JPH11501045A - コルチコステロイド含有薬物組成物 - Google Patents
コルチコステロイド含有薬物組成物Info
- Publication number
- JPH11501045A JPH11501045A JP8526697A JP52669796A JPH11501045A JP H11501045 A JPH11501045 A JP H11501045A JP 8526697 A JP8526697 A JP 8526697A JP 52669796 A JP52669796 A JP 52669796A JP H11501045 A JPH11501045 A JP H11501045A
- Authority
- JP
- Japan
- Prior art keywords
- drug composition
- effervescent
- composition according
- alcohol
- effervescent drug
- 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
- 239000000203 mixture Substances 0.000 title claims abstract description 107
- 229940079593 drug Drugs 0.000 title claims abstract description 37
- 239000003814 drug Substances 0.000 title claims abstract description 37
- 239000003246 corticosteroid Substances 0.000 title claims abstract description 29
- 150000002191 fatty alcohols Chemical class 0.000 claims abstract description 24
- 239000003380 propellant Substances 0.000 claims abstract description 19
- 239000000872 buffer Substances 0.000 claims abstract description 16
- XLYOFNOQVPJJNP-UHFFFAOYSA-N water Substances O XLYOFNOQVPJJNP-UHFFFAOYSA-N 0.000 claims abstract description 12
- 201000004681 Psoriasis Diseases 0.000 claims abstract description 11
- 239000004094 surface-active agent Substances 0.000 claims abstract description 11
- 239000004088 foaming agent Substances 0.000 claims abstract description 7
- 210000004761 scalp Anatomy 0.000 claims abstract description 7
- 208000017520 skin disease Diseases 0.000 claims abstract description 6
- LFQSCWFLJHTTHZ-UHFFFAOYSA-N Ethanol Chemical compound CCO LFQSCWFLJHTTHZ-UHFFFAOYSA-N 0.000 claims description 23
- BXWNKGSJHAJOGX-UHFFFAOYSA-N hexadecan-1-ol Chemical compound CCCCCCCCCCCCCCCCO BXWNKGSJHAJOGX-UHFFFAOYSA-N 0.000 claims description 20
- 239000013543 active substance Substances 0.000 claims description 18
- 229960004311 betamethasone valerate Drugs 0.000 claims description 13
- SNHRLVCMMWUAJD-SUYDQAKGSA-N betamethasone valerate Chemical compound C1CC2=CC(=O)C=C[C@]2(C)[C@]2(F)[C@@H]1[C@@H]1C[C@H](C)[C@@](C(=O)CO)(OC(=O)CCCC)[C@@]1(C)C[C@@H]2O SNHRLVCMMWUAJD-SUYDQAKGSA-N 0.000 claims description 13
- 239000006260 foam Substances 0.000 claims description 12
- GLDOVTGHNKAZLK-UHFFFAOYSA-N octadecan-1-ol Chemical compound CCCCCCCCCCCCCCCCCCO GLDOVTGHNKAZLK-UHFFFAOYSA-N 0.000 claims description 12
- JYGXADMDTFJGBT-VWUMJDOOSA-N hydrocortisone Chemical compound O=C1CC[C@]2(C)[C@H]3[C@@H](O)C[C@](C)([C@@](CC4)(O)C(=O)CO)[C@@H]4[C@@H]3CCC2=C1 JYGXADMDTFJGBT-VWUMJDOOSA-N 0.000 claims description 10
- 201000004624 Dermatitis Diseases 0.000 claims description 9
- 229960000541 cetyl alcohol Drugs 0.000 claims description 9
- DNIAPMSPPWPWGF-GSVOUGTGSA-N (R)-(-)-Propylene glycol Chemical compound C[C@@H](O)CO DNIAPMSPPWPWGF-GSVOUGTGSA-N 0.000 claims description 8
- 208000010668 atopic eczema Diseases 0.000 claims description 8
- KFZMGEQAYNKOFK-UHFFFAOYSA-N Isopropanol Chemical compound CC(C)O KFZMGEQAYNKOFK-UHFFFAOYSA-N 0.000 claims description 6
- OKKJLVBELUTLKV-UHFFFAOYSA-N Methanol Chemical compound OC OKKJLVBELUTLKV-UHFFFAOYSA-N 0.000 claims description 6
- 229940070710 valerate Drugs 0.000 claims description 6
- QTBSBXVTEAMEQO-UHFFFAOYSA-N Acetic acid Natural products CC(O)=O QTBSBXVTEAMEQO-UHFFFAOYSA-N 0.000 claims description 5
- FBPFZTCFMRRESA-FSIIMWSLSA-N D-Glucitol Natural products OC[C@H](O)[C@H](O)[C@@H](O)[C@H](O)CO FBPFZTCFMRRESA-FSIIMWSLSA-N 0.000 claims description 5
- 229960000890 hydrocortisone Drugs 0.000 claims description 5
- GOQYKNQRPGWPLP-UHFFFAOYSA-N n-heptadecyl alcohol Natural products CCCCCCCCCCCCCCCCCO GOQYKNQRPGWPLP-UHFFFAOYSA-N 0.000 claims description 5
- 239000000600 sorbitol Substances 0.000 claims description 5
- -1 stearin ester Chemical class 0.000 claims description 5
- 206010012438 Dermatitis atopic Diseases 0.000 claims description 4
- 206010012442 Dermatitis contact Diseases 0.000 claims description 4
- LRHPLDYGYMQRHN-UHFFFAOYSA-N N-Butanol Chemical compound CCCCO LRHPLDYGYMQRHN-UHFFFAOYSA-N 0.000 claims description 4
- 201000009053 Neurodermatitis Diseases 0.000 claims description 4
- 206010039793 Seborrhoeic dermatitis Diseases 0.000 claims description 4
- 150000008064 anhydrides Chemical class 0.000 claims description 4
- 201000008937 atopic dermatitis Diseases 0.000 claims description 4
- 229960000870 betamethasone benzoate Drugs 0.000 claims description 4
- 208000010247 contact dermatitis Diseases 0.000 claims description 4
- 208000005005 intertrigo Diseases 0.000 claims description 4
- 208000008742 seborrheic dermatitis Diseases 0.000 claims description 4
- HLZKNKRTKFSKGZ-UHFFFAOYSA-N tetradecan-1-ol Chemical compound CCCCCCCCCCCCCCO HLZKNKRTKFSKGZ-UHFFFAOYSA-N 0.000 claims description 4
- 206010062639 Herpes dermatitis Diseases 0.000 claims description 3
- 229960002537 betamethasone Drugs 0.000 claims description 3
- UREBDLICKHMUKA-DVTGEIKXSA-N betamethasone Chemical compound C1CC2=CC(=O)C=C[C@]2(C)[C@]2(F)[C@@H]1[C@@H]1C[C@H](C)[C@@](C(=O)CO)(O)[C@@]1(C)C[C@@H]2O UREBDLICKHMUKA-DVTGEIKXSA-N 0.000 claims description 3
- SOQJPQZCPBDOMF-YCUXZELOSA-N betamethasone benzoate Chemical group O([C@]1([C@@]2(C)C[C@H](O)[C@]3(F)[C@@]4(C)C=CC(=O)C=C4CC[C@H]3[C@@H]2C[C@@H]1C)C(=O)CO)C(=O)C1=CC=CC=C1 SOQJPQZCPBDOMF-YCUXZELOSA-N 0.000 claims description 3
- 229960001102 betamethasone dipropionate Drugs 0.000 claims description 3
- CIWBQSYVNNPZIQ-XYWKZLDCSA-N betamethasone dipropionate Chemical compound C1CC2=CC(=O)C=C[C@]2(C)[C@]2(F)[C@@H]1[C@@H]1C[C@H](C)[C@@](C(=O)COC(=O)CC)(OC(=O)CC)[C@@]1(C)C[C@@H]2O CIWBQSYVNNPZIQ-XYWKZLDCSA-N 0.000 claims description 3
- FEBLZLNTKCEFIT-VSXGLTOVSA-N fluocinolone acetonide Chemical compound C1([C@@H](F)C2)=CC(=O)C=C[C@]1(C)[C@]1(F)[C@@H]2[C@@H]2C[C@H]3OC(C)(C)O[C@@]3(C(=O)CO)[C@@]2(C)C[C@@H]1O FEBLZLNTKCEFIT-VSXGLTOVSA-N 0.000 claims description 3
- 229960005294 triamcinolone Drugs 0.000 claims description 3
- GFNANZIMVAIWHM-OBYCQNJPSA-N triamcinolone Chemical compound O=C1C=C[C@]2(C)[C@@]3(F)[C@@H](O)C[C@](C)([C@@]([C@H](O)C4)(O)C(=O)CO)[C@@H]4[C@@H]3CCC2=C1 GFNANZIMVAIWHM-OBYCQNJPSA-N 0.000 claims description 3
- VOVIALXJUBGFJZ-KWVAZRHASA-N Budesonide Chemical compound C1CC2=CC(=O)C=C[C@]2(C)[C@@H]2[C@@H]1[C@@H]1C[C@H]3OC(CCC)O[C@@]3(C(=O)CO)[C@@]1(C)C[C@@H]2O VOVIALXJUBGFJZ-KWVAZRHASA-N 0.000 claims description 2
- FBPFZTCFMRRESA-JGWLITMVSA-N D-glucitol Chemical compound OC[C@H](O)[C@@H](O)[C@H](O)[C@H](O)CO FBPFZTCFMRRESA-JGWLITMVSA-N 0.000 claims description 2
- IAYPIBMASNFSPL-UHFFFAOYSA-N Ethylene oxide Chemical compound C1CO1 IAYPIBMASNFSPL-UHFFFAOYSA-N 0.000 claims description 2
- DCXXMTOCNZCJGO-UHFFFAOYSA-N Glycerol trioctadecanoate Natural products CCCCCCCCCCCCCCCCCC(=O)OCC(OC(=O)CCCCCCCCCCCCCCCCC)COC(=O)CCCCCCCCCCCCCCCCC DCXXMTOCNZCJGO-UHFFFAOYSA-N 0.000 claims description 2
- HVUMOYIDDBPOLL-XWVZOOPGSA-N Sorbitan monostearate Chemical group CCCCCCCCCCCCCCCCCC(=O)OC[C@@H](O)[C@H]1OC[C@H](O)[C@H]1O HVUMOYIDDBPOLL-XWVZOOPGSA-N 0.000 claims description 2
- FBRAWBYQGRLCEK-UHFFFAOYSA-N [17-(2-chloroacetyl)-9-fluoro-10,13,16-trimethyl-3,11-dioxo-7,8,12,14,15,16-hexahydro-6h-cyclopenta[a]phenanthren-17-yl] butanoate Chemical compound C1CC2=CC(=O)C=CC2(C)C2(F)C1C1CC(C)C(C(=O)CCl)(OC(=O)CCC)C1(C)CC2=O FBRAWBYQGRLCEK-UHFFFAOYSA-N 0.000 claims description 2
- 229960004436 budesonide Drugs 0.000 claims description 2
- 229940069078 citric acid / sodium citrate Drugs 0.000 claims description 2
- 229960004703 clobetasol propionate Drugs 0.000 claims description 2
- CBGUOGMQLZIXBE-XGQKBEPLSA-N clobetasol propionate Chemical compound C1CC2=CC(=O)C=C[C@]2(C)[C@]2(F)[C@@H]1[C@@H]1C[C@H](C)[C@@](C(=O)CCl)(OC(=O)CC)[C@@]1(C)C[C@@H]2O CBGUOGMQLZIXBE-XGQKBEPLSA-N 0.000 claims description 2
- 229960005465 clobetasone butyrate Drugs 0.000 claims description 2
- LQZZUXJYWNFBMV-UHFFFAOYSA-N dodecan-1-ol Chemical compound CCCCCCCCCCCCO LQZZUXJYWNFBMV-UHFFFAOYSA-N 0.000 claims description 2
- 229940042902 flumethasone pivalate Drugs 0.000 claims description 2
- JWRMHDSINXPDHB-OJAGFMMFSA-N flumethasone pivalate Chemical compound C1([C@@H](F)C2)=CC(=O)C=C[C@]1(C)[C@]1(F)[C@@H]2[C@@H]2C[C@@H](C)[C@@](C(=O)COC(=O)C(C)(C)C)(O)[C@@]2(C)C[C@@H]1O JWRMHDSINXPDHB-OJAGFMMFSA-N 0.000 claims description 2
- 229960001347 fluocinolone acetonide Drugs 0.000 claims description 2
- 229950008509 fluocortin butyl Drugs 0.000 claims description 2
- IPCSVZSSVZVIGE-UHFFFAOYSA-M hexadecanoate Chemical compound CCCCCCCCCCCCCCCC([O-])=O IPCSVZSSVZVIGE-UHFFFAOYSA-M 0.000 claims description 2
- 229940043348 myristyl alcohol Drugs 0.000 claims description 2
- 229940049964 oleate Drugs 0.000 claims description 2
- ZQPPMHVWECSIRJ-KTKRTIGZSA-N oleic acid Chemical compound CCCCCCCC\C=C/CCCCCCCC(O)=O ZQPPMHVWECSIRJ-KTKRTIGZSA-N 0.000 claims description 2
- 238000002360 preparation method Methods 0.000 claims description 2
- NQPDZGIKBAWPEJ-UHFFFAOYSA-N valeric acid Chemical compound CCCCC(O)=O NQPDZGIKBAWPEJ-UHFFFAOYSA-N 0.000 claims description 2
- 229940126534 drug product Drugs 0.000 claims 4
- 238000000034 method Methods 0.000 claims 4
- 239000000825 pharmaceutical preparation Substances 0.000 claims 4
- VHRSUDSXCMQTMA-PJHHCJLFSA-N 6alpha-methylprednisolone Chemical compound C([C@@]12C)=CC(=O)C=C1[C@@H](C)C[C@@H]1[C@@H]2[C@@H](O)C[C@]2(C)[C@@](O)(C(=O)CO)CC[C@H]21 VHRSUDSXCMQTMA-PJHHCJLFSA-N 0.000 claims 1
- QTBSBXVTEAMEQO-UHFFFAOYSA-M Acetate Chemical compound CC([O-])=O QTBSBXVTEAMEQO-UHFFFAOYSA-M 0.000 claims 1
- BMTAFVWTTFSTOG-UHFFFAOYSA-N Butylate Chemical compound CCSC(=O)N(CC(C)C)CC(C)C BMTAFVWTTFSTOG-UHFFFAOYSA-N 0.000 claims 1
- MUQNGPZZQDCDFT-JNQJZLCISA-N Halcinonide Chemical compound C1CC2=CC(=O)CC[C@]2(C)[C@]2(F)[C@@H]1[C@@H]1C[C@H]3OC(C)(C)O[C@@]3(C(=O)CCl)[C@@]1(C)C[C@@H]2O MUQNGPZZQDCDFT-JNQJZLCISA-N 0.000 claims 1
- IGFHQQFPSIBGKE-UHFFFAOYSA-N Nonylphenol Natural products CCCCCCCCCC1=CC=C(O)C=C1 IGFHQQFPSIBGKE-UHFFFAOYSA-N 0.000 claims 1
- 229910019142 PO4 Inorganic materials 0.000 claims 1
- 125000000218 acetic acid group Chemical group C(C)(=O)* 0.000 claims 1
- 239000006172 buffering agent Substances 0.000 claims 1
- 229960003662 desonide Drugs 0.000 claims 1
- WBGKWQHBNHJJPZ-LECWWXJVSA-N desonide Chemical compound C1CC2=CC(=O)C=C[C@]2(C)[C@@H]2[C@@H]1[C@@H]1C[C@H]3OC(C)(C)O[C@@]3(C(=O)CO)[C@@]1(C)C[C@@H]2O WBGKWQHBNHJJPZ-LECWWXJVSA-N 0.000 claims 1
- 229960002593 desoximetasone Drugs 0.000 claims 1
- VWVSBHGCDBMOOT-IIEHVVJPSA-N desoximetasone Chemical compound C1CC2=CC(=O)C=C[C@]2(C)[C@]2(F)[C@@H]1[C@@H]1C[C@@H](C)[C@H](C(=O)CO)[C@@]1(C)C[C@@H]2O VWVSBHGCDBMOOT-IIEHVVJPSA-N 0.000 claims 1
- 230000001747 exhibiting effect Effects 0.000 claims 1
- 229960000785 fluocinonide Drugs 0.000 claims 1
- 229960002383 halcinonide Drugs 0.000 claims 1
- 238000006317 isomerization reaction Methods 0.000 claims 1
- 229960004584 methylprednisolone Drugs 0.000 claims 1
- SNQQPOLDUKLAAF-UHFFFAOYSA-N nonylphenol Chemical compound CCCCCCCCCC1=CC=CC=C1O SNQQPOLDUKLAAF-UHFFFAOYSA-N 0.000 claims 1
- 239000008194 pharmaceutical composition Substances 0.000 claims 1
- NBIIXXVUZAFLBC-UHFFFAOYSA-K phosphate Chemical compound [O-]P([O-])([O-])=O NBIIXXVUZAFLBC-UHFFFAOYSA-K 0.000 claims 1
- 239000008363 phosphate buffer Substances 0.000 claims 1
- 239000007974 sodium acetate buffer Substances 0.000 claims 1
- 239000012064 sodium phosphate buffer Substances 0.000 claims 1
- 210000003491 skin Anatomy 0.000 description 13
- 235000019441 ethanol Nutrition 0.000 description 11
- 210000002615 epidermis Anatomy 0.000 description 8
- ATUOYWHBWRKTHZ-UHFFFAOYSA-N Propane Chemical compound CCC ATUOYWHBWRKTHZ-UHFFFAOYSA-N 0.000 description 6
- KRKNYBCHXYNGOX-UHFFFAOYSA-N citric acid Chemical compound OC(=O)CC(O)(C(O)=O)CC(O)=O KRKNYBCHXYNGOX-UHFFFAOYSA-N 0.000 description 6
- 230000007797 corrosion Effects 0.000 description 6
- 238000005260 corrosion Methods 0.000 description 6
- 238000009472 formulation Methods 0.000 description 6
- 230000000699 topical effect Effects 0.000 description 6
- 229960001334 corticosteroids Drugs 0.000 description 5
- 239000003906 humectant Substances 0.000 description 5
- 239000003112 inhibitor Substances 0.000 description 5
- 239000006071 cream Substances 0.000 description 4
- 239000004604 Blowing Agent Substances 0.000 description 3
- 241000195940 Bryophyta Species 0.000 description 3
- 229920001214 Polysorbate 60 Polymers 0.000 description 3
- DNIAPMSPPWPWGF-UHFFFAOYSA-N Propylene glycol Chemical group CC(O)CO DNIAPMSPPWPWGF-UHFFFAOYSA-N 0.000 description 3
- 229960004543 anhydrous citric acid Drugs 0.000 description 3
- 239000008346 aqueous phase Substances 0.000 description 3
- 239000001273 butane Substances 0.000 description 3
- 239000006210 lotion Substances 0.000 description 3
- 235000011929 mousse Nutrition 0.000 description 3
- IJDNQMDRQITEOD-UHFFFAOYSA-N n-butane Chemical compound CCCC IJDNQMDRQITEOD-UHFFFAOYSA-N 0.000 description 3
- OFBQJSOFQDEBGM-UHFFFAOYSA-N n-pentane Natural products CCCCC OFBQJSOFQDEBGM-UHFFFAOYSA-N 0.000 description 3
- 230000035515 penetration Effects 0.000 description 3
- 239000012071 phase Substances 0.000 description 3
- 239000001818 polyoxyethylene sorbitan monostearate Substances 0.000 description 3
- 235000010989 polyoxyethylene sorbitan monostearate Nutrition 0.000 description 3
- 229940113124 polysorbate 60 Drugs 0.000 description 3
- 239000001508 potassium citrate Substances 0.000 description 3
- 229960002635 potassium citrate Drugs 0.000 description 3
- QEEAPRPFLLJWCF-UHFFFAOYSA-K potassium citrate (anhydrous) Chemical compound [K+].[K+].[K+].[O-]C(=O)CC(O)(CC([O-])=O)C([O-])=O QEEAPRPFLLJWCF-UHFFFAOYSA-K 0.000 description 3
- 235000011082 potassium citrates Nutrition 0.000 description 3
- 239000001294 propane Substances 0.000 description 3
- 239000000243 solution Substances 0.000 description 3
- 235000010356 sorbitol Nutrition 0.000 description 3
- 239000000126 substance Substances 0.000 description 3
- PEDCQBHIVMGVHV-UHFFFAOYSA-N Glycerine Chemical compound OCC(O)CO PEDCQBHIVMGVHV-UHFFFAOYSA-N 0.000 description 2
- NBIIXXVUZAFLBC-UHFFFAOYSA-N Phosphoric acid Chemical compound OP(O)(O)=O NBIIXXVUZAFLBC-UHFFFAOYSA-N 0.000 description 2
- 239000000654 additive Substances 0.000 description 2
- 230000001476 alcoholic effect Effects 0.000 description 2
- XAGFODPZIPBFFR-UHFFFAOYSA-N aluminium Chemical compound [Al] XAGFODPZIPBFFR-UHFFFAOYSA-N 0.000 description 2
- 229910052782 aluminium Inorganic materials 0.000 description 2
- WPYMKLBDIGXBTP-UHFFFAOYSA-N benzoic acid Chemical compound OC(=O)C1=CC=CC=C1 WPYMKLBDIGXBTP-UHFFFAOYSA-N 0.000 description 2
- 239000007979 citrate buffer Substances 0.000 description 2
- XWTIDFOGTCVGQB-FHIVUSPVSA-N fluocortin butyl Chemical group C1([C@@H](F)C2)=CC(=O)C=C[C@]1(C)[C@@H]1[C@@H]2[C@@H]2C[C@@H](C)[C@H](C(=O)C(=O)OCCCC)[C@@]2(C)C[C@@H]1O XWTIDFOGTCVGQB-FHIVUSPVSA-N 0.000 description 2
- 229960002650 fluprednidene acetate Drugs 0.000 description 2
- DEFOZIFYUBUHHU-IYQKUMFPSA-N fluprednidene acetate Chemical compound C1CC2=CC(=O)C=C[C@]2(C)[C@]2(F)[C@@H]1[C@@H]1CC(=C)[C@@](C(=O)COC(=O)C)(O)[C@@]1(C)C[C@@H]2O DEFOZIFYUBUHHU-IYQKUMFPSA-N 0.000 description 2
- 230000007794 irritation Effects 0.000 description 2
- 239000007788 liquid Substances 0.000 description 2
- 229960002744 mometasone furoate Drugs 0.000 description 2
- WOFMFGQZHJDGCX-ZULDAHANSA-N mometasone furoate Chemical compound O([C@]1([C@@]2(C)C[C@H](O)[C@]3(Cl)[C@@]4(C)C=CC(=O)C=C4CC[C@H]3[C@@H]2C[C@H]1C)C(=O)CCl)C(=O)C1=CC=CO1 WOFMFGQZHJDGCX-ZULDAHANSA-N 0.000 description 2
- 230000037368 penetrate the skin Effects 0.000 description 2
- 239000000546 pharmaceutical excipient Substances 0.000 description 2
- 239000008213 purified water Substances 0.000 description 2
- 239000002904 solvent Substances 0.000 description 2
- DDMOUSALMHHKOS-UHFFFAOYSA-N 1,2-dichloro-1,1,2,2-tetrafluoroethane Chemical compound FC(F)(Cl)C(F)(F)Cl DDMOUSALMHHKOS-UHFFFAOYSA-N 0.000 description 1
- CHHHXKFHOYLYRE-UHFFFAOYSA-M 2,4-Hexadienoic acid, potassium salt (1:1), (2E,4E)- Chemical compound [K+].CC=CC=CC([O-])=O CHHHXKFHOYLYRE-UHFFFAOYSA-M 0.000 description 1
- IEORSVTYLWZQJQ-UHFFFAOYSA-N 2-(2-nonylphenoxy)ethanol Chemical compound CCCCCCCCCC1=CC=CC=C1OCCO IEORSVTYLWZQJQ-UHFFFAOYSA-N 0.000 description 1
- 239000005711 Benzoic acid Substances 0.000 description 1
- QWOJMRHUQHTCJG-UHFFFAOYSA-N CC([CH2-])=O Chemical compound CC([CH2-])=O QWOJMRHUQHTCJG-UHFFFAOYSA-N 0.000 description 1
- KRKNYBCHXYNGOX-UHFFFAOYSA-K Citrate Chemical compound [O-]C(=O)CC(O)(CC([O-])=O)C([O-])=O KRKNYBCHXYNGOX-UHFFFAOYSA-K 0.000 description 1
- FBRAWBYQGRLCEK-AVVSTMBFSA-N Clobetasone butyrate Chemical compound C1CC2=CC(=O)C=C[C@]2(C)[C@]2(F)[C@@H]1[C@@H]1C[C@H](C)[C@@](C(=O)CCl)(OC(=O)CCC)[C@@]1(C)CC2=O FBRAWBYQGRLCEK-AVVSTMBFSA-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
- 239000004338 Dichlorodifluoromethane Substances 0.000 description 1
- 239000004593 Epoxy Substances 0.000 description 1
- 239000004341 Octafluorocyclobutane Substances 0.000 description 1
- VMHLLURERBWHNL-UHFFFAOYSA-M Sodium acetate Chemical compound [Na+].CC([O-])=O VMHLLURERBWHNL-UHFFFAOYSA-M 0.000 description 1
- 239000012190 activator Substances 0.000 description 1
- 230000000996 additive effect Effects 0.000 description 1
- 229910000147 aluminium phosphate Inorganic materials 0.000 description 1
- 229960003099 amcinonide Drugs 0.000 description 1
- ILKJAFIWWBXGDU-MOGDOJJUSA-N amcinonide Chemical compound O([C@@]1([C@H](O2)C[C@@H]3[C@@]1(C[C@H](O)[C@]1(F)[C@@]4(C)C=CC(=O)C=C4CC[C@H]13)C)C(=O)COC(=O)C)C12CCCC1 ILKJAFIWWBXGDU-MOGDOJJUSA-N 0.000 description 1
- 235000010233 benzoic acid Nutrition 0.000 description 1
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- 230000015572 biosynthetic process Effects 0.000 description 1
- 230000003139 buffering effect Effects 0.000 description 1
- AJNWGKMIJZNIBI-UHFFFAOYSA-N butanoic acid;dihydrochloride Chemical compound Cl.Cl.CCCC(O)=O AJNWGKMIJZNIBI-UHFFFAOYSA-N 0.000 description 1
- 239000003795 chemical substances by application Substances 0.000 description 1
- 229960001146 clobetasone Drugs 0.000 description 1
- 239000002131 composite material Substances 0.000 description 1
- 150000001875 compounds Chemical class 0.000 description 1
- PXBRQCKWGAHEHS-UHFFFAOYSA-N dichlorodifluoromethane Chemical compound FC(F)(Cl)Cl PXBRQCKWGAHEHS-UHFFFAOYSA-N 0.000 description 1
- 235000019404 dichlorodifluoromethane Nutrition 0.000 description 1
- 229940087091 dichlorotetrafluoroethane Drugs 0.000 description 1
- 235000014113 dietary fatty acids Nutrition 0.000 description 1
- 238000001035 drying Methods 0.000 description 1
- 230000000694 effects Effects 0.000 description 1
- 239000003995 emulsifying agent Substances 0.000 description 1
- BEFDCLMNVWHSGT-UHFFFAOYSA-N ethenylcyclopentane Chemical compound C=CC1CCCC1 BEFDCLMNVWHSGT-UHFFFAOYSA-N 0.000 description 1
- 238000001704 evaporation Methods 0.000 description 1
- 230000008020 evaporation Effects 0.000 description 1
- 229930195729 fatty acid Natural products 0.000 description 1
- 239000000194 fatty acid Substances 0.000 description 1
- 150000004665 fatty acids Chemical class 0.000 description 1
- 229940043075 fluocinolone Drugs 0.000 description 1
- 229960005355 fluocortin Drugs 0.000 description 1
- 238000005187 foaming Methods 0.000 description 1
- 235000011187 glycerol Nutrition 0.000 description 1
- 239000012456 homogeneous solution Substances 0.000 description 1
- 230000003993 interaction Effects 0.000 description 1
- 239000007769 metal material Substances 0.000 description 1
- 125000002496 methyl group Chemical group [H]C([H])([H])* 0.000 description 1
- 230000007935 neutral effect Effects 0.000 description 1
- 229920000847 nonoxynol Polymers 0.000 description 1
- BCCOBQSFUDVTJQ-UHFFFAOYSA-N octafluorocyclobutane Chemical compound FC1(F)C(F)(F)C(F)(F)C1(F)F BCCOBQSFUDVTJQ-UHFFFAOYSA-N 0.000 description 1
- 235000019407 octafluorocyclobutane Nutrition 0.000 description 1
- 229940101267 panthenol Drugs 0.000 description 1
- 235000020957 pantothenol Nutrition 0.000 description 1
- 239000011619 pantothenol Substances 0.000 description 1
- 230000000149 penetrating effect Effects 0.000 description 1
- 239000004302 potassium sorbate Substances 0.000 description 1
- 235000010241 potassium sorbate Nutrition 0.000 description 1
- 229940069338 potassium sorbate Drugs 0.000 description 1
- 229960005205 prednisolone Drugs 0.000 description 1
- OIGNJSKKLXVSLS-VWUMJDOOSA-N prednisolone Chemical compound O=C1C=C[C@]2(C)[C@H]3[C@@H](O)C[C@](C)([C@@](CC4)(O)C(=O)CO)[C@@H]4[C@@H]3CCC2=C1 OIGNJSKKLXVSLS-VWUMJDOOSA-N 0.000 description 1
- 230000002028 premature Effects 0.000 description 1
- 230000002035 prolonged effect Effects 0.000 description 1
- 239000001632 sodium acetate Substances 0.000 description 1
- 235000017281 sodium acetate Nutrition 0.000 description 1
- WXMKPNITSTVMEF-UHFFFAOYSA-M sodium benzoate Chemical compound [Na+].[O-]C(=O)C1=CC=CC=C1 WXMKPNITSTVMEF-UHFFFAOYSA-M 0.000 description 1
- 239000004299 sodium benzoate Substances 0.000 description 1
- 235000010234 sodium benzoate Nutrition 0.000 description 1
- 229960003885 sodium benzoate Drugs 0.000 description 1
- 239000001488 sodium phosphate Substances 0.000 description 1
- 229910000162 sodium phosphate Inorganic materials 0.000 description 1
- 239000007787 solid Substances 0.000 description 1
- 239000004334 sorbic acid Substances 0.000 description 1
- 235000010199 sorbic acid Nutrition 0.000 description 1
- 229940075582 sorbic acid Drugs 0.000 description 1
- 238000003756 stirring Methods 0.000 description 1
- 239000005028 tinplate Substances 0.000 description 1
- 229940125379 topical corticosteroid Drugs 0.000 description 1
- RYFMWSXOAZQYPI-UHFFFAOYSA-K trisodium phosphate Chemical compound [Na+].[Na+].[Na+].[O-]P([O-])([O-])=O RYFMWSXOAZQYPI-UHFFFAOYSA-K 0.000 description 1
Classifications
-
- 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
- A61K31/56—Compounds containing cyclopenta[a]hydrophenanthrene ring systems; Derivatives thereof, e.g. steroids
- A61K31/57—Compounds containing cyclopenta[a]hydrophenanthrene ring systems; Derivatives thereof, e.g. steroids substituted in position 17 beta by a chain of two carbon atoms, e.g. pregnane or progesterone
- A61K31/573—Compounds containing cyclopenta[a]hydrophenanthrene ring systems; Derivatives thereof, e.g. steroids substituted in position 17 beta by a chain of two carbon atoms, e.g. pregnane or progesterone substituted in position 21, e.g. cortisone, dexamethasone, prednisone or aldosterone
-
- 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
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K9/00—Medicinal preparations characterised by special physical form
- A61K9/10—Dispersions; Emulsions
- A61K9/12—Aerosols; Foams
- A61K9/122—Foams; Dry foams
-
- 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
- A61P17/06—Antipsoriatics
-
- 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
- A61P17/08—Antiseborrheics
Abstract
Description
Claims (1)
- 【特許請求の範囲】 1.コルチコステロイド活性物質、迅速崩壊発泡剤、プロペラント及び緩衝剤 からなる、発泡性薬物組成物。 2.迅速崩壊発泡剤、プロペラント、緩衝剤及びコルチコステロイド活性物質 からなり、コルチコステロイド活性物質が、異性を示し且つより大きい活性の異 性体及びより小さい活性の異性体を有する種類のものであり、コルチコステロイ ド活性物質がより大きい活性の異性体として存在し、そして緩衝剤が、より小さ い活性の異性体への異性化に対してより大きい活性の異性体を安定化させるため に有効な量で存在する、発泡性薬物組成物。 3.3.0〜6.0の範囲内のpHに緩衝されている、請求項1又は2記載の 発泡性薬物組成物。 4.4.0〜5.0の範囲内のpHに緩衝されている、請求項3記載の発泡性 薬物組成物。 5.緩衝剤が0.01〜1.0%w/wの量で存在する、上記請求項の何れか 1項記載の発泡性薬物組成物。 6.緩衝剤が0.05〜0.2%w/wの量で存在する、請求項5記載の発泡 性薬物組成物。 7.緩衝剤が、酢酸/酢酸ナトリウム緩衝剤、クエン酸/クエン酸ナトリウム 緩衝剤及びリン酸/リン酸ナトリウム緩衝剤から選択 される上記請求項の何れか1項記載の発泡性薬物組成物。 8.コルチコステロイド活性物質が、 ジプロピオン酸アルクロメタゾン フルクロロロンアセトニド アムシノニド フルオシノロンアセトニド ジプロピオン酸ベクラメタゾン フルオシノニド 安息香酸ベタメタゾン フルオコルチンブチル ジプロピオン酸ベタメタゾン フルオコルトロン製剤 吉草酸ベタメタゾン 酢酸フルプレドニデン ブデソニド フルランドレノロン プロピオン酸クロベタゾール ハルシノニド 酪酸クロベタゾン ヒドロコルチゾン デソニド 酢酸ヒドロコルチゾン デスオキシメタゾン 酪酸ヒドロコルチゾン ジ酢酸ジフロラゾン 酢酸メチルプレドニゾロン 吉草酸ジフルコルトロン フロ酸モメタゾン ピバリン酸フルメタゾン トリアムシノロンアセトニド 及びこれらの薬物的に有効な混合物 から選択された局所的に効果のあるコルチコステロイドである上記請求項の何れ か1項記載の発泡性薬物組成物。 9.コルチコステロイド活性物質が、ベタメタゾン又はその誘導体である上記 請求項の何れか1項記載の発泡性薬物組成物。 10.コルチコステロイド活性物質が、安息香酸ベタメタゾン、ジプロピオン 酸ベタメタゾン及び吉草酸ベタメタゾンから選択される請求項9記載の発泡薬物 組成物。 11.コルチコステロイド活性物質が吉草酸ベタメタゾンである請求項10記 載の発泡薬物組成物。 12.コルチコステロイド活性物質が、0.01〜1.0%w/wの量で存在 する上記請求項の何れか1項記載の発泡性薬物組成物。 13.コルチコステロイド活性物質が、0.5〜0.2%w/wの量で存在す る請求項12記載の発泡性薬物組成物。 14.迅速崩壊発泡剤が、脂肪族アルコール、水、脂肪アルコール及び界面活 性剤からなる上記請求項の何れか1項記載の発泡性薬物組成物。 15.脂肪族アルコールが、組成物の全重量の40〜90重量%に相当する量 で存在する請求項14記載の発泡性薬物組成物。 16.脂肪族アルコールが、組成物の55〜70重量%に相当する量で存在す る請求項15記載の発泡性薬物組成物。 17.脂肪族アルコールが、組成物の57〜59重量%に相当する量で存在す る請求項16記載の発泡性薬物組成物。 18.脂肪族アルコールが、メタノール、エタノール、イソプロピルアルコー ル及びブチルアルコール並びにこれらの2種又は3種以上の混合物から選択され る請求項14乃至17の何れか1項記載の発泡性薬物組成物。 19.脂肪族アルコールがエタノールである請求項18記載の発泡性薬物組成 物。 20.水が組成物の10〜40重量%の範囲内の量で存在する請求項14乃至 19の何れか1項記載の発泡性薬物組成物。 21.脂肪アルコールが組成物の0.5〜10重量%に相当する量で存在する 請求項14乃至20の何れか1項記載の発泡性薬物組成物。 22.脂肪アルコールが、セチルアルコール、ステアリルアルコール、ラウリ ルアルコール、ミリスチルアルコール及びパルミチルアルコール並びにこれらの 2種又は3種以上の混合物から選択される請求項14乃至21の何れか1項記載 の発泡性薬物組成物。 23.脂肪アルコールが、セチルアルコールとステアリルアルコールとの混合 物である請求項22記載の発泡性薬物組成物。 24.界面活性剤が組成物の0.1〜15%w/wの量で存在する請求項14 乃至23の何れか1項記載の発泡性薬物組成物。 25.界面活性剤が、エトキシル化ソルビタンステアラート、パルミタート、 オレアート、ノニルフェノール又は脂肪アルコール並びにこれらの2種又は3種 以上の混合物から選択される請求項14乃至24の何れか1項記載の発泡性薬物 組成物。 26.界面活性剤が、ソルビトール及びその無水物1モル当たりエチレンオキ シド約20モルと共重合させたソルビトールの部分ステアリンエステルとその無 水物との混合物である請求項25記載の発泡性薬物組成物。 27.プロペラントガスの圧力に耐えることができ、圧力下に泡として発泡性 組成物を投薬するためのバルブ又はノズルを有する容器内に含有されている、上 記請求項の何れか1項記載の発泡性薬物組成物からなる薬物製品。 28.下記の組成: を有する請求項1記載の発泡性薬物組成物。 29.湿疹、乳児湿疹、アトピー性皮膚炎、疱疹状皮膚炎、接触 皮膚炎、脂漏性皮膚炎、神経皮膚炎、乾癬及び間擦疹の治療で使用するための、 請求項1乃至27の何れか1項記載の発泡性薬物組成物又は請求項28記載の薬 物製品。 30.頭皮乾癬の治療で使用するための請求項29記載の発泡性薬物組成物又 は薬物製品。 31.コルチコステロイド活性物質による治療を受けさせる皮膚疾患の治療方 法であって、それが必要な患者に、有効量の請求項1乃至26の何れか1項記載 の発泡性薬物組成物又は請求項27記載の薬物製品を局所的に投薬することから なる方法。 32.皮膚疾患が、湿疹、乳児湿疹、アトピー性皮膚炎、疱疹状皮膚炎、接触 皮膚炎、脂漏性皮膚炎、神経皮膚炎、乾癬及び間擦疹から選択される請求項31 記載の方法。 33.人患者の頭皮乾癬を治療するための請求項32記載の方法。
Applications Claiming Priority (3)
Application Number | Priority Date | Filing Date | Title |
---|---|---|---|
GBGB9504265.1A GB9504265D0 (en) | 1995-03-03 | 1995-03-03 | Corticosteroid-containing pharmaceutical composition |
GB9504265.1 | 1995-03-03 | ||
PCT/GB1996/000490 WO1996027376A1 (en) | 1995-03-03 | 1996-03-01 | Corticosteroid-containing pharmaceutical composition |
Publications (2)
Publication Number | Publication Date |
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JPH11501045A true JPH11501045A (ja) | 1999-01-26 |
JP4557310B2 JP4557310B2 (ja) | 2010-10-06 |
Family
ID=10770568
Family Applications (1)
Application Number | Title | Priority Date | Filing Date |
---|---|---|---|
JP52669796A Expired - Lifetime JP4557310B2 (ja) | 1995-03-03 | 1996-03-01 | コルチコステロイド含有薬物組成物 |
Country Status (21)
Country | Link |
---|---|
US (3) | US6126920A (ja) |
EP (1) | EP0813413B1 (ja) |
JP (1) | JP4557310B2 (ja) |
KR (1) | KR100427492B1 (ja) |
CN (1) | CN1082817C (ja) |
AT (1) | ATE253367T1 (ja) |
AU (1) | AU709320B2 (ja) |
BR (1) | BR9607687A (ja) |
CA (1) | CA2214436C (ja) |
CZ (1) | CZ285913B6 (ja) |
DE (1) | DE69630593T2 (ja) |
DK (1) | DK0813413T3 (ja) |
ES (1) | ES2210349T3 (ja) |
GB (1) | GB9504265D0 (ja) |
HU (1) | HU228890B1 (ja) |
MX (1) | MX9706698A (ja) |
NZ (1) | NZ302727A (ja) |
PL (1) | PL183730B1 (ja) |
PT (1) | PT813413E (ja) |
SK (1) | SK283049B6 (ja) |
WO (1) | WO1996027376A1 (ja) |
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- 1996-03-01 HU HU9900801A patent/HU228890B1/hu unknown
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