JP5980488B2 - Pharmaceutical composition for the treatment of stomatitis - Google Patents
Pharmaceutical composition for the treatment of stomatitis Download PDFInfo
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- JP5980488B2 JP5980488B2 JP2011207778A JP2011207778A JP5980488B2 JP 5980488 B2 JP5980488 B2 JP 5980488B2 JP 2011207778 A JP2011207778 A JP 2011207778A JP 2011207778 A JP2011207778 A JP 2011207778A JP 5980488 B2 JP5980488 B2 JP 5980488B2
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- 239000008194 pharmaceutical composition Substances 0.000 title claims description 24
- 208000003265 stomatitis Diseases 0.000 title claims description 22
- 239000003814 drug Substances 0.000 claims description 18
- 239000004480 active ingredient Substances 0.000 claims description 4
- 230000001225 therapeutic effect Effects 0.000 claims description 2
- 229940121375 antifungal agent Drugs 0.000 description 18
- 239000003429 antifungal agent Substances 0.000 description 17
- 201000004624 Dermatitis Diseases 0.000 description 13
- 208000010668 atopic eczema Diseases 0.000 description 13
- RAXXELZNTBOGNW-UHFFFAOYSA-N imidazole Natural products C1=CNC=N1 RAXXELZNTBOGNW-UHFFFAOYSA-N 0.000 description 12
- 241000233866 Fungi Species 0.000 description 11
- 229940079593 drug Drugs 0.000 description 10
- VVJKKWFAADXIJK-UHFFFAOYSA-N Allylamine Chemical compound NCC=C VVJKKWFAADXIJK-UHFFFAOYSA-N 0.000 description 8
- GNVMUORYQLCPJZ-UHFFFAOYSA-M Thiocarbamate Chemical compound NC([S-])=O GNVMUORYQLCPJZ-UHFFFAOYSA-M 0.000 description 6
- 230000000694 effects Effects 0.000 description 6
- 239000006071 cream Substances 0.000 description 5
- 239000000126 substance Substances 0.000 description 5
- 241000222120 Candida <Saccharomycetales> Species 0.000 description 3
- OCAPBUJLXMYKEJ-UHFFFAOYSA-N 1-[biphenyl-4-yl(phenyl)methyl]imidazole Chemical compound C1=NC=CN1C(C=1C=CC(=CC=1)C=1C=CC=CC=1)C1=CC=CC=C1 OCAPBUJLXMYKEJ-UHFFFAOYSA-N 0.000 description 2
- 241000894006 Bacteria Species 0.000 description 2
- 208000003322 Coinfection Diseases 0.000 description 2
- 230000000843 anti-fungal effect Effects 0.000 description 2
- WGQKYBSKWIADBV-UHFFFAOYSA-N benzylamine Chemical compound NCC1=CC=CC=C1 WGQKYBSKWIADBV-UHFFFAOYSA-N 0.000 description 2
- 229960002206 bifonazole Drugs 0.000 description 2
- 239000011248 coating agent Substances 0.000 description 2
- 238000005336 cracking Methods 0.000 description 2
- 238000006748 scratching Methods 0.000 description 2
- 230000002393 scratching effect Effects 0.000 description 2
- 208000024891 symptom Diseases 0.000 description 2
- DOMXUEMWDBAQBQ-WEVVVXLNSA-N terbinafine Chemical compound C1=CC=C2C(CN(C\C=C\C#CC(C)(C)C)C)=CC=CC2=C1 DOMXUEMWDBAQBQ-WEVVVXLNSA-N 0.000 description 2
- 229960000699 terbinafine hydrochloride Drugs 0.000 description 2
- 230000029663 wound healing Effects 0.000 description 2
- XMAYWYJOQHXEEK-OZXSUGGESA-N (2R,4S)-ketoconazole Chemical compound C1CN(C(=O)C)CCN1C(C=C1)=CC=C1OC[C@@H]1O[C@@](CN2C=NC=C2)(C=2C(=CC(Cl)=CC=2)Cl)OC1 XMAYWYJOQHXEEK-OZXSUGGESA-N 0.000 description 1
- AFNXATANNDIXLG-SFHVURJKSA-N 1-[(2r)-2-[(4-chlorophenyl)methylsulfanyl]-2-(2,4-dichlorophenyl)ethyl]imidazole Chemical compound C1=CC(Cl)=CC=C1CS[C@H](C=1C(=CC(Cl)=CC=1)Cl)CN1C=NC=C1 AFNXATANNDIXLG-SFHVURJKSA-N 0.000 description 1
- LEZWWPYKPKIXLL-UHFFFAOYSA-N 1-{2-(4-chlorobenzyloxy)-2-(2,4-dichlorophenyl)ethyl}imidazole Chemical compound C1=CC(Cl)=CC=C1COC(C=1C(=CC(Cl)=CC=1)Cl)CN1C=NC=C1 LEZWWPYKPKIXLL-UHFFFAOYSA-N 0.000 description 1
- 208000000412 Avitaminosis Diseases 0.000 description 1
- WHPAGCJNPTUGGD-UHFFFAOYSA-N Croconazole Chemical compound ClC1=CC=CC(COC=2C(=CC=CC=2)C(=C)N2C=NC=C2)=C1 WHPAGCJNPTUGGD-UHFFFAOYSA-N 0.000 description 1
- LFQSCWFLJHTTHZ-UHFFFAOYSA-N Ethanol Chemical compound CCO LFQSCWFLJHTTHZ-UHFFFAOYSA-N 0.000 description 1
- 206010021135 Hypovitaminosis Diseases 0.000 description 1
- 206010061218 Inflammation Diseases 0.000 description 1
- 102000011782 Keratins Human genes 0.000 description 1
- 108010076876 Keratins Proteins 0.000 description 1
- ZRTQSJFIDWNVJW-WYMLVPIESA-N Lanoconazole Chemical compound ClC1=CC=CC=C1C(CS\1)SC/1=C(\C#N)N1C=NC=C1 ZRTQSJFIDWNVJW-WYMLVPIESA-N 0.000 description 1
- BYBLEWFAAKGYCD-UHFFFAOYSA-N Miconazole Chemical compound ClC1=CC(Cl)=CC=C1COC(C=1C(=CC(Cl)=CC=1)Cl)CN1C=NC=C1 BYBLEWFAAKGYCD-UHFFFAOYSA-N 0.000 description 1
- 239000004909 Moisturizer Substances 0.000 description 1
- CZPWVGJYEJSRLH-UHFFFAOYSA-N Pyrimidine Chemical compound C1=CN=CN=C1 CZPWVGJYEJSRLH-UHFFFAOYSA-N 0.000 description 1
- 241000295644 Staphylococcaceae Species 0.000 description 1
- 208000002474 Tinea Diseases 0.000 description 1
- 241000893966 Trichophyton verrucosum Species 0.000 description 1
- 239000000443 aerosol Substances 0.000 description 1
- 239000003242 anti bacterial agent Substances 0.000 description 1
- 229940088710 antibiotic agent Drugs 0.000 description 1
- 238000003287 bathing Methods 0.000 description 1
- 230000017531 blood circulation Effects 0.000 description 1
- 239000003795 chemical substances by application Substances 0.000 description 1
- 229960004022 clotrimazole Drugs 0.000 description 1
- VNFPBHJOKIVQEB-UHFFFAOYSA-N clotrimazole Chemical compound ClC1=CC=CC=C1C(N1C=NC=C1)(C=1C=CC=CC=1)C1=CC=CC=C1 VNFPBHJOKIVQEB-UHFFFAOYSA-N 0.000 description 1
- 229960002042 croconazole Drugs 0.000 description 1
- 230000006378 damage Effects 0.000 description 1
- 229960003913 econazole Drugs 0.000 description 1
- 230000002708 enhancing effect Effects 0.000 description 1
- 239000000499 gel Substances 0.000 description 1
- 239000003349 gelling agent Substances 0.000 description 1
- 208000015181 infectious disease Diseases 0.000 description 1
- 230000004054 inflammatory process Effects 0.000 description 1
- 239000004615 ingredient Substances 0.000 description 1
- 238000002347 injection Methods 0.000 description 1
- 239000007924 injection Substances 0.000 description 1
- -1 isconazole Chemical compound 0.000 description 1
- 229960004125 ketoconazole Drugs 0.000 description 1
- 229950010163 lanoconazole Drugs 0.000 description 1
- 239000007788 liquid Substances 0.000 description 1
- 239000006210 lotion Substances 0.000 description 1
- 239000003120 macrolide antibiotic agent Substances 0.000 description 1
- 229960002509 miconazole Drugs 0.000 description 1
- 238000012986 modification Methods 0.000 description 1
- 230000004048 modification Effects 0.000 description 1
- 230000001333 moisturizer Effects 0.000 description 1
- 210000004400 mucous membrane Anatomy 0.000 description 1
- VWOIKFDZQQLJBJ-DTQAZKPQSA-N neticonazole Chemical compound CCCCCOC1=CC=CC=C1\C(=C/SC)N1C=NC=C1 VWOIKFDZQQLJBJ-DTQAZKPQSA-N 0.000 description 1
- 229950010757 neticonazole Drugs 0.000 description 1
- 235000014593 oils and fats Nutrition 0.000 description 1
- 239000002674 ointment Substances 0.000 description 1
- 239000003960 organic solvent Substances 0.000 description 1
- 229960003483 oxiconazole Drugs 0.000 description 1
- QRJJEGAJXVEBNE-MOHJPFBDSA-N oxiconazole Chemical compound ClC1=CC(Cl)=CC=C1CO\N=C(C=1C(=CC(Cl)=CC=1)Cl)\CN1C=NC=C1 QRJJEGAJXVEBNE-MOHJPFBDSA-N 0.000 description 1
- 150000004291 polyenes Chemical class 0.000 description 1
- 210000002374 sebum Anatomy 0.000 description 1
- 230000037380 skin damage Effects 0.000 description 1
- 208000017520 skin disease Diseases 0.000 description 1
- 229960002607 sulconazole Drugs 0.000 description 1
- 150000003852 triazoles Chemical class 0.000 description 1
- 208000030401 vitamin deficiency disease Diseases 0.000 description 1
- XLYOFNOQVPJJNP-UHFFFAOYSA-N water Substances O XLYOFNOQVPJJNP-UHFFFAOYSA-N 0.000 description 1
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- Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Acyclic And Carbocyclic Compounds In Medicinal Compositions (AREA)
Description
本発明は、口角炎を治療するための医薬組成物に関する。 The present invention relates to a pharmaceutical composition for treating stomatitis .
口角炎は口角の皮膚および粘膜に炎症等が生じる皮膚疾患である。口角炎は、ビタミンの欠乏などの種々の誘因によって、口角部の皮膚が損傷し、細菌、真菌などの2次感染が起こったものであると考えられている。2次感染を起こすものとして、ブドウ球菌、連鎖球菌などの細菌、カンジダ属菌などの真菌などが知られている。 Stomatitis is a skin disease in which inflammation or the like occurs in the skin and mucous membrane of the mouth corner. It is believed that stomatitis is a result of secondary infections such as bacteria and fungi caused by damage to the skin of the mouth corner due to various causes such as vitamin deficiency. Known causes of secondary infection include bacteria such as staphylococci and streptococci, and fungi such as Candida spp.
また、亀裂性湿疹は、「あかぎれ」とも呼ばれ、冬などの寒い時期に、血行の不良、皮脂不足などの原因によって、手足等に生じる湿疹の一つである。 In addition, fissure eczema is also referred to as “Akagure”, and is one of eczema that occurs on limbs and the like due to poor blood circulation, lack of sebum, etc. in cold seasons such as winter.
特許文献1には、皮膚の損傷等を改善または治療するための、創傷治癒促進剤、ケラチン親和性の高い抗真菌剤および保湿剤を含有する外用医薬組成物が記載されている。また、特許文献2には、抗真菌性物質を有効成分として含有するうがい剤が記載されている。 Patent Document 1 describes an external pharmaceutical composition containing a wound healing promoter, an antifungal agent having a high affinity for keratin, and a moisturizer for improving or treating skin damage and the like. Patent Document 2 describes a gargle containing an antifungal substance as an active ingredient.
しかし、特許文献1では、創傷治癒促進剤の効果を亢進させる目的で抗真菌剤を使用しており、抗真菌剤が口角炎または亀裂性湿疹に対する効果を有することは、特許文献１には全く記載も示唆もされていない。 However, in Patent Document 1, an antifungal agent is used for the purpose of enhancing the effect of the wound healing promoter, and it is completely disclosed in Patent Document 1 that the antifungal agent has an effect on stomatitis or fissure eczema. Neither listed nor suggested.
また、上述したように、口角炎には、カンジダ属菌などの真菌以外の原因のものも存在する。しかし、特許文献2には、抗真菌剤がこのような口角炎全般に対する効果を有することについては、全く記載も示唆もされていない。また、亀裂性湿疹についても、特許文献２には全く記載されていない。 In addition, as described above, stomatitis has causes other than fungi such as Candida spp. However, Patent Document 2 neither describes nor suggests that the antifungal agent has an effect on such stomatitis in general. In addition, Patent Document 2 does not describe any cracked eczema.
本発明は、上述した従来技術が有する問題に鑑みてなされたものであり、その目的は、
口角炎の治療に好適に用いることができる新規な医薬組成物を提供することにある。
The present invention has been made in view of the problems of the above-described prior art, and its purpose is as follows.
An object of the present invention is to provide a novel pharmaceutical composition that can be suitably used for the treatment of stomatitis .
本発明者は、上記課題を解決するために鋭意検討した結果、抗真菌剤が、口角炎および亀裂性湿疹に対して効果を発揮することを見出した。抗真菌剤が、真菌に対する効果以外に、このような口角炎および亀裂性湿疹に対する効果を有することについては、これまで知られていなかった。本発明者は、この知見に基づいて本発明を完成させた。 As a result of intensive studies to solve the above problems, the present inventor has found that an antifungal agent exhibits an effect on stomatitis and fissure eczema. It has not been known so far that an antifungal agent has an effect on such stomatitis and fissure eczema other than an effect on a fungus. The present inventor has completed the present invention based on this finding.
また、本発明は、リラナフタートを有効成分として含む、口角炎の治療用医薬組成物を提供する。
また、外用薬である、上記治療用医薬組成物を提供する。
In addition , the present invention provides a pharmaceutical composition for treating stomatitis, comprising rilanaphthate as an active ingredient.
Moreover, the said pharmaceutical composition for a treatment which is an external medicine is provided.
本発明は、口角炎の治療に好適に用いることができる。 The present invention can be suitably used for the treatment of stomatitis .
本発明に係る医薬組成物は、抗真菌剤を有効成分として含む。 The pharmaceutical composition according to the present invention contains an antifungal agent as an active ingredient.
抗真菌剤とは、カンジダ属菌および白癬菌等の真菌の生育を阻害する物質である。抗真菌剤は、真菌全般に対して効果のある物質であってもよいし、一部の真菌に対して効果のある物質であってもよい。なお、本発明に係る医薬組成物は、1種類の抗真菌剤を含んでいてもよいし、複数種類の抗真菌剤を含んでいてもよい。 An antifungal agent is a substance that inhibits the growth of fungi such as Candida and Ringworm. The antifungal agent may be a substance effective against all fungi, or a substance effective against some fungi. The pharmaceutical composition according to the present invention may contain one type of antifungal agent or may contain a plurality of types of antifungal agents.
本発明に係る医薬組成物による治療の対象となる口角炎または亀裂性湿疹は、真菌に起因したものであってもよいし、なくてもよい。すなわち、本発明に係る医薬組成物は、真菌に起因する口角炎または亀裂性湿疹だけでなく、真菌に起因しない口角炎または亀裂性湿疹の治療用医薬組成物としても用いることができる。 The stomatitis or fissure eczema to be treated with the pharmaceutical composition according to the present invention may or may not be caused by a fungus. That is, the pharmaceutical composition according to the present invention can be used not only for stomatitis or fissure eczema caused by fungi, but also for the treatment of stomatitis or fissure eczema not caused by fungi.
抗真菌剤としては、特に限定されないが、たとえばチオカルバメート系、イミダゾール系、アリルアミン系、ポリエンマクロライド系、ピリミジン系、トリアゾール系、キャンディン系、チオカルバメート系、ベンジルアミン系およびモルホミン系等の薬剤、抗生物質などが挙げられる。なかでも、本発明における抗真菌剤は、チオカルバメート系薬剤、イミダゾール系薬剤およびアリルアミン系薬剤からなる群より選択される少なくとも一つであることができる。 Examples of antifungal agents include, but are not limited to, for example, thiocarbamate, imidazole, allylamine, polyene macrolide, pyrimidine, triazole, candin, thiocarbamate, benzylamine, and morphomine And antibiotics. Among them, the antifungal agent in the present invention can be at least one selected from the group consisting of thiocarbamate drugs, imidazole drugs, and allylamine drugs.
チオカルバメート系薬剤としては、たとえばリラナフタートおよびトルナフタートなどを挙げることができる。イミダゾール系薬剤としては、たとえばクロトリマゾール、ミコナゾール、スルコナゾール、オキシコナゾール、ケトコナゾール、ビホナゾール、エコナゾール、イソコナゾール、クロコナゾール、ネチコナゾールおよびラノコナゾールなどを挙げることができる。アリルアミン系薬剤としては、たとえば塩酸テルビナフィンなどを挙げることができる。 Examples of the thiocarbamate drug include rylanaphthalate and tolnaphthalate. Examples of the imidazole drugs include clotrimazole, miconazole, sulconazole, oxyconazole, ketoconazole, bifonazole, econazole, isconazole, croconazole, neticonazole, and lanoconazole. Examples of allylamine drugs include terbinafine hydrochloride.
本発明に係る医薬組成物は、これらの抗真菌剤を、真菌に対して治療的な効果を有することが従来から知られている量にて含んでいてもよい。 The pharmaceutical composition according to the present invention may contain these antifungal agents in amounts conventionally known to have a therapeutic effect on fungi.
本発明に係る医薬組成物は、抗真菌剤以外の他の物質をさらに含んでいてもよい。たとえば医薬組成物は、抗真菌剤を保持するための基剤をさらに含んでいてもよく、基剤としては、水、アルコール等の有機溶媒、油脂およびゲル化剤などが挙げられる。また、医薬組成物は、他の薬効成分をさらに含んでいてもよい。 The pharmaceutical composition according to the present invention may further contain a substance other than the antifungal agent. For example, the pharmaceutical composition may further contain a base for holding an antifungal agent, and examples of the base include water, organic solvents such as alcohol, oils and fats, gelling agents, and the like. The pharmaceutical composition may further contain other medicinal ingredients.
本発明に係る医薬組成物は、たとえば外用薬、内服薬、注射薬等であってもよく、なかでも外用薬であることが好ましい。外用薬としては、たとえば塗布剤、貼付剤およびエアゾール剤等が挙げられる。塗布剤としては、たとえばクリーム剤、軟膏剤、液剤、ゲル剤、ローション剤およびチック剤等が挙げられる。 The pharmaceutical composition according to the present invention may be, for example, an external medicine, an internal medicine, an injection medicine or the like, and is preferably an external medicine. As an external medicine, a coating agent, a patch, an aerosol agent etc. are mentioned, for example. Examples of the coating agent include creams, ointments, liquids, gels, lotions, and tics.
本発明に係る医薬組成物は、従来の抗真菌活性を有する医薬品と同様に製造することができる。たとえば、本発明に係る医薬組成物は、上記の既存の抗真菌剤と同じ成分の医薬品として製造することができる。 The pharmaceutical composition concerning this invention can be manufactured similarly to the pharmaceutical which has the conventional antifungal activity. For example, the pharmaceutical composition according to the present invention can be produced as a pharmaceutical having the same components as the above-mentioned existing antifungal agents.
本発明に係る医薬組成物を患者に投与する場合には、投与する頻度および期間などは、患者の年齢、症状などに応じて適宜設定することが好ましい。たとえば投与する頻度は、特に限定されないが、1日あたり1〜数回、好ましくは1日あたり1または2回であることが好ましい。また投与する期間は、症状が治まるまでであってもよく、たとえば1日〜数か月であってもよい。 When the pharmaceutical composition according to the present invention is administered to a patient, the frequency and period of administration are preferably set as appropriate according to the age, symptoms, etc. of the patient. For example, the frequency of administration is not particularly limited, but it is preferably 1 to several times per day, preferably 1 or 2 times per day. Further, the administration period may be until symptoms are resolved, and may be, for example, 1 day to several months.
本発明は、上述した実施形態および下記の実施例に限定されるものではなく、特許請求の範囲に示した範囲で種々の変更が可能である。 The present invention is not limited to the above-described embodiment and the following examples, and various modifications can be made within the scope shown in the claims.
〔実施例1〕
口角炎を患っている患者（40代男性）の患部に対し、チオカルバメート系薬剤であるリラナフタートを含む医薬組成物（商品名：ゼフナートクリーム（鳥居薬品株式会社製））を塗布した。その結果、１回塗布したのみで、口角炎が治った。
Example 1
A pharmaceutical composition (trade name: Zefnate Cream (manufactured by Torii Pharmaceutical Co., Ltd.)) containing rilanaphthate, a thiocarbamate drug, was applied to the affected area of a patient (male in their 40s) suffering from stomatitis. As a result, the stomatitis was cured with only one application.
〔実施例2〕
口角炎を患っている10人の患者（0〜5歳）の各患部に対し、チオカルバメート系薬剤であるリラナフタートを含む医薬組成物（商品名：ゼフナートクリーム（鳥居薬品株式会社製））を塗布した。その結果、全ての患者において、口角炎が完治した。
(Example 2)
A pharmaceutical composition (trade name: zefnate cream (manufactured by Torii Pharmaceutical Co., Ltd.)) containing rilanaphthate, a thiocarbamate drug, is applied to each affected area of 10 patients (0-5 years old) who have stomatitis. did. As a result, stomatitis was completely cured in all patients.
〔実施例3〕
手にあかぎれ（亀裂性湿疹）を患っている患者（37歳女性）の患部に対し、イミダゾール系薬剤であるビホナゾールを含む医薬組成物（商品名：マイコスポールクリーム（バイエル薬品株式会社製））を塗布した。塗布するタイミングは朝および入浴後の1日2回とし、2ヶ月続けた。その結果、亀裂性湿疹が完治した。
Example 3
A pharmaceutical composition containing bifonazole, an imidazole drug (product name: Mycospol cream (manufactured by Bayer Yakuhin Co., Ltd.)), is applied to the affected part of a patient (37-year-old woman) suffering from scratching (cracking eczema) in his hand did. The application timing was twice a day in the morning and after bathing and continued for 2 months. As a result, fissure eczema was completely cured.
〔実施例4〕
手にあかぎれ（亀裂性湿疹）を患っている患者（40歳女性）の患部に対し、アリルアミン系薬剤である塩酸テルビナフィンを含む医薬組成物（商品名：ラミシールクリーム（ノバルティスファーマ株式会社製））を塗布した。塗布するタイミングは1日1回とし、約4ヶ月続けた。その結果、亀裂性湿疹が完治した。
(Example 4)
A pharmaceutical composition containing terbinafine hydrochloride, an allylamine-based drug (trade name: Ramisir Cream (manufactured by Novartis Pharma Co., Ltd.)) for the affected part of a patient (40-year-old female) suffering from scratching (cracking eczema) in his hand Applied. The application timing was once a day and continued for about 4 months. As a result, fissure eczema was completely cured.
本発明は、口角炎の治療に好適に用いることができるため、口角炎を治療するための医薬品などに好適に利用することができる。 Since the present invention can be suitably used for the treatment of stomatitis, it can be suitably used for pharmaceuticals for treating stomatitis .
Claims (2)
Priority Applications (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| JP2011207778A JP5980488B2 (en) | 2011-09-22 | 2011-09-22 | Pharmaceutical composition for the treatment of stomatitis |
Applications Claiming Priority (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| JP2011207778A JP5980488B2 (en) | 2011-09-22 | 2011-09-22 | Pharmaceutical composition for the treatment of stomatitis |
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