JP2009108038A - Minoxidil-containing liquid for external use - Google Patents
Minoxidil-containing liquid for external use Download PDFInfo
- Publication number
- JP2009108038A JP2009108038A JP2008255904A JP2008255904A JP2009108038A JP 2009108038 A JP2009108038 A JP 2009108038A JP 2008255904 A JP2008255904 A JP 2008255904A JP 2008255904 A JP2008255904 A JP 2008255904A JP 2009108038 A JP2009108038 A JP 2009108038A
- Authority
- JP
- Japan
- Prior art keywords
- minoxidil
- liquid
- external
- ethanol
- hyaluronic acid
- 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.)
- Granted
Links
- 239000007788 liquid Substances 0.000 title claims abstract description 38
- ZFMITUMMTDLWHR-UHFFFAOYSA-N Minoxidil Chemical compound NC1=[N+]([O-])C(N)=CC(N2CCCCC2)=N1 ZFMITUMMTDLWHR-UHFFFAOYSA-N 0.000 title claims abstract description 34
- 229960003632 minoxidil Drugs 0.000 title claims abstract description 34
- LFQSCWFLJHTTHZ-UHFFFAOYSA-N Ethanol Chemical compound CCO LFQSCWFLJHTTHZ-UHFFFAOYSA-N 0.000 claims abstract description 52
- PUPZLCDOIYMWBV-UHFFFAOYSA-N (+/-)-1,3-Butanediol Chemical compound CC(O)CCO PUPZLCDOIYMWBV-UHFFFAOYSA-N 0.000 claims abstract description 38
- KIUKXJAPPMFGSW-DNGZLQJQSA-N (2S,3S,4S,5R,6R)-6-[(2S,3R,4R,5S,6R)-3-Acetamido-2-[(2S,3S,4R,5R,6R)-6-[(2R,3R,4R,5S,6R)-3-acetamido-2,5-dihydroxy-6-(hydroxymethyl)oxan-4-yl]oxy-2-carboxy-4,5-dihydroxyoxan-3-yl]oxy-5-hydroxy-6-(hydroxymethyl)oxan-4-yl]oxy-3,4,5-trihydroxyoxane-2-carboxylic acid Chemical compound CC(=O)N[C@H]1[C@H](O)O[C@H](CO)[C@@H](O)[C@@H]1O[C@H]1[C@H](O)[C@@H](O)[C@H](O[C@H]2[C@@H]([C@@H](O[C@H]3[C@@H]([C@@H](O)[C@H](O)[C@H](O3)C(O)=O)O)[C@H](O)[C@@H](CO)O2)NC(C)=O)[C@@H](C(O)=O)O1 KIUKXJAPPMFGSW-DNGZLQJQSA-N 0.000 claims abstract description 20
- 229920002674 hyaluronan Polymers 0.000 claims abstract description 20
- 229960003160 hyaluronic acid Drugs 0.000 claims abstract description 20
- 229940058015 1,3-butylene glycol Drugs 0.000 claims abstract description 19
- 235000019437 butane-1,3-diol Nutrition 0.000 claims abstract description 19
- XLYOFNOQVPJJNP-UHFFFAOYSA-N water Substances O XLYOFNOQVPJJNP-UHFFFAOYSA-N 0.000 claims abstract description 18
- 150000003839 salts Chemical class 0.000 claims abstract description 13
- 238000002360 preparation method Methods 0.000 claims description 28
- 238000000034 method Methods 0.000 claims description 4
- KRKNYBCHXYNGOX-UHFFFAOYSA-N citric acid Chemical compound OC(=O)CC(O)(C(O)=O)CC(O)=O KRKNYBCHXYNGOX-UHFFFAOYSA-N 0.000 description 18
- RTZKZFJDLAIYFH-UHFFFAOYSA-N Diethyl ether Chemical compound CCOCC RTZKZFJDLAIYFH-UHFFFAOYSA-N 0.000 description 16
- 239000000243 solution Substances 0.000 description 15
- 230000000052 comparative effect Effects 0.000 description 13
- 238000012360 testing method Methods 0.000 description 12
- 238000002156 mixing Methods 0.000 description 11
- 239000003795 chemical substances by application Substances 0.000 description 9
- NOOLISFMXDJSKH-KXUCPTDWSA-N (-)-Menthol Chemical compound CC(C)[C@@H]1CC[C@@H](C)C[C@H]1O NOOLISFMXDJSKH-KXUCPTDWSA-N 0.000 description 8
- ZAKOWWREFLAJOT-CEFNRUSXSA-N D-alpha-tocopherylacetate Chemical compound CC(=O)OC1=C(C)C(C)=C2O[C@@](CCC[C@H](C)CCC[C@H](C)CCCC(C)C)(C)CCC2=C1C ZAKOWWREFLAJOT-CEFNRUSXSA-N 0.000 description 8
- ZAKOWWREFLAJOT-UHFFFAOYSA-N d-alpha-Tocopheryl acetate Natural products CC(=O)OC1=C(C)C(C)=C2OC(CCCC(C)CCCC(C)CCCC(C)C)(C)CCC2=C1C ZAKOWWREFLAJOT-UHFFFAOYSA-N 0.000 description 8
- 239000008213 purified water Substances 0.000 description 8
- 229940042585 tocopherol acetate Drugs 0.000 description 8
- 239000003814 drug Substances 0.000 description 7
- DNIAPMSPPWPWGF-UHFFFAOYSA-N Propylene glycol Chemical compound CC(O)CO DNIAPMSPPWPWGF-UHFFFAOYSA-N 0.000 description 6
- 229920002385 Sodium hyaluronate Polymers 0.000 description 6
- 229940010747 sodium hyaluronate Drugs 0.000 description 6
- YWIVKILSMZOHHF-QJZPQSOGSA-N sodium;(2s,3s,4s,5r,6r)-6-[(2s,3r,4r,5s,6r)-3-acetamido-2-[(2s,3s,4r,5r,6r)-6-[(2r,3r,4r,5s,6r)-3-acetamido-2,5-dihydroxy-6-(hydroxymethyl)oxan-4-yl]oxy-2-carboxy-4,5-dihydroxyoxan-3-yl]oxy-5-hydroxy-6-(hydroxymethyl)oxan-4-yl]oxy-3,4,5-trihydroxyoxane-2- Chemical compound [Na+].CC(=O)N[C@H]1[C@H](O)O[C@H](CO)[C@@H](O)[C@@H]1O[C@H]1[C@H](O)[C@@H](O)[C@H](O[C@H]2[C@@H]([C@@H](O[C@H]3[C@@H]([C@@H](O)[C@H](O)[C@H](O3)C(O)=O)O)[C@H](O)[C@@H](CO)O2)NC(C)=O)[C@@H](C(O)=O)O1 YWIVKILSMZOHHF-QJZPQSOGSA-N 0.000 description 6
- 239000000203 mixture Substances 0.000 description 5
- CIWBSHSKHKDKBQ-JLAZNSOCSA-N Ascorbic acid Chemical compound OC[C@H](O)[C@H]1OC(=O)C(O)=C1O CIWBSHSKHKDKBQ-JLAZNSOCSA-N 0.000 description 4
- PEDCQBHIVMGVHV-UHFFFAOYSA-N Glycerine Chemical compound OCC(O)CO PEDCQBHIVMGVHV-UHFFFAOYSA-N 0.000 description 4
- 230000000694 effects Effects 0.000 description 4
- 238000011156 evaluation Methods 0.000 description 4
- 230000001953 sensory effect Effects 0.000 description 4
- VEXZGXHMUGYJMC-UHFFFAOYSA-N Hydrochloric acid Chemical compound Cl VEXZGXHMUGYJMC-UHFFFAOYSA-N 0.000 description 3
- 210000003128 head Anatomy 0.000 description 3
- 239000002904 solvent Substances 0.000 description 3
- 239000002562 thickening agent Substances 0.000 description 3
- YBJHBAHKTGYVGT-ZKWXMUAHSA-N (+)-Biotin Chemical compound N1C(=O)N[C@@H]2[C@H](CCCCC(=O)O)SC[C@@H]21 YBJHBAHKTGYVGT-ZKWXMUAHSA-N 0.000 description 2
- RGHNJXZEOKUKBD-SQOUGZDYSA-N D-gluconic acid Chemical compound OC[C@@H](O)[C@@H](O)[C@H](O)[C@@H](O)C(O)=O RGHNJXZEOKUKBD-SQOUGZDYSA-N 0.000 description 2
- NOOLISFMXDJSKH-UHFFFAOYSA-N DL-menthol Natural products CC(C)C1CCC(C)CC1O NOOLISFMXDJSKH-UHFFFAOYSA-N 0.000 description 2
- FWKQNCXZGNBPFD-UHFFFAOYSA-N Guaiazulene Chemical compound CC(C)C1=CC=C(C)C2=CC=C(C)C2=C1 FWKQNCXZGNBPFD-UHFFFAOYSA-N 0.000 description 2
- NBIIXXVUZAFLBC-UHFFFAOYSA-N Phosphoric acid Chemical compound OP(O)(O)=O NBIIXXVUZAFLBC-UHFFFAOYSA-N 0.000 description 2
- XSQUKJJJFZCRTK-UHFFFAOYSA-N Urea Chemical compound NC(N)=O XSQUKJJJFZCRTK-UHFFFAOYSA-N 0.000 description 2
- OIRDTQYFTABQOQ-KQYNXXCUSA-N adenosine Chemical compound C1=NC=2C(N)=NC=NC=2N1[C@@H]1O[C@H](CO)[C@@H](O)[C@H]1O OIRDTQYFTABQOQ-KQYNXXCUSA-N 0.000 description 2
- 235000010323 ascorbic acid Nutrition 0.000 description 2
- 229960005070 ascorbic acid Drugs 0.000 description 2
- 239000011668 ascorbic acid Substances 0.000 description 2
- KVYGGMBOZFWZBQ-UHFFFAOYSA-N benzyl nicotinate Chemical compound C=1C=CN=CC=1C(=O)OCC1=CC=CC=C1 KVYGGMBOZFWZBQ-UHFFFAOYSA-N 0.000 description 2
- RMRCNWBMXRMIRW-BYFNXCQMSA-M cyanocobalamin Chemical compound N#C[Co+]N([C@]1([H])[C@H](CC(N)=O)[C@]\2(CCC(=O)NC[C@H](C)OP(O)(=O)OC3[C@H]([C@H](O[C@@H]3CO)N3C4=CC(C)=C(C)C=C4N=C3)O)C)C/2=C(C)\C([C@H](C/2(C)C)CCC(N)=O)=N\C\2=C\C([C@H]([C@@]/2(CC(N)=O)C)CCC(N)=O)=N\C\2=C(C)/C2=N[C@]1(C)[C@@](C)(CC(N)=O)[C@@H]2CCC(N)=O RMRCNWBMXRMIRW-BYFNXCQMSA-M 0.000 description 2
- 230000007423 decrease Effects 0.000 description 2
- -1 etc.) Substances 0.000 description 2
- 239000000284 extract Substances 0.000 description 2
- 239000003205 fragrance Substances 0.000 description 2
- 235000011187 glycerol Nutrition 0.000 description 2
- 230000003779 hair growth Effects 0.000 description 2
- 239000003676 hair preparation Substances 0.000 description 2
- JVTAAEKCZFNVCJ-UHFFFAOYSA-N lactic acid Chemical compound CC(O)C(O)=O JVTAAEKCZFNVCJ-UHFFFAOYSA-N 0.000 description 2
- 229940041616 menthol Drugs 0.000 description 2
- 239000003002 pH adjusting agent Substances 0.000 description 2
- YGSDEFSMJLZEOE-UHFFFAOYSA-N salicylic acid Chemical compound OC(=O)C1=CC=CC=C1O YGSDEFSMJLZEOE-UHFFFAOYSA-N 0.000 description 2
- GEHJYWRUCIMESM-UHFFFAOYSA-L sodium sulfite Chemical compound [Na+].[Na+].[O-]S([O-])=O GEHJYWRUCIMESM-UHFFFAOYSA-L 0.000 description 2
- 150000005846 sugar alcohols Polymers 0.000 description 2
- 239000004094 surface-active agent Substances 0.000 description 2
- DSSYKIVIOFKYAU-XCBNKYQSSA-N (R)-camphor Chemical compound C1C[C@@]2(C)C(=O)C[C@@H]1C2(C)C DSSYKIVIOFKYAU-XCBNKYQSSA-N 0.000 description 1
- HMUNWXXNJPVALC-UHFFFAOYSA-N 1-[4-[2-(2,3-dihydro-1H-inden-2-ylamino)pyrimidin-5-yl]piperazin-1-yl]-2-(2,4,6,7-tetrahydrotriazolo[4,5-c]pyridin-5-yl)ethanone Chemical compound C1C(CC2=CC=CC=C12)NC1=NC=C(C=N1)N1CCN(CC1)C(CN1CC2=C(CC1)NN=N2)=O HMUNWXXNJPVALC-UHFFFAOYSA-N 0.000 description 1
- SPSPIUSUWPLVKD-UHFFFAOYSA-N 2,3-dibutyl-6-methylphenol Chemical compound CCCCC1=CC=C(C)C(O)=C1CCCC SPSPIUSUWPLVKD-UHFFFAOYSA-N 0.000 description 1
- CIVCELMLGDGMKZ-UHFFFAOYSA-N 2,4-dichloro-6-methylpyridine-3-carboxylic acid Chemical compound CC1=CC(Cl)=C(C(O)=O)C(Cl)=N1 CIVCELMLGDGMKZ-UHFFFAOYSA-N 0.000 description 1
- VZSRBBMJRBPUNF-UHFFFAOYSA-N 2-(2,3-dihydro-1H-inden-2-ylamino)-N-[3-oxo-3-(2,4,6,7-tetrahydrotriazolo[4,5-c]pyridin-5-yl)propyl]pyrimidine-5-carboxamide Chemical compound C1C(CC2=CC=CC=C12)NC1=NC=C(C=N1)C(=O)NCCC(N1CC2=C(CC1)NN=N2)=O VZSRBBMJRBPUNF-UHFFFAOYSA-N 0.000 description 1
- WZFUQSJFWNHZHM-UHFFFAOYSA-N 2-[4-[2-(2,3-dihydro-1H-inden-2-ylamino)pyrimidin-5-yl]piperazin-1-yl]-1-(2,4,6,7-tetrahydrotriazolo[4,5-c]pyridin-5-yl)ethanone Chemical compound C1C(CC2=CC=CC=C12)NC1=NC=C(C=N1)N1CCN(CC1)CC(=O)N1CC2=C(CC1)NN=N2 WZFUQSJFWNHZHM-UHFFFAOYSA-N 0.000 description 1
- ZIMGGGWCDYVHOY-UHFFFAOYSA-N 3-hydroxy-2-imino-6-(1-piperidinyl)-4-pyrimidinamine Chemical compound N=C1N(O)C(N)=CC(N2CCCCC2)=N1 ZIMGGGWCDYVHOY-UHFFFAOYSA-N 0.000 description 1
- IJALWSVNUBBQRA-UHFFFAOYSA-N 4-Isopropyl-3-methylphenol Chemical compound CC(C)C1=CC=C(O)C=C1C IJALWSVNUBBQRA-UHFFFAOYSA-N 0.000 description 1
- HBTAOSGHCXUEKI-UHFFFAOYSA-N 4-chloro-n,n-dimethyl-3-nitrobenzenesulfonamide Chemical compound CN(C)S(=O)(=O)C1=CC=C(Cl)C([N+]([O-])=O)=C1 HBTAOSGHCXUEKI-UHFFFAOYSA-N 0.000 description 1
- HIQIXEFWDLTDED-UHFFFAOYSA-N 4-hydroxy-1-piperidin-4-ylpyrrolidin-2-one Chemical compound O=C1CC(O)CN1C1CCNCC1 HIQIXEFWDLTDED-UHFFFAOYSA-N 0.000 description 1
- SQDAZGGFXASXDW-UHFFFAOYSA-N 5-bromo-2-(trifluoromethoxy)pyridine Chemical compound FC(F)(F)OC1=CC=C(Br)C=N1 SQDAZGGFXASXDW-UHFFFAOYSA-N 0.000 description 1
- 239000002126 C01EB10 - Adenosine Substances 0.000 description 1
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- 235000007862 Capsicum baccatum Nutrition 0.000 description 1
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- RGHNJXZEOKUKBD-UHFFFAOYSA-N D-gluconic acid Natural products OCC(O)C(O)C(O)C(O)C(O)=O RGHNJXZEOKUKBD-UHFFFAOYSA-N 0.000 description 1
- SNPLKNRPJHDVJA-ZETCQYMHSA-N D-panthenol Chemical compound OCC(C)(C)[C@@H](O)C(=O)NCCCO SNPLKNRPJHDVJA-ZETCQYMHSA-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
- ZGTMUACCHSMWAC-UHFFFAOYSA-L EDTA disodium salt (anhydrous) Chemical compound [Na+].[Na+].OC(=O)CN(CC([O-])=O)CCN(CC(O)=O)CC([O-])=O ZGTMUACCHSMWAC-UHFFFAOYSA-L 0.000 description 1
- 235000006679 Mentha X verticillata Nutrition 0.000 description 1
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- 235000001636 Mentha x rotundifolia Nutrition 0.000 description 1
- 239000004909 Moisturizer Substances 0.000 description 1
- NWBJYWHLCVSVIJ-UHFFFAOYSA-N N-benzyladenine Chemical compound N=1C=NC=2NC=NC=2C=1NCC1=CC=CC=C1 NWBJYWHLCVSVIJ-UHFFFAOYSA-N 0.000 description 1
- 244000178231 Rosmarinus officinalis Species 0.000 description 1
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- 240000002299 Symphytum officinale Species 0.000 description 1
- 235000005865 Symphytum officinale Nutrition 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
- 239000002253 acid Substances 0.000 description 1
- 239000012190 activator Substances 0.000 description 1
- 239000004480 active ingredient Substances 0.000 description 1
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- 239000000443 aerosol Substances 0.000 description 1
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- 235000020958 biotin Nutrition 0.000 description 1
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- 229950003631 carpronium chloride Drugs 0.000 description 1
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- YZIYKJHYYHPJIB-UUPCJSQJSA-N chlorhexidine gluconate Chemical compound OC[C@@H](O)[C@@H](O)[C@H](O)[C@@H](O)C(O)=O.OC[C@@H](O)[C@@H](O)[C@H](O)[C@@H](O)C(O)=O.C1=CC(Cl)=CC=C1NC(=N)NC(=N)NCCCCCCNC(=N)NC(=N)NC1=CC=C(Cl)C=C1 YZIYKJHYYHPJIB-UUPCJSQJSA-N 0.000 description 1
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- 235000015165 citric acid Nutrition 0.000 description 1
- 238000007796 conventional method Methods 0.000 description 1
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- 229960000525 diphenhydramine hydrochloride Drugs 0.000 description 1
- 229940079593 drug Drugs 0.000 description 1
- 238000001035 drying Methods 0.000 description 1
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Images
Abstract
Description
本発明は、ミノキシジルを有効成分とする外用液剤に関し、医薬品及び医薬部外品の分野に応用することができる。 The present invention relates to an external solution containing minoxidil as an active ingredient, and can be applied to the fields of pharmaceuticals and quasi drugs.
ミノキシジルは化学名を６−（１−ピペリジニル）−２，４−ピリミジンジアミン−３−オキサイドと称し、育毛剤としての適応が知られている（特許文献１参照）。そして、ミノキシジル含有外用液剤を提供するためには、ミノキシジルが水に溶解しないため、ミノキシジルを溶解させる性質を有する溶媒、例えばアルコールの配合が必須となる。しかし、ミノキシジル含有外用液剤を頭部に塗布する場合には、液だれによる目への混入、それに伴うアルコールの眼への刺激が懸念される。この液だれを防止する方法としては、粘ちょう化剤の配合が試みられるが、べたつきが強く感じられ、乾燥の遅さ等の使用感上の課題があった。 Minoxidil has a chemical name of 6- (1-piperidinyl) -2,4-pyrimidinediamine-3-oxide and is known to be used as a hair restorer (see Patent Document 1). In order to provide a minoxidil-containing external preparation, since minoxidil does not dissolve in water, a solvent having a property of dissolving minoxidil, such as an alcohol, is essential. However, when a minoxidil-containing external preparation is applied to the head, there is a concern about dripping into the eyes due to dripping and accompanying alcohol irritation to the eyes. As a method for preventing such dripping, a thickener is tried, but stickiness is felt strongly, and there are problems in use feeling such as slow drying.
ここで、ヒアルロン酸は優れた保水力をもち、希薄な溶液でも粘ちょうなゲルを形成する事が知られている（非特許文献１参照）。また、保湿剤としての効果を発揮するため、比較的高濃度のヒアルロン酸を配合した製剤が知られている（特許文献２参照）。 Here, it is known that hyaluronic acid has an excellent water retention ability and forms a viscous gel even in a dilute solution (see Non-Patent Document 1). Moreover, in order to exhibit the effect as a humectant, the formulation which mix | blended comparatively high concentration hyaluronic acid is known (refer patent document 2).
しかし、ヒアルロン酸は添加の際にゲル形成能力により、粘度が上昇する一方で、べたつき感等の、粘ちょう化剤が有するのと同様な課題があった。 However, while hyaluronic acid is added, its viscosity increases due to its ability to form a gel, but there are problems similar to those of a thickening agent such as stickiness.
本発明の目的は、粘ちょう化剤のもつ短所を伴わずに、液だれしない外用液剤を提供することであり、べたつき感が少なく使用感が良好なミノキシジル含有外用液剤を提供することである。 An object of the present invention is to provide a liquid preparation for external use which does not spill without accompanying the disadvantages of a thickening agent, and to provide a liquid preparation containing minoxidil which has little stickiness and good usability.
本発明者らは、上記課題を解決すべく鋭意研究を行った結果、ミノキシジル含有エタノール含水液剤に、ヒアルロン酸又はその塩、及び特定の多価アルコールを配合することにより、液だれし難く、良好な使用感を保持したミノキシジル含有外用液剤が得られることを見出し、本発明を完成した。 As a result of diligent research to solve the above-mentioned problems, the inventors have found that it is difficult to dripping by blending hyaluronic acid or a salt thereof and a specific polyhydric alcohol into a minoxidil-containing ethanol water-containing liquid. The present invention was completed by finding that a minoxidil-containing external preparation containing an excellent feeling of use was obtained.
すなわち本発明は、
（１）ミノキシジル、ヒアルロン酸又はその塩、１，３−ブチレングリコール、エタノール及び水を含有することを特徴とする外用液剤、
（２）ヒアルロン酸又はその塩の含有量が０．００５〜０．０２ｗ/ｖ％である（１）記載の外用液剤、
（３）１，３−ブチレングリコールの含有量が５〜３０ｗ/ｖ％である（１）又は（２）に記載の外用液剤、
（４）水の含有量が５〜３０ｗ/ｖ％である（１）〜（３）の何れか１つに記載の外用液剤、
（５）エタノールの含有量が２５〜７０ｗ/ｖ％である（１）〜（４）の何れか１つに記載の外用液剤、
（６）ｐＨが５．５〜９．５である（１）〜（５）の何れか１つに記載の外用液剤、
（７）ミノキシジル、エタノール及び水を含有する外用液剤において、ヒアルロン酸又はその塩及び１，３−ブチレングリコールを配合することにより液だれを防止する方法、である。
That is, the present invention
(1) A liquid preparation for external use comprising minoxidil, hyaluronic acid or a salt thereof, 1,3-butylene glycol, ethanol and water,
(2) External liquid preparation according to (1), wherein the content of hyaluronic acid or a salt thereof is 0.005 to 0.02 w / v%,
(3) The external solution according to (1) or (2), wherein the content of 1,3-butylene glycol is 5 to 30 w / v%,
(4) External liquid agent as described in any one of (1)-(3) whose content of water is 5-30 w / v%,
(5) External liquid formulation as described in any one of (1)-(4) whose content of ethanol is 25-70 w / v%,
(6) The external preparation according to any one of (1) to (5), wherein the pH is 5.5 to 9.5,
(7) A method for preventing dripping by blending hyaluronic acid or a salt thereof and 1,3-butylene glycol in an external liquid preparation containing minoxidil, ethanol and water.
本発明により、液だれをしない、良好な使用感を保持したミノキシジル含有外用液剤を提供することができた。 INDUSTRIAL APPLICABILITY According to the present invention, it was possible to provide a minoxidil-containing external preparation that does not sag and retains a good feeling of use.
本発明を以下に詳細に説明する。 The present invention is described in detail below.
ミノキシジルを含有するエタノール含水溶液の液だれを抑制するために、ヒアルロン酸又はその塩、及び１，３−ブチレングリコールを配合したところ、粘ちょう性の増加に伴うべたつき感等の使用感低下は生じず、液だれをしにくいミノキシジル含有外用液剤を得ることができた。 When hyaluronic acid or its salt and 1,3-butylene glycol are blended in order to suppress dripping of an aqueous solution containing ethanol containing minoxidil, a decrease in feeling of use such as stickiness accompanying an increase in stickiness occurs. In addition, a minoxidil-containing external preparation that hardly drips liquid could be obtained.
本発明において、ミノキシジルの配合（含有）量は特に限定されないが、発毛効果を十分期待できる１ｗ／ｖ％以上が好ましく、１〜１０ｗ/ｖ％がより好ましい。用いるミノキシジルは、通常医薬品に用いられる品質のものを適宜使用することができる。 In the present invention, the blending (content) amount of minoxidil is not particularly limited, but is preferably 1 w / v% or more, and more preferably 1 to 10 w / v%, from which a hair growth effect can be sufficiently expected. As the minoxidil to be used, those having the quality usually used for pharmaceuticals can be appropriately used.
ヒアルロン酸の塩としては、例えばナトリウム塩が挙げられる。ヒアルロン酸又はその塩の配合（含有）量は、液剤中０．００５〜０．０２ｗ/ｖ％が好ましい。ヒアルロン酸の分子量は特に限定されないが、扱いやすさなどの面から５０万から２００万が好ましい。また、用いるヒアルロン酸又はその塩は、通常医薬品に用いられる品質のものを適宜使用することができる。 Examples of the salt of hyaluronic acid include a sodium salt. The blending (content) amount of hyaluronic acid or a salt thereof is preferably 0.005 to 0.02 w / v% in the liquid. The molecular weight of hyaluronic acid is not particularly limited, but is preferably 500,000 to 2,000,000 in terms of ease of handling. Moreover, the hyaluronic acid or its salt to be used can be used as appropriate in quality usually used for pharmaceuticals.
エタノールの配合（含有）量は、液剤中２５〜７０ｗ/ｖ％、水の配合（含有）量は、液剤中５〜３０ｗ/ｖ％とすることが好ましく、１，３−ブチレングリコールの配合（含有）量は、液剤中５〜３０ｗ/ｖ％が好ましく、更に好ましくは液剤中５〜２０ｗ/ｖ％である。用いるエタノール、水及び１，３−ブチレングリコールにおいては、それぞれ医薬品に用いられる品質のものを適宜使用することができる。 The blending (containment) amount of ethanol is preferably 25 to 70 w / v% in the liquid agent, and the blending (containment) amount of water is preferably 5 to 30 w / v% in the liquid agent, and the blending of 1,3-butylene glycol ( The content is preferably 5 to 30 w / v% in the liquid, and more preferably 5 to 20 w / v% in the liquid. As ethanol, water and 1,3-butylene glycol to be used, those of quality used for pharmaceuticals can be appropriately used.
本発明液剤のｐＨは、５．５〜９．５の範囲とすることが好ましく、特に、中性である６〜８の範囲とすることがより好ましい。液剤のｐＨ調整には、適当な酸及び／又は塩基をｐＨ調整剤として使用することができ、ｐＨ調整剤の例としては、クエン酸、塩酸、乳酸、リン酸、酒石酸、及びグルコン酸等を使用することができ、それぞれ医薬品に用いられる品質のものを適宜使用することができる。 The pH of the solution of the present invention is preferably in the range of 5.5 to 9.5, and more preferably in the range of 6 to 8 which is neutral. For adjusting the pH of the solution, an appropriate acid and / or base can be used as the pH adjuster. Examples of the pH adjuster include citric acid, hydrochloric acid, lactic acid, phosphoric acid, tartaric acid, and gluconic acid. These can be used, and those of the quality used for pharmaceuticals can be used as appropriate.
更に、本発明液剤に配合することができる成分としては、メントール、ビタミンＥアセテート、及びパントテニールエチルエーテルから成る群より選ばれる成分（以下、「選択成分」という）が挙げられ、その配合量に特に制約はなく、使用感やミノキシジルの安定性等を考慮しながら定めることができ、例えば、メントールは液剤中０．２〜０．４ｗ/ｖ％、ビタミンＥアセテートは液剤中０．０１〜０．１５ｗ/ｖ％、パントテニールエチルエーテルは液剤中０．５〜１．５ｗ/ｖ％となるよう配合することができる。用いる選択成分は、それぞれ医薬品に用いられる品質のものを適宜使用することができる。 Furthermore, as a component which can be mix | blended with this invention liquid, the component (henceforth a "selective component") chosen from the group which consists of menthol, vitamin E acetate, and pantotenyl ethyl ether is mentioned, There is no restriction in particular, and it can be determined taking into consideration the feeling of use and the stability of minoxidil. For example, menthol is 0.2 to 0.4 w / v% in the liquid, and vitamin E acetate is 0.01 to 0 in the liquid. .15 w / v%, pantotenyl ethyl ether can be blended so as to be 0.5 to 1.5 w / v% in the liquid. As the selection components to be used, those of the quality used for pharmaceuticals can be used as appropriate.
本発明の液剤においては、上記した成分の他、一般の外用剤に使用される種々の成分、賦形剤、育毛成分（６−ベンジルアミノプリン、アデノシン、ペンタデカン酸グリセリド、何首鳥、竹節人参等）、血管拡張剤（塩化カルプロニウム、ニコチン酸ベンジル、センブリ抽出液、オタネニンジンエキス、トウガラシチンキ等）、抗ヒスタミン剤（塩酸ジフェンヒドラミン、塩酸イソチペンジル等）、抗炎症剤（グアイアズレン等）、角質溶解剤（尿素、サリチル酸等）、殺菌剤（グルコン酸クロルヘキシジン、イソプロピルメチルフェノール、第４級アンモニウム塩、ピロクトンオラミン等）、保湿剤（コンドロイチン硫酸等）、各種動植物（イチイ、ボタンピ、カンゾウ、オトギリソウ、附子、ビワ、カワラヨモギ、コンフリー、アシタバ、サフラン、サンシシ、ローズマリー、セージ、モッコウ、セイモッコウ、ホップ、プラセンタ等）からの抽出物、ビタミン類（酢酸レチノール、アスコルビン酸、硝酸チアミン、シアノコバラミン、ビオチン等）、抗酸化剤（ジブチルヒドロキシトルエン、ピロ亜硫酸ナトリウム、トコフェロール、エデト酸ナトリウム、アスコルビン酸、イソプロピルガレート等）、溶解補助剤（アジピン酸ジイソプロピル、ミリスチン酸イソプロピル、各種植物油、各種動物油、炭化水素類等）、代謝賦活剤（パンテノール等）、高分子（カルボキシビニルポリマー等）、粘着剤、香料、清涼化剤（ハッカ油、カンフル等）、及び染料等の通常使用される成分を本発明の効果を損なわない範囲で配合することができる。しかしながら、界面活性剤の添加は、ミノキシジルの皮膚吸収に影響を与えるため、本発明の液剤は実質的に界面活性剤を含まないものとすることが好ましい。 In the liquid preparation of the present invention, in addition to the above-mentioned components, various components, excipients, and hair-growth components (6-benzylaminopurine, adenosine, pentadecanoic acid glyceride, chicks ), Vasodilators (carpronium chloride, benzyl nicotinate, assembly extract, ginseng extract, red pepper tincture, etc.), antihistamines (diphenhydramine hydrochloride, isotipezil hydrochloride, etc.), anti-inflammatory agents (guaiazulene, etc.), keratolytic agents (urea, Salicylic acid, etc.), bactericides (chlorhexidine gluconate, isopropylmethylphenol, quaternary ammonium salts, piroctone olamine, etc.), moisturizers (chondroitin sulfate, etc.) , Kawaramugi, Comfrey, Ashitaba Extracts from saffron, sanshishi, rosemary, sage, mokko, seimokko, hop, placenta, etc., vitamins (retinol acetate, ascorbic acid, thiamine nitrate, cyanocobalamin, biotin, etc.), antioxidants (dibutylhydroxytoluene, pyro Sodium sulfite, tocopherol, sodium edetate, ascorbic acid, isopropyl gallate, etc.), solubilizers (diisopropyl adipate, isopropyl myristate, various vegetable oils, various animal oils, hydrocarbons, etc.), metabolic activators (pantenol, etc.), Commonly used components such as a polymer (carboxyvinyl polymer, etc.), an adhesive, a fragrance, a refreshing agent (mint oil, camphor, etc.), and a dye can be blended within a range that does not impair the effects of the present invention. However, since the addition of a surfactant affects the skin absorption of minoxidil, it is preferable that the liquid preparation of the present invention does not substantially contain a surfactant.
本発明の液剤の調製は、常法に従い、上記各成分を配合することにより調製される。例えば、ミノキシジル、ヒアルロン酸又はその塩、１，３−ブチレングリコール及びエタノールを含む各成分を混合し、溶解した後、ｐＨを調製し、更に精製水を加えて容量調整し、必要に応じて濾過を行うことにより目的のミノキシジル含有外用液剤を得ることができる。 The liquid preparation of the present invention is prepared by blending each of the above components according to a conventional method. For example, after mixing and dissolving each component including minoxidil, hyaluronic acid or its salt, 1,3-butylene glycol and ethanol, adjust the pH, adjust the volume by adding purified water, and filter as necessary. By carrying out the above, the desired minoxidil-containing external preparation can be obtained.
かくして得られる本発明の液剤は、ローション剤、エアゾール剤、トニック剤等の適当な外用液剤、より具体的には頭髪用剤、皮膚適用製剤等として使用することができる。 The liquid preparation of the present invention thus obtained can be used as an appropriate external liquid preparation such as a lotion preparation, an aerosol preparation or a tonic preparation, more specifically as a hair preparation, a skin application preparation or the like.
以下に実施例を挙げ、本発明をさらに具体的に説明するが、本発明はこれら実施例等により何ら制約されるものではない。なおヒアルロン酸ナトリウムは、分子量が５０万から２００万のものを使用した。 The present invention will be described more specifically with reference to the following examples. However, the present invention is not limited by these examples. Sodium hyaluronate having a molecular weight of 500,000 to 2,000,000 was used.
実施例１
ミノキシジル１ｇ、Ｌ−メントール０．３ｇ、ビタミンＥアセテート０．０８ｇ、パントテニールエチルエーテル１ｇ、ヒアルロン酸ナトリウム０．０１７ｇ、１，３−ブチレングリコール１０ｇ、およびエタノール６０ｇを混合、撹枠して溶解し、クエン酸を適量添加しｐＨを８に調整した後、精製水を加えて１００ｍＬとし、液剤を得た。
Example 1
1 g of minoxidil, 0.3 g of L-menthol, 0.08 g of vitamin E acetate, 1 g of pantotenyl ethyl ether, 0.017 g of sodium hyaluronate, 10 g of 1,3-butylene glycol, and 60 g of ethanol are mixed, stirred and dissolved. Then, an appropriate amount of citric acid was added to adjust the pH to 8, and then purified water was added to make 100 mL to obtain a solution.
実施例２
ミノキシジル１ｇ、Ｌ−メントール０．３ｇ、ビタミンＥアセテート０．０８ｇ、パントテニールエチルエーテル１ｇ、ヒアルロン酸ナトリウム０．００５ｇ、１，３−ブチレングリコール１０ｇ、およびエタノール６０ｇを混合、撹枠して溶解し、クエン酸を適量添加しｐＨを８に調整した後、精製水を加えて１００ｍＬとし、液剤を得た。
Example 2
1 g of minoxidil, 0.3 g of L-menthol, 0.08 g of vitamin E acetate, 1 g of pantotenyl ethyl ether, 0.005 g of sodium hyaluronate, 10 g of 1,3-butylene glycol, and 60 g of ethanol are mixed and stirred to dissolve. Then, an appropriate amount of citric acid was added to adjust the pH to 8, and then purified water was added to make 100 mL to obtain a solution.
比較例１
ミノキシジル１ｇ、Ｌ−メントール０．３ｇ、ビタミンＥアセテート０．０８ｇ、パントテニールエチルエーテル１ｇ、１，３−ブチレングリコール１０ｇ、およびエタノール６０ｇを混合、撹枠して溶解し、クエン酸を適量添加しｐＨを８に調整した後、精製水を加えて１００ｍＬとし、液剤を得た。
比較例２
ミノキシジル１ｇ、プロピレングリコール１０ｇ、およびエタノール６０ｇを混合、撹枠して溶解した後、精製水を加えて１００ｍＬとし、液剤を得た。
比較例３
ミノキシジル１ｇ、Ｌ−メントール０．３ｇ、ビタミンＥアセテート０．０８ｇ、パントテニールエチルエーテル１ｇ、ヒアルロン酸ナトリウム０．００２ｇ、１，３−ブチレングリコール１０ｇ、およびエタノール６０ｇを混合、撹枠して溶解し、クエン酸を適量添加しｐＨを８に調整した後、精製水を加えて１００ｍＬとし、液剤を得た。
比較例４
ミノキシジル１ｇ、Ｌ−メントール０．３ｇ、ビタミンＥアセテート０．０８ｇ、パントテニールエチルエーテル１ｇ、ヒアルロン酸ナトリウム０．０６ｇ、１，３−ブチレングリコール１０ｇ、およびエタノール６０ｇを混合、撹枠して溶解し、クエン酸を適量添加しｐＨを８に調整した後、精製水を加えて１００ｍＬとし、液剤を得た。
比較例５
ミノキシジル１ｇ、Ｌ−メントール０．３ｇ、ビタミンＥアセテート０．０８ｇ、パントテニールエチルエーテル１ｇ、ヒアルロン酸ナトリウム０．０１７ｇ、グリセリン１０ｇ、およびエタノール６０ｇを混合、撹枠して溶解し、クエン酸を適量添加しｐＨを８に調整した後、精製水を加えて１００ｍＬとし、液剤を得た。
Comparative Example 1
Mix 1 g of minoxidil, 0.3 g of L-menthol, 0.08 g of vitamin E acetate, 1 g of pantotenyl ethyl ether, 10 g of 1,3-butylene glycol and 60 g of ethanol, dissolve them in a stirring frame, and add an appropriate amount of citric acid. After adjusting the pH to 8, purified water was added to 100 mL to obtain a liquid.
Comparative Example 2
1 g of minoxidil, 10 g of propylene glycol, and 60 g of ethanol were mixed, stirred and dissolved, and then purified water was added to make 100 mL to obtain a solution.
Comparative Example 3
1 g of minoxidil, 0.3 g of L-menthol, 0.08 g of vitamin E acetate, 1 g of pantotenyl ethyl ether, 0.002 g of sodium hyaluronate, 10 g of 1,3-butylene glycol, and 60 g of ethanol are mixed, stirred and dissolved. Then, an appropriate amount of citric acid was added to adjust the pH to 8, and then purified water was added to make 100 mL to obtain a solution.
Comparative Example 4
1 g of minoxidil, 0.3 g of L-menthol, 0.08 g of vitamin E acetate, 1 g of pantotenyl ethyl ether, 0.06 g of sodium hyaluronate, 10 g of 1,3-butylene glycol, and 60 g of ethanol are mixed, stirred and dissolved. Then, an appropriate amount of citric acid was added to adjust the pH to 8, and then purified water was added to make 100 mL to obtain a solution.
Comparative Example 5
Mix 1 g of minoxidil, 0.3 g of L-menthol, 0.08 g of vitamin E acetate, 1 g of pantotenyl ethyl ether, 0.017 g of sodium hyaluronate, 10 g of glycerin, and 60 g of ethanol After adding and adjusting pH to 8, purified water was added to make 100 mL, and the liquid agent was obtained.
試験例１
実施例１及び２、並びに比較例１〜５の液剤を使用し、感熱紙を４０°の角度で平板に設置した。地面に対して９０°の角度で各サンプルを２０μL吐出し、３０秒後感熱紙上の液だれ距離を測定した。その結果を図１に示した。
Test example 1
Using the liquid agents of Examples 1 and 2 and Comparative Examples 1 to 5, thermal paper was placed on a flat plate at an angle of 40 °. 20 μL of each sample was discharged at an angle of 90 ° with respect to the ground, and after 30 seconds, the dripping distance on the thermal paper was measured. The results are shown in FIG.
試験例２
被験者６名により、実施例１及び比較例２の液剤の使用感を官能試験により評価した。評価方法としては、ハーフヘッドによる左右一対比較による方法を用いた。すなわち、被験者の頭部の左側に実施例１の液剤を、左側に比較例２の液剤を各々１ｍL塗布し、べたつき感について評価した。なお、被験者には液剤の内容が識別出来ないようにして試験を実施した。評価基準は以下の通りである。なお、スコア５の「わからない」はべたつきがあるか否かわからないことを指す。
スコア５：わからない
スコア４：ない
スコア３：ややある
スコア２：ある
スコア１：非常にある
更に、べたつき感の評価において、その結果をスコア１〜スコア３としたパネラーには、液剤のべたつきが気になるか否かについても評価してもらった。官能試験の結果を表１に示した。
Test example 2
The feeling of use of the liquid preparations of Example 1 and Comparative Example 2 was evaluated by a sensory test by six subjects. As an evaluation method, a method based on a left-right pair comparison using a half head was used. That is, 1 mL of the solution of Example 1 was applied to the left side of the subject's head and 1 mL of the solution of Comparative Example 2 was applied to the left side, and the stickiness was evaluated. The test was conducted so that the subject could not identify the contents of the liquid. The evaluation criteria are as follows. A score of “I don't know” means that I don't know if there is stickiness.
Score 5: Don't know Score 4: No score 3: Somewhat score 2: Some score 1: Very good Furthermore, in the evaluation of stickiness, the panelists who gave the result of score 1 to score 3 were apt to notice the stickiness of the solution. It was also evaluated whether or not. The results of the sensory test are shown in Table 1.
試験例３
被験者４名により、比較例２〜５の液剤の使用感を官能試験により評価した。評価方法としては、被験者の片方の腕に比較例３〜５の液剤を、もう片方の腕に比較例２の液剤を各々１００μL塗布し、べたつき感について評価した。なお、被験者には液剤の内容が識別出来ないようにして試験を実施した。官能試験の結果を表２に示した。
Test example 3
The feeling of use of the liquid agents of Comparative Examples 2 to 5 was evaluated by a sensory test by four test subjects. As an evaluation method, 100 μL of the solution of Comparative Examples 3 to 5 was applied to one arm of the subject and 100 μL of the solution of Comparative Example 2 was applied to the other arm, and the stickiness was evaluated. The test was conducted so that the subject could not identify the contents of the liquid. The results of the sensory test are shown in Table 2.
試験例１〜２より、実施例１の液剤は、ヒアルロン酸と１，３−ブチレングリコールを配合したことにより、べたつき感及びべたつきの気になる程度は比較例と同様に望ましい効果を保持しており、液だれ距離は比較例に比べ効果的に抑制していた。
試験例１〜３より、溶剤として１，３−ブチレングルコールを配合する場合に、ヒアルロン酸の配合（含有）量が０．０６ｗ／ｖ％以上となると、べたつき感などの使用感が低下することから、ヒアルロン酸濃度には最適範囲があり、本発明の効果は、製剤全体の配合バランスが寄与していると考えられた。一方、１，３−ブチレングルコールの代わりに同じ多価アルコールであるグリセリンやプロピレングルコールを配合した処方では、液だれを効果的に抑制し、かつ使用感を良好に保つことはできなかった。
From Test Examples 1 and 2, the liquid agent of Example 1 was blended with hyaluronic acid and 1,3-butylene glycol. The dripping distance was effectively suppressed as compared with the comparative example.
From Test Examples 1 to 3, when 1,3-butylene glycol is blended as a solvent, when the blending (content) amount of hyaluronic acid is 0.06 w / v% or more, the feeling of use such as stickiness decreases. Therefore, the hyaluronic acid concentration has an optimum range, and it was considered that the effect of the present invention contributed to the blending balance of the whole preparation. On the other hand, in the prescription in which glycerin or propylene glycol, which are the same polyhydric alcohols, was used instead of 1,3-butylene glycol, dripping was effectively suppressed and the feeling of use could not be kept good. .
本発明により、ミノキシジル含有液剤の液だれを効果的に抑制し、その使用感を良好に保つことができるため、扱いやすいミノキシジル含有頭髪用剤等を提供することができる。 According to the present invention, since dripping of the minoxidil-containing liquid agent can be effectively suppressed and the feeling of use can be kept good, an easy-to-handle minoxidil-containing hair preparation and the like can be provided.
Claims (7)
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Cited By (3)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| JP2013032320A (en) * | 2011-08-03 | 2013-02-14 | Milbon Co Ltd | External preparation for head |
| JP2021070671A (en) * | 2019-11-01 | 2021-05-06 | 富士化学工業株式会社 | Topical liquid |
| CN115475168A (en) * | 2022-10-18 | 2022-12-16 | 湖北工业大学 | Minoxidil-containing pharmaceutical composition, and preparation method and application thereof |
Citations (3)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| JPH0748230A (en) * | 1993-07-31 | 1995-02-21 | Hideo Horiuchi | Production of hair tonic |
| JPH11236319A (en) * | 1997-12-16 | 1999-08-31 | Shiseido Co Ltd | Composition for scalp and hair |
| JP2004505906A (en) * | 2000-08-09 | 2004-02-26 | フアーマシア アクチエボラグ | New composition of minoxidil |
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2008
- 2008-10-01 JP JP2008255904A patent/JP5353168B2/en active Active
Patent Citations (3)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| JPH0748230A (en) * | 1993-07-31 | 1995-02-21 | Hideo Horiuchi | Production of hair tonic |
| JPH11236319A (en) * | 1997-12-16 | 1999-08-31 | Shiseido Co Ltd | Composition for scalp and hair |
| JP2004505906A (en) * | 2000-08-09 | 2004-02-26 | フアーマシア アクチエボラグ | New composition of minoxidil |
Cited By (5)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| JP2013032320A (en) * | 2011-08-03 | 2013-02-14 | Milbon Co Ltd | External preparation for head |
| JP2021070671A (en) * | 2019-11-01 | 2021-05-06 | 富士化学工業株式会社 | Topical liquid |
| JP7379094B2 (en) | 2019-11-01 | 2023-11-14 | 富士化学工業株式会社 | External liquid |
| CN115475168A (en) * | 2022-10-18 | 2022-12-16 | 湖北工业大学 | Minoxidil-containing pharmaceutical composition, and preparation method and application thereof |
| CN115475168B (en) * | 2022-10-18 | 2024-02-13 | 湖北工业大学 | Minoxidil-containing pharmaceutical composition and preparation method and application thereof |
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