AU2014334222B2 - Icotinib-containing topical skin pharmaceutical composition and use thereof - Google Patents
Icotinib-containing topical skin pharmaceutical composition and use thereof Download PDFInfo
- Publication number
- AU2014334222B2 AU2014334222B2 AU2014334222A AU2014334222A AU2014334222B2 AU 2014334222 B2 AU2014334222 B2 AU 2014334222B2 AU 2014334222 A AU2014334222 A AU 2014334222A AU 2014334222 A AU2014334222 A AU 2014334222A AU 2014334222 B2 AU2014334222 B2 AU 2014334222B2
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- Australia
- Prior art keywords
- pharmaceutical composition
- composition according
- group
- icotinib
- concentration
- Prior art date
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- QQLKULDARVNMAL-UHFFFAOYSA-N icotinib Chemical compound C#CC1=CC=CC(NC=2C3=CC=4OCCOCCOCCOC=4C=C3N=CN=2)=C1 QQLKULDARVNMAL-UHFFFAOYSA-N 0.000 title claims abstract description 100
- 229950007440 icotinib Drugs 0.000 title claims abstract description 100
- 230000000699 topical effect Effects 0.000 title claims abstract description 24
- 239000008194 pharmaceutical composition Substances 0.000 title claims description 48
- 238000002360 preparation method Methods 0.000 claims abstract description 59
- 239000004480 active ingredient Substances 0.000 claims abstract description 20
- 150000003839 salts Chemical class 0.000 claims abstract description 13
- 102000004022 Protein-Tyrosine Kinases Human genes 0.000 claims abstract description 6
- 108090000412 Protein-Tyrosine Kinases Proteins 0.000 claims abstract description 6
- 230000002401 inhibitory effect Effects 0.000 claims abstract description 5
- 229940079593 drug Drugs 0.000 claims description 31
- 239000003814 drug Substances 0.000 claims description 31
- XLYOFNOQVPJJNP-UHFFFAOYSA-N water Substances O XLYOFNOQVPJJNP-UHFFFAOYSA-N 0.000 claims description 30
- 239000006071 cream Substances 0.000 claims description 29
- 239000011159 matrix material Substances 0.000 claims description 27
- DNIAPMSPPWPWGF-UHFFFAOYSA-N Propylene glycol Chemical compound CC(O)CO DNIAPMSPPWPWGF-UHFFFAOYSA-N 0.000 claims description 25
- -1 dimethylsiloxane Chemical group 0.000 claims description 23
- 239000000546 pharmaceutical excipient Substances 0.000 claims description 23
- LFQSCWFLJHTTHZ-UHFFFAOYSA-N Ethanol Chemical compound CCO LFQSCWFLJHTTHZ-UHFFFAOYSA-N 0.000 claims description 22
- PEDCQBHIVMGVHV-UHFFFAOYSA-N Glycerine Chemical compound OCC(O)CO PEDCQBHIVMGVHV-UHFFFAOYSA-N 0.000 claims description 20
- 201000004681 Psoriasis Diseases 0.000 claims description 20
- 229920002125 Sokalan® Polymers 0.000 claims description 20
- GLDOVTGHNKAZLK-UHFFFAOYSA-N octadecan-1-ol Chemical compound CCCCCCCCCCCCCCCCCCO GLDOVTGHNKAZLK-UHFFFAOYSA-N 0.000 claims description 20
- NIXOWILDQLNWCW-UHFFFAOYSA-N Acrylic acid Chemical compound OC(=O)C=C NIXOWILDQLNWCW-UHFFFAOYSA-N 0.000 claims description 19
- 208000037265 diseases, disorders, signs and symptoms Diseases 0.000 claims description 19
- HEMHJVSKTPXQMS-UHFFFAOYSA-M Sodium hydroxide Chemical compound [OH-].[Na+] HEMHJVSKTPXQMS-UHFFFAOYSA-M 0.000 claims description 18
- 229960001631 carbomer Drugs 0.000 claims description 18
- KRKNYBCHXYNGOX-UHFFFAOYSA-N citric acid Chemical compound OC(=O)CC(O)(C(O)=O)CC(O)=O KRKNYBCHXYNGOX-UHFFFAOYSA-N 0.000 claims description 18
- 206010020718 hyperplasia Diseases 0.000 claims description 17
- 208000017520 skin disease Diseases 0.000 claims description 17
- 206010048768 Dermatosis Diseases 0.000 claims description 16
- 239000012458 free base Substances 0.000 claims description 15
- 239000000499 gel Substances 0.000 claims description 15
- IAZDPXIOMUYVGZ-UHFFFAOYSA-N Dimethylsulphoxide Chemical compound CS(C)=O IAZDPXIOMUYVGZ-UHFFFAOYSA-N 0.000 claims description 14
- VZCYOOQTPOCHFL-UPHRSURJSA-N maleic acid Chemical compound OC(=O)\C=C/C(O)=O VZCYOOQTPOCHFL-UPHRSURJSA-N 0.000 claims description 14
- VZCYOOQTPOCHFL-UHFFFAOYSA-N trans-butenedioic acid Natural products OC(=O)C=CC(O)=O VZCYOOQTPOCHFL-UHFFFAOYSA-N 0.000 claims description 14
- 238000011282 treatment Methods 0.000 claims description 14
- 239000003995 emulsifying agent Substances 0.000 claims description 13
- 239000002202 Polyethylene glycol Substances 0.000 claims description 11
- 229920001223 polyethylene glycol Polymers 0.000 claims description 11
- 239000000375 suspending agent Substances 0.000 claims description 11
- 229910019142 PO4 Inorganic materials 0.000 claims description 10
- XXJWXESWEXIICW-UHFFFAOYSA-N diethylene glycol monoethyl ether Chemical group CCOCCOCCO XXJWXESWEXIICW-UHFFFAOYSA-N 0.000 claims description 10
- 239000000194 fatty acid Substances 0.000 claims description 10
- 238000000034 method Methods 0.000 claims description 10
- 239000010452 phosphate Substances 0.000 claims description 10
- NBIIXXVUZAFLBC-UHFFFAOYSA-K phosphate Chemical compound [O-]P([O-])([O-])=O NBIIXXVUZAFLBC-UHFFFAOYSA-K 0.000 claims description 10
- KWYUFKZDYYNOTN-UHFFFAOYSA-M Potassium hydroxide Chemical compound [OH-].[K+] KWYUFKZDYYNOTN-UHFFFAOYSA-M 0.000 claims description 9
- 239000003623 enhancer Substances 0.000 claims description 9
- 239000004403 ethyl p-hydroxybenzoate Substances 0.000 claims description 9
- 235000010228 ethyl p-hydroxybenzoate Nutrition 0.000 claims description 9
- NUVBSKCKDOMJSU-UHFFFAOYSA-N ethylparaben Chemical compound CCOC(=O)C1=CC=C(O)C=C1 NUVBSKCKDOMJSU-UHFFFAOYSA-N 0.000 claims description 9
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- 235000011187 glycerol Nutrition 0.000 claims description 8
- 229940057995 liquid paraffin Drugs 0.000 claims description 8
- 239000003755 preservative agent Substances 0.000 claims description 8
- GSEJCLTVZPLZKY-UHFFFAOYSA-N Triethanolamine Chemical compound OCCN(CCO)CCO GSEJCLTVZPLZKY-UHFFFAOYSA-N 0.000 claims description 7
- BXWNKGSJHAJOGX-UHFFFAOYSA-N hexadecan-1-ol Chemical group CCCCCCCCCCCCCCCCO BXWNKGSJHAJOGX-UHFFFAOYSA-N 0.000 claims description 7
- QTBSBXVTEAMEQO-UHFFFAOYSA-N Acetic acid Chemical compound CC(O)=O QTBSBXVTEAMEQO-UHFFFAOYSA-N 0.000 claims description 6
- DBMJMQXJHONAFJ-UHFFFAOYSA-M Sodium laurylsulphate Chemical compound [Na+].CCCCCCCCCCCCOS([O-])(=O)=O DBMJMQXJHONAFJ-UHFFFAOYSA-M 0.000 claims description 6
- OSASVXMJTNOKOY-UHFFFAOYSA-N chlorobutanol Chemical compound CC(C)(O)C(Cl)(Cl)Cl OSASVXMJTNOKOY-UHFFFAOYSA-N 0.000 claims description 6
- 208000035475 disorder Diseases 0.000 claims description 6
- 230000003211 malignant effect Effects 0.000 claims description 6
- 239000002674 ointment Substances 0.000 claims description 6
- 235000019333 sodium laurylsulphate Nutrition 0.000 claims description 6
- 239000004698 Polyethylene Substances 0.000 claims description 5
- 229920000573 polyethylene Polymers 0.000 claims description 5
- CFKMVGJGLGKFKI-UHFFFAOYSA-N 4-chloro-m-cresol Chemical compound CC1=CC(O)=CC=C1Cl CFKMVGJGLGKFKI-UHFFFAOYSA-N 0.000 claims description 4
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- 206010012601 diabetes mellitus Diseases 0.000 claims description 4
- BEFDCLMNVWHSGT-UHFFFAOYSA-N ethenylcyclopentane Chemical compound C=CC1CCCC1 BEFDCLMNVWHSGT-UHFFFAOYSA-N 0.000 claims description 4
- 125000005456 glyceride group Chemical group 0.000 claims description 4
- 229930195733 hydrocarbon Natural products 0.000 claims description 4
- 150000002430 hydrocarbons Chemical class 0.000 claims description 4
- 239000001866 hydroxypropyl methyl cellulose Substances 0.000 claims description 4
- 235000010979 hydroxypropyl methyl cellulose Nutrition 0.000 claims description 4
- 229920003088 hydroxypropyl methyl cellulose Polymers 0.000 claims description 4
- UFVKGYZPFZQRLF-UHFFFAOYSA-N hydroxypropyl methyl cellulose Chemical compound OC1C(O)C(OC)OC(CO)C1OC1C(O)C(O)C(OC2C(C(O)C(OC3C(C(O)C(O)C(CO)O3)O)C(CO)O2)O)C(CO)O1 UFVKGYZPFZQRLF-UHFFFAOYSA-N 0.000 claims description 4
- 150000002632 lipids Chemical class 0.000 claims description 4
- 229920005862 polyol Polymers 0.000 claims description 4
- 229920000056 polyoxyethylene ether Chemical class 0.000 claims description 4
- 229940051841 polyoxyethylene ether Drugs 0.000 claims description 4
- 239000000344 soap Substances 0.000 claims description 4
- 239000001509 sodium citrate Substances 0.000 claims description 4
- NLJMYIDDQXHKNR-UHFFFAOYSA-K sodium citrate Chemical compound O.O.[Na+].[Na+].[Na+].[O-]C(=O)CC(O)(CC([O-])=O)C([O-])=O NLJMYIDDQXHKNR-UHFFFAOYSA-K 0.000 claims description 4
- 239000004334 sorbic acid Substances 0.000 claims description 4
- 235000010199 sorbic acid Nutrition 0.000 claims description 4
- 229940075582 sorbic acid Drugs 0.000 claims description 4
- 235000013871 bee wax Nutrition 0.000 claims description 3
- 239000012166 beeswax Substances 0.000 claims description 3
- 229960004926 chlorobutanol Drugs 0.000 claims description 3
- 229940075557 diethylene glycol monoethyl ether Drugs 0.000 claims description 3
- 239000003921 oil Substances 0.000 claims description 3
- 235000019198 oils Nutrition 0.000 claims description 3
- 229920000036 polyvinylpyrrolidone Polymers 0.000 claims description 3
- 239000001267 polyvinylpyrrolidone Substances 0.000 claims description 3
- 235000013855 polyvinylpyrrolidone Nutrition 0.000 claims description 3
- 239000003549 soybean oil Substances 0.000 claims description 3
- 235000012424 soybean oil Nutrition 0.000 claims description 3
- RZRNAYUHWVFMIP-KTKRTIGZSA-N 1-oleoylglycerol Chemical compound CCCCCCCC\C=C/CCCCCCCC(=O)OCC(O)CO RZRNAYUHWVFMIP-KTKRTIGZSA-N 0.000 claims description 2
- 150000005168 4-hydroxybenzoic acids Chemical class 0.000 claims description 2
- VHUUQVKOLVNVRT-UHFFFAOYSA-N Ammonium hydroxide Chemical compound [NH4+].[OH-] VHUUQVKOLVNVRT-UHFFFAOYSA-N 0.000 claims description 2
- 108010010803 Gelatin Proteins 0.000 claims description 2
- 229920001503 Glucan Polymers 0.000 claims description 2
- 239000004166 Lanolin Substances 0.000 claims description 2
- RVGRUAULSDPKGF-UHFFFAOYSA-N Poloxamer Chemical compound C1CO1.CC1CO1 RVGRUAULSDPKGF-UHFFFAOYSA-N 0.000 claims description 2
- 229920001214 Polysorbate 60 Polymers 0.000 claims description 2
- 229920002651 Polysorbate 85 Polymers 0.000 claims description 2
- VMHLLURERBWHNL-UHFFFAOYSA-M Sodium acetate Chemical compound [Na+].CC([O-])=O VMHLLURERBWHNL-UHFFFAOYSA-M 0.000 claims description 2
- PHYFQTYBJUILEZ-UHFFFAOYSA-N Trioleoylglycerol Natural products CCCCCCCCC=CCCCCCCCC(=O)OCC(OC(=O)CCCCCCCC=CCCCCCCCC)COC(=O)CCCCCCCC=CCCCCCCCC PHYFQTYBJUILEZ-UHFFFAOYSA-N 0.000 claims description 2
- DPXJVFZANSGRMM-UHFFFAOYSA-N acetic acid;2,3,4,5,6-pentahydroxyhexanal;sodium Chemical compound [Na].CC(O)=O.OCC(O)C(O)C(O)C(O)C=O DPXJVFZANSGRMM-UHFFFAOYSA-N 0.000 claims description 2
- 125000000217 alkyl group Chemical group 0.000 claims description 2
- 239000000908 ammonium hydroxide Substances 0.000 claims description 2
- VBICKXHEKHSIBG-UHFFFAOYSA-N beta-monoglyceryl stearate Natural products CCCCCCCCCCCCCCCCCC(=O)OCC(O)CO VBICKXHEKHSIBG-UHFFFAOYSA-N 0.000 claims description 2
- 239000000872 buffer Substances 0.000 claims description 2
- 239000001768 carboxy methyl cellulose Substances 0.000 claims description 2
- 239000004359 castor oil Substances 0.000 claims description 2
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- 229920002678 cellulose Polymers 0.000 claims description 2
- 229960002242 chlorocresol Drugs 0.000 claims description 2
- ZBCBWPMODOFKDW-UHFFFAOYSA-N diethanolamine Chemical compound OCCNCCO ZBCBWPMODOFKDW-UHFFFAOYSA-N 0.000 claims description 2
- BNIILDVGGAEEIG-UHFFFAOYSA-L disodium hydrogen phosphate Chemical compound [Na+].[Na+].OP([O-])([O-])=O BNIILDVGGAEEIG-UHFFFAOYSA-L 0.000 claims description 2
- 229940043351 ethyl-p-hydroxybenzoate Drugs 0.000 claims description 2
- 239000008273 gelatin Substances 0.000 claims description 2
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- 235000019322 gelatine Nutrition 0.000 claims description 2
- 235000011852 gelatine desserts Nutrition 0.000 claims description 2
- ZEMPKEQAKRGZGQ-XOQCFJPHSA-N glycerol triricinoleate Natural products CCCCCC[C@@H](O)CC=CCCCCCCCC(=O)OC[C@@H](COC(=O)CCCCCCCC=CC[C@@H](O)CCCCCC)OC(=O)CCCCCCCC=CC[C@H](O)CCCCCC ZEMPKEQAKRGZGQ-XOQCFJPHSA-N 0.000 claims description 2
- 235000019388 lanolin Nutrition 0.000 claims description 2
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- LXCFILQKKLGQFO-UHFFFAOYSA-N methylparaben Chemical compound COC(=O)C1=CC=C(O)C=C1 LXCFILQKKLGQFO-UHFFFAOYSA-N 0.000 claims description 2
- 229910000403 monosodium phosphate Inorganic materials 0.000 claims description 2
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- IWZKICVEHNUQTL-UHFFFAOYSA-M potassium hydrogen phthalate Chemical compound [K+].OC(=O)C1=CC=CC=C1C([O-])=O IWZKICVEHNUQTL-UHFFFAOYSA-M 0.000 claims description 2
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Landscapes
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| CNPCT/CN2013/085042 | 2013-10-11 | ||
| CN2013085042 | 2013-10-11 | ||
| PCT/CN2014/088344 WO2015051763A1 (zh) | 2013-10-11 | 2014-10-11 | 一种含埃克替尼的皮肤外用药物组合物及其应用 |
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| EP (1) | EP3056206A4 (https=) |
| JP (1) | JP6463745B2 (https=) |
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| KR102270538B1 (ko) * | 2013-06-09 | 2021-06-29 | 베타 파머수티컬 컴퍼니 리미티드 | 이코티닙 포스페이트의 신규한 다형체 형태 및 이의 용도 |
| WO2022022434A1 (zh) * | 2020-07-27 | 2022-02-03 | 杭州和正医药有限公司 | 含托法替尼药学上可接受的盐的药物组合物、制剂及应用 |
| CN116829152A (zh) * | 2021-02-02 | 2023-09-29 | 贝达药业股份有限公司 | 埃克替尼在非小细胞肺癌术后辅助治疗中的应用 |
| CN116492293A (zh) * | 2022-01-25 | 2023-07-28 | 杭州和正医药有限公司 | 一种含托法替尼的局部用药的药物组合物、制剂及应用 |
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| US20110182882A1 (en) * | 2008-07-08 | 2011-07-28 | Beta Pharma, Inc. | Icotinib Hydrochloride, Synthesis, Crystalline Forms, Pharmaceutical Compositions, and Uses Thereof |
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| BRPI0618933A2 (pt) * | 2005-11-24 | 2016-09-13 | Basf Se | método para produzir uma molécula efetora que se liga à queratina, molécula efetora que se liga à queratina, uso das moléculas efetoras que se ligam à queratina, composto, e, dermocosmético |
| FR2909284B1 (fr) * | 2006-11-30 | 2012-09-21 | Galderma Sa | Nouvelles compositions sous forme d'onguent sans vaseline comprenant un derive de vitamine d et eventuellement un anti-inflammatoire steroidien |
| GB201010954D0 (en) * | 2010-06-29 | 2010-08-11 | Edko Pazarlama Tanitim Ticaret | Compositions |
| MX2013004296A (es) * | 2010-10-21 | 2013-09-26 | Cadila Healthcare Ltd | Composiciones farmaceuticas topicas que contienen gotas de tamaño nanometrico para el tratamiento de soriasis. |
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| US20110182882A1 (en) * | 2008-07-08 | 2011-07-28 | Beta Pharma, Inc. | Icotinib Hydrochloride, Synthesis, Crystalline Forms, Pharmaceutical Compositions, and Uses Thereof |
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| JP6463745B2 (ja) | 2019-02-06 |
| IL245015A0 (en) | 2016-05-31 |
| WO2015051763A1 (zh) | 2015-04-16 |
| RU2698796C2 (ru) | 2019-08-30 |
| CA2926874A1 (en) | 2015-04-16 |
| CA2926874C (en) | 2018-12-11 |
| US20190321369A1 (en) | 2019-10-24 |
| AU2014334222A1 (en) | 2016-05-05 |
| NZ718802A (en) | 2017-09-29 |
| EP3056206A1 (en) | 2016-08-17 |
| TW201513894A (zh) | 2015-04-16 |
| RU2016118063A (ru) | 2017-11-16 |
| BR112016007627A2 (pt) | 2017-08-01 |
| JP2016532659A (ja) | 2016-10-20 |
| TWI630921B (zh) | 2018-08-01 |
| US20160235757A1 (en) | 2016-08-18 |
| HK1213813A1 (zh) | 2016-07-15 |
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