JP6836991B2 - 経皮製剤 - Google Patents
経皮製剤 Download PDFInfo
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- JP6836991B2 JP6836991B2 JP2017528802A JP2017528802A JP6836991B2 JP 6836991 B2 JP6836991 B2 JP 6836991B2 JP 2017528802 A JP2017528802 A JP 2017528802A JP 2017528802 A JP2017528802 A JP 2017528802A JP 6836991 B2 JP6836991 B2 JP 6836991B2
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- UNHGSHHVDNGCFN-UHFFFAOYSA-N naratriptan Chemical compound C=12[CH]C(CCS(=O)(=O)NC)=CC=C2N=CC=1C1CCN(C)CC1 UNHGSHHVDNGCFN-UHFFFAOYSA-N 0.000 description 1
- 239000004081 narcotic agent Substances 0.000 description 1
- 125000001971 neopentyl group Chemical group [H]C([*])([H])C(C([H])([H])[H])(C([H])([H])[H])C([H])([H])[H] 0.000 description 1
- 210000005036 nerve Anatomy 0.000 description 1
- 230000002232 neuromuscular Effects 0.000 description 1
- 229960002667 norelgestromin Drugs 0.000 description 1
- 229960001652 norethindrone acetate Drugs 0.000 description 1
- 229960000417 norgestimate Drugs 0.000 description 1
- KIQQMECNKUGGKA-NMYWJIRASA-N norgestimate Chemical compound O/N=C/1CC[C@@H]2[C@H]3CC[C@](CC)([C@](CC4)(OC(C)=O)C#C)[C@@H]4[C@@H]3CCC2=C\1 KIQQMECNKUGGKA-NMYWJIRASA-N 0.000 description 1
- QIQXTHQIDYTFRH-UHFFFAOYSA-N octadecanoic acid Chemical compound CCCCCCCCCCCCCCCCCC(O)=O QIQXTHQIDYTFRH-UHFFFAOYSA-N 0.000 description 1
- OQCDKBAXFALNLD-UHFFFAOYSA-N octadecanoic acid Natural products CCCCCCCC(C)CCCCCCCCC(O)=O OQCDKBAXFALNLD-UHFFFAOYSA-N 0.000 description 1
- 229940012843 omega-3 fatty acid Drugs 0.000 description 1
- 239000006014 omega-3 oil Substances 0.000 description 1
- 235000020665 omega-6 fatty acid Nutrition 0.000 description 1
- 229940033080 omega-6 fatty acid Drugs 0.000 description 1
- 229960005343 ondansetron Drugs 0.000 description 1
- 239000003402 opiate agonist Substances 0.000 description 1
- 239000003401 opiate antagonist Substances 0.000 description 1
- 229940111617 oregano oil Drugs 0.000 description 1
- 239000010661 oregano oil Substances 0.000 description 1
- 229960002085 oxycodone Drugs 0.000 description 1
- 229940094443 oxytocics prostaglandins Drugs 0.000 description 1
- 229960002131 palonosetron Drugs 0.000 description 1
- CPZBLNMUGSZIPR-NVXWUHKLSA-N palonosetron Chemical compound C1N(CC2)CCC2[C@@H]1N1C(=O)C(C=CC=C2CCC3)=C2[C@H]3C1 CPZBLNMUGSZIPR-NVXWUHKLSA-N 0.000 description 1
- FJKROLUGYXJWQN-UHFFFAOYSA-N papa-hydroxy-benzoic acid Natural products OC(=O)C1=CC=C(O)C=C1 FJKROLUGYXJWQN-UHFFFAOYSA-N 0.000 description 1
- 229960002296 paroxetine Drugs 0.000 description 1
- 230000001575 pathological effect Effects 0.000 description 1
- 230000037368 penetrate the skin Effects 0.000 description 1
- 239000003961 penetration enhancing agent Substances 0.000 description 1
- MWMPEAHGUXCSMY-UHFFFAOYSA-N pentacosanoic acid Chemical compound CCCCCCCCCCCCCCCCCCCCCCCCC(O)=O MWMPEAHGUXCSMY-UHFFFAOYSA-N 0.000 description 1
- TYZSSXPDTCVAMM-UHFFFAOYSA-N pentatriacontanoic acid Chemical compound CCCCCCCCCCCCCCCCCCCCCCCCCCCCCCCCCCC(O)=O.CCCCCCCCCCCCCCCCCCCCCCCCCCCCCCCCCCC(O)=O TYZSSXPDTCVAMM-UHFFFAOYSA-N 0.000 description 1
- 239000000810 peripheral vasodilating agent Substances 0.000 description 1
- 229960002116 peripheral vasodilator Drugs 0.000 description 1
- 229950000688 phenothiazine Drugs 0.000 description 1
- 125000001997 phenyl group Chemical group [H]C1=C([H])C([H])=C(*)C([H])=C1[H] 0.000 description 1
- QYSPLQLAKJAUJT-UHFFFAOYSA-N piroxicam Chemical compound OC=1C2=CC=CC=C2S(=O)(=O)N(C)C=1C(=O)NC1=CC=CC=N1 QYSPLQLAKJAUJT-UHFFFAOYSA-N 0.000 description 1
- 229960002702 piroxicam Drugs 0.000 description 1
- 239000004014 plasticizer Substances 0.000 description 1
- 229920000642 polymer Polymers 0.000 description 1
- 239000002157 polynucleotide Substances 0.000 description 1
- 108091033319 polynucleotide Proteins 0.000 description 1
- 102000040430 polynucleotide Human genes 0.000 description 1
- 239000000256 polyoxyethylene sorbitan monolaurate Substances 0.000 description 1
- 235000010486 polyoxyethylene sorbitan monolaurate Nutrition 0.000 description 1
- 229920001184 polypeptide Polymers 0.000 description 1
- 229960003089 pramipexole Drugs 0.000 description 1
- FASDKYOPVNHBLU-ZETCQYMHSA-N pramipexole Chemical compound C1[C@@H](NCCC)CCC2=C1SC(N)=N2 FASDKYOPVNHBLU-ZETCQYMHSA-N 0.000 description 1
- 229960004618 prednisone Drugs 0.000 description 1
- XOFYZVNMUHMLCC-ZPOLXVRWSA-N prednisone Chemical compound O=C1C=C[C@]2(C)[C@H]3C(=O)C[C@](C)([C@@](CC4)(O)C(=O)CO)[C@@H]4[C@@H]3CCC2=C1 XOFYZVNMUHMLCC-ZPOLXVRWSA-N 0.000 description 1
- 239000003755 preservative agent Substances 0.000 description 1
- WIKYUJGCLQQFNW-UHFFFAOYSA-N prochlorperazine Chemical compound C1CN(C)CCN1CCCN1C2=CC(Cl)=CC=C2SC2=CC=CC=C21 WIKYUJGCLQQFNW-UHFFFAOYSA-N 0.000 description 1
- 229960003111 prochlorperazine Drugs 0.000 description 1
- 239000000651 prodrug Substances 0.000 description 1
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- 229960003910 promethazine Drugs 0.000 description 1
- 230000001737 promoting effect Effects 0.000 description 1
- 239000003380 propellant Substances 0.000 description 1
- 125000004368 propenyl group Chemical group C(=CC)* 0.000 description 1
- 125000002568 propynyl group Chemical group [*]C#CC([H])([H])[H] 0.000 description 1
- GMVPRGQOIOIIMI-DWKJAMRDSA-N prostaglandin E1 Chemical compound CCCCC[C@H](O)\C=C\[C@H]1[C@H](O)CC(=O)[C@@H]1CCCCCCC(O)=O GMVPRGQOIOIIMI-DWKJAMRDSA-N 0.000 description 1
- 150000003180 prostaglandins Chemical class 0.000 description 1
- 229940127293 prostanoid Drugs 0.000 description 1
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- XNSAINXGIQZQOO-SRVKXCTJSA-N protirelin Chemical compound NC(=O)[C@@H]1CCCN1C(=O)[C@@H](NC(=O)[C@H]1NC(=O)CC1)CC1=CN=CN1 XNSAINXGIQZQOO-SRVKXCTJSA-N 0.000 description 1
- 229940001470 psychoactive drug Drugs 0.000 description 1
- 239000004089 psychotropic agent Substances 0.000 description 1
- 235000008160 pyridoxine Nutrition 0.000 description 1
- 239000011677 pyridoxine Substances 0.000 description 1
- 150000004040 pyrrolidinones Chemical class 0.000 description 1
- 229960001150 ramelteon Drugs 0.000 description 1
- 229940044551 receptor antagonist Drugs 0.000 description 1
- 239000002464 receptor antagonist Substances 0.000 description 1
- 230000001105 regulatory effect Effects 0.000 description 1
- 229930002330 retinoic acid Natural products 0.000 description 1
- 230000005070 ripening Effects 0.000 description 1
- 229960004136 rivastigmine Drugs 0.000 description 1
- 229960000425 rizatriptan Drugs 0.000 description 1
- TXHZXHICDBAVJW-UHFFFAOYSA-N rizatriptan Chemical compound C=1[C]2C(CCN(C)C)=CN=C2C=CC=1CN1C=NC=N1 TXHZXHICDBAVJW-UHFFFAOYSA-N 0.000 description 1
- UHSKFQJFRQCDBE-UHFFFAOYSA-N ropinirole Chemical compound CCCN(CCC)CCC1=CC=CC2=C1CC(=O)N2 UHSKFQJFRQCDBE-UHFFFAOYSA-N 0.000 description 1
- 229960001879 ropinirole Drugs 0.000 description 1
- JBYXPOFIGCOSSB-UQGDGPGGSA-N rumenic acid Chemical compound CCCCCC\C=C/C=C/CCCCCCCC(O)=O JBYXPOFIGCOSSB-UQGDGPGGSA-N 0.000 description 1
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- 229960003310 sildenafil Drugs 0.000 description 1
- 230000007480 spreading Effects 0.000 description 1
- 239000008117 stearic acid Substances 0.000 description 1
- 150000003431 steroids Chemical class 0.000 description 1
- 239000000021 stimulant Substances 0.000 description 1
- 239000000126 substance Substances 0.000 description 1
- GGCSSNBKKAUURC-UHFFFAOYSA-N sufentanil Chemical group C1CN(CCC=2SC=CC=2)CCC1(COC)N(C(=O)CC)C1=CC=CC=C1 GGCSSNBKKAUURC-UHFFFAOYSA-N 0.000 description 1
- 229960003708 sumatriptan Drugs 0.000 description 1
- KQKPFRSPSRPDEB-UHFFFAOYSA-N sumatriptan Chemical compound CNS(=O)(=O)CC1=CC=C2NC=C(CCN(C)C)C2=C1 KQKPFRSPSRPDEB-UHFFFAOYSA-N 0.000 description 1
- 229960000835 tadalafil Drugs 0.000 description 1
- IEHKWSGCTWLXFU-IIBYNOLFSA-N tadalafil Chemical compound C1=C2OCOC2=CC([C@@H]2C3=C([C]4C=CC=CC4=N3)C[C@H]3N2C(=O)CN(C3=O)C)=C1 IEHKWSGCTWLXFU-IIBYNOLFSA-N 0.000 description 1
- RZHACVKGHNMWOP-ZWZRQGCWSA-N tetracosatetraenoic acid n-6 Chemical compound CCCCCCCCCCCCCCC\C=C\C=C\C=C\C=C\C(O)=O RZHACVKGHNMWOP-ZWZRQGCWSA-N 0.000 description 1
- 239000002562 thickening agent Substances 0.000 description 1
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- 230000001748 thyrotropin Effects 0.000 description 1
- 229940034199 thyrotropin-releasing hormone Drugs 0.000 description 1
- UIERETOOQGIECD-ONEGZZNKSA-N tiglic acid Chemical compound C\C=C(/C)C(O)=O UIERETOOQGIECD-ONEGZZNKSA-N 0.000 description 1
- LLPOLZWFYMWNKH-UHFFFAOYSA-N trans-dihydrocodeinone Natural products C1C(N(CCC234)C)C2CCC(=O)C3OC2=C4C1=CC=C2OC LLPOLZWFYMWNKH-UHFFFAOYSA-N 0.000 description 1
- 229960001727 tretinoin Drugs 0.000 description 1
- 125000002469 tricosyl group Chemical group [H]C([*])([H])C([H])([H])C([H])([H])C([H])([H])C([H])([H])C([H])([H])C([H])([H])C([H])([H])C([H])([H])C([H])([H])C([H])([H])C([H])([H])C([H])([H])C([H])([H])C([H])([H])C([H])([H])C([H])([H])C([H])([H])C([H])([H])C([H])([H])C([H])([H])C([H])([H])C([H])([H])[H] 0.000 description 1
- 239000003029 tricyclic antidepressant agent Substances 0.000 description 1
- PHYFQTYBJUILEZ-IUPFWZBJSA-N triolein Chemical compound CCCCCCCC\C=C/CCCCCCCC(=O)OCC(OC(=O)CCCCCCC\C=C/CCCCCCCC)COC(=O)CCCCCCC\C=C/CCCCCCCC PHYFQTYBJUILEZ-IUPFWZBJSA-N 0.000 description 1
- 229960003688 tropisetron Drugs 0.000 description 1
- UIVFDCIXTSJXBB-ITGUQSILSA-N tropisetron Chemical compound C1=CC=C[C]2C(C(=O)O[C@H]3C[C@H]4CC[C@@H](C3)N4C)=CN=C21 UIVFDCIXTSJXBB-ITGUQSILSA-N 0.000 description 1
- 229960000200 ulipristal Drugs 0.000 description 1
- 235000021122 unsaturated fatty acids Nutrition 0.000 description 1
- 150000004670 unsaturated fatty acids Chemical class 0.000 description 1
- 229940005605 valeric acid Drugs 0.000 description 1
- MSRILKIQRXUYCT-UHFFFAOYSA-M valproate semisodium Chemical compound [Na+].CCCC(C(O)=O)CCC.CCCC(C([O-])=O)CCC MSRILKIQRXUYCT-UHFFFAOYSA-M 0.000 description 1
- 229960000604 valproic acid Drugs 0.000 description 1
- 229960002381 vardenafil Drugs 0.000 description 1
- 125000000391 vinyl group Chemical group [H]C([*])=C([H])[H] 0.000 description 1
- 235000019166 vitamin D Nutrition 0.000 description 1
- 239000011710 vitamin D Substances 0.000 description 1
- 150000003710 vitamin D derivatives Chemical class 0.000 description 1
- 239000011647 vitamin D3 Substances 0.000 description 1
- 235000005282 vitamin D3 Nutrition 0.000 description 1
- QYSXJUFSXHHAJI-YRZJJWOYSA-N vitamin D3 Chemical compound C1(/[C@@H]2CC[C@@H]([C@]2(CCC1)C)[C@H](C)CCCC(C)C)=C\C=C1\C[C@@H](O)CCC1=C QYSXJUFSXHHAJI-YRZJJWOYSA-N 0.000 description 1
- 229940011671 vitamin b6 Drugs 0.000 description 1
- 229940046008 vitamin d Drugs 0.000 description 1
- 229940021056 vitamin d3 Drugs 0.000 description 1
- 230000003442 weekly effect Effects 0.000 description 1
- 229960004010 zaleplon Drugs 0.000 description 1
- HUNXMJYCHXQEGX-UHFFFAOYSA-N zaleplon Chemical compound CCN(C(C)=O)C1=CC=CC(C=2N3N=CC(=C3N=CC=2)C#N)=C1 HUNXMJYCHXQEGX-UHFFFAOYSA-N 0.000 description 1
- 229960001360 zolmitriptan Drugs 0.000 description 1
- UTAZCRNOSWWEFR-ZDUSSCGKSA-N zolmitriptan Chemical compound C=1[C]2C(CCN(C)C)=CN=C2C=CC=1C[C@H]1COC(=O)N1 UTAZCRNOSWWEFR-ZDUSSCGKSA-N 0.000 description 1
- 229960001475 zolpidem Drugs 0.000 description 1
- ZAFYATHCZYHLPB-UHFFFAOYSA-N zolpidem Chemical compound N1=C2C=CC(C)=CN2C(CC(=O)N(C)C)=C1C1=CC=C(C)C=C1 ZAFYATHCZYHLPB-UHFFFAOYSA-N 0.000 description 1
Classifications
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- A61K9/0014—Skin, i.e. galenical aspects of topical compositions
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- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K38/00—Medicinal preparations containing peptides
- A61K38/16—Peptides having more than 20 amino acids; Gastrins; Somatostatins; Melanotropins; Derivatives thereof
- A61K38/17—Peptides having more than 20 amino acids; Gastrins; Somatostatins; Melanotropins; Derivatives thereof from animals; from humans
- A61K38/22—Hormones
- A61K38/28—Insulins
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- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K45/00—Medicinal preparations containing active ingredients not provided for in groups A61K31/00 - A61K41/00
- A61K45/06—Mixtures of active ingredients without chemical characterisation, e.g. antiphlogistics and cardiaca
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- A61K47/00—Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient
- A61K47/06—Organic compounds, e.g. natural or synthetic hydrocarbons, polyolefins, mineral oil, petrolatum or ozokerite
- A61K47/08—Organic compounds, e.g. natural or synthetic hydrocarbons, polyolefins, mineral oil, petrolatum or ozokerite containing oxygen, e.g. ethers, acetals, ketones, quinones, aldehydes, peroxides
- A61K47/10—Alcohols; Phenols; Salts thereof, e.g. glycerol; Polyethylene glycols [PEG]; Poloxamers; PEG/POE alkyl ethers
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- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
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- A61K47/06—Organic compounds, e.g. natural or synthetic hydrocarbons, polyolefins, mineral oil, petrolatum or ozokerite
- A61K47/08—Organic compounds, e.g. natural or synthetic hydrocarbons, polyolefins, mineral oil, petrolatum or ozokerite containing oxygen, e.g. ethers, acetals, ketones, quinones, aldehydes, peroxides
- A61K47/12—Carboxylic acids; Salts or anhydrides thereof
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- A—HUMAN NECESSITIES
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- A61K47/06—Organic compounds, e.g. natural or synthetic hydrocarbons, polyolefins, mineral oil, petrolatum or ozokerite
- A61K47/22—Heterocyclic compounds, e.g. ascorbic acid, tocopherol or pyrrolidones
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- A61K8/18—Cosmetics or similar toiletry preparations characterised by the composition
- A61K8/30—Cosmetics or similar toiletry preparations characterised by the composition containing organic compounds
- A61K8/33—Cosmetics or similar toiletry preparations characterised by the composition containing organic compounds containing oxygen
- A61K8/34—Alcohols
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- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
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- A61K8/18—Cosmetics or similar toiletry preparations characterised by the composition
- A61K8/30—Cosmetics or similar toiletry preparations characterised by the composition containing organic compounds
- A61K8/33—Cosmetics or similar toiletry preparations characterised by the composition containing organic compounds containing oxygen
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- A61K8/361—Carboxylic acids having more than seven carbon atoms in an unbroken chain; Salts or anhydrides thereof
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- A61K8/4906—Cosmetics or similar toiletry preparations characterised by the composition containing organic compounds containing heterocyclic compounds with one nitrogen as the only hetero atom
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Landscapes
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- Animal Behavior & Ethology (AREA)
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- Dermatology (AREA)
- Diabetes (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Endocrinology (AREA)
- Immunology (AREA)
- Proteomics, Peptides & Aminoacids (AREA)
- Gastroenterology & Hepatology (AREA)
- Zoology (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- Organic Chemistry (AREA)
- Obesity (AREA)
- Hematology (AREA)
- Toxicology (AREA)
- Medicinal Preparation (AREA)
- Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Cosmetics (AREA)
- Acyclic And Carbocyclic Compounds In Medicinal Compositions (AREA)
Description
[0001]本願は、2014年12月23日出願の米国仮特許出願第62/096,148号に基づく利益を主張し、その全文を引用によって本明細書に援用する。
− 式Iの化合物:
R−(OCH2CH2)y−OH (I)
[式中、RはC1−20アルキル、C2−20アルケニル;又はC2−20アルキニルであり;そしてyは1〜25である];
− 第一ヒドロキシル基を末端基とする四官能性ブロックコポリマー界面活性剤;
− ソルビタン誘導体;
− C8−10アルキルアンモニウム塩;
− 式IIの化合物:
HO−(CH2CH2O)m−C(CH3)(C4H9)−C≡C−C(CH3)(C4H9)−(OCH2CH2)n−OH (II)
[式中、m及びnはそれぞれ独立に1〜25である];
又はそれらの組合せ
を含む。
[0018]第一の成分が式Iの化合物である態様において、yは1〜25である。好適な態様において、yは5〜15、好ましくは8〜10で、9が特に好適である。他の態様において、yは、1、2、3、4、5、6、7、8、9、10、11、12、13、14、15、16、17、18、19、20、21、22、23、24、又は25である。
[0023]本開示の組成物は、約0.1体積%〜約40体積%の第一の成分を含みうる。好適な態様において、組成物は、約1体積%〜約40体積%の第一の成分を含む。他の態様において、組成物は、約0.1体積%〜約5体積%の第一の成分を含む。例えば、組成物は、約0.1、0.2、0.3、0.4、0.5、0.6、0.7、0.8、0.9、1、1.5、2、2.5、3、3.5、4、4.5、5、5.5、6、6.5、7、7.5、8、8.5、9、9.5、10、11、12、13、14、15、16、17、18、19、20、21、22、23、24、25、26、27、28、29、30、31、32、33、34、35、36、37、38、39、又は約40体積%の第一の成分を含みうる。
− 式IIIの化合物:
R2−N(R1)−C(O)−R3 (III)
[式中、各R1は、独立に、H又はC1−3アルキルであり;そして
R2及びR3は、独立に、C1−7アルキルであるか、又はそれらが結合している原子と一緒になって3〜10個の炭素原子を有するラクタムを形成する];
− スルホキシド;
− 尿素;
− 酢酸エチル;
又はそれらの組合せ
を含む。
[0029]他の態様において、第二の成分は尿素、例えばイミダゾリジノンである。
[0032]本開示の組成物に使用するためのアルコールは、少なくとも一つの−OH部分又は少なくとも二つの−OH部分を有するC2−10アルキルアルコールである。例えば、好適なアルコールは、グリセロール、プロピレングリコール、エタノール、イソプロパノール、1−プロパノール、ブタノール、t−ブタノール、ペンタノール、1−オクタノール、及びそれらの組合せなどであるが、エタノールが特に好適である。
[0046]本発明の組成物に使用するのに適切な治療薬の具体例は、ロピニロール(ropinirole)、プラミペキソール(pramipexole)、スマトリプタン(sumatriptan)、ゾルミトリプタン(zolmitriptan)、リザトリプタン(rizatriptan)、アルモトリプタン(almotriptan)、エレトリプタン(eletriptan)、ナラトリプタン(naratriptan)、フロバトリプタン(frovatriptan)、ゾルピデム(zolpidem)、ザレプロン(zaleplon)、エスゾピクロン(eszopiclone)、ラメルテオン(ramelteon)、ドキセピン(doxepin)、ケトプロフェン(ketoprofen)、ケトロラク(ketorolac)、ピロキシカム(piroxicam)、メロキシカム(meloxicam)、ジクロフェナク(diclofenac)、ミフェプリストン(mifepristone)、ウリプリスタル(ulipristal)、シルデナフィル(sildenafil)、バルデナフィル(vardenafil)、タダラフィル(tadalafil)、アルプロスタジル(alprostadil)、レトロゾール(letrozole)、アナストロゾール(anastrozole)、オキシコドン(oxycodone)、ヒドロコドン(hydrocodone)、ブプレノルフィン(buprenorphine)、フェンタニル(fentanyl)、スフェンタニル(sufentanyl)、アルフェンタニル(alfentanyl)、モルヒネ(morphine)、ナロキソン(naloxone)、ナルトレキソン(naltrexone)、ロイプロリド(leuprolide)、ゴセレリン(goserelin)、ヒストレリン(histrelin)、ピリドキシン(pyridoxine)、ドキシラミン(doxylamine)、ジメンヒドロナート(dimenhydronate)、ジフェンヒドラミン(diphenhydramine)、メクリジン(meclizine)、プロメタジン(promethazine)、プロクロルペラジン(prochlorperazine)、ドロペリドール(droperidol)、メタクロプラミド(metaclopramide)、ハロペリドール(haloperidol)、プレドニゾン(prednisone)、メチルプレドニゾン(methylprednisolone)、コルチゾール(cortisol)、チロトロピン(thyrotropin)、チロトロピン放出ホルモン(thyrotropin-releasing hormone)、エストラジオール(estradiol)、プロゲステロン(progesterone)、ゴナドトロピン放出ホルモン(gonadotropin- releasing hormone)、ゴナドトロピン放出ホルモンアゴニスト又はアンタゴニスト(gonadotropin-releasing hormone agonists or antagonists)、及びインスリン(insulin)などである。
[0061]ノナエチレングリコールモノドデシルエーテル(3mL、5.14体積%)、1−メチル−2−ピロリジノン(0.3mL、0.515体積%)、エタノール(4mL、6.86体積%)、オレイン酸(1mL、1.72体積%)、及び水(50mL、85.8体積%)を合わせて混合物を形成する。得られた組成物を、乾燥しているか又は乾燥肌の症状を緩和するために水分を必要としている皮膚の領域に適用する。
[0062]ノナエチレングリコールモノドデシルエーテル(3mL)、1−メチル−2−ピロリジノン(0.3mL)、エタノール(4mL)、オレイン酸(1mL)、及び水(50mL)を合わせて混合物を形成する。有効量の治療薬を前記混合物と合わせ、経皮組成物を形成する。この経皮組成物を患者の皮膚に、治療薬が皮膚から浸透し、患者の血流に入って治療効果を達成するために十分な量及び時間、適用する。
[0063]ノナエチレングリコールモノドデシルエーテル(3mL)、1−メチル−2−ピロリジノン(0.3mL)、エタノール(4mL)、及びオレイン酸(1mL)を合わせて混合物を形成する。有効量の治療薬を前記混合物と合わせ、経皮組成物を形成する。
[0064]実施例3の経皮組成物を患者の皮膚に、治療薬が皮膚から浸透し、患者の血流に入って治療効果を達成するために十分な量及び時間、適用する。
[0065]実施例3の組成物(1mL)を99mLの水と混合する。得られた水性組成物は、敏感組織、例えば粘膜に、治療薬が敏感組織から浸透し、患者の血流に入って治療効果を達成するために十分な時間、適用できる。
[0066]実施例3の組成物(1mL)を49mLの水と混合する。得られた水性組成物は、普通肌に、治療薬が皮膚から浸透し、患者の血流に入って治療効果を達成するために十分な時間、適用できる。
[0067]ノナエチレングリコールモノドデシルエーテル(3mL)、1−メチル−2−ピロリジノン(0.3mL)、エタノール(4mL)、及びリノール酸(1mL)を混合する。次に、インスリン(3mL、100単位/mL、LANTUS SOLOSTAR,Sanofi社)を加えて混合物を形成する。次に、混合物(1mL)を24mLの水と合わせる。得られた水性組成物は、皮膚又は組織に、インスリンが皮膚又は組織から浸透し、患者の血流に入って治療効果を達成するために十分な時間、適用できる。
[0068]ノナエチレングリコールモノドデシルエーテル(3mL)、1−メチル−2−ピ
ロリジノン(0.3mL)、エタノール(4mL)、及びリノール酸(1mL)を混合す
る。次に、インスリン(3mL、100単位/mL、LANTUS SOLOSTAR,
Sanofi社)を加えて混合物を形成する。次に、混合物(1mL)を32.3mLの
水と合わせる。得られた水性組成物は、皮膚又は組織に、インスリンが皮膚又は組織から
浸透し、患者の血流に入って治療効果を達成するために十分な時間、適用できる。
以下に、出願時の特許請求の範囲の記載を示す。
[請求項1]
組成物であって、
・下記を含む第一の成分:
− 式Iの化合物:
R−(OCH2CH2)y−OH (I)
[式中、RはC1−20アルキル、C2−20アルケニル;又はC2−20アルキニルで
あり;そしてyは1〜25である];
− 第一ヒドロキシル基を末端基とする四官能性ブロックコポリマー界面活性剤;
− ソルビタン誘導体;
− C8−10アルキルアンモニウム塩;
− 式IIの化合物:
HO−(CH2CH2O)m−C(CH3)(C4H9)−C≡C−C(CH3)(C4
H9)−(OCH2CH2)n−OH (II)
[式中、m及びnはそれぞれ独立に1〜25である];
− 又はそれらの組合せ;
・下記を含む第二の成分:
− 式IIIのアミド:
R2 −N(R1)−C(O)−R3 (III)
[式中、各R1は、独立に、H又はC1−3アルキルであり;そして
R2及びR3は、独立に、C1−7アルキルであるか、又はそれらが結合している原子と
一緒になって3〜10個の炭素原子を有するラクタムを形成する];
− スルホキシド;
− 尿素;
− 酢酸エチル;
− 又はそれらの組合せ;
・C2−10アルキルアルコール;
・1〜25個の炭素原子を有する有機酸;及び
・任意に水
を含む組成物。
[請求項2]
第一の成分が式Iの化合物である、請求項1に記載の組成物。
[請求項3]
RがC1−20アルキルである、請求項2に記載の組成物。
[請求項4]
式Iの化合物が、セトマクロゴール1000;オクタデカン−1−オール,エトキシレ
ーテド;ポリオキシエチレン(12)トリデシルエーテル;ポリオキシエチレン(10)
トリデシルエーテル;脂肪アルコールポリオキシエチレンエーテル、ポリオキシエチレン
分枝ノニルシクロヘキシルエーテル、ノナエチレングリコールモノドデシルエーテル、2
3−{[4−(2,4,4−トリメチル−2−ペンタニル)シクロヘキシル]オキシ}−
3,6,9,12,15,18,21−ヘプタオキサトリコサン−1−オール、又はそれ
らの組合せである、請求項3に記載の組成物。
[請求項5]
式Iの化合物がノナエチレングリコールモノドデシルエーテルである、請求項3に記載
の組成物。
[請求項6]
RがC2−20アルケニルである、請求項2に記載の組成物。
[請求項7]
式Iの化合物が、ポリオキシ(10)オレイルエーテル、ポリエチレングリコール t
ert−オクチルフェニルエーテル、又はそれらの組合せである、請求項6に記載の組成
物。
[請求項8]
RがC2−20アルキニルである、請求項2に記載の組成物。
[請求項9]
yが5〜15である、請求項1〜8のいずれか1項に記載の組成物。
[請求項10]
yが8〜10、好ましくは9である、請求項1〜9のいずれか1項に記載の組成物。
[請求項11]
第一の成分が、第一ヒドロキシル基を末端基とする四官能性ブロックコポリマー界面活
性剤である、請求項1に記載の組成物。
[請求項12]
第一ヒドロキシル基を末端基とする四官能性ブロックコポリマー界面活性剤が、エチレ
ンジアミンテトラキス(エトキシレート−ブロック−プロポキシレート)である、請求項
11に記載の組成物。
[請求項13]
第一の成分がソルビタン誘導体である、請求項1に記載の組成物。
[請求項14]
ソルビタン誘導体が、ポリオキシエチレンソルビタンテトラオレエート、1,4−アン
ヒドロ−6−O−パルミトイル−D−グルシトール(ソルビタン,モノヘキサデカノエー
ト)、ポリエチレングリコールソルビタンモノラウレート、又はそれらの組合せである、
請求項13に記載の組成物。
[請求項15]
第一の成分がC8−10アルキルアンモニウム塩である、請求項1に記載の組成物。
[請求項16]
C8−10アルキルアンモニウム塩がメチルトリアルキル(C8−C10)アンモニウ
ムクロリド(ADOGEN 464)である、請求項15に記載の組成物。
[請求項17]
第一の成分が式IIの化合物である、請求項1に記載の組成物。
[請求項18]
水を含む、請求項1〜17のいずれか1項に記載の組成物。
[請求項19]
塩化ナトリウムを含む、請求項18に記載の組成物。
[請求項20]
第二の成分が式IIIの化合物である、請求項1〜19のいずれか1項に記載の組成物。
[請求項21]
R1がメチル、エチル、又はプロピルである、請求項20に記載の組成物。
[請求項22]
R2及びR3が、それらが結合している原子と一緒になって3〜10個の炭素原子を有
するラクタムを形成している、請求項20又は21に記載の組成物。
[請求項23]
ラクタムがピロリドンである、請求項22に記載の組成物。
[請求項24]
ピロリドンが、2−ピロリドン、1−メチル−2−ピロリドン、5−メチル−2−ピロ
リドン、又は1−エチル−2−ピロリドンである、請求項23に記載の組成物。
[請求項25]
ピロリジノンが1−メチル−2−ピロリジノンである、請求項23に記載の組成物。
[請求項26]
第二の成分がスルホキシドである、請求項1〜18のいずれか1項に記載の組成物。
[請求項27]
スルホキシドがジメチルスルホキシドである、請求項26に記載の組成物。
[請求項28]
第二の成分が尿素である、請求項1〜18のいずれか1項に記載の組成物。
[請求項29]
尿素がイミダゾリジノンである、請求項28に記載の組成物。
[請求項30]
第二の成分が酢酸エチルである、請求項1〜18のいずれか1項に記載の組成物。
[請求項31]
C2−10アルキルアルコールが、グリセロール、プロピレングリコール、エタノール
、イソプロパノール、1−プロパノール、ブタノール、t−ブタノール、ペンタノール、
1−オクタノール、又はそれらの組合せである、請求項1〜30のいずれか1項に記載の
組成物。
[請求項32]
C2−10アルキルアルコールがエタノールである、請求項31に記載の組成物。
[請求項33]
有機酸が脂肪酸である、請求項1〜32のいずれか1項に記載の組成物。
[請求項34]
有機酸がC1−6アルキル酸である、請求項1〜32のいずれか1項に記載の組成物。
[請求項35]
有機酸が、酢酸、アスコルビン酸、乳酸、グリコール酸、プロピオン酸、又はそれらの
組合せである、請求項34に記載の組成物。
[請求項36]
第一の成分対第二の成分の比が約10:1である、請求項1〜35のいずれか1項に記
載の組成物。
[請求項37]
約36体積%の第一の成分と;
約4体積%の第二の成分と;
約48体積%のC2−10アルキルアルコールと;そして
約12体積%の有機酸と
を含む、請求項1〜36のいずれか1項に記載の組成物。
[請求項38]
約5体積%の第一の成分と;
約0.5体積%の第二の成分と;
約7体積%のC2−10アルキルアルコールと;
約2体積%の有機酸と;そして
約85体積%の水と
を含む、請求項1〜36のいずれか1項に記載の組成物。
[請求項39]
ゲル、経皮パッチ、ローション、クリーム、スプレー、エマルション、又は分散剤の形
態である、請求項1〜38のいずれか1項に記載の組成物。
[請求項40]
治療薬をさらに含む、請求項1〜39のいずれか1項に記載の組成物。
[請求項41]
請求項1〜39のいずれか1項に記載の組成物を、哺乳動物の皮膚に、前記組成物の少
なくとも一部が前記皮膚を通過するのを達成するのに有効な時間と条件下で投与すること
を含む方法。
[請求項42]
哺乳動物において水分量が望ましくないほど低いレベルである皮膚の領域を識別し、そ
して請求項1〜39のいずれか1項に記載された組成物を前記皮膚に適用する工程を含む
方法。
[請求項43]
請求項40に記載の組成物を哺乳動物の皮膚に、治療薬の少なくとも一部が皮膚を通じ
て浸透するのを達成するのに足る時間、適用することを含む方法。
Claims (14)
- 組成物であって、
・0.1体積%〜40体積%の、ノナエチレングリコールモノドデシルエーテルを含む第一の成分;
・0.01体積%〜10体積%の、1−メチル−2−ピロリドンを含む第二の成分;
・0.1体積%〜50体積%の、C2−10アルキルアルコール;
・0.01体積%〜15体積%の、1〜25個の炭素原子を有する、脂肪酸である有機酸;及び
・任意に水
を含む組成物。 - 水を含む、請求項1に記載の組成物。
- 所定量の生理的に許容可能な塩を含む、請求項2に記載の組成物。
- 当該生理的に許容可能な塩が、塩化ナトリウム、塩化カリウム、又はそれらの混合物で
ある、請求項3に記載の組成物。 - C2−10アルキルアルコールが、グリセロール、プロピレングリコール、エタノール
、イソプロパノール、1−プロパノール、ブタノール、t−ブタノール、ペンタノール、
1−オクタノール、又はそれらの組合せである、請求項1〜4のいずれか1項に記載の
組成物。 - C2−10アルキルアルコールがエタノールである、請求項5に記載の組成物。
- 第一の成分対第二の成分の比が約10:1である、請求項1〜6のいずれか1項に記
載の組成物。 - 約36体積%の第一の成分と;
約4体積%の第二の成分と;
約48体積%のC2−10アルキルアルコールと;そして
約12体積%の前記有機酸と
を含む、請求項1〜7のいずれか1項に記載の組成物。 - 約5体積%の第一の成分と;
約0.5体積%の第二の成分と;
約7体積%のC2−10アルキルアルコールと;
約2体積%の前記有機酸と;そして
約85体積%の水と
を含む、請求項1〜8のいずれか1項に記載の組成物。 - ゲル、経皮パッチ、ローション、クリーム、スプレー、エマルション、又は分散剤の形
態である、請求項1〜9のいずれか1項に記載の組成物。 - 治療薬をさらに含む、請求項1〜10のいずれか1項に記載の組成物。
- 請求項1〜11のいずれか1項に記載の組成物であって、
哺乳動物の皮膚に、前記組成物の少なくとも一部が前記皮膚を通過するのを達成するのに
有効な時間と条件下で当該組成物を投与することを含む方法において用いるためのもので
ある、前記組成物。 - 請求項1〜11のいずれか1項に記載の組成物であって、
哺乳動物において水分量が望ましくないほど低いレベルである皮膚の領域を識別し、そし
て当該組成物を前記皮膚に適用する工程を含む方法において用いるためのものである、前
記組成物。 - 請求項1〜11のいずれか1項に記載の組成物であって、
当該組成物を哺乳動物の皮膚に、治療薬の少なくとも一部が皮膚を通じて浸透するのを達
成するのに足る時間、適用することを含む方法において用いるためのものである、前記組
成物。
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CN (1) | CN107405298A (ja) |
AU (1) | AU2015371253B2 (ja) |
BR (1) | BR112017013329A2 (ja) |
CA (1) | CA2968046A1 (ja) |
EA (1) | EA035087B1 (ja) |
ES (1) | ES2953955T3 (ja) |
IL (1) | IL252062A0 (ja) |
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US10272068B2 (en) | 2012-01-17 | 2019-04-30 | Tyme, Inc. | Pharmaceutical compositions and methods |
US10646552B2 (en) | 2012-01-17 | 2020-05-12 | Tyme, Inc. | Pharmaceutical compositions and methods |
US20130183263A1 (en) | 2012-01-17 | 2013-07-18 | Steven Hoffman | Pharmaceutical compositions and methods |
JP2018506715A (ja) | 2015-01-23 | 2018-03-08 | ヴァンダービルト ユニバーシティー | 堅固なインターフェロメーター及びその使用方法 |
EP3612225A1 (en) * | 2017-04-21 | 2020-02-26 | Steven Hoffman | Compositions and methods for treating retinopathy |
JP2020534272A (ja) * | 2017-09-15 | 2020-11-26 | タイム,インコーポレーテッド | 経皮製剤 |
US20200163952A1 (en) * | 2018-11-26 | 2020-05-28 | Steven Hoffman | Compositions and methods for treating nerve agent exposure |
US20200282014A1 (en) * | 2019-03-05 | 2020-09-10 | Hoffman Technologies Llc | Percutaneous anti-microbiota formulations |
US11534420B2 (en) | 2019-05-14 | 2022-12-27 | Tyme, Inc. | Compositions and methods for treating cancer |
EP4132561A4 (en) * | 2020-04-08 | 2024-04-24 | Hoffman Tech Llc | METHODS FOR TREATING DISEASES CHARACTERIZED BY INSULIN DEFICIENCY IN ANIMALS |
US10905698B1 (en) | 2020-05-14 | 2021-02-02 | Tyme, Inc. | Methods of treating SARS-COV-2 infections |
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JPS61210024A (ja) * | 1985-03-14 | 1986-09-18 | Yamanouchi Pharmaceut Co Ltd | 外用塩酸ニカルジピン製剤 |
US4677131A (en) | 1985-11-01 | 1987-06-30 | Merck & Co., Inc. | Cyclic ureas as dermal penetration enhancers |
US5238933A (en) | 1991-10-28 | 1993-08-24 | Sri International | Skin permeation enhancer compositions |
US5618850A (en) | 1995-03-09 | 1997-04-08 | Focal, Inc. | Hydroxy-acid cosmetics |
US20040121023A1 (en) | 1998-11-02 | 2004-06-24 | Victor Stevens | Composition to alleviate pain and topical method of applying same |
EP1150675B1 (en) | 1999-02-09 | 2006-02-01 | Samyang Corporation | A transdermal composition of an antivomiting agent and a preparation containing the same |
CN1167412C (zh) * | 2000-08-03 | 2004-09-22 | 浙江大学 | 一种经皮理疗用药物凝胶 |
DE10158199A1 (de) | 2001-11-27 | 2003-06-18 | Beiersdorf Ag | Juckreizstillende kosmetische und dermatologische Zubereitungen |
AU2012216593B2 (en) | 2002-11-01 | 2014-09-25 | Allergan Sales, Llc | Compositions and methods for transdermal oxybutynin therapy |
ES2377932T3 (es) | 2003-10-10 | 2012-04-03 | Ferring Bv | Formulación farmacéutica transdérmica para minimizar los residuos sobre la piel |
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KR100658436B1 (ko) | 2005-12-09 | 2006-12-27 | 한국화학연구원 | 아데노실코발라민 함유 피부질환 치료용 외용제 조성물 |
US9393218B2 (en) * | 2005-12-23 | 2016-07-19 | Epinamics Gmbh | Use of film-forming hair care polymers from the group of polyurethanes and pharmaceutical preparations and patches that contain these polymers |
EP1800671A1 (de) * | 2005-12-23 | 2007-06-27 | Bayer Schering Pharma Aktiengesellschaft | Verwendung filmbildender Haarpflegepolymere und diese Polymere enthaltenden pharmazeutischen Zubereitungen und Pflaster |
MX2008008211A (es) * | 2005-12-23 | 2008-09-03 | Epinamics Gmbh | Uso de polimeros para el cuidado del cabello formando peliculas del grupo de los poliuretanos y preparaciones farmaceuticas y parches conteniendo estos polimeros. |
CN101045041A (zh) * | 2007-04-29 | 2007-10-03 | 武汉兵兵药业有限公司 | 含布洛芬的巴布剂及其制备方法和应用 |
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EP3488848A1 (en) * | 2012-01-17 | 2019-05-29 | Tyme, Inc. | Tyrosine hydroxylase inhibitors for use in treating cancer |
US20150272666A1 (en) * | 2012-11-02 | 2015-10-01 | Lixiao Wang | Chemical Ablation Formulations and Methods of Treatments for Various Diseases |
KR20160030162A (ko) * | 2013-07-11 | 2016-03-16 | 가부시키가이샤 폴라 파마 | 사용시 거품상을 나타내는 외용 조성물 |
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MX2017008423A (es) | 2017-10-26 |
US10786574B2 (en) | 2020-09-29 |
CA2968046A1 (en) | 2016-06-30 |
JP2021020955A (ja) | 2021-02-18 |
EP3237013C0 (en) | 2023-06-07 |
JP2017538694A (ja) | 2017-12-28 |
EP3237013B1 (en) | 2023-06-07 |
IL252062A0 (en) | 2017-07-31 |
US20160193339A1 (en) | 2016-07-07 |
US20210008214A1 (en) | 2021-01-14 |
PH12017500836A1 (en) | 2017-10-30 |
AU2015371253B2 (en) | 2020-07-23 |
BR112017013329A2 (pt) | 2019-09-03 |
WO2016105530A1 (en) | 2016-06-30 |
EP3237013A1 (en) | 2017-11-01 |
US20190192663A1 (en) | 2019-06-27 |
KR20170117390A (ko) | 2017-10-23 |
CN107405298A (zh) | 2017-11-28 |
ES2953955T3 (es) | 2023-11-17 |
EA035087B1 (ru) | 2020-04-27 |
AU2015371253A1 (en) | 2017-06-01 |
EA201791454A1 (ru) | 2017-12-29 |
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