JPH01226820A - External medicine containing vitamin b1 derivative - Google Patents
External medicine containing vitamin b1 derivativeInfo
- Publication number
- JPH01226820A JPH01226820A JP5155088A JP5155088A JPH01226820A JP H01226820 A JPH01226820 A JP H01226820A JP 5155088 A JP5155088 A JP 5155088A JP 5155088 A JP5155088 A JP 5155088A JP H01226820 A JPH01226820 A JP H01226820A
- Authority
- JP
- Japan
- Prior art keywords
- vitamin
- derivative
- external medicine
- fat
- diseased part
- 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
- 150000003544 thiamines Chemical class 0.000 title claims abstract 4
- 239000003814 drug Substances 0.000 title abstract description 5
- 238000002360 preparation method Methods 0.000 claims description 10
- 239000004480 active ingredient Substances 0.000 claims description 2
- 229960003495 thiamine Drugs 0.000 abstract description 11
- 229930003451 Vitamin B1 Natural products 0.000 abstract description 10
- DPJRMOMPQZCRJU-UHFFFAOYSA-M thiamine hydrochloride Chemical compound Cl.[Cl-].CC1=C(CCO)SC=[N+]1CC1=CN=C(C)N=C1N DPJRMOMPQZCRJU-UHFFFAOYSA-M 0.000 abstract description 10
- 235000010374 vitamin B1 Nutrition 0.000 abstract description 10
- 239000011691 vitamin B1 Substances 0.000 abstract description 10
- WNCAVNGLACHSRZ-KAMYIIQDSA-N Allithiamine Chemical compound C=CCSSC(/CCO)=C(/C)N(C=O)CC1=CN=C(C)N=C1N WNCAVNGLACHSRZ-KAMYIIQDSA-N 0.000 abstract description 5
- WNCAVNGLACHSRZ-UHFFFAOYSA-N Allithiamine Natural products C=CCSSC(CCO)=C(C)N(C=O)CC1=CN=C(C)N=C1N WNCAVNGLACHSRZ-UHFFFAOYSA-N 0.000 abstract description 5
- 208000000112 Myalgia Diseases 0.000 abstract description 5
- 230000000694 effects Effects 0.000 abstract description 5
- 208000004296 neuralgia Diseases 0.000 abstract description 5
- AZJUFRDUYTYIHV-NKFKGCMQSA-N Dibenzoyl Thiamine Chemical compound C=1C=CC=CC=1C(=O)OCC\C(SC(=O)C=1C=CC=CC=1)=C(/C)N(C=O)CC1=CN=C(C)N=C1N AZJUFRDUYTYIHV-NKFKGCMQSA-N 0.000 abstract description 4
- 208000008930 Low Back Pain Diseases 0.000 abstract description 3
- BTNNPSLJPBRMLZ-LGMDPLHJSA-N benfotiamine Chemical compound C=1C=CC=CC=1C(=O)SC(/CCOP(O)(O)=O)=C(/C)N(C=O)CC1=CN=C(C)N=C1N BTNNPSLJPBRMLZ-LGMDPLHJSA-N 0.000 abstract description 3
- 208000024891 symptom Diseases 0.000 abstract description 3
- 208000006820 Arthralgia Diseases 0.000 abstract description 2
- 208000034656 Contusions Diseases 0.000 abstract description 2
- 208000010040 Sprains and Strains Diseases 0.000 abstract description 2
- 238000010521 absorption reaction Methods 0.000 abstract description 2
- 150000001875 compounds Chemical class 0.000 abstract description 2
- 208000008035 Back Pain Diseases 0.000 abstract 1
- 206010024453 Ligament sprain Diseases 0.000 abstract 1
- 206010053156 Musculoskeletal discomfort Diseases 0.000 abstract 1
- 208000034526 bruise Diseases 0.000 abstract 1
- 239000011248 coating agent Substances 0.000 abstract 1
- 238000000576 coating method Methods 0.000 abstract 1
- 239000002674 ointment Substances 0.000 description 5
- 239000004020 conductor Substances 0.000 description 4
- 208000013465 muscle pain Diseases 0.000 description 4
- 229940088594 vitamin Drugs 0.000 description 4
- 229930003231 vitamin Natural products 0.000 description 4
- 235000013343 vitamin Nutrition 0.000 description 4
- 239000011782 vitamin Substances 0.000 description 4
- 208000002193 Pain Diseases 0.000 description 3
- 229930003270 Vitamin B Natural products 0.000 description 3
- 239000004615 ingredient Substances 0.000 description 3
- 210000001519 tissue Anatomy 0.000 description 3
- 235000019156 vitamin B Nutrition 0.000 description 3
- 239000011720 vitamin B Substances 0.000 description 3
- 150000003722 vitamin derivatives Chemical class 0.000 description 3
- PEDCQBHIVMGVHV-UHFFFAOYSA-N Glycerine Chemical compound OCC(O)CO PEDCQBHIVMGVHV-UHFFFAOYSA-N 0.000 description 2
- 208000012902 Nervous system disease Diseases 0.000 description 2
- 208000025966 Neurological disease Diseases 0.000 description 2
- 238000003287 bathing Methods 0.000 description 2
- 210000001035 gastrointestinal tract Anatomy 0.000 description 2
- OSWPMRLSEDHDFF-UHFFFAOYSA-N methyl salicylate Chemical compound COC(=O)C1=CC=CC=C1O OSWPMRLSEDHDFF-UHFFFAOYSA-N 0.000 description 2
- 239000000203 mixture Substances 0.000 description 2
- 230000001225 therapeutic effect Effects 0.000 description 2
- MGSRCZKZVOBKFT-UHFFFAOYSA-N thymol Chemical compound CC(C)C1=CC=C(C)C=C1O MGSRCZKZVOBKFT-UHFFFAOYSA-N 0.000 description 2
- 239000005995 Aluminium silicate Substances 0.000 description 1
- AUNGANRZJHBGPY-UHFFFAOYSA-N D-Lyxoflavin Natural products OCC(O)C(O)C(O)CN1C=2C=C(C)C(C)=CC=2N=C2C1=NC(=O)NC2=O AUNGANRZJHBGPY-UHFFFAOYSA-N 0.000 description 1
- BWGNESOTFCXPMA-UHFFFAOYSA-N Dihydrogen disulfide Chemical compound SS BWGNESOTFCXPMA-UHFFFAOYSA-N 0.000 description 1
- VEXZGXHMUGYJMC-UHFFFAOYSA-N Hydrochloric acid Chemical compound Cl VEXZGXHMUGYJMC-UHFFFAOYSA-N 0.000 description 1
- 229910002651 NO3 Inorganic materials 0.000 description 1
- NHNBFGGVMKEFGY-UHFFFAOYSA-N Nitrate Chemical compound [O-][N+]([O-])=O NHNBFGGVMKEFGY-UHFFFAOYSA-N 0.000 description 1
- 241000700159 Rattus Species 0.000 description 1
- AUNGANRZJHBGPY-SCRDCRAPSA-N Riboflavin Chemical compound OC[C@@H](O)[C@@H](O)[C@@H](O)CN1C=2C=C(C)C(C)=CC=2N=C2C1=NC(=O)NC2=O AUNGANRZJHBGPY-SCRDCRAPSA-N 0.000 description 1
- JZRWCGZRTZMZEH-UHFFFAOYSA-N Thiamine Natural products CC1=C(CCO)SC=[N+]1CC1=CN=C(C)N=C1N JZRWCGZRTZMZEH-UHFFFAOYSA-N 0.000 description 1
- 239000005844 Thymol Substances 0.000 description 1
- 229930003471 Vitamin B2 Natural products 0.000 description 1
- 230000037374 absorbed through the skin Effects 0.000 description 1
- 239000008186 active pharmaceutical agent Substances 0.000 description 1
- 235000012211 aluminium silicate Nutrition 0.000 description 1
- 125000003118 aryl group Chemical group 0.000 description 1
- 210000004369 blood Anatomy 0.000 description 1
- 239000008280 blood Substances 0.000 description 1
- 239000003795 chemical substances by application Substances 0.000 description 1
- 239000003086 colorant Substances 0.000 description 1
- 239000006071 cream Substances 0.000 description 1
- 229940079593 drug Drugs 0.000 description 1
- 238000002474 experimental method Methods 0.000 description 1
- 235000011187 glycerol Nutrition 0.000 description 1
- 238000010438 heat treatment Methods 0.000 description 1
- 239000007924 injection Substances 0.000 description 1
- 238000002347 injection Methods 0.000 description 1
- NLYAJNPCOHFWQQ-UHFFFAOYSA-N kaolin Chemical compound O.O.O=[Al]O[Si](=O)O[Si](=O)O[Al]=O NLYAJNPCOHFWQQ-UHFFFAOYSA-N 0.000 description 1
- 239000000865 liniment Substances 0.000 description 1
- 239000006210 lotion Substances 0.000 description 1
- 229960001047 methyl salicylate Drugs 0.000 description 1
- 239000003921 oil Substances 0.000 description 1
- 229940126701 oral medication Drugs 0.000 description 1
- 239000000546 pharmaceutical excipient Substances 0.000 description 1
- 239000003755 preservative agent Substances 0.000 description 1
- 229960002477 riboflavin Drugs 0.000 description 1
- 150000003839 salts Chemical class 0.000 description 1
- 239000003381 stabilizer Substances 0.000 description 1
- 230000009469 supplementation Effects 0.000 description 1
- KYMBYSLLVAOCFI-UHFFFAOYSA-N thiamine Chemical compound CC1=C(CCO)SCN1CC1=CN=C(C)N=C1N KYMBYSLLVAOCFI-UHFFFAOYSA-N 0.000 description 1
- 235000019157 thiamine Nutrition 0.000 description 1
- 239000011721 thiamine Substances 0.000 description 1
- 229960000790 thymol Drugs 0.000 description 1
- 235000019164 vitamin B2 Nutrition 0.000 description 1
- 239000011716 vitamin B2 Substances 0.000 description 1
- 239000000341 volatile oil Substances 0.000 description 1
- XLYOFNOQVPJJNP-UHFFFAOYSA-N water Substances O XLYOFNOQVPJJNP-UHFFFAOYSA-N 0.000 description 1
Abstract
Description
【発明の詳細な説明】
［産業上の利用分野コ
本発明は医療用として有用な外用剤に関し、詳しくは神
経痛、筋肉痛、Ｒ痛、肩こり、関節痛。DETAILED DESCRIPTION OF THE INVENTION [Industrial Field of Application] The present invention relates to an external preparation useful for medical purposes, specifically for neuralgia, muscle pain, R pain, stiff shoulders, and joint pain.
打身、捻挫等の治療および症状の緩和のため、シ部に塗
布あるいは湿布して使用し、脂溶性ビタミンＢ、誘導体
を局所的に経皮吸収させることにより、患部でのビタミ
ンＢ１濃度を高く維持して治療効果を高めるようにした
ビタミンＢ１含有外用剤に関する。For the treatment of bruises, sprains, etc. and alleviation of symptoms, apply it to the affected area or apply it as a poultice to increase the concentration of vitamin B1 in the affected area by locally absorbing fat-soluble vitamin B and derivatives through the skin. The present invention relates to an external preparation containing vitamin B1, which maintains the vitamin B1 content and enhances the therapeutic effect.
［従来の技術及び発明が解決しようとする課題］アリチ
アミンは、腸管からの吸収性３組織親和性に優れたビタ
ミンＢ２話導体（−５−５−Ｒ型）であり、ビタミンＢ
１の補給、神経痛、筋肉痛、腰痛。[Prior art and problems to be solved by the invention] Allithiamin is a vitamin B2 conductor (-5-5-R type) with excellent absorption from the intestinal tract and affinity for tissues.
1 supplementation, neuralgia, muscle pain, lower back pain.
肩こり等の症状の緩和の目的で内服剤、注射剤として広
く使用されている。従来、アリチアミンの用途は内用剤
に限られ、外用剤としてはまったく利用されていなかっ
たが、本発明者らはアリチアミンを外用的に用いた場合
、アリチアミンが経皮吸収されるという事実を見出し、
外用剤としての利用を図ることに成功した。It is widely used as an oral medication or injection to alleviate symptoms such as stiff shoulders. Conventionally, the use of allithiamine was limited to internal use and was not used at all as an external preparation, but the present inventors discovered the fact that allithiamine is absorbed transdermally when used externally. ,
We succeeded in using it as an external preparation.
しかしながら、アリチアミン以外にも脂溶性ビかった。However, other than allithiamin was also found to be fat-soluble.
神経痛、筋肉痛、＊痛、肩こり等の神経性疾患の治療に
はビタミンＢ１は有効であり、疾患部組織中のビタミン
Ｂ１濃度を高く維持することにより治療効果をより高め
ることが可能である。しかし、ビタミン８１話導体の内
服により腸管から物理的に吸収させて体全体の組織、血
中のビタミンＢ１濃度を十分に高めるには限界があった
。Vitamin B1 is effective in treating neurological diseases such as neuralgia, muscle pain, *pain, and stiff shoulders, and the therapeutic effect can be further enhanced by maintaining a high concentration of vitamin B1 in diseased tissue. However, there was a limit to the ability to physically absorb vitamin B1 from the intestinal tract and sufficiently increase the concentration of vitamin B1 in tissues and blood throughout the body by taking it orally.
［課題を解決するための手段］
本発明者らは、既にアリチアミンの浴用剤としての温浴
効果について研究し、このものに顕著なした。[Means for Solving the Problems] The present inventors have already studied the hot bathing effect of alithiamin as a bathing agent, and have found this to be remarkable.
その後、さらに研究を続け、アリチアミン以外の脂溶性
ビタミンＢ、誘導体にも同様の作用効果が認められるこ
とを見出し、これらもアリチアミンと同じく軟膏、パッ
プ剤等として用い、疾患部の皮膚に塗布又は貼付するこ
とにより、直接疾患部に吸収させ疾患部のみを高く維持
することが可能であることを知見し、本発明を完成する
に至った。Subsequently, further research was conducted and it was discovered that similar effects were observed in fat-soluble vitamin B and derivatives other than allithiamine.They were also used as ointments, poultices, etc., and applied or pasted onto the affected skin. By doing so, they discovered that it is possible to maintain a high level only in the diseased area by directly absorbing it into the diseased area, and have completed the present invention.
すなわち本発明は、アリチアミン以外の脂溶性ビタミン
８１銹導体を有効成分として含有することを特徴とする
外用剤を提供するものである。That is, the present invention provides an external preparation characterized by containing a fat-soluble vitamin 81 conductor other than alithiamin as an active ingredient.
本発明の外用剤に配合させる藤溶性ビタミン８１誘導体
は−Ｓ−Ｒ型および−０−Ｒ’型の化合物であり、たと
えばジベンゾイルチアミン（ＤＢＴ） 、 Ｓ−ベンゾ
イルチアミン・モノホスフェート（ＢＴＭＰ）、 ０−
３−ジカルブエトキシ・チアミン（ＤＣＥＴ）、 Ｏ−
ベベノ
ンゾイルチアミンジサルファイド（ＢＴＤＳ）などやこ
れらの塩類（たとえば塩酸塩、硝酸塩等）が挙げられる
。これらは単独又は２ ｆｉ以上を組み合わせて使用す
ることができる。なお、ビタミン８１話導体の配合量は
その使用目的等を考慮して適宜決定すればよい。The Fuji-soluble vitamin 81 derivatives to be incorporated into the external preparation of the present invention are -S-R type and -0-R' type compounds, such as dibenzoylthiamine (DBT), S-benzoylthiamine monophosphate (BTMP), 0-
3-dicarbuethoxy thiamine (DCET), O-
Examples include bebenonezoylthiamine disulfide (BTDS) and salts thereof (eg, hydrochloride, nitrate, etc.). These can be used alone or in combination of 2 fi or more. Incidentally, the amount of the vitamin 81 conductor to be blended may be appropriately determined in consideration of the purpose of use and the like.
また、本発明のビタミンＢ１話導体を配合できる外用剤
としては軟膏剤、硬軟剤、受刑、パップ剤、リニメント
剤、ローション剤、クリーム剤等が挙げられる。Further, examples of external preparations in which the vitamin B1 conductor of the present invention can be incorporated include ointments, softeners, poultices, liniments, lotions, creams, and the like.
これらの外用剤には一般に配合される医薬成分、生薬成
分、精油、芳香成分、ビタミン類１着色剤、保存剤、安
定剤、賦形剤等を適宜配合することが出来る。These external preparations can appropriately contain commonly used pharmaceutical ingredients, crude drug ingredients, essential oils, aromatic ingredients, vitamins, colorants, preservatives, stabilizers, excipients, and the like.
［実施例〕 次に、本発明を実施例により説明する。[Example〕 Next, the present invention will be explained by examples.
実施例１
単軟膏９５ｇをとり、水浴上で加温して溶した後、ＢＴ
ＤＳ５ ｇを加えてかき混ぜ、加温をやめて固まるまで
よくかき混ぜ、ＢＴＤＳを含有する軟膏１００ ｇを得
た。Example 1 Take 95g of a single ointment, heat it on a water bath to dissolve it, and then add BT
5 g of DS was added and stirred, and heating was stopped and the mixture was stirred well until solidified to obtain 100 g of ointment containing BTDS.
実施例２
カオリン５５ｇ 、 ＤＢＴ ５ ｇをとり、濃グリセ
リン４０ｇとよく混和し、チモール０．０５ｇ、サリチ
ル酸メチル０．２ｍ！ ′ＥＬびハツカ油０．０５ｍｊ
を加えて均等になるまでよく練り、パップ剤約１００ｇ
を得た。Example 2 Take 55 g of kaolin and 5 g of DBT, mix well with 40 g of concentrated glycerin, add 0.05 g of thymol, and 0.2 m of methyl salicylate! 'EL Bihatsuka Oil 0.05mj
Add it and knead it well until it is evenly distributed, and make about 100g of poultice.
I got it.
上記実施例で得た軟膏やパップ剤はラットを用いた実験
で疾患部から経皮吸収することを確認した。It was confirmed in experiments using rats that the ointments and poultices obtained in the above examples were absorbed transdermally from diseased areas.
［発明の効果］
本発明の外用剤は局所的に通用できるため、含有される
ビタミンＢ、誘導体が疾患部の皮膚から直接吸収され、
疾患部分のビタミンＢ１濃度を著しく高め、かつ維持す
るため、神経性疾患、特に神経痛、筋肉痛、腰痛、肩こ
り等の治療と痛みの緩和に浸れた効果を示す。[Effects of the Invention] Since the external preparation of the present invention can be used locally, the vitamin B and derivatives contained therein are directly absorbed through the skin of the diseased area.
Because it significantly increases and maintains the vitamin B1 concentration in diseased areas, it is effective in treating neurological diseases, especially neuralgia, muscle pain, lower back pain, stiff shoulders, etc., and alleviating pain.
Claims (1)
成分として含有する外用剤。An external preparation containing a fat-soluble vitamin B_1 derivative other than allithiamin as an active ingredient.
Priority Applications (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| JP5155088A JPH01226820A (en) | 1988-03-07 | 1988-03-07 | External medicine containing vitamin b1 derivative |
Applications Claiming Priority (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| JP5155088A JPH01226820A (en) | 1988-03-07 | 1988-03-07 | External medicine containing vitamin b1 derivative |
Publications (1)
| Publication Number | Publication Date |
|---|---|
| JPH01226820A true JPH01226820A (en) | 1989-09-11 |
Family
ID=12890122
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP5155088A Pending JPH01226820A (en) | 1988-03-07 | 1988-03-07 | External medicine containing vitamin b1 derivative |
Country Status (1)
| Country | Link |
|---|---|
| JP (1) | JPH01226820A (en) |
Cited By (1)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| JPH05221857A (en) * | 1992-02-14 | 1993-08-31 | Arakusu:Kk | Compounded antipyretic analgesic agent |
-
1988
- 1988-03-07 JP JP5155088A patent/JPH01226820A/en active Pending
Cited By (1)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| JPH05221857A (en) * | 1992-02-14 | 1993-08-31 | Arakusu:Kk | Compounded antipyretic analgesic agent |
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