFAOYSA-N 0.000 description 2
- FBPFZTCFMRRESA-FSIIMWSLSA-N D-Glucitol Natural products OC[C@H](O)[C@H](O)[C@@H](O)[C@H](O)CO FBPFZTCFMRRESA-FSIIMWSLSA-N 0.000 description 2
- VEXZGXHMUGYJMC-UHFFFAOYSA-N Hydrochloric acid Chemical compound Cl VEXZGXHMUGYJMC-UHFFFAOYSA-N 0.000 description 2
- 206010061218 Inflammation Diseases 0.000 description 2
- 150000001298 alcohols Chemical class 0.000 description 2
- 230000015572 biosynthetic process Effects 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
- KCIDZIIHRGYJAE-YGFYJFDDSA-L dipotassium;[(2r,3r,4s,5r,6r)-3,4,5-trihydroxy-6-(hydroxymethyl)oxan-2-yl] phosphate Chemical compound [K+].[K+].OC[C@H]1O[C@H](OP([O-])([O-])=O)[C@H](O)[C@@H](O)[C@H]1O KCIDZIIHRGYJAE-YGFYJFDDSA-L 0.000 description 2
- 230000004054 inflammatory process Effects 0.000 description 2
- 239000007788 liquid Substances 0.000 description 2
- 229920001223 polyethylene glycol Polymers 0.000 description 2
- 239000000600 sorbitol Substances 0.000 description 2
- 150000005846 sugar alcohols Polymers 0.000 description 2
- BJEPYKJPYRNKOW-REOHCLBHSA-N (S)-malic acid Chemical compound OC(=O)[C@@H](O)CC(O)=O BJEPYKJPYRNKOW-REOHCLBHSA-N 0.000 description 1
- 229940058015 1,3-butylene glycol Drugs 0.000 description 1
- 241000894006 Bacteria Species 0.000 description 1
- 206010006326 Breath odour Diseases 0.000 description 1
- VEXZGXHMUGYJMC-UHFFFAOYSA-M Chloride anion Chemical compound [Cl-] VEXZGXHMUGYJMC-UHFFFAOYSA-M 0.000 description 1
- FBPFZTCFMRRESA-JGWLITMVSA-N D-glucitol Chemical compound OC[C@H](O)[C@@H](O)[C@H](O)[C@H](O)CO FBPFZTCFMRRESA-JGWLITMVSA-N 0.000 description 1
- FEWJPZIEWOKRBE-JCYAYHJZSA-N Dextrotartaric acid Chemical compound OC(=O)[C@H](O)[C@@H](O)C(O)=O FEWJPZIEWOKRBE-JCYAYHJZSA-N 0.000 description 1
- LYCAIKOWRPUZTN-UHFFFAOYSA-N Ethylene glycol Chemical compound OCCO LYCAIKOWRPUZTN-UHFFFAOYSA-N 0.000 description 1
- IAYPIBMASNFSPL-UHFFFAOYSA-N Ethylene oxide Chemical compound C1CO1 IAYPIBMASNFSPL-UHFFFAOYSA-N 0.000 description 1
- 241000202807 Glycyrrhiza Species 0.000 description 1
- 235000001453 Glycyrrhiza echinata Nutrition 0.000 description 1
- 235000006200 Glycyrrhiza glabra Nutrition 0.000 description 1
- 235000017382 Glycyrrhiza lepidota Nutrition 0.000 description 1
- LPHGQDQBBGAPDZ-UHFFFAOYSA-N Isocaffeine Natural products CN1C(=O)N(C)C(=O)C2=C1N(C)C=N2 LPHGQDQBBGAPDZ-UHFFFAOYSA-N 0.000 description 1
- 101000783705 Myxoma virus (strain Uriarra) Envelope protein A28 homolog Proteins 0.000 description 1
- 201000007100 Pharyngitis Diseases 0.000 description 1
- 239000002202 Polyethylene glycol Substances 0.000 description 1
- FEWJPZIEWOKRBE-UHFFFAOYSA-N Tartaric acid Natural products [H+].[H+].[O-]C(=O)C(O)C(O)C([O-])=O FEWJPZIEWOKRBE-UHFFFAOYSA-N 0.000 description 1
- BJEPYKJPYRNKOW-UHFFFAOYSA-N alpha-hydroxysuccinic acid Natural products OC(=O)C(O)CC(O)=O BJEPYKJPYRNKOW-UHFFFAOYSA-N 0.000 description 1
- 229940121363 anti-inflammatory agent Drugs 0.000 description 1
- 239000002260 anti-inflammatory agent Substances 0.000 description 1
- 230000001580 bacterial effect Effects 0.000 description 1
- 244000052616 bacterial pathogen Species 0.000 description 1
- 229960000686 benzalkonium chloride Drugs 0.000 description 1
- 229960001950 benzethonium chloride Drugs 0.000 description 1
- UREZNYTWGJKWBI-UHFFFAOYSA-M benzethonium chloride Chemical compound [Cl-].C1=CC(C(C)(C)CC(C)(C)C)=CC=C1OCCOCC[N+](C)(C)CC1=CC=CC=C1 UREZNYTWGJKWBI-UHFFFAOYSA-M 0.000 description 1
- CADWTSSKOVRVJC-UHFFFAOYSA-N benzyl(dimethyl)azanium;chloride Chemical compound [Cl-].C[NH+](C)CC1=CC=CC=C1 CADWTSSKOVRVJC-UHFFFAOYSA-N 0.000 description 1
- 235000019437 butane-1,3-diol Nutrition 0.000 description 1
- 229960001948 caffeine Drugs 0.000 description 1
- VJEONQKOZGKCAK-UHFFFAOYSA-N caffeine Natural products CN1C(=O)N(C)C(=O)C2=C1C=CN2C VJEONQKOZGKCAK-UHFFFAOYSA-N 0.000 description 1
- 239000010630 cinnamon oil Substances 0.000 description 1
- 235000015165 citric acid Nutrition 0.000 description 1
- 239000003086 colorant Substances 0.000 description 1
- 239000002826 coolant Substances 0.000 description 1
- 201000010099 disease Diseases 0.000 description 1
- 208000037265 diseases, disorders, signs and symptoms Diseases 0.000 description 1
- 238000011156 evaluation Methods 0.000 description 1
- 239000000796 flavoring agent Substances 0.000 description 1
- 235000013355 food flavoring agent Nutrition 0.000 description 1
- 235000003599 food sweetener Nutrition 0.000 description 1
- 239000003205 fragrance Substances 0.000 description 1
- 230000001771 impaired effect Effects 0.000 description 1
- 239000004615 ingredient Substances 0.000 description 1
- 230000003993 interaction Effects 0.000 description 1
- 229940010454 licorice Drugs 0.000 description 1
- 238000004811 liquid chromatography Methods 0.000 description 1
- 229960003511 macrogol Drugs 0.000 description 1
- 206010025482 malaise Diseases 0.000 description 1
- 239000001630 malic acid Substances 0.000 description 1
- 235000011090 malic acid Nutrition 0.000 description 1
- 238000000034 method Methods 0.000 description 1
- 239000011259 mixed solution Substances 0.000 description 1
- 239000003921 oil Substances 0.000 description 1
- 150000007524 organic acids Chemical class 0.000 description 1
- 229920000642 polymer Polymers 0.000 description 1
- 239000003755 preservative agent Substances 0.000 description 1
- 238000004062 sedimentation Methods 0.000 description 1
- 239000003381 stabilizer Substances 0.000 description 1
- 230000001954 sterilising effect Effects 0.000 description 1
- 238000004659 sterilization and disinfection Methods 0.000 description 1
- 208000003265 stomatitis Diseases 0.000 description 1
- 239000004094 surface-active agent Substances 0.000 description 1
- 239000003765 sweetening agent Substances 0.000 description 1
- 239000011975 tartaric acid Substances 0.000 description 1
- 235000002906 tartaric acid Nutrition 0.000 description 1
- 239000012085 test solution Substances 0.000 description 1
- 238000002560 therapeutic procedure Methods 0.000 description 1
- 206010044008 tonsillitis Diseases 0.000 description 1
- CCXAYLQLOLXXKE-DWJAGBRCSA-K trisodium;(2s,3s,4s,5r,6r)-6-[(2s,3r,4s,5s,6s)-2-[[(3s,4ar,6ar,6bs,8as,11s,12ar,14ar,14bs)-11-carboxylato-4,4,6a,6b,8a,11,14b-heptamethyl-14-oxo-2,3,4a,5,6,7,8,9,10,12,12a,14a-dodecahydro-1h-picen-3-yl]oxy]-6-carboxylato-4,5-dihydroxyoxan-3-yl]oxy-3,4,5-t Chemical compound [Na+].[Na+].[Na+].O([C@@H]1[C@@H](O)[C@H](O)[C@H](O[C@@H]1O[C@H]1CC[C@]2(C)[C@H]3C(=O)C=C4[C@@H]5C[C@](C)(CC[C@@]5(CC[C@@]4(C)[C@]3(C)CC[C@H]2C1(C)C)C)C([O-])=O)C([O-])=O)[C@@H]1O[C@H](C([O-])=O)[C@@H](O)[C@H](O)[C@H]1O CCXAYLQLOLXXKE-DWJAGBRCSA-K 0.000 description 1
Abstract
Description
【０００１】[0001]
【発明の属する技術分野】本発明は、咽頭疾患用組成物
に関し、更に詳しくは４級アンモニウム塩およびグリチ
ルリチン酸又はその塩類（以下グリチルリチン酸類と略
することもある）を配合した系において、良好な殺菌能
を保持し、製剤的に安定な咽頭疾患用組成物に関する。[0001] The present invention relates to a composition for pharyngeal diseases, and more particularly to a composition containing a quaternary ammonium salt and glycyrrhizic acid or a salt thereof (hereinafter sometimes abbreviated as glycyrrhizic acid). The present invention relates to a composition for pharyngeal diseases, which has a sterilizing ability and is pharmaceutically stable.
【０００２】[0002]
【従来の技術】咽頭疾患は、患部の細菌が増加すること
で引き起こされ、その治療には殺菌作用を有する４級ア
ンモニウム塩が用いられている。そこで、さらに抗炎症
剤のグリチルリチン酸又はその塩類で炎症を抑え、殺菌
作用を有する４級アンモニウム塩を配合し病原菌を死滅
させることは有用な治療方法であり、両薬剤を同時に配
合した製剤は咽頭疾患用剤として有用であると考えられ
る。ところがグリチルリチン酸又はその塩類に４級アン
モニウム塩を配合すると、相互作用を起こし、４級アン
モニウム塩の殺菌力は低下し、さらにグリチルリチン酸
類の含量も低下し、また経時的な沈殿生成も認めらる。
現在までに、両薬物を配合した製剤的に安定な咽頭疾患
用組成物は得られていない。2. Description of the Related Art Pharyngeal diseases are caused by an increase in the number of bacteria in the affected area, and quaternary ammonium salts having a bactericidal action are used for the treatment. Therefore, it is a useful therapeutic method to suppress inflammation with the anti-inflammatory agent glycyrrhizic acid or salts thereof and to kill germs by adding a quaternary ammonium salt having a bactericidal action. It is considered to be useful as an agent for diseases. However, when a quaternary ammonium salt is added to glycyrrhizic acid or a salt thereof, an interaction occurs, the bactericidal activity of the quaternary ammonium salt is reduced, the glycyrrhizic acid content is further reduced, and sedimentation with time is observed. .
To date, a pharmaceutically stable pharyngeal disease composition containing both drugs has not been obtained.
【０００３】[0003]
【発明が解決しようとする課題】本発明の目的は、４級
アンモニウム塩が殺菌能を保持し、グリチルリチン酸類
の含量低下がなく、経時的にも沈殿生成がない製剤的に
安定な咽頭疾患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 pharmaceutically acceptable solution for pharyngeal diseases in which a quaternary ammonium salt retains bactericidal activity, does not cause a decrease in the content of glycyrrhizic acids, and does not precipitate over time. It is to provide a composition.
【０００４】[0004]
【課題を解決するための手段】上記課題を解決するため
に種々検討を加えた結果、基剤としてグリセリンと水を
用い、且つ特定の割合に配合することにより、４級アン
モニウム塩の殺菌作用を保持し、グリチルリチン酸類の
含量低下がなく、経時的に沈殿生成を認めない安定な製
剤を見出し、本発明を完成した。即ち本発明は、（Ａ）
殺菌作用を有する４級アンモニウム塩、（Ｂ）グリチル
リチン酸又はその塩類、（Ｃ）製剤全量に対して１６．
０〜４０．０Ｗ／Ｖ％の水、および（Ｄ）製剤全量に対
して５０〜９０Ｗ／Ｖ％のグリセリンからなることを特
徴とする咽頭疾患用組成物、に関する。本発明におい
て、咽頭疾患用組成物とは、のどに直接噴霧あるいは塗
布して用いるものをいい、例えばストリーム剤、スプレ
ー剤として用いられる。As a result of various studies in order to solve the above-mentioned problems, the bactericidal action of quaternary ammonium salts is reduced by using glycerin and water as bases and mixing them in a specific ratio. The present invention was completed by finding a stable preparation which was maintained, did not decrease the content of glycyrrhizic acids, and did not show precipitation over time. That is, the present invention relates to (A)
15. a quaternary ammonium salt having a bactericidal action, (B) glycyrrhizic acid or salts thereof, (C) a total amount of the preparation.
A pharyngeal disease composition comprising: 0 to 40.0 W / V% water; and (D) 50 to 90 W / V% glycerin based on the total amount of the preparation. In the present invention, the composition for pharyngeal diseases refers to a composition which is directly sprayed or applied to the throat, and is used, for example, as a stream agent or a spray agent.
【０００５】[0005]
【発明の実施の形態】本発明において、殺菌作用を有す
る４級アンモニウム塩とは、塩化ベンザルコニウム、塩
化ベンゼトニウム、塩化デカリニウム又は塩化セチルピ
リジニウムをいい、好ましいものとして塩化セチルピリ
ジニウムを挙げることができる。４級アンモニウム塩の
配合量は製剤全量に対して０．００５〜２．５Ｗ／Ｖ％
が好ましく、さらに０．０１〜０．３Ｗ／Ｖ％がより好
ましい。BEST MODE FOR CARRYING OUT THE INVENTION In the present invention, a quaternary ammonium salt having a bactericidal action refers to benzalkonium chloride, benzethonium chloride, decalinium chloride or cetylpyridinium chloride, and preferred is cetylpyridinium chloride. . The amount of the quaternary ammonium salt is 0.005 to 2.5 W / V% based on the total amount of the preparation.
Is preferable, and 0.01 to 0.3 W / V% is more preferable.
【０００６】本発明においてグリチルリチン酸の塩類と
は、グリチルリチン酸二カリウム、グリチルリチン酸二
ナトリウム、グリチルリチン酸三ナトリウム又はグリチ
ルリチン酸二アンモニウム等をいい、好ましいものとし
てグリチルリチン酸二カリウムを挙げることができる。
グリチルリチン酸類の配合量は製剤全量に対して０．０
０１〜２．０Ｗ／Ｖ％が好ましく、さらに０．００５〜
１.0Ｗ／Ｖ％がより好ましい。なお、グリチルリチン酸
類には甘草エキスとして用いる場合も含まれ、常法に従
い、甘草を水、アルコール類およびこれらの混合溶液で
抽出したのち、濃縮或いは乾燥したものを用いる。甘草
エキスの配合量は原生薬換算で製剤全量に対して０．１
〜２２．０Ｗ／Ｖ％で用いることができる。In the present invention, the salts of glycyrrhizic acid include dipotassium glycyrrhizinate, disodium glycyrrhizinate, trisodium glycyrrhizinate or diammonium glycyrrhizinate, and preferred examples include dipotassium glycyrrhizinate.
The amount of glycyrrhizic acid is 0.0
01 to 2.0 W / V% is preferable, and 0.005 to
1.0 W / V% is more preferable. Glycyrrhizic acids include those used as a licorice extract, and licorice is extracted with water, alcohols, or a mixed solution thereof, and then concentrated or dried according to a conventional method. The amount of licorice extract is 0.1
２22.0 W / V%.
【０００７】本発明において、グリチルリチン酸二カリ
ウムと塩化セチルピリジニウムの配合比はグリチルリチ
ン酸二カリウム１重量部に対して塩化セチルピリジニウ
ムを０．１〜２０重量部で用いるのが好ましい。In the present invention, the mixing ratio of dipotassium glycyrrhizinate and cetylpyridinium chloride is preferably 0.1 to 20 parts by weight of cetylpyridinium chloride per 1 part by weight of dipotassium glycyrrhizinate.
【０００８】本発明において、水の配合量は、製剤全量
に対して１６．０〜４０．０Ｗ／Ｖ％、およびグリセリ
ンの配合量は製剤全量に対して５０〜９０Ｗ／Ｖ％が好
ましい。これらの範囲外になると、沈殿を生成したり、
殺菌能が損なわれたり、グリチルリチン酸類の含量低下
をきたす恐れがある。In the present invention, the amount of water is preferably 16.0 to 40.0 W / V% based on the total amount of the preparation, and the amount of glycerin is preferably 50 to 90 W / V% based on the total amount of the preparation. Outside of these ranges, a precipitate may form,
The bactericidal ability may be impaired or the content of glycyrrhizic acids may be reduced.
【０００９】さらに、本発明においては１価アルコール
および上記のグリセリン以外にも多価アルコールを１種
又は２種以上を配合することができる。１価アルコール
はエタノールが好ましく、多価アルコールとしては、プ
ロピレングリコール、１,３−ブチレングリコール、ポ
リエチレングリコール類をいい、ここで、ポリエチレン
グリコール類とは、エチレンオキシドと水との付加重合
体で、マクロゴールとも称され、分子量の小さい液状の
ものが好ましく、例えばマクロゴール２００、３００、
４００、６００を挙げることができる。Further, in the present invention, one or more polyhydric alcohols can be blended in addition to the monohydric alcohol and the above-mentioned glycerin. The monohydric alcohol is preferably ethanol, and the polyhydric alcohol includes propylene glycol, 1,3-butylene glycol, and polyethylene glycols, where polyethylene glycol is an addition polymer of ethylene oxide and water, It is also called a goal, and a liquid having a small molecular weight is preferable. For example, macrogol 200, 300,
400 and 600.
【００１０】本発明の咽頭疾患用組成物は、必要に応じ
て、塩酸、水酸化ナトリウム、或いはクエン酸、リンゴ
酸、酒石酸等の有機酸で常法によりｐＨを調整できる。The pH of the composition for pharyngeal diseases of the present invention can be adjusted by an ordinary method using hydrochloric acid, sodium hydroxide, or an organic acid such as citric acid, malic acid or tartaric acid, if necessary.
【００１１】本発明の咽頭疾患用組成物には配合が許さ
れる医薬成分、生薬および生薬抽出物、さらには香料、
清涼化剤、着色料、安定化剤、甘味剤、矯味剤、防腐
剤、界面活性剤等を適宜加えることができる。The composition for pharyngeal diseases of the present invention is allowed to be blended with a pharmaceutical ingredient, a crude drug and a crude drug extract, and further, a fragrance,
Cooling agents, coloring agents, stabilizers, sweeteners, flavoring agents, preservatives, surfactants and the like can be added as appropriate.
【００１２】本発明の咽頭疾患用組成物は、常法により
各成分を秤り、水に溶解する成分は水に溶解し、その他
の成分はアルコール類に溶解し、両者をあわせ、最終的
に水で定容して調製する。患部に直接塗布するか、噴霧
して用いる。使用を容易にするためにポンプ容器に充填
して使用することができる。In the composition for pharyngeal diseases of the present invention, each component is weighed by a conventional method, the component soluble in water is dissolved in water, and the other components are dissolved in alcohols. Make up to constant volume with water. Apply directly to the affected area or spray. It can be used by filling into a pump container for easy use.
【００１３】本発明の咽頭疾患用組成物はのどの殺菌・
消毒、扁桃腺炎、口内炎、のどの諸炎症の消炎、口臭の
除去、のどのあれ、のどの不快感、声がれなどに有効で
あるThe composition for pharyngeal diseases of the present invention is characterized by
It is effective for disinfection, tonsillitis, stomatitis, inflammation of throat inflammation, removal of bad breath, throat, throat discomfort, voice sickness, etc.
【００１４】。[0014]
【発明の効果】本発明によって、４級アンモニウム塩お
よびグリチルリチン酸類を配合した系において、水およ
びグリセリンの配合量を適切な範囲にすることにより良
好な殺菌能を保持し、且つグリチルリチン酸類の含量低
下がなく、経時的に沈殿も生じない製剤的に安定な咽頭
疾患用組成物を提供することが可能となった。According to the present invention, in a system containing a quaternary ammonium salt and glycyrrhizic acids, good bactericidal activity can be maintained and the content of glycyrrhizic acids can be reduced by adjusting the amounts of water and glycerin in an appropriate range. Thus, it has become possible to provide a composition for pharyngeal diseases which is stable and does not cause precipitation over time.
【００１５】[0015]
【実施例】以下、実施例、比較例、および試験例を示
し、本発明を更に具体的に説明する。The present invention will be described more specifically below with reference to examples, comparative examples and test examples.
【００１６】 実施例１ グリチルリチン酸二カリウム ０．１５ｇ 塩化セチルピリジニウム ０．１ｇ エタノール（ｄ：約０．８） ２１ｇ グリセリン（ｄ：約１．２） ６９ｇ 精製水 １８．５ｇ（全１００ｍＬ） グリチルリチン酸二カリウムを精製水に溶解した液を、
塩化セチルピリジニウムをエタノール溶解し、さらにグ
リセリンを加えた液に加え、精製水で１００ｍＬとし
た。この溶液をポンプ容器に充填して咽頭用ストリーム
剤とした。Example 1 Dipotassium glycyrrhizinate 0.15 g Cetylpyridinium chloride 0.1 g Ethanol (d: about 0.8) 21 g Glycerin (d: about 1.2) 69 g Purified water 18.5 g (100 mL in total) Glycyrrhizic acid A solution prepared by dissolving dipotassium in purified water,
Cetylpyridinium chloride was dissolved in ethanol, added to a solution to which glycerin was further added, and made up to 100 mL with purified water. This solution was filled into a pump container to give a pharyngeal stream.
【００１７】 実施例２ グリチルリチン酸二カリウム ０．１５ｇ 塩化セチルピリジニウム ０．１ｇ ケイヒ油 ０．０１ｇ エタノール（ｄ：約０．８） １０ｇ グリセリン（ｄ：約１．２） ６０ｇ ソルビトール ２０ｇ 精製水 ２９ｇ（全１００ｍＬ） グリチルリチン酸二カリウムおよびソルビトールを精製
水に溶解した液を、塩化セチルピリジニウムおよびケイ
ヒ油をエタノールに溶解し、さらにグリセリンを加えた
液に加え、精製水で１００ｍＬとした。この溶液をポン
プ容器に充填して咽頭用スプレー剤とした。Example 2 Dipotassium glycyrrhizinate 0.15 g Cetylpyridinium chloride 0.1 g Caffeine oil 0.01 g Ethanol (d: about 0.8) 10 g Glycerin (d: about 1.2) 60 g Sorbitol 20 g Purified water 29 g ( A solution obtained by dissolving dipotassium glycyrrhizinate and sorbitol in purified water was dissolved in cetylpyridinium chloride and cinnamon oil in ethanol, and further added to a solution containing glycerin, and the solution was made up to 100 mL with purified water. This solution was filled into a pump container to obtain a pharyngeal spray.
【００１８】 比較例１ グリチルリチン酸二カリウム ０．１５ｇ 塩化セチルピリジニウム ０．１ｇ エタノール（ｄ：約０．８） １０ｇ グリセリン（ｄ：約１．２） ９５ｇ 精製水 １２ｇ（全１００ｍＬ） 実施例１と同様に調製した。Comparative Example 1 Dipotassium glycyrrhizinate 0.15 g Cetylpyridinium chloride 0.1 g Ethanol (d: about 0.8) 10 g Glycerin (d: about 1.2) 95 g Purified water 12 g (100 mL in total) Prepared similarly.
【００１９】 比較例２ グリチルリチン酸二カリウム ０．１５ｇ 塩化セチルピリジニウム ０．１ｇ エタノール（ｄ：約０．８） １６ｇ グリセリン（ｄ：約１．２） ３８ｇ 精製水 ５０ｇ（全１００ｍＬ） 実施例１と同様に調製した。Comparative Example 2 Dipotassium glycyrrhizinate 0.15 g Cetylpyridinium chloride 0.1 g Ethanol (d: about 0.8) 16 g Glycerin (d: about 1.2) 38 g Purified water 50 g (100 mL in total) Prepared similarly.
【００２０】試験例１−殺菌効力試験− 実施例１、２、比較例１、２を試験液とし、常法により
殺菌効力試験を行った。試験菌種はＳｔａｐｈｌｏｃｏ
ｃｃｕｓ ａｕｒｅｕｓを使用し、各試験液５００μＬ
をとり、１８時間前培養した試験菌液２０μＬと混合
し、１分後にその１０μＬを２５０μＬのＳＣＤＬＰ培
地に接種し、３５℃、２４時間培養した。殺菌効力は、
培地の混濁の有無により判定した。Test Example 1-Bactericidal efficacy test-Using Examples 1 and 2 and Comparative Examples 1 and 2 as test liquids, a bactericidal efficacy test was carried out by a conventional method. The test strain is Staphloco
500 μL of each test solution using ccus aureus
Was mixed with 20 μL of the test bacterial solution pre-cultured for 18 hours. One minute later, 10 μL of the mixture was inoculated into 250 μL of SCDLP medium, and cultured at 35 ° C. for 24 hours. The bactericidal efficacy is
It was determined by the presence or absence of turbidity in the medium.
【００２１】試験例２−グリチルリチン酸二カリウムの
安定性− 実施例１、２、比較例１、２を６５℃、２週間保存し、
グリチルリチン酸二カリウムの残存率を液体クロマトグ
ラフィーを用いて測定した。安定性の評価は、６５℃、
２週間後の残存率が８０％以上あるか否かにより判定し
た。Test Example 2-Stability of dipotassium glycyrrhizinate-Examples 1 and 2 and Comparative Examples 1 and 2 were stored at 65 ° C for 2 weeks.
The residual ratio of dipotassium glycyrrhizinate was measured using liquid chromatography. The stability was evaluated at 65 ° C.
Judgment was made based on whether the residual ratio after 2 weeks was 80% or more.
【００２２】試験例３−沈殿の生成の有無− 実施例１、２、比較例１、２を６５℃、２週間保存し、
外観の変化を肉眼で観察した。評価は沈殿の生成の有無
により判定した。Test Example 3-Presence or absence of formation of precipitate-Examples 1 and 2 and Comparative Examples 1 and 2 were stored at 65 ° C for 2 weeks.
Changes in appearance were visually observed. The evaluation was made based on whether or not a precipitate was formed.
【００２３】結果：試験例１、２、３の結果をまとめて
表１に示した。表１から明らかなように製剤全量に対し
て水およびグリセリンの配合量が１８．５Ｗ／Ｖ％、６
９Ｗ／Ｖ％（実施例１）、２９Ｗ／Ｖ％、６０Ｗ／Ｖ％
（実施例２）においては１２Ｗ／Ｖ％、９５Ｗ／Ｖ％
（比較例１）、５０Ｗ／Ｖ％、３８Ｗ／Ｖ％（比較例
２）に比べて良好な殺菌能を保持し、グリチルリチン酸
二カリウムの残存率も８０％以上を示し、また沈殿の生
成も認められずすべての項目において良好な結果が得ら
れた。Results: Table 1 summarizes the results of Test Examples 1, 2, and 3. As is clear from Table 1, the blending amount of water and glycerin was 18.5 W / V%, 6
9 W / V% (Example 1), 29 W / V%, 60 W / V%
In Example 2, 12 W / V% and 95 W / V%
(Comparative Example 1), 50 W / V%, 38 W / V%, maintaining good bactericidal activity as compared with (Comparative Example 2), the residual rate of dipotassium glycyrrhizinate also shows 80% or more, and the formation of precipitates Good results were obtained in all items without recognition.
【００２４】[0024]
【表１】 [Table 1]
───────────────────────────────────────────────────── フロントページの続き (51)Int.Cl.7 識別記号 ＦＩ テーマコート゛(参考） Ａ６１Ｋ 47/10 Ａ６１Ｋ 47/10 (72)発明者 相川 勝義 東京都豊島区高田３丁目24番１号 大正製 薬株式会社内 (72)発明者 小畑 清隆 東京都豊島区高田３丁目24番１号 大正製 薬株式会社内 Ｆターム(参考） 4C076 AA12 BB03 CC04 CC31 DD37 DD38 DD67 FF15 FF36 FF63 4C086 AA01 AA02 EA19 MA03 MA05 MA08 MA10 MA56 NA03 ZA34 ZB11 ZB35 4C088 AB60 BA08 MA02 MA56 NA03 ZA34 ZB11 ZB35 4C206 AA01 AA02 FA41 MA03 MA05 MA28 MA76 NA03 ZA34 ZB11 ZB35 ──────────────────────────────────────────────────の Continued on the front page (51) Int.Cl. 7 Identification symbol FI Theme coat ゛ (Reference) A61K 47/10 A61K 47/10 (72) Inventor Katsuyoshi Aikawa 3-24-1, Takada, Toshima-ku, Tokyo Taisho (72) Inventor Kiyotaka Obata 3-24-1, Takada, Toshima-ku, Tokyo Taisho Pharmaceutical Co., Ltd. F-term (reference) 4C076 AA12 BB03 CC04 CC31 DD37 DD38 DD67 FF15 FF36 FF63 4C086 AA01 AA02 EA19 MA03 MA05 MA08 MA10 MA56 NA03 ZA34 ZB11 ZB35 4C088 AB60 BA08 MA02 MA56 NA03 ZA34 ZB11 ZB35 4C206 AA01 AA02 FA41 MA03 MA05 MA28 MA76 NA03 ZA34 ZB11 ZB35
Claims (5)
塩、（Ｂ）グリチルリチン酸又はその塩類、（Ｃ）製剤
全量に対して１６．０〜４０．０Ｗ／Ｖ％の水、および
（Ｄ）製剤全量に対して５０〜９０Ｗ／Ｖ％のグリセリ
ンからなることを特徴とする咽頭疾患用組成物。1. A quaternary ammonium salt having a bactericidal action, (B) glycyrrhizic acid or a salt thereof, (C) water of 16.0 to 40.0 W / V% based on the total amount of the preparation, and (D) ) A composition for pharyngeal diseases, comprising glycerin in an amount of 50 to 90 W / V% based on the total amount of the preparation.
化セチルピリジニウムである請求項１に記載の咽頭疾患
用組成物。2. The composition for pharyngeal diseases according to claim 1, wherein the quaternary ammonium salt having a bactericidal action is cetylpyridinium chloride.
量に対して０．００５〜２．５Ｗ／Ｖ％である請求項２
に記載の咽頭疾患用組成物。3. The compounding amount of cetylpyridinium chloride is 0.005 to 2.5 W / V% based on the total amount of the preparation.
The composition for pharyngeal diseases according to the above.
酸二カリウム、グリチルリチン酸二ナトリウム、グリチ
ルリチン酸二アンモニウム又は甘草エキスの少なくとも
１種である請求項１〜３のいずれかに記載の咽頭疾患用
組成物。4. The composition for pharyngeal diseases according to claim 1, wherein the salt of glycyrrhizic acid is at least one of dipotassium glycyrrhizinate, disodium glycyrrhizinate, diammonium glycyrrhizinate or licorice extract.
剤全量に対して０．００５〜１．０Ｗ／Ｖ％である請求
項４に記載の咽頭疾患用組成物。5. The composition for pharyngeal diseases according to claim 4, wherein the compounding amount of dipotassium glycyrrhizinate is 0.005 to 1.0 W / V% based on the total amount of the preparation.
Priority Applications (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| JP11058239A JP2000256186A (en) | 1999-03-05 | 1999-03-05 | Composition for pharyngeal disease |
Applications Claiming Priority (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| JP11058239A JP2000256186A (en) | 1999-03-05 | 1999-03-05 | Composition for pharyngeal disease |
Publications (1)
| Publication Number | Publication Date |
|---|---|
| JP2000256186A true JP2000256186A (en) | 2000-09-19 |
Family
ID=13078565
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP11058239A Withdrawn JP2000256186A (en) | 1999-03-05 | 1999-03-05 | Composition for pharyngeal disease |
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| Country | Link |
|---|---|
| JP (1) | JP2000256186A (en) |
Cited By (3)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| KR20020041118A (en) * | 2000-11-27 | 2002-06-01 | 김용철 박홍양 | Treating and Prophylactic Preparation for Poultry Newcastle Disease |
| WO2004072017A1 (en) * | 2003-02-14 | 2004-08-26 | Aziende Chimiche Riunite Angelini Francesco A.C.R.A.F. S.P.A. | Cetylpyridinium salt of an anti-inflammatory agent and pharmaceutical compositions containing it |
| CN104666580A (en) * | 2015-02-08 | 2015-06-03 | 吕金旺 | Traditional Chinese medicine powder for treating throat inflammation |
-
1999
- 1999-03-05 JP JP11058239A patent/JP2000256186A/en not_active Withdrawn
Cited By (5)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| KR20020041118A (en) * | 2000-11-27 | 2002-06-01 | 김용철 박홍양 | Treating and Prophylactic Preparation for Poultry Newcastle Disease |
| WO2004072017A1 (en) * | 2003-02-14 | 2004-08-26 | Aziende Chimiche Riunite Angelini Francesco A.C.R.A.F. S.P.A. | Cetylpyridinium salt of an anti-inflammatory agent and pharmaceutical compositions containing it |
| EA008003B1 (en) * | 2003-02-14 | 2007-02-27 | Ацьенде Кимике Рьюните Анджелини Франческо A.K.P.A.Ф. С.П.А. | Cetylpyridinium salt of an anti-inflammatory agent and pharmaceutical compositions containing it |
| US7250428B2 (en) | 2003-02-14 | 2007-07-31 | Aziende Chimiche Riunite Angelini Francesco A.C.R.A.F. S.P.A. | Cetylpyridinium salt of an anti-inflammatory agent and pharmaceutical compositions containing it |
| CN104666580A (en) * | 2015-02-08 | 2015-06-03 | 吕金旺 | Traditional Chinese medicine powder for treating throat inflammation |
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