JP6907527B2 - 外用組成物 - Google Patents
外用組成物 Download PDFInfo
- Publication number
- JP6907527B2 JP6907527B2 JP2016248844A JP2016248844A JP6907527B2 JP 6907527 B2 JP6907527 B2 JP 6907527B2 JP 2016248844 A JP2016248844 A JP 2016248844A JP 2016248844 A JP2016248844 A JP 2016248844A JP 6907527 B2 JP6907527 B2 JP 6907527B2
- Authority
- JP
- Japan
- Prior art keywords
- acid
- external composition
- minoxidil
- present
- alcohol
- 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.)
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- 239000000203 mixture Substances 0.000 title claims description 96
- 230000000699 topical effect Effects 0.000 title description 4
- LFQSCWFLJHTTHZ-UHFFFAOYSA-N Ethanol Chemical compound CCO LFQSCWFLJHTTHZ-UHFFFAOYSA-N 0.000 claims description 62
- ZFMITUMMTDLWHR-UHFFFAOYSA-N Minoxidil Chemical compound NC1=[N+]([O-])C(N)=CC(N2CCCCC2)=N1 ZFMITUMMTDLWHR-UHFFFAOYSA-N 0.000 claims description 55
- 229960003632 minoxidil Drugs 0.000 claims description 55
- PUPZLCDOIYMWBV-UHFFFAOYSA-N (+/-)-1,3-Butanediol Chemical compound CC(O)CCO PUPZLCDOIYMWBV-UHFFFAOYSA-N 0.000 claims description 34
- XLYOFNOQVPJJNP-UHFFFAOYSA-N water Substances O XLYOFNOQVPJJNP-UHFFFAOYSA-N 0.000 claims description 29
- FEWJPZIEWOKRBE-UHFFFAOYSA-N Tartaric acid Natural products [H+].[H+].[O-]C(=O)C(O)C(O)C([O-])=O FEWJPZIEWOKRBE-UHFFFAOYSA-N 0.000 claims description 25
- 239000011975 tartaric acid Substances 0.000 claims description 25
- 235000002906 tartaric acid Nutrition 0.000 claims description 25
- 150000003839 salts Chemical class 0.000 claims description 22
- DNIAPMSPPWPWGF-UHFFFAOYSA-N Propylene glycol Chemical compound CC(O)CO DNIAPMSPPWPWGF-UHFFFAOYSA-N 0.000 claims description 21
- 229940058015 1,3-butylene glycol Drugs 0.000 claims description 17
- 235000019437 butane-1,3-diol Nutrition 0.000 claims description 17
- JVTAAEKCZFNVCJ-UHFFFAOYSA-N lactic acid Chemical compound CC(O)C(O)=O JVTAAEKCZFNVCJ-UHFFFAOYSA-N 0.000 claims description 16
- 150000005846 sugar alcohols Polymers 0.000 claims description 12
- PEDCQBHIVMGVHV-UHFFFAOYSA-N Glycerine Chemical compound OCC(O)CO PEDCQBHIVMGVHV-UHFFFAOYSA-N 0.000 claims description 8
- 239000004310 lactic acid Substances 0.000 claims description 8
- 235000014655 lactic acid Nutrition 0.000 claims description 8
- 235000011187 glycerol Nutrition 0.000 claims description 4
- 235000013772 propylene glycol Nutrition 0.000 claims description 2
- FEWJPZIEWOKRBE-JCYAYHJZSA-N Dextrotartaric acid Chemical compound OC(=O)[C@H](O)[C@@H](O)C(O)=O FEWJPZIEWOKRBE-JCYAYHJZSA-N 0.000 description 32
- 238000001556 precipitation Methods 0.000 description 23
- QTBSBXVTEAMEQO-UHFFFAOYSA-N Acetic acid Chemical compound CC(O)=O QTBSBXVTEAMEQO-UHFFFAOYSA-N 0.000 description 21
- 239000002253 acid Substances 0.000 description 21
- KRKNYBCHXYNGOX-UHFFFAOYSA-N citric acid Chemical compound OC(=O)CC(O)(C(O)=O)CC(O)=O KRKNYBCHXYNGOX-UHFFFAOYSA-N 0.000 description 21
- NBIIXXVUZAFLBC-UHFFFAOYSA-N Phosphoric acid Chemical compound OP(O)(O)=O NBIIXXVUZAFLBC-UHFFFAOYSA-N 0.000 description 18
- 239000008213 purified water Substances 0.000 description 16
- VEXZGXHMUGYJMC-UHFFFAOYSA-N Hydrochloric acid Chemical compound Cl VEXZGXHMUGYJMC-UHFFFAOYSA-N 0.000 description 13
- 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 12
- 238000002360 preparation method Methods 0.000 description 12
- 230000000052 comparative effect Effects 0.000 description 10
- 229910000147 aluminium phosphate Inorganic materials 0.000 description 9
- 239000013078 crystal Substances 0.000 description 9
- QAOWNCQODCNURD-UHFFFAOYSA-N Sulfuric acid Chemical compound OS(O)(=O)=O QAOWNCQODCNURD-UHFFFAOYSA-N 0.000 description 8
- 229940095064 tartrate Drugs 0.000 description 8
- CIWBSHSKHKDKBQ-JLAZNSOCSA-N Ascorbic acid Chemical compound OC[C@H](O)[C@H]1OC(=O)C(O)=C1O CIWBSHSKHKDKBQ-JLAZNSOCSA-N 0.000 description 6
- 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 6
- -1 diacetone alcohols Chemical class 0.000 description 6
- 239000000174 gluconic acid Substances 0.000 description 6
- 235000012208 gluconic acid Nutrition 0.000 description 6
- GLDOVTGHNKAZLK-UHFFFAOYSA-N octadecan-1-ol Chemical compound CCCCCCCCCCCCCCCCCCO GLDOVTGHNKAZLK-UHFFFAOYSA-N 0.000 description 6
- OFOBLEOULBTSOW-UHFFFAOYSA-N Propanedioic acid Natural products OC(=O)CC(O)=O OFOBLEOULBTSOW-UHFFFAOYSA-N 0.000 description 5
- 239000004615 ingredient Substances 0.000 description 5
- VZCYOOQTPOCHFL-UPHRSURJSA-N maleic acid Chemical compound OC(=O)\C=C/C(O)=O VZCYOOQTPOCHFL-UPHRSURJSA-N 0.000 description 5
- 239000011976 maleic acid Substances 0.000 description 5
- 239000004094 surface-active agent Substances 0.000 description 5
- VZCYOOQTPOCHFL-UHFFFAOYSA-N trans-butenedioic acid Natural products OC(=O)C=CC(O)=O VZCYOOQTPOCHFL-UHFFFAOYSA-N 0.000 description 5
- WNWHHMBRJJOGFJ-UHFFFAOYSA-N 16-methylheptadecan-1-ol Chemical compound CC(C)CCCCCCCCCCCCCCCO WNWHHMBRJJOGFJ-UHFFFAOYSA-N 0.000 description 4
- XDOFQFKRPWOURC-UHFFFAOYSA-N 16-methylheptadecanoic acid Chemical compound CC(C)CCCCCCCCCCCCCCC(O)=O XDOFQFKRPWOURC-UHFFFAOYSA-N 0.000 description 4
- MPDGHEJMBKOTSU-YKLVYJNSSA-N 18beta-glycyrrhetic acid Chemical compound C([C@H]1C2=CC(=O)[C@H]34)[C@@](C)(C(O)=O)CC[C@]1(C)CC[C@@]2(C)[C@]4(C)CC[C@@H]1[C@]3(C)CC[C@H](O)C1(C)C MPDGHEJMBKOTSU-YKLVYJNSSA-N 0.000 description 4
- GRYLNZFGIOXLOG-UHFFFAOYSA-N Nitric acid Chemical compound O[N+]([O-])=O GRYLNZFGIOXLOG-UHFFFAOYSA-N 0.000 description 4
- KGBXLFKZBHKPEV-UHFFFAOYSA-N boric acid Chemical compound OB(O)O KGBXLFKZBHKPEV-UHFFFAOYSA-N 0.000 description 4
- 239000004327 boric acid Substances 0.000 description 4
- 125000004432 carbon atom Chemical group C* 0.000 description 4
- NOPFSRXAKWQILS-UHFFFAOYSA-N docosan-1-ol Chemical compound CCCCCCCCCCCCCCCCCCCCCCO NOPFSRXAKWQILS-UHFFFAOYSA-N 0.000 description 4
- 230000000694 effects Effects 0.000 description 4
- GOQYKNQRPGWPLP-UHFFFAOYSA-N heptadecan-1-ol Chemical compound CCCCCCCCCCCCCCCCCO GOQYKNQRPGWPLP-UHFFFAOYSA-N 0.000 description 4
- BXWNKGSJHAJOGX-UHFFFAOYSA-N hexadecan-1-ol Chemical compound CCCCCCCCCCCCCCCCO BXWNKGSJHAJOGX-UHFFFAOYSA-N 0.000 description 4
- 229910017604 nitric acid Inorganic materials 0.000 description 4
- YGSDEFSMJLZEOE-UHFFFAOYSA-N salicylic acid Chemical compound OC(=O)C1=CC=CC=C1O YGSDEFSMJLZEOE-UHFFFAOYSA-N 0.000 description 4
- ZQPPMHVWECSIRJ-UHFFFAOYSA-N Oleic acid Natural products CCCCCCCCC=CCCCCCCCC(O)=O ZQPPMHVWECSIRJ-UHFFFAOYSA-N 0.000 description 3
- 239000004480 active ingredient Substances 0.000 description 3
- 150000001298 alcohols Chemical class 0.000 description 3
- 235000010323 ascorbic acid Nutrition 0.000 description 3
- 229960005070 ascorbic acid Drugs 0.000 description 3
- 239000011668 ascorbic acid Substances 0.000 description 3
- 239000003795 chemical substances by application Substances 0.000 description 3
- 235000014113 dietary fatty acids Nutrition 0.000 description 3
- ZQPPMHVWECSIRJ-MDZDMXLPSA-N elaidic acid Chemical compound CCCCCCCC\C=C\CCCCCCCC(O)=O ZQPPMHVWECSIRJ-MDZDMXLPSA-N 0.000 description 3
- 229930195729 fatty acid Natural products 0.000 description 3
- 239000000194 fatty acid Substances 0.000 description 3
- 150000004665 fatty acids Chemical class 0.000 description 3
- 210000004209 hair Anatomy 0.000 description 3
- 230000003779 hair growth Effects 0.000 description 3
- QXJSBBXBKPUZAA-UHFFFAOYSA-N isooleic acid Natural products CCCCCCCC=CCCCCCCCCC(O)=O QXJSBBXBKPUZAA-UHFFFAOYSA-N 0.000 description 3
- 238000002156 mixing Methods 0.000 description 3
- 239000000825 pharmaceutical preparation Substances 0.000 description 3
- 229940127557 pharmaceutical product Drugs 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
- NOOLISFMXDJSKH-KXUCPTDWSA-N (-)-Menthol Chemical compound CC(C)[C@@H]1CC[C@@H](C)C[C@H]1O NOOLISFMXDJSKH-KXUCPTDWSA-N 0.000 description 2
- MRAMPOPITCOOIN-VIFPVBQESA-N (2r)-n-(3-ethoxypropyl)-2,4-dihydroxy-3,3-dimethylbutanamide Chemical compound CCOCCCNC(=O)[C@H](O)C(C)(C)CO MRAMPOPITCOOIN-VIFPVBQESA-N 0.000 description 2
- ALSTYHKOOCGGFT-KTKRTIGZSA-N (9Z)-octadecen-1-ol Chemical compound CCCCCCCC\C=C/CCCCCCCCO ALSTYHKOOCGGFT-KTKRTIGZSA-N 0.000 description 2
- WRIDQFICGBMAFQ-UHFFFAOYSA-N (E)-8-Octadecenoic acid Natural products CCCCCCCCCC=CCCCCCCC(O)=O WRIDQFICGBMAFQ-UHFFFAOYSA-N 0.000 description 2
- 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 2
- CAYHVMBQBLYQMT-UHFFFAOYSA-N 2-decyltetradecan-1-ol Chemical compound CCCCCCCCCCCCC(CO)CCCCCCCCCC CAYHVMBQBLYQMT-UHFFFAOYSA-N 0.000 description 2
- LEACJMVNYZDSKR-UHFFFAOYSA-N 2-octyldodecan-1-ol Chemical compound CCCCCCCCCCC(CO)CCCCCCCC LEACJMVNYZDSKR-UHFFFAOYSA-N 0.000 description 2
- LQJBNNIYVWPHFW-UHFFFAOYSA-N 20:1omega9c fatty acid Natural products CCCCCCCCCCC=CCCCCCCCC(O)=O LQJBNNIYVWPHFW-UHFFFAOYSA-N 0.000 description 2
- QSBYPNXLFMSGKH-UHFFFAOYSA-N 9-Heptadecensaeure Natural products CCCCCCCC=CCCCCCCCC(O)=O QSBYPNXLFMSGKH-UHFFFAOYSA-N 0.000 description 2
- 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 2
- SNPLKNRPJHDVJA-ZETCQYMHSA-N D-panthenol Chemical compound OCC(C)(C)[C@@H](O)C(=O)NCCCO SNPLKNRPJHDVJA-ZETCQYMHSA-N 0.000 description 2
- NOOLISFMXDJSKH-UHFFFAOYSA-N DL-menthol Natural products CC(C)C1CCC(C)CC1O NOOLISFMXDJSKH-UHFFFAOYSA-N 0.000 description 2
- MPDGHEJMBKOTSU-UHFFFAOYSA-N Glycyrrhetinsaeure Natural products C12C(=O)C=C3C4CC(C)(C(O)=O)CCC4(C)CCC3(C)C1(C)CCC1C2(C)CCC(O)C1(C)C MPDGHEJMBKOTSU-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
- KFZMGEQAYNKOFK-UHFFFAOYSA-N Isopropanol Chemical compound CC(C)O KFZMGEQAYNKOFK-UHFFFAOYSA-N 0.000 description 2
- 239000005642 Oleic acid Substances 0.000 description 2
- XSQUKJJJFZCRTK-UHFFFAOYSA-N Urea Chemical compound NC(N)=O XSQUKJJJFZCRTK-UHFFFAOYSA-N 0.000 description 2
- 238000010521 absorption reaction Methods 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
- MBMBGCFOFBJSGT-KUBAVDMBSA-N all-cis-docosa-4,7,10,13,16,19-hexaenoic acid Chemical compound CC\C=C/C\C=C/C\C=C/C\C=C/C\C=C/C\C=C/CCC(O)=O MBMBGCFOFBJSGT-KUBAVDMBSA-N 0.000 description 2
- 239000003963 antioxidant agent Substances 0.000 description 2
- 235000006708 antioxidants Nutrition 0.000 description 2
- YZXBAPSDXZZRGB-DOFZRALJSA-N arachidonic acid Chemical compound CCCCC\C=C/C\C=C/C\C=C/C\C=C/CCCC(O)=O YZXBAPSDXZZRGB-DOFZRALJSA-N 0.000 description 2
- BTFJIXJJCSYFAL-UHFFFAOYSA-N arachidyl alcohol Natural products CCCCCCCCCCCCCCCCCCCCO BTFJIXJJCSYFAL-UHFFFAOYSA-N 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
- FUWUEFKEXZQKKA-UHFFFAOYSA-N beta-thujaplicin Chemical compound CC(C)C=1C=CC=C(O)C(=O)C=1 FUWUEFKEXZQKKA-UHFFFAOYSA-N 0.000 description 2
- 150000001732 carboxylic acid derivatives Chemical class 0.000 description 2
- RZMKWKZIJJNSLQ-UHFFFAOYSA-M carpronium chloride Chemical compound [Cl-].COC(=O)CCC[N+](C)(C)C RZMKWKZIJJNSLQ-UHFFFAOYSA-M 0.000 description 2
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- GHVNFZFCNZKVNT-UHFFFAOYSA-N decanoic acid Chemical compound CCCCCCCCCC(O)=O GHVNFZFCNZKVNT-UHFFFAOYSA-N 0.000 description 2
- SWXVUIWOUIDPGS-UHFFFAOYSA-N diacetone alcohol Chemical compound CC(=O)CC(C)(C)O SWXVUIWOUIDPGS-UHFFFAOYSA-N 0.000 description 2
- 229960000525 diphenhydramine hydrochloride Drugs 0.000 description 2
- UKMSUNONTOPOIO-UHFFFAOYSA-N docosanoic acid Chemical compound CCCCCCCCCCCCCCCCCCCCCC(O)=O UKMSUNONTOPOIO-UHFFFAOYSA-N 0.000 description 2
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- 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 description 1
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Description
(1)(a)ミノキシジル、(b)酒石酸及び/又はその塩、(c)リン酸、クエン酸、乳酸、塩酸、グルコン酸、酢酸、硫酸、ホウ酸、硝酸、及びマレイン酸からなる群から選ばれる少なくとも1種の酸及び/又はこれらの塩、及び(d)水を含有し、かつ(b)の含有量が(d)1質量部に対し0.025質量部未満であることを特徴とする外用組成物、
(2)(c)成分が、リン酸、クエン酸、乳酸、塩酸、グルコン酸、及び酢酸からなる群から選ばれる少なくとも1種の酸及び/又はこれらの塩である、(1)に記載の外用組成物、
(3)(a)の含有量が5w/v%以上である、(1)に記載の外用組成物、
(4)更に、多価アルコールを含有する(1)〜(3)に記載の外用組成物、
(5)多価アルコールが、1,3−ブチレングリコール、プロピレングリコール、及びグリセリンからなる群から選ばれる少なくとも1つである、(4)に記載の外用組成物、
(6)多価アルコールの含有量が2〜50w/v%である、(4)または(5)に記載の外用組成物、
(7)更に、低級アルコールを含有する(1)〜(6)のいずれかに記載の外用組成物、
(8)低級アルコールの含有量が50w/v%以上である(7)に記載の外用組成物、
(9)(d)の含有量が5〜30w/v%である、(1)に記載の外用組成物、
(10)pHが5.0〜7.0である、(1)〜(9)のいずれかに記載の外用組成物、
である。
本発明の外用組成物において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。また、本発明における外用組成物において、ミノキシジルの含有量が多くなるにつれ溶解性の課題が大きくなるため、外用組成物中におけるミノキシルの濃度が高いほど、本発明を実施する意義が大きい。具体的には、本発明の外用組成物中1w/v%以上が好ましく、より好ましくは3w/v%以上であり、更に好ましくは5w/v%以上である。
また、本発明の外用組成物は、主薬成分のミノキシジルの安定性、使用時の肌への刺激感、薬物の浸透性、使用感等の点から、そのpHを4.0〜8.0の範囲に調整することが好ましく、5.0〜7.0の範囲が更に好ましい。
ミノキシジル5g、1,3−ブチレングリコール10g、精製水10g、酒石酸0.2g、リン酸適量、エタノールで全量を100mLとし、撹拌してpH6.3の外用組成物を得た。
ミノキシジル5g、1,3−ブチレングリコール10g、精製水10g、酒石酸0.2g、クエン酸適量、エタノールで全量を100mLとし、撹拌してpH6.3の外用組成物を得た。
ミノキシジル5g、1,3−ブチレングリコール10g、精製水10g、酒石酸0.2g、乳酸適量、エタノールで全量を100mLとし、撹拌してpH6.3の外用組成物を得た。
ミノキシジル5g、1,3−ブチレングリコール10g、精製水10g、酒石酸0.2g、塩酸適量、エタノールで全量を100mLとし、撹拌してpH6.3の外用組成物を得た。
ミノキシジル5g、1,3−ブチレングリコール10g、精製水10g、酒石酸0.2g、グルコン酸適量、エタノールで全量を100mLとし、撹拌してpH6.3の外用組成物を得た。
ミノキシジル5g、1,3−ブチレングリコール10g、精製水10g、酒石酸0.2g、酢酸適量、エタノールで全量を100mLとし、撹拌してpH6.3の外用組成物を得た。
ミノキシジル5g、1,3−ブチレングリコール10g、精製水10g、酒石酸0.2g、硫酸適量、エタノールで全量を100mLとし、撹拌してpH6.3の外用組成物を得た。
ミノキシジル5g、1,3−ブチレングリコール10g、精製水10g、酒石酸0.2g、ホウ酸適量、エタノールで全量を100mLとし、撹拌してpH6.3の外用組成物を得た。
ミノキシジル5g、1,3−ブチレングリコール10g、精製水10g、酒石酸0.2g、硝酸適量、エタノールで全量を100mLとし、撹拌してpH6.3の外用組成物を得た。
ミノキシジル5g、1,3−ブチレングリコール10g、精製水10g、酒石酸0.2g、マレイン酸適量、エタノールで全量を100mLとし、撹拌してpH6.3の外用組成物を得た。
ミノキシジル5g、プロピレングリコール10g、精製水10g、酒石酸0.2g、リン酸適量、エタノールで全量を100mLとし、撹拌してpH6.3の外用組成物を得た。
ミノキシジル5g、グリセリン10g、精製水10g、酒石酸0.2g、リン酸適量、エタノールで全量を100mLとし、撹拌してpH6.3の外用組成物を得た。
ミノキシジル5g、1,3−ブチレングリコール10g、精製水10g、酒石酸0.2g、エタノールで全量を100mLとし、撹拌して外用組成物を得た。
ミノキシジル5g、1,3−ブチレングリコール10g、精製水10g、酒石酸0.25g、エタノールで全量を100mLとし、撹拌して外用組成物を得た。
ミノキシジル5g、1,3−ブチレングリコール10g、精製水10g、酒石酸0.2g、dl-リンゴ酸適量、エタノールで全量を100mLとし、撹拌してpH6.3の外用組成物を得た。
ミノキシジル5g、1,3−ブチレングリコール5g、プロピレングリコール5g、セチルアルコール0.1g、精製水10g、酒石酸0.2g、l-メントール0.3g、塩酸ピリドキシン0.05g、ビタミンEアセテート0.08g、パントテニルエチルエーテル1g、パンテノール1g、塩化カルプロニウム2g、グリチルレチン酸0.1g、塩酸ジフェンヒドラミン0.1g、ヒノキチオール0.05g、サリチル酸0.2g、抗酸化剤適量、リン酸適量、エタノールで全量を100mLとし、撹拌溶解してpH5.9の外用組成物を得た。
比較例1、2に関し、調製段階で生じたミノキシジル以外の析出が、調製直後に認められなかったものを○、析出が認められたものを×とした。結果を表4に示す。
比較例1〜3、実施例1〜12に関し、調製直後にミノキシジルが完全に溶解したものを○、溶解しなかったものを×とした。結果を表4〜6に示す。
実施例1〜12及び比較例3の外用組成物に関し、調製段階で生じたミノキシジル以外の析出を調製直後に目視で確認し、析出が認められなかったものを◎、極わずかに析出が認められたが問題ないものを○、析出が全体的に認められて白濁し問題であるものを×とした。結果を表5、6に示す。
Claims (8)
- (a)ミノキシジル、(b)酒石酸及び/又はその塩、(c)乳酸及び/又はその塩、及び(d)水を含有し、かつ(b)の含有量が(d)1質量部に対して0.025質量部未満であり、pHが5.0〜7.0であることを特徴とする外用組成物。
- (a)の含有量が5w/v%以上である、請求項1に記載の外用組成物。
- 更に、多価アルコールを含有する請求項1又は2のいずれかに記載の外用組成物。
- 多価アルコールが、1,3−ブチレングリコール、プロピレングリコール、及びグリセ
リンからなる群から選ばれる少なくとも1つである、請求項3に記載の外用組成物。 - 多価アルコールの含有量が2〜50w/v%である、請求項3または4に記載の外用組
成物。 - 更に、低級アルコールを含有する請求項1〜5のいずれかに記載の外用組成物。
- 低級アルコールの含有量が50w/v%以上である、請求項6に記載の外用組成物。
- (d)の含有量が5〜30w/v%である、請求項1〜7のいずれかに記載の外用組成物。
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JP2020037517A (ja) * | 2017-09-04 | 2020-03-12 | ロート製薬株式会社 | ミノキシジルを含有する外用組成物、および、ミノキシジルの析出防止方法 |
JP7194553B2 (ja) * | 2017-10-12 | 2022-12-22 | ロート製薬株式会社 | 外用組成物 |
JP2019131474A (ja) * | 2018-01-29 | 2019-08-08 | 富士化学工業株式会社 | ミノキシジル含有外用組成物 |
JP7304463B2 (ja) * | 2018-01-29 | 2023-07-06 | 富士化学工業株式会社 | ミノキシジル含有外用組成物 |
JP7118743B2 (ja) * | 2018-05-29 | 2022-08-16 | 興和株式会社 | 組成物 |
JP2020186218A (ja) * | 2019-05-17 | 2020-11-19 | ロート製薬株式会社 | 発毛因子産生促進剤及び/又は毛再生剤及び/又は脱毛抑制剤 |
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