JP2015038129A - 日光角化症の処置のための局所用組成物 - Google Patents
日光角化症の処置のための局所用組成物 Download PDFInfo
- Publication number
- JP2015038129A JP2015038129A JP2014211989A JP2014211989A JP2015038129A JP 2015038129 A JP2015038129 A JP 2015038129A JP 2014211989 A JP2014211989 A JP 2014211989A JP 2014211989 A JP2014211989 A JP 2014211989A JP 2015038129 A JP2015038129 A JP 2015038129A
- Authority
- JP
- Japan
- Prior art keywords
- weight
- composition according
- composition
- active agent
- actinic keratosis
- 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.)
- Withdrawn
Links
- 239000000203 mixture Substances 0.000 title claims abstract description 111
- 208000009621 actinic keratosis Diseases 0.000 title claims abstract description 37
- 230000000699 topical effect Effects 0.000 title claims abstract description 9
- 239000013543 active substance Substances 0.000 claims abstract description 37
- 239000003960 organic solvent Substances 0.000 claims abstract description 16
- YGSDEFSMJLZEOE-UHFFFAOYSA-N salicylic acid Chemical compound OC(=O)C1=CC=CC=C1O YGSDEFSMJLZEOE-UHFFFAOYSA-N 0.000 claims abstract description 14
- 229920001577 copolymer Polymers 0.000 claims abstract description 12
- 229960002949 fluorouracil Drugs 0.000 claims abstract description 12
- QTBSBXVTEAMEQO-UHFFFAOYSA-N Acetic acid Chemical compound CC(O)=O QTBSBXVTEAMEQO-UHFFFAOYSA-N 0.000 claims abstract description 9
- 229920002678 cellulose Polymers 0.000 claims abstract description 8
- 230000000340 anti-metabolite Effects 0.000 claims abstract description 7
- 229940100197 antimetabolite Drugs 0.000 claims abstract description 7
- 239000002256 antimetabolite Substances 0.000 claims abstract description 7
- 239000001913 cellulose Substances 0.000 claims abstract description 7
- FJKROLUGYXJWQN-UHFFFAOYSA-N papa-hydroxy-benzoic acid Natural products OC(=O)C1=CC=C(O)C=C1 FJKROLUGYXJWQN-UHFFFAOYSA-N 0.000 claims abstract description 7
- 229960004889 salicylic acid Drugs 0.000 claims abstract description 7
- XLYOFNOQVPJJNP-UHFFFAOYSA-N water Substances O XLYOFNOQVPJJNP-UHFFFAOYSA-N 0.000 claims abstract description 7
- AEMRFAOFKBGASW-UHFFFAOYSA-N Glycolic acid Chemical compound OCC(O)=O AEMRFAOFKBGASW-UHFFFAOYSA-N 0.000 claims abstract description 6
- 229920001519 homopolymer Polymers 0.000 claims abstract description 6
- JVTAAEKCZFNVCJ-UHFFFAOYSA-N lactic acid Chemical compound CC(O)C(O)=O JVTAAEKCZFNVCJ-UHFFFAOYSA-N 0.000 claims abstract description 6
- 229940042129 topical gel Drugs 0.000 claims abstract description 6
- 239000002599 prostaglandin synthase inhibitor Substances 0.000 claims abstract description 5
- XSQUKJJJFZCRTK-UHFFFAOYSA-N urea group Chemical group NC(=O)N XSQUKJJJFZCRTK-UHFFFAOYSA-N 0.000 claims abstract description 5
- 125000000391 vinyl group Chemical group [H]C([*])=C([H])[H] 0.000 claims abstract description 4
- 229920002554 vinyl polymer Polymers 0.000 claims abstract description 4
- 239000004202 carbamide Substances 0.000 claims abstract description 3
- 239000004310 lactic acid Substances 0.000 claims abstract description 3
- 235000014655 lactic acid Nutrition 0.000 claims abstract description 3
- LFQSCWFLJHTTHZ-UHFFFAOYSA-N Ethanol Chemical compound CCO LFQSCWFLJHTTHZ-UHFFFAOYSA-N 0.000 claims description 13
- 239000003795 chemical substances by application Substances 0.000 claims description 11
- 239000003961 penetration enhancing agent Substances 0.000 claims description 11
- 150000001298 alcohols Chemical class 0.000 claims description 9
- 150000002148 esters Chemical class 0.000 claims description 9
- IAZDPXIOMUYVGZ-UHFFFAOYSA-N dimethyl sulfoxide Natural products CS(C)=O IAZDPXIOMUYVGZ-UHFFFAOYSA-N 0.000 claims description 7
- 125000001931 aliphatic group Chemical group 0.000 claims description 4
- 229920001515 polyalkylene glycol Polymers 0.000 claims description 4
- 150000003505 terpenes Chemical class 0.000 claims description 4
- 238000009835 boiling Methods 0.000 claims description 3
- 150000001732 carboxylic acid derivatives Chemical class 0.000 claims description 3
- 238000000034 method Methods 0.000 claims description 3
- 150000007524 organic acids Chemical class 0.000 claims description 3
- 235000005985 organic acids Nutrition 0.000 claims description 3
- 229940044601 receptor agonist Drugs 0.000 claims description 3
- 239000000018 receptor agonist Substances 0.000 claims description 3
- 102000027483 retinoid hormone receptors Human genes 0.000 claims description 3
- 108091008679 retinoid hormone receptors Proteins 0.000 claims description 3
- 150000003462 sulfoxides Chemical class 0.000 claims description 3
- NIXOWILDQLNWCW-UHFFFAOYSA-M Acrylate Chemical compound [O-]C(=O)C=C NIXOWILDQLNWCW-UHFFFAOYSA-M 0.000 claims description 2
- 150000001735 carboxylic acids Chemical class 0.000 claims description 2
- 150000004040 pyrrolidinones Chemical class 0.000 claims description 2
- 235000007586 terpenes Nutrition 0.000 claims description 2
- 231100000223 dermal penetration Toxicity 0.000 claims 1
- 210000003491 skin Anatomy 0.000 description 22
- 239000000499 gel Substances 0.000 description 19
- 239000003814 drug Substances 0.000 description 8
- 238000009472 formulation Methods 0.000 description 8
- 229940079593 drug Drugs 0.000 description 5
- VVQNEPGJFQJSBK-UHFFFAOYSA-N Methyl methacrylate Chemical compound COC(=O)C(C)=C VVQNEPGJFQJSBK-UHFFFAOYSA-N 0.000 description 4
- 239000006071 cream Substances 0.000 description 4
- 230000000694 effects Effects 0.000 description 4
- SMZOUWXMTYCWNB-UHFFFAOYSA-N 2-(2-methoxy-5-methylphenyl)ethanamine Chemical compound COC1=CC=C(C)C=C1CCN SMZOUWXMTYCWNB-UHFFFAOYSA-N 0.000 description 3
- NIXOWILDQLNWCW-UHFFFAOYSA-N 2-Propenoic acid Natural products OC(=O)C=C NIXOWILDQLNWCW-UHFFFAOYSA-N 0.000 description 3
- -1 5′-fluorouracil Chemical compound 0.000 description 3
- CSCPPACGZOOCGX-UHFFFAOYSA-N Acetone Chemical compound CC(C)=O CSCPPACGZOOCGX-UHFFFAOYSA-N 0.000 description 3
- XEKOWRVHYACXOJ-UHFFFAOYSA-N Ethyl acetate Chemical compound CCOC(C)=O XEKOWRVHYACXOJ-UHFFFAOYSA-N 0.000 description 3
- PEDCQBHIVMGVHV-UHFFFAOYSA-N Glycerine Chemical compound OCC(O)CO PEDCQBHIVMGVHV-UHFFFAOYSA-N 0.000 description 3
- CERQOIWHTDAKMF-UHFFFAOYSA-N Methacrylic acid Chemical compound CC(=C)C(O)=O CERQOIWHTDAKMF-UHFFFAOYSA-N 0.000 description 3
- DNIAPMSPPWPWGF-UHFFFAOYSA-N Propylene glycol Chemical compound CC(O)CO DNIAPMSPPWPWGF-UHFFFAOYSA-N 0.000 description 3
- 239000003921 oil Substances 0.000 description 3
- 239000002904 solvent Substances 0.000 description 3
- KFZMGEQAYNKOFK-UHFFFAOYSA-N Isopropanol Chemical compound CC(C)O KFZMGEQAYNKOFK-UHFFFAOYSA-N 0.000 description 2
- LRHPLDYGYMQRHN-UHFFFAOYSA-N N-Butanol Chemical compound CCCCO LRHPLDYGYMQRHN-UHFFFAOYSA-N 0.000 description 2
- FPIPGXGPPPQFEQ-OVSJKPMPSA-N all-trans-retinol Chemical compound OC\C=C(/C)\C=C\C=C(/C)\C=C\C1=C(C)CCCC1(C)C FPIPGXGPPPQFEQ-OVSJKPMPSA-N 0.000 description 2
- 229960001259 diclofenac Drugs 0.000 description 2
- DCOPUUMXTXDBNB-UHFFFAOYSA-N diclofenac Chemical compound OC(=O)CC1=CC=CC=C1NC1=C(Cl)C=CC=C1Cl DCOPUUMXTXDBNB-UHFFFAOYSA-N 0.000 description 2
- 239000003623 enhancer Substances 0.000 description 2
- 210000002615 epidermis Anatomy 0.000 description 2
- 229960002751 imiquimod Drugs 0.000 description 2
- DOUYETYNHWVLEO-UHFFFAOYSA-N imiquimod Chemical compound C1=CC=CC2=C3N(CC(C)C)C=NC3=C(N)N=C21 DOUYETYNHWVLEO-UHFFFAOYSA-N 0.000 description 2
- 230000035515 penetration Effects 0.000 description 2
- 230000000144 pharmacologic effect Effects 0.000 description 2
- 125000000714 pyrimidinyl group Chemical group 0.000 description 2
- 201000010106 skin squamous cell carcinoma Diseases 0.000 description 2
- 238000002560 therapeutic procedure Methods 0.000 description 2
- PUPZLCDOIYMWBV-UHFFFAOYSA-N (+/-)-1,3-Butanediol Chemical compound CC(O)CCO PUPZLCDOIYMWBV-UHFFFAOYSA-N 0.000 description 1
- FPIPGXGPPPQFEQ-UHFFFAOYSA-N 13-cis retinol Natural products OCC=C(C)C=CC=C(C)C=CC1=C(C)CCCC1(C)C FPIPGXGPPPQFEQ-UHFFFAOYSA-N 0.000 description 1
- ZXBCLVSLRUWISJ-UHFFFAOYSA-N 2-methyl-1-(2-methylpropyl)imidazo[4,5-c][1,5]naphthyridin-4-amine Chemical compound C1=CC=NC2=C3N(CC(C)C)C(C)=NC3=C(N)N=C21 ZXBCLVSLRUWISJ-UHFFFAOYSA-N 0.000 description 1
- DKPFZGUDAPQIHT-UHFFFAOYSA-N Butyl acetate Natural products CCCCOC(C)=O DKPFZGUDAPQIHT-UHFFFAOYSA-N 0.000 description 1
- 201000009030 Carcinoma Diseases 0.000 description 1
- 206010008805 Chromosomal abnormalities Diseases 0.000 description 1
- 208000031404 Chromosome Aberrations Diseases 0.000 description 1
- 229920003136 Eudragit® L polymer Polymers 0.000 description 1
- 229920003153 Eudragit® NE polymer Polymers 0.000 description 1
- 229920003137 Eudragit® S polymer Polymers 0.000 description 1
- 229920003134 Eudragit® polymer Polymers 0.000 description 1
- HEFNNWSXXWATRW-UHFFFAOYSA-N Ibuprofen Chemical compound CC(C)CC1=CC=C(C(C)C(O)=O)C=C1 HEFNNWSXXWATRW-UHFFFAOYSA-N 0.000 description 1
- 206010062016 Immunosuppression Diseases 0.000 description 1
- SHGAZHPCJJPHSC-NUEINMDLSA-N Isotretinoin Chemical compound OC(=O)C=C(C)/C=C/C=C(C)C=CC1=C(C)CCCC1(C)C SHGAZHPCJJPHSC-NUEINMDLSA-N 0.000 description 1
- 239000000020 Nitrocellulose Substances 0.000 description 1
- 108010017842 Telomerase Proteins 0.000 description 1
- 108700025716 Tumor Suppressor Genes Proteins 0.000 description 1
- 102000044209 Tumor Suppressor Genes Human genes 0.000 description 1
- OGQICQVSFDPSEI-UHFFFAOYSA-N Zorac Chemical compound N1=CC(C(=O)OCC)=CC=C1C#CC1=CC=C(SCCC2(C)C)C2=C1 OGQICQVSFDPSEI-UHFFFAOYSA-N 0.000 description 1
- FJWGYAHXMCUOOM-QHOUIDNNSA-N [(2s,3r,4s,5r,6r)-2-[(2r,3r,4s,5r,6s)-4,5-dinitrooxy-2-(nitrooxymethyl)-6-[(2r,3r,4s,5r,6s)-4,5,6-trinitrooxy-2-(nitrooxymethyl)oxan-3-yl]oxyoxan-3-yl]oxy-3,5-dinitrooxy-6-(nitrooxymethyl)oxan-4-yl] nitrate Chemical compound O([C@@H]1O[C@@H]([C@H]([C@H](O[N+]([O-])=O)[C@H]1O[N+]([O-])=O)O[C@H]1[C@@H]([C@@H](O[N+]([O-])=O)[C@H](O[N+]([O-])=O)[C@@H](CO[N+]([O-])=O)O1)O[N+]([O-])=O)CO[N+](=O)[O-])[C@@H]1[C@@H](CO[N+]([O-])=O)O[C@@H](O[N+]([O-])=O)[C@H](O[N+]([O-])=O)[C@H]1O[N+]([O-])=O FJWGYAHXMCUOOM-QHOUIDNNSA-N 0.000 description 1
- 206010000496 acne Diseases 0.000 description 1
- 230000001154 acute effect Effects 0.000 description 1
- 229960002916 adapalene Drugs 0.000 description 1
- LZCDAPDGXCYOEH-UHFFFAOYSA-N adapalene Chemical compound C1=C(C(O)=O)C=CC2=CC(C3=CC=C(C(=C3)C34CC5CC(CC(C5)C3)C4)OC)=CC=C21 LZCDAPDGXCYOEH-UHFFFAOYSA-N 0.000 description 1
- 230000001476 alcoholic effect Effects 0.000 description 1
- SHGAZHPCJJPHSC-YCNIQYBTSA-N all-trans-retinoic acid Chemical compound OC(=O)\C=C(/C)\C=C\C=C(/C)\C=C\C1=C(C)CCCC1(C)C SHGAZHPCJJPHSC-YCNIQYBTSA-N 0.000 description 1
- BVKZGUZCCUSVTD-UHFFFAOYSA-N carbonic acid Chemical class OC(O)=O BVKZGUZCCUSVTD-UHFFFAOYSA-N 0.000 description 1
- 229960000590 celecoxib Drugs 0.000 description 1
- RZEKVGVHFLEQIL-UHFFFAOYSA-N celecoxib Chemical compound C1=CC(C)=CC=C1C1=CC(C(F)(F)F)=NN1C1=CC=C(S(N)(=O)=O)C=C1 RZEKVGVHFLEQIL-UHFFFAOYSA-N 0.000 description 1
- 238000002681 cryosurgery Methods 0.000 description 1
- 230000009089 cytolysis Effects 0.000 description 1
- 238000003745 diagnosis Methods 0.000 description 1
- 239000003937 drug carrier Substances 0.000 description 1
- 238000002651 drug therapy Methods 0.000 description 1
- 208000037828 epithelial carcinoma Diseases 0.000 description 1
- XFBVBWWRPKNWHW-UHFFFAOYSA-N etodolac Chemical compound C1COC(CC)(CC(O)=O)C2=N[C]3C(CC)=CC=CC3=C21 XFBVBWWRPKNWHW-UHFFFAOYSA-N 0.000 description 1
- 229960005293 etodolac Drugs 0.000 description 1
- 238000001704 evaporation Methods 0.000 description 1
- 230000008020 evaporation Effects 0.000 description 1
- 230000001815 facial effect Effects 0.000 description 1
- 150000002334 glycols Chemical class 0.000 description 1
- FUZZWVXGSFPDMH-UHFFFAOYSA-N hexanoic acid Chemical compound CCCCCC(O)=O FUZZWVXGSFPDMH-UHFFFAOYSA-N 0.000 description 1
- 229960001680 ibuprofen Drugs 0.000 description 1
- 230000001506 immunosuppresive effect Effects 0.000 description 1
- 239000004615 ingredient Substances 0.000 description 1
- 229960005280 isotretinoin Drugs 0.000 description 1
- 210000002510 keratinocyte Anatomy 0.000 description 1
- 238000002647 laser therapy Methods 0.000 description 1
- 238000004519 manufacturing process Methods 0.000 description 1
- 238000002483 medication Methods 0.000 description 1
- 239000002480 mineral oil Substances 0.000 description 1
- 235000010446 mineral oil Nutrition 0.000 description 1
- 229960005406 motretinide Drugs 0.000 description 1
- IYIYMCASGKQOCZ-DJRRULDNSA-N motretinide Chemical compound CCNC(=O)\C=C(/C)\C=C\C=C(/C)\C=C\C1=C(C)C=C(OC)C(C)=C1C IYIYMCASGKQOCZ-DJRRULDNSA-N 0.000 description 1
- 230000035772 mutation Effects 0.000 description 1
- 229920001220 nitrocellulos Polymers 0.000 description 1
- 238000001050 pharmacotherapy Methods 0.000 description 1
- 238000000053 physical method Methods 0.000 description 1
- 229960002702 piroxicam Drugs 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
- 239000011505 plaster Substances 0.000 description 1
- 229960003471 retinol Drugs 0.000 description 1
- 235000020944 retinol Nutrition 0.000 description 1
- 239000011607 retinol Substances 0.000 description 1
- 230000035807 sensation Effects 0.000 description 1
- 229950008380 sotirimod Drugs 0.000 description 1
- 210000000434 stratum corneum Anatomy 0.000 description 1
- 150000005846 sugar alcohols Polymers 0.000 description 1
- 230000008833 sun damage Effects 0.000 description 1
- 239000000725 suspension Substances 0.000 description 1
- 229960000565 tazarotene Drugs 0.000 description 1
- 229960001727 tretinoin Drugs 0.000 description 1
Classifications
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K9/00—Medicinal preparations characterised by special physical form
- A61K9/06—Ointments; Bases therefor; Other semi-solid forms, e.g. creams, sticks, gels
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K31/00—Medicinal preparations containing organic active ingredients
- A61K31/185—Acids; Anhydrides, halides or salts thereof, e.g. sulfur acids, imidic, hydrazonic or hydroximic acids
- A61K31/19—Carboxylic acids, e.g. valproic acid
- A61K31/195—Carboxylic acids, e.g. valproic acid having an amino group
- A61K31/196—Carboxylic acids, e.g. valproic acid having an amino group the amino group being directly attached to a ring, e.g. anthranilic acid, mefenamic acid, diclofenac, chlorambucil
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K31/00—Medicinal preparations containing organic active ingredients
- A61K31/33—Heterocyclic compounds
- A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
- A61K31/495—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with two or more nitrogen atoms as the only ring heteroatoms, e.g. piperazine or tetrazines
- A61K31/505—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim
- A61K31/513—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim having oxo groups directly attached to the heterocyclic ring, e.g. cytosine
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K31/00—Medicinal preparations containing organic active ingredients
- A61K31/60—Salicylic acid; Derivatives thereof
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- 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
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- 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
- A61K47/30—Macromolecular organic or inorganic compounds, e.g. inorganic polyphosphates
- A61K47/32—Macromolecular compounds obtained by reactions only involving carbon-to-carbon unsaturated bonds, e.g. carbomers, poly(meth)acrylates, or polyvinyl pyrrolidone
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K9/00—Medicinal preparations characterised by special physical form
- A61K9/0012—Galenical forms characterised by the site of application
- A61K9/0014—Skin, i.e. galenical aspects of topical compositions
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P17/00—Drugs for dermatological disorders
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P17/00—Drugs for dermatological disorders
- A61P17/02—Drugs for dermatological disorders for treating wounds, ulcers, burns, scars, keloids, or the like
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P17/00—Drugs for dermatological disorders
- A61P17/12—Keratolytics, e.g. wart or anti-corn preparations
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P35/00—Antineoplastic agents
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P37/00—Drugs for immunological or allergic disorders
- A61P37/02—Immunomodulators
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P43/00—Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
Landscapes
- Health & Medical Sciences (AREA)
- Chemical & Material Sciences (AREA)
- General Health & Medical Sciences (AREA)
- Veterinary Medicine (AREA)
- Medicinal Chemistry (AREA)
- Public Health (AREA)
- Pharmacology & Pharmacy (AREA)
- Life Sciences & Earth Sciences (AREA)
- Animal Behavior & Ethology (AREA)
- Epidemiology (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- Organic Chemistry (AREA)
- General Chemical & Material Sciences (AREA)
- Chemical Kinetics & Catalysis (AREA)
- Engineering & Computer Science (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Dermatology (AREA)
- Immunology (AREA)
- Inorganic Chemistry (AREA)
- Acyclic And Carbocyclic Compounds In Medicinal Compositions (AREA)
- Medicinal Preparation (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
Abstract
【解決手段】光角化症の処置における使用のための、(a)0.25〜4.5重量%の、シクロオキシゲナーゼ阻害剤、局所用免疫モジュレーター、代謝拮抗物質、およびそれらの混合物かるなる群より選択される日光角化症の処置のための活性薬剤、(b)角質溶解性の活性薬剤、(c)ゲル形成剤、および(d)有機溶媒ならびに、5重量%未満の水を含んでなる、局所用ゲル組成物。該組成物は、実質的には水を含んでいないことが好ましい。該日光角化症の処置のための活性薬剤は、5'−フルオロウラシルであることが好ましい。該角質溶解性活性薬剤としては、尿素、グリコール酸、酢酸、乳酸、サリチル酸であることが好ましい。該ゲル形成剤としては、ビニルホモポリマーおよびコポリマー、セルロース誘導体であることが好ましい。
【選択図】なし
Description
(a)日光角化症の処置のための活性薬剤、
(b)角質溶解性(keratolytically)の活性薬剤、
(c)ゲル形成剤、および
(d)有機溶媒
を含んでなる局所用ゲル組成物を提供する。
(a)日光角化症の処置のための活性薬剤、好ましくは5'−フルオロウラシルを0.25〜4.5重量%、特に0.4〜1重量%、
(b)角質溶解性(keratolytically)の活性薬剤、好ましくはサリチル酸を2〜20重量%、特に5〜15重量%、
(c)ゲル形成剤、好ましくは(メタ)アクリレートホモポリマーまたはコポリマーおよびセルロース誘導体の組み合わせを2〜20重量%、特に5〜15重量%、
(d)C1−C4アルコールのC2−C4カルボン酸とのエステルを40〜70重量%、特に50〜60重量%、
(e)C1−C4アルコールを5〜30重量%、特に10〜20重量%、および
(f)皮膚浸透促進剤、好ましくはジメチルスルホキシドを3〜15重量%、特に5〜10重量%
含んでなる。
Claims (32)
- 日光角化症の処置における使用のための、
(a)日光角化症の処置のための活性薬剤、
(b)角質溶解性(keratolytically)の活性薬剤、
(c)ゲル形成剤、および
(d)有機溶媒
を含んでなる局所用ゲル組成物。 - 組成物が5重量%未満の水を含んでなる、請求項1に記載の組成物。
- 1重量%未満の水を含んでなる、請求項2に記載の組成物。
- 実質的には水を含んでいない、請求項3に記載の組成物。
- ゲルが20℃で300〜1500mPasの範囲内の粘度を有する、請求項1〜4のいずれかに記載の組成物。
- ゲルが20℃で600〜900mPasの範囲内の粘度を有する、請求項5に記載の組成物。
- 日光角化症の処置のための活性薬剤が、シクロオキシゲナーゼ阻害剤、局所用免疫モジュレーター、代謝拮抗物質、およびそれらの混合物よりなる群から選択される、請求項1〜6のいずれかに記載の組成物。
- 日光角化症の処置のための活性薬剤が5'−フルオロウラシルである、請求項7に記載の組成物。
- 組成物が日光角化症の処置のための活性薬剤を0.25〜4.5重量%含んでなる、請求項1〜8のいずれかに記載の組成物。
- 日光角化症の処置のための活性薬剤を0.4〜1重量%含んでなる、請求項9に記載の組成物。
- 角質溶解性(keratolytically)の活性薬剤が、レチノイド受容体アゴニスト、尿素、有機酸、およびそれらの混合物よりなる群から選択される、請求項1〜10のいずれかに記載の組成物。
- 角質溶解性(keratolytically)の活性薬剤が、グリコール酸、酢酸、乳酸、サリチル酸、およびそれらの混合物よりなる群から選択される、請求項11に記載の組成物。
- 角質溶解性(keratolytically)の活性薬剤がサリチル酸である、請求項11に記載の組成物。
- 角質溶解性(keratolytically)の活性薬剤を0.025〜30重量%含んでなる、請求項1〜13のいずれかに記載の組成物。
- 角質溶解性(keratolytically)の活性薬剤を5〜15重量%含んでなる、請求項14に記載の組成物。
- ゲル形成剤が、ビニルホモポリマーおよびコポリマー、セルロース誘導体、並びにそれらの混合物よりなる群から選択される、請求項1〜15のいずれかに記載の組成物。
- ゲル形成剤を1〜30重量%含んでなる、請求項1〜16のいずれかに記載の組成物。
- ゲル形成剤を5〜15重量%含んでなる、請求項17に記載の組成物。
- 有機溶媒が、C1−C10アルコール、C1−C10アルコールのC1−C10カルボン酸とのエステル、およびそれらの混合物よりなる群から選択される、請求項1〜18のいずれかに記載の組成物。
- 有機溶媒がC1−C6アルコールおよびC1−C6アルコールのC2−C6カルボン酸とのエステルを含んでなる、請求項19に記載の組成物。
- 有機溶媒が100℃以下の沸点を有する、請求項1〜20のいずれかに記載の組成物。
- 有機溶媒が80℃以下の沸点を有する、請求項21に記載の組成物。
- 有機溶媒を1〜90重量%含んでなる、請求項1〜22のいずれかに記載の組成物。
- 有機溶媒を60〜75重量%含んでなる、請求項23に記載の組成物。
- 皮膚浸透促進剤をさらに含んでなる、請求項1〜24のいずれかに記載の組成物。
- 皮膚浸透促進剤が、多価脂肪族C2−C10アルコール、C2−C4アルキレン基を有するポリアルキレングリコール、多価脂肪族C2−C10アルコールおよびC2−C4アルキレン基を有するポリアルキレングリコールの非アルコキシル化エステル、アゾン、テルペン、テルペノイド、ピロリドン、スルホキシド、並びにそれらの混合物よりなる群から選択される、請求項25に記載の組成物。
- 皮膚浸透促進剤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。
- 皮膚浸透促進剤を1〜50重量%含んでなる、請求項25〜27のいずれかに記載の組成物。
- 皮膚浸透促進剤を5〜10重量%含んでなる、請求項28に記載の組成物。
- 請求項1に記載の組成物であって、
(a)日光角化症の処置のための活性薬剤を0.25〜4.5重量%、
(b)角質溶解性(keratolytically)の活性薬剤を2〜20重量%、
(c)ゲル形成剤を2〜20重量%、
(d)C1−C4アルコールのC2−C4カルボン酸とのエステルを40〜70重量%、
(e)C1−C4アルコールを5〜30重量%、および
(f)皮膚浸透促進剤を3〜15重量%
含んでなる組成物。 - 請求項30に記載の組成物であって、
(a)5'−フルオロウラシルを0.25〜4.5重量%、
(b)サリチル酸を2〜20重量%、
(c)(メタ)アクリレートホモポリマーまたはコポリマーおよびセルロース誘導体の組み合わせであるゲル形成剤を2〜20重量%、
(d)C1−C4アルコールのC2−C4カルボン酸とのエステルを40〜70重量%、
(e)C1−C4アルコールを5〜30重量%、並びに
(f)ジメチルスルホキシドを3〜15重量%
含んでなる組成物。 - 患者における日光角化症を処置する方法であって、請求項1〜31のいずれかに記載の局所用ゲル組成物を皮膚の患部に塗布することを含んでなる方法。
Applications Claiming Priority (2)
Application Number | Priority Date | Filing Date | Title |
---|---|---|---|
EP08012237.7 | 2008-07-07 | ||
EP08012237A EP2143421A1 (en) | 2008-07-07 | 2008-07-07 | Topical composition for the treatment of actinic keratosis |
Related Parent Applications (1)
Application Number | Title | Priority Date | Filing Date |
---|---|---|---|
JP2011516999A Division JP5654987B2 (ja) | 2008-07-07 | 2009-06-29 | 日光角化症の処置のための局所用組成物 |
Publications (1)
Publication Number | Publication Date |
---|---|
JP2015038129A true JP2015038129A (ja) | 2015-02-26 |
Family
ID=40039993
Family Applications (2)
Application Number | Title | Priority Date | Filing Date |
---|---|---|---|
JP2011516999A Expired - Fee Related JP5654987B2 (ja) | 2008-07-07 | 2009-06-29 | 日光角化症の処置のための局所用組成物 |
JP2014211989A Withdrawn JP2015038129A (ja) | 2008-07-07 | 2014-10-16 | 日光角化症の処置のための局所用組成物 |
Family Applications Before (1)
Application Number | Title | Priority Date | Filing Date |
---|---|---|---|
JP2011516999A Expired - Fee Related JP5654987B2 (ja) | 2008-07-07 | 2009-06-29 | 日光角化症の処置のための局所用組成物 |
Country Status (32)
Country | Link |
---|---|
US (1) | US8569320B2 (ja) |
EP (2) | EP2143421A1 (ja) |
JP (2) | JP5654987B2 (ja) |
KR (1) | KR101689898B1 (ja) |
CN (2) | CN104825384A (ja) |
AR (1) | AR072685A1 (ja) |
AU (1) | AU2009267471B2 (ja) |
BR (1) | BRPI0915439B8 (ja) |
CA (1) | CA2729974A1 (ja) |
CL (1) | CL2010001642A1 (ja) |
CO (1) | CO6351710A2 (ja) |
CY (1) | CY1116111T1 (ja) |
DK (1) | DK2315581T3 (ja) |
EA (1) | EA019533B1 (ja) |
EC (1) | ECSP11010762A (ja) |
ES (1) | ES2532948T3 (ja) |
HK (1) | HK1154793A1 (ja) |
HR (1) | HRP20150222T1 (ja) |
IL (1) | IL210134A (ja) |
ME (1) | ME02147B (ja) |
MX (1) | MX2011000054A (ja) |
MY (1) | MY158428A (ja) |
NZ (1) | NZ590288A (ja) |
PE (1) | PE20110330A1 (ja) |
PL (1) | PL2315581T3 (ja) |
PT (1) | PT2315581E (ja) |
RS (1) | RS53887B1 (ja) |
SI (1) | SI2315581T1 (ja) |
TW (1) | TWI433692B (ja) |
UA (1) | UA101044C2 (ja) |
WO (1) | WO2010003568A1 (ja) |
ZA (1) | ZA201100653B (ja) |
Families Citing this family (13)
Publication number | Priority date | Publication date | Assignee | Title |
---|---|---|---|---|
RU2552470C2 (ru) * | 2009-10-08 | 2015-06-10 | Эм Эс Ди Консьюмер Кэар, Инк. | Композиция с низким содержанием простого эфира и устройство для ее доставки |
JP5950528B2 (ja) * | 2011-09-30 | 2016-07-13 | 小林製薬株式会社 | 皮膜形成性外用製剤 |
US20140348905A1 (en) * | 2011-12-12 | 2014-11-27 | Leo Laboratories Limited | Gel compositions |
NZ606177A (en) * | 2012-01-30 | 2014-03-28 | Dolorgiet Gmbh & Co Kg | Compositions for the treatment of actinic keratosis |
GB201222405D0 (en) * | 2012-12-12 | 2013-01-23 | Leo Lab Ltd | Gel compositions |
CA2956831A1 (en) * | 2014-07-31 | 2016-02-04 | Sun Pharmaceutical Industries Limited | Oral pharmaceutical composition of isotretinoin |
AU2015314287B2 (en) | 2014-09-12 | 2019-04-18 | UNION therapeutics A/S | Antibacterial use of halogenated salicylanilides |
GB201509326D0 (en) | 2015-05-29 | 2015-07-15 | Antibio Tx Aps | Novel use |
AU2015402192B2 (en) | 2015-07-10 | 2021-06-10 | Infectopharm Arzneimittel Und Consilium Gmbh | Use of potassium hydroxide in the treatment of actinic keratosis |
GB201604484D0 (en) * | 2016-03-16 | 2016-04-27 | Antibiotx Aps And Københavns Uni University Of Copenhagen | Topical antibacterial compositions |
WO2018165647A1 (en) | 2017-03-10 | 2018-09-13 | Athenex, Inc. | Methods of treating and/or preventing actinic keratosis |
US11419834B2 (en) | 2019-02-25 | 2022-08-23 | Rhode Island Hospital | Methods for treating diseases or infections caused by or associated with H. pylori using a halogenated salicylanilide |
US20220175769A1 (en) * | 2020-12-08 | 2022-06-09 | Ankh Life Sciences Limited | Method of treatment of actinic keratoses |
Citations (8)
Publication number | Priority date | Publication date | Assignee | Title |
---|---|---|---|---|
JPH0558914A (ja) * | 1991-08-27 | 1993-03-09 | Shiseido Co Ltd | 皮膚外用剤 |
JPH06263644A (ja) * | 1990-10-31 | 1994-09-20 | Efamol Holdings Plc | リチウム治療剤 |
WO1996032112A1 (en) * | 1995-04-12 | 1996-10-17 | Katz Bruce E | Dermatological preparation and method for treating actinic keratoses |
JP2000501429A (ja) * | 1996-09-13 | 2000-02-08 | ジョンソン・アンド・ジョンソン・コンシューマー・カンパニーズ・インコーポレイテッド | 局所治療用および化粧用製剤の組成物基剤 |
JP2000513347A (ja) * | 1996-06-20 | 2000-10-10 | ラヴィファーム エス エー | ざ瘡の局所治療用用具及びその製造方法 |
JP2006527734A (ja) * | 2003-06-19 | 2006-12-07 | フィタ,フェルナンド ボウファルド | 局所投与のための麻酔用組成物 |
JP2007211030A (ja) * | 1996-10-18 | 2007-08-23 | Virotex Corp | 粘膜表面および身体組織に付与可能な薬学的ゲル調製物 |
JP2008504272A (ja) * | 2004-06-24 | 2008-02-14 | アイデックス ラボラトリーズ,インコーポレイティド | 薬物送達のための医薬組成物及びそれを使用する症状の治療又は予防法 |
Family Cites Families (13)
Publication number | Priority date | Publication date | Assignee | Title |
---|---|---|---|---|
US2802005A (en) | 1957-08-06 | S-eluorourace | ||
US4234599A (en) * | 1978-10-04 | 1980-11-18 | Scott Eugene J Van | Treatment of skin keratoses with α-hydroxy acids and related compounds |
US5091171B2 (en) * | 1986-12-23 | 1997-07-15 | Tristrata Inc | Amphoteric compositions and polymeric forms of alpha hydroxyacids and their therapeutic use |
US5167649A (en) * | 1988-08-22 | 1992-12-01 | Zook Gerald P | Drug delivery system for the removal of dermal lesions |
US5093360A (en) * | 1989-04-07 | 1992-03-03 | Yu Ruey J | Retinal, derivatives and their therapeutic use |
US6462071B1 (en) * | 2000-03-02 | 2002-10-08 | Vitreo-Retinal Technologies, Inc. | Agents for intravitreal administration to treat or prevent disorders of the eye |
CN1856294A (zh) * | 2003-08-25 | 2006-11-01 | 弗米克斯有限公司 | 渗透性药物泡沫 |
WO2005027977A2 (en) * | 2003-09-22 | 2005-03-31 | Agis Industries (1983) Ltd. | Diclofenac compositions for the treatment of skin disorders |
US20070053984A1 (en) | 2005-03-03 | 2007-03-08 | Monique Spann-Wade | Topical gels compositions |
EP1890687B1 (en) * | 2005-06-14 | 2008-09-17 | Uni-Pharma Kleon Tsetis Pharmaceutical Laboratories S.A. | Stable pharmaceutical gel of diclofenac sodium |
US7851431B2 (en) * | 2005-07-27 | 2010-12-14 | Prescription Dispensing Laboratories | Treatment of actinic keratoses with calcium channel blockers |
US20070264317A1 (en) * | 2006-05-15 | 2007-11-15 | Perrigo Israel Pharmaceuticals Ltd. | Imiquimod cream formulation |
WO2008047857A1 (fr) * | 2006-10-18 | 2008-04-24 | Fujifilm Corporation | Procédé de production d'une composition comprenant un composé difficilement soluble dans l'eau incorporé dans une matrice hydrophile et préparation pour une utilisation externe comprenant un agent ou médicament anticancéreux ayant un coefficient de partage octanol/eau (log p) de -3,0 ou plus mais pas plus de 3,0, incorporé |
-
2008
- 2008-07-07 EP EP08012237A patent/EP2143421A1/en not_active Withdrawn
-
2009
- 2009-06-29 CN CN201510185320.3A patent/CN104825384A/zh active Pending
- 2009-06-29 RS RS20150185A patent/RS53887B1/en unknown
- 2009-06-29 EA EA201100020A patent/EA019533B1/ru unknown
- 2009-06-29 CA CA2729974A patent/CA2729974A1/en not_active Abandoned
- 2009-06-29 NZ NZ590288A patent/NZ590288A/xx unknown
- 2009-06-29 PL PL09776876T patent/PL2315581T3/pl unknown
- 2009-06-29 UA UAA201101405A patent/UA101044C2/ru unknown
- 2009-06-29 PT PT97768766T patent/PT2315581E/pt unknown
- 2009-06-29 ME MEP-2015-38A patent/ME02147B/me unknown
- 2009-06-29 CN CN2009801266635A patent/CN102088957A/zh active Pending
- 2009-06-29 MX MX2011000054A patent/MX2011000054A/es active IP Right Grant
- 2009-06-29 US US13/002,971 patent/US8569320B2/en active Active
- 2009-06-29 PE PE2010001215A patent/PE20110330A1/es not_active Application Discontinuation
- 2009-06-29 WO PCT/EP2009/004682 patent/WO2010003568A1/en active Application Filing
- 2009-06-29 AU AU2009267471A patent/AU2009267471B2/en active Active
- 2009-06-29 SI SI200931142T patent/SI2315581T1/sl unknown
- 2009-06-29 MY MYPI2011000028A patent/MY158428A/en unknown
- 2009-06-29 EP EP09776876.6A patent/EP2315581B1/en active Active
- 2009-06-29 JP JP2011516999A patent/JP5654987B2/ja not_active Expired - Fee Related
- 2009-06-29 DK DK09776876T patent/DK2315581T3/en active
- 2009-06-29 ES ES09776876.6T patent/ES2532948T3/es active Active
- 2009-06-29 KR KR1020117002825A patent/KR101689898B1/ko active IP Right Grant
- 2009-06-29 BR BRPI0915439A patent/BRPI0915439B8/pt active IP Right Grant
- 2009-07-03 AR ARP090102493A patent/AR072685A1/es unknown
- 2009-07-06 TW TW098122756A patent/TWI433692B/zh active
-
2010
- 2010-12-20 IL IL210134A patent/IL210134A/en active IP Right Grant
- 2010-12-30 CL CL2010001642A patent/CL2010001642A1/es unknown
-
2011
- 2011-01-17 EC ECSP11010762 patent/ECSP11010762A/es unknown
- 2011-01-26 ZA ZA2011/00653A patent/ZA201100653B/en unknown
- 2011-02-07 CO CO11013458A patent/CO6351710A2/es not_active Application Discontinuation
- 2011-08-29 HK HK11109094.3A patent/HK1154793A1/xx unknown
-
2014
- 2014-10-16 JP JP2014211989A patent/JP2015038129A/ja not_active Withdrawn
-
2015
- 2015-02-26 HR HRP20150222TT patent/HRP20150222T1/hr unknown
- 2015-03-13 CY CY20151100254T patent/CY1116111T1/el unknown
Patent Citations (8)
Publication number | Priority date | Publication date | Assignee | Title |
---|---|---|---|---|
JPH06263644A (ja) * | 1990-10-31 | 1994-09-20 | Efamol Holdings Plc | リチウム治療剤 |
JPH0558914A (ja) * | 1991-08-27 | 1993-03-09 | Shiseido Co Ltd | 皮膚外用剤 |
WO1996032112A1 (en) * | 1995-04-12 | 1996-10-17 | Katz Bruce E | Dermatological preparation and method for treating actinic keratoses |
JP2000513347A (ja) * | 1996-06-20 | 2000-10-10 | ラヴィファーム エス エー | ざ瘡の局所治療用用具及びその製造方法 |
JP2000501429A (ja) * | 1996-09-13 | 2000-02-08 | ジョンソン・アンド・ジョンソン・コンシューマー・カンパニーズ・インコーポレイテッド | 局所治療用および化粧用製剤の組成物基剤 |
JP2007211030A (ja) * | 1996-10-18 | 2007-08-23 | Virotex Corp | 粘膜表面および身体組織に付与可能な薬学的ゲル調製物 |
JP2006527734A (ja) * | 2003-06-19 | 2006-12-07 | フィタ,フェルナンド ボウファルド | 局所投与のための麻酔用組成物 |
JP2008504272A (ja) * | 2004-06-24 | 2008-02-14 | アイデックス ラボラトリーズ,インコーポレイティド | 薬物送達のための医薬組成物及びそれを使用する症状の治療又は予防法 |
Non-Patent Citations (2)
Title |
---|
JPN6014032117; American Family Physician Vol.76,No.5, 2007, p.667-671 * |
JPN6016017129; British Journal of Dermatology Vol.92, 1975, p.85-88 * |
Also Published As
Similar Documents
Publication | Publication Date | Title |
---|---|---|
JP5654987B2 (ja) | 日光角化症の処置のための局所用組成物 | |
JP5850889B2 (ja) | 薬物の皮膚送達のための接着性外皮形成製剤とそれを使用する方法 | |
JP6023181B2 (ja) | 爪に投与するための医薬組成物 | |
AU2006326018B2 (en) | Compositions and methods for dermally treating pain | |
US20070190124A1 (en) | Two or more solidifying agent-containing compositions and methods for dermal delivery of drugs | |
WO2010086726A1 (en) | Compositions for nail and skin treatment | |
JP2004505900A5 (ja) | ||
AU2006326034A1 (en) | Flux-enabling compositions and methods for dermal delivery of drugs | |
JP2009540019A (ja) | 局所組成物 | |
RU2008114352A (ru) | Композиции для местного применения | |
JP2010536745A5 (ja) | ||
KR20080049797A (ko) | 항진균 조성물 | |
KR101490708B1 (ko) | 록소프로펜 또는 그의 염을 포함하는 경피 흡수용 조성물및 이를 포함하는 경피 투여 첩부제 | |
NL2016000B1 (en) | Composition for the treatment of keratosis. | |
JP2003321395A (ja) | 外用剤 |
Legal Events
Date | Code | Title | Description |
---|---|---|---|
A131 | Notification of reasons for refusal |
Free format text: JAPANESE INTERMEDIATE CODE: A131 Effective date: 20150908 |
|
A601 | Written request for extension of time |
Free format text: JAPANESE INTERMEDIATE CODE: A601 Effective date: 20151207 |
|
A521 | Request for written amendment filed |
Free format text: JAPANESE INTERMEDIATE CODE: A523 Effective date: 20151214 |
|
A131 | Notification of reasons for refusal |
Free format text: JAPANESE INTERMEDIATE CODE: A131 Effective date: 20160517 |
|
A601 | Written request for extension of time |
Free format text: JAPANESE INTERMEDIATE CODE: A601 Effective date: 20160816 |
|
A601 | Written request for extension of time |
Free format text: JAPANESE INTERMEDIATE CODE: A601 Effective date: 20161014 |
|
A761 | Written withdrawal of application |
Free format text: JAPANESE INTERMEDIATE CODE: A761 Effective date: 20161116 |