JP2014501286A5 - - Google Patents

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Publication number

JP2014501286A5

JP2014501286A5 JP2013547686A JP2013547686A JP2014501286A5 JP 2014501286 A5 JP2014501286 A5 JP 2014501286A5 JP 2013547686 A JP2013547686 A JP 2013547686A JP 2013547686 A JP2013547686 A JP 2013547686A JP 2014501286 A5 JP2014501286 A5 JP 2014501286A5

Authority

JP

Japan

Prior art keywords

item

composition

items

composition according

concentration

Prior art date

2011-12-29

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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Links

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• 239000000203 mixture Substances 0.000 claims description 430
• DNIAPMSPPWPWGF-UHFFFAOYSA-N Propylene glycol Chemical compound CC(O)CO DNIAPMSPPWPWGF-UHFFFAOYSA-N 0.000 claims description 90
• 150000003839 salts Chemical class 0.000 claims description 74
• TWRXJAOTZQYOKJ-UHFFFAOYSA-L Magnesium chloride Chemical compound [Mg+2].[Cl-].[Cl-] TWRXJAOTZQYOKJ-UHFFFAOYSA-L 0.000 claims description 62
• 239000002840 nitric oxide donor Substances 0.000 claims description 62
• 229920000136 polysorbate Polymers 0.000 claims description 52
• 229950008882 polysorbate Drugs 0.000 claims description 52
• 229920000642 polymer Polymers 0.000 claims description 51
• 239000004094 surface-active agent Substances 0.000 claims description 48
• 230000000087 stabilizing effect Effects 0.000 claims description 47
• 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 claims description 36
• 229960002722 terbinafine Drugs 0.000 claims description 36
• FAPWRFPIFSIZLT-UHFFFAOYSA-M Sodium chloride Chemical compound [Na+].[Cl-] FAPWRFPIFSIZLT-UHFFFAOYSA-M 0.000 claims description 34
• 210000003491 skin Anatomy 0.000 claims description 33
• 229910001629 magnesium chloride Inorganic materials 0.000 claims description 31
• 230000000699 topical effect Effects 0.000 claims description 23
• 239000011780 sodium chloride Substances 0.000 claims description 17
• 239000000230 xanthan gum Substances 0.000 claims description 10
• 229920001285 xanthan gum Polymers 0.000 claims description 10
• 229940082509 xanthan gum Drugs 0.000 claims description 10
• 235000010493 xanthan gum Nutrition 0.000 claims description 10
• ODKSFYDXXFIFQN-BYPYZUCNSA-N L-arginine Chemical compound OC(=O)[C@@H](N)CCCN=C(N)N ODKSFYDXXFIFQN-BYPYZUCNSA-N 0.000 claims description 9
• 229930064664 L-arginine Natural products 0.000 claims description 9
• 235000014852 L-arginine Nutrition 0.000 claims description 9
• 239000001763 2-hydroxyethyl(trimethyl)azanium Substances 0.000 claims description 7
• UXVMQQNJUSDDNG-UHFFFAOYSA-L Calcium chloride Chemical compound [Cl-].[Cl-].[Ca+2] UXVMQQNJUSDDNG-UHFFFAOYSA-L 0.000 claims description 7
• 235000019743 Choline chloride Nutrition 0.000 claims description 7
• 229920001213 Polysorbate 20 Polymers 0.000 claims description 7
• 239000001110 calcium chloride Substances 0.000 claims description 7
• 229910001628 calcium chloride Inorganic materials 0.000 claims description 7
• SGMZJAMFUVOLNK-UHFFFAOYSA-M choline chloride Chemical compound [Cl-].C[N+](C)(C)CCO SGMZJAMFUVOLNK-UHFFFAOYSA-M 0.000 claims description 7
• 229960003178 choline chloride Drugs 0.000 claims description 7
• 239000006071 cream Substances 0.000 claims description 7
• 239000000256 polyoxyethylene sorbitan monolaurate Substances 0.000 claims description 7
• 235000010486 polyoxyethylene sorbitan monolaurate Nutrition 0.000 claims description 7
• 229940068977 polysorbate 20 Drugs 0.000 claims description 7
• 210000000434 stratum corneum Anatomy 0.000 claims description 7
• 125000002059 L-arginyl group Chemical class O=C([*])[C@](N([H])[H])([H])C([H])([H])C([H])([H])C([H])([H])N([H])C(=N[H])N([H])[H] 0.000 claims description 5
• 238000000034 method Methods 0.000 description 41
• 229940121375 antifungal agent Drugs 0.000 description 38
• 150000003852 triazoles Chemical class 0.000 description 38
• 239000003429 antifungal agent Substances 0.000 description 26
• BXWNKGSJHAJOGX-UHFFFAOYSA-N hexadecan-1-ol Chemical compound CCCCCCCCCCCCCCCCO BXWNKGSJHAJOGX-UHFFFAOYSA-N 0.000 description 24
• PRAKJMSDJKAYCZ-UHFFFAOYSA-N squalane Chemical compound CC(C)CCCC(C)CCCC(C)CCCCC(C)CCCC(C)CCCC(C)C PRAKJMSDJKAYCZ-UHFFFAOYSA-N 0.000 description 23
• XLYOFNOQVPJJNP-UHFFFAOYSA-N water Substances O XLYOFNOQVPJJNP-UHFFFAOYSA-N 0.000 description 22
• 150000003841 chloride salts Chemical class 0.000 description 20
• 239000003981 vehicle Substances 0.000 description 18
• 235000019901 KELTROL® Nutrition 0.000 description 17
• WRIDQFICGBMAFQ-UHFFFAOYSA-N (E)-8-Octadecenoic acid Natural products CCCCCCCCCC=CCCCCCCC(O)=O WRIDQFICGBMAFQ-UHFFFAOYSA-N 0.000 description 12
• VBICKXHEKHSIBG-UHFFFAOYSA-N 1-monostearoylglycerol Chemical compound CCCCCCCCCCCCCCCCCC(=O)OCC(O)CO VBICKXHEKHSIBG-UHFFFAOYSA-N 0.000 description 12
• LQJBNNIYVWPHFW-UHFFFAOYSA-N 20:1omega9c fatty acid Natural products CCCCCCCCCCC=CCCCCCCCC(O)=O LQJBNNIYVWPHFW-UHFFFAOYSA-N 0.000 description 12
• HIQIXEFWDLTDED-UHFFFAOYSA-N 4-hydroxy-1-piperidin-4-ylpyrrolidin-2-one Chemical compound O=C1CC(O)CN1C1CCNCC1 HIQIXEFWDLTDED-UHFFFAOYSA-N 0.000 description 12
• QSBYPNXLFMSGKH-UHFFFAOYSA-N 9-Heptadecensaeure Natural products CCCCCCCC=CCCCCCCCC(O)=O QSBYPNXLFMSGKH-UHFFFAOYSA-N 0.000 description 12
• ZQPPMHVWECSIRJ-UHFFFAOYSA-N Oleic acid Natural products CCCCCCCCC=CCCCCCCCC(O)=O ZQPPMHVWECSIRJ-UHFFFAOYSA-N 0.000 description 12
• 239000005642 Oleic acid Substances 0.000 description 12
• WCUXLLCKKVVCTQ-UHFFFAOYSA-M Potassium chloride Chemical compound [Cl-].[K+] WCUXLLCKKVVCTQ-UHFFFAOYSA-M 0.000 description 12
• 229960000541 cetyl alcohol Drugs 0.000 description 12
• 229940075529 glyceryl stearate Drugs 0.000 description 12
• QXJSBBXBKPUZAA-UHFFFAOYSA-N isooleic acid Natural products CCCCCCCC=CCCCCCCCCC(O)=O QXJSBBXBKPUZAA-UHFFFAOYSA-N 0.000 description 12
• ZQPPMHVWECSIRJ-KTKRTIGZSA-N oleic acid Chemical compound CCCCCCCC\C=C/CCCCCCCC(O)=O ZQPPMHVWECSIRJ-KTKRTIGZSA-N 0.000 description 12
• JXTPJDDICSTXJX-UHFFFAOYSA-N n-Triacontane Natural products CCCCCCCCCCCCCCCCCCCCCCCCCCCCCC JXTPJDDICSTXJX-UHFFFAOYSA-N 0.000 description 11
• 229940032094 squalane Drugs 0.000 description 11
• 150000001875 compounds Chemical class 0.000 description 8
• 239000006210 lotion Substances 0.000 description 6
• 239000001103 potassium chloride Substances 0.000 description 6
• 235000011164 potassium chloride Nutrition 0.000 description 6
• ZISSAWUMDACLOM-UHFFFAOYSA-N triptane Chemical compound CC(C)C(C)(C)C ZISSAWUMDACLOM-UHFFFAOYSA-N 0.000 description 6
• KWTQSFXGGICVPE-WCCKRBBISA-N Arginine hydrochloride Chemical compound Cl.OC(=O)[C@@H](N)CCCN=C(N)N KWTQSFXGGICVPE-WCCKRBBISA-N 0.000 description 4
• 102000008186 Collagen Human genes 0.000 description 4
• 108010035532 Collagen Proteins 0.000 description 4
• 230000017531 blood circulation Effects 0.000 description 4
• 229920001436 collagen Polymers 0.000 description 4
• 229960002337 magnesium chloride Drugs 0.000 description 4
• 229960002816 potassium chloride Drugs 0.000 description 4
• 229960002668 sodium chloride Drugs 0.000 description 4
• VHVPQPYKVGDNFY-DFMJLFEVSA-N 2-[(2r)-butan-2-yl]-4-[4-[4-[4-[[(2r,4s)-2-(2,4-dichlorophenyl)-2-(1,2,4-triazol-1-ylmethyl)-1,3-dioxolan-4-yl]methoxy]phenyl]piperazin-1-yl]phenyl]-1,2,4-triazol-3-one Chemical compound O=C1N([C@H](C)CC)N=CN1C1=CC=C(N2CCN(CC2)C=2C=CC(OC[C@@H]3O[C@](CN4N=CN=C4)(OC3)C=3C(=CC(Cl)=CC=3)Cl)=CC=2)C=C1 VHVPQPYKVGDNFY-DFMJLFEVSA-N 0.000 description 2
• XZIIFPSPUDAGJM-UHFFFAOYSA-N 6-chloro-2-n,2-n-diethylpyrimidine-2,4-diamine Chemical group CCN(CC)C1=NC(N)=CC(Cl)=N1 XZIIFPSPUDAGJM-UHFFFAOYSA-N 0.000 description 2
• WQZGKKKJIJFFOK-GASJEMHNSA-N Glucose Natural products OC[C@H]1OC(O)[C@H](O)[C@@H](O)[C@@H]1O WQZGKKKJIJFFOK-GASJEMHNSA-N 0.000 description 2
• 239000000839 emulsion Substances 0.000 description 2
• 239000008103 glucose Substances 0.000 description 2
• 229960004130 itraconazole Drugs 0.000 description 2
• 239000002502 liposome Substances 0.000 description 2
• HGASFNYMVGEKTF-UHFFFAOYSA-N octan-1-ol;hydrate Chemical compound O.CCCCCCCCO HGASFNYMVGEKTF-UHFFFAOYSA-N 0.000 description 2
• 238000005192 partition Methods 0.000 description 2
• 102000004196 processed proteins & peptides Human genes 0.000 description 2
• 108090000765 processed proteins & peptides Proteins 0.000 description 2
• 159000000000 sodium salts Chemical class 0.000 description 2
• YYGNTYWPHWGJRM-UHFFFAOYSA-N (6E,10E,14E,18E)-2,6,10,15,19,23-hexamethyltetracosa-2,6,10,14,18,22-hexaene Chemical compound CC(C)=CCCC(C)=CCCC(C)=CCCC=C(C)CCC=C(C)CCC=C(C)C YYGNTYWPHWGJRM-UHFFFAOYSA-N 0.000 description 1
• AEKNYBWUEYNWMJ-QWOOXDRHSA-N Pramiconazole Chemical group O=C1N(C(C)C)CCN1C1=CC=C(N2CCN(CC2)C=2C=CC(OC[C@@H]3O[C@](CN4N=CN=C4)(CO3)C=3C(=CC(F)=CC=3)F)=CC=2)C=C1 AEKNYBWUEYNWMJ-QWOOXDRHSA-N 0.000 description 1
• BHEOSNUKNHRBNM-UHFFFAOYSA-N Tetramethylsqualene Natural products CC(=C)C(C)CCC(=C)C(C)CCC(C)=CCCC=C(C)CCC(C)C(=C)CCC(C)C(C)=C BHEOSNUKNHRBNM-UHFFFAOYSA-N 0.000 description 1
• RWTNPBWLLIMQHL-UHFFFAOYSA-N fexofenadine Chemical group C1=CC(C(C)(C(O)=O)C)=CC=C1C(O)CCCN1CCC(C(O)(C=2C=CC=CC=2)C=2C=CC=CC=2)CC1 RWTNPBWLLIMQHL-UHFFFAOYSA-N 0.000 description 1
• 229960003592 fexofenadine Drugs 0.000 description 1
• 229960001589 posaconazole Drugs 0.000 description 1
• RAGOYPUPXAKGKH-XAKZXMRKSA-N posaconazole Chemical group O=C1N([C@H]([C@H](C)O)CC)N=CN1C1=CC=C(N2CCN(CC2)C=2C=CC(OC[C@H]3C[C@@](CN4N=CN=C4)(OC3)C=3C(=CC(F)=CC=3)F)=CC=2)C=C1 RAGOYPUPXAKGKH-XAKZXMRKSA-N 0.000 description 1
• 229950001086 pramiconazole Drugs 0.000 description 1
• 229940031439 squalene Drugs 0.000 description 1
• TUHBEKDERLKLEC-UHFFFAOYSA-N squalene Natural products CC(=CCCC(=CCCC(=CCCC=C(/C)CCC=C(/C)CC=C(C)C)C)C)C TUHBEKDERLKLEC-UHFFFAOYSA-N 0.000 description 1
• 229960004740 voriconazole Drugs 0.000 description 1
• BCEHBSKCWLPMDN-MGPLVRAMSA-N voriconazole Chemical compound C1([C@H](C)[C@](O)(CN2N=CN=C2)C=2C(=CC(F)=CC=2)F)=NC=NC=C1F BCEHBSKCWLPMDN-MGPLVRAMSA-N 0.000 description 1