JP2021511317A5 - - Google Patents
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- Publication number
- JP2021511317A5 JP2021511317A5 JP2020539288A JP2020539288A JP2021511317A5 JP 2021511317 A5 JP2021511317 A5 JP 2021511317A5 JP 2020539288 A JP2020539288 A JP 2020539288A JP 2020539288 A JP2020539288 A JP 2020539288A JP 2021511317 A5 JP2021511317 A5 JP 2021511317A5
- Authority
- JP
- Japan
- Prior art keywords
- cyclodextrin
- pharmaceutical composition
- pharmaceutically acceptable
- ophthalmic pharmaceutical
- acceptable salt
- 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
- 229920000858 Cyclodextrin Polymers 0.000 claims 29
- 239000001116 FEMA 4028 Substances 0.000 claims 29
- 229960004853 betadex Drugs 0.000 claims 29
- 239000008194 pharmaceutical composition Substances 0.000 claims 28
- 150000003839 salts Chemical class 0.000 claims 23
- 235000011175 beta-cyclodextrine Nutrition 0.000 claims 18
- WHGYBXFWUBPSRW-FOUAGVGXSA-N beta-cyclodextrin Chemical class OC[C@H]([C@H]([C@@H]([C@H]1O)O)O[C@H]2O[C@@H]([C@@H](O[C@H]3O[C@H](CO)[C@H]([C@@H]([C@H]3O)O)O[C@H]3O[C@H](CO)[C@H]([C@@H]([C@H]3O)O)O[C@H]3O[C@H](CO)[C@H]([C@@H]([C@H]3O)O)O[C@H]3O[C@H](CO)[C@H]([C@@H]([C@H]3O)O)O3)[C@H](O)[C@H]2O)CO)O[C@@H]1O[C@H]1[C@H](O)[C@@H](O)[C@@H]3O[C@@H]1CO WHGYBXFWUBPSRW-FOUAGVGXSA-N 0.000 claims 14
- ACCMWZWAEFYUGZ-UHFFFAOYSA-N bilastine Chemical compound N=1C2=CC=CC=C2N(CCOCC)C=1C(CC1)CCN1CCC1=CC=C(C(C)(C)C(O)=O)C=C1 ACCMWZWAEFYUGZ-UHFFFAOYSA-N 0.000 claims 12
- 229960004314 bilastine Drugs 0.000 claims 12
- 239000012453 solvate Substances 0.000 claims 12
- KIUKXJAPPMFGSW-DNGZLQJQSA-N (2S,3S,4S,5R,6R)-6-[(2S,3R,4R,5S,6R)-3-Acetamido-2-[(2S,3S,4R,5R,6R)-6-[(2R,3R,4R,5S,6R)-3-acetamido-2,5-dihydroxy-6-(hydroxymethyl)oxan-4-yl]oxy-2-carboxy-4,5-dihydroxyoxan-3-yl]oxy-5-hydroxy-6-(hydroxymethyl)oxan-4-yl]oxy-3,4,5-trihydroxyoxane-2-carboxylic acid Chemical compound CC(=O)N[C@H]1[C@H](O)O[C@H](CO)[C@@H](O)[C@@H]1O[C@H]1[C@H](O)[C@@H](O)[C@H](O[C@H]2[C@@H]([C@@H](O[C@H]3[C@@H]([C@@H](O)[C@H](O)[C@H](O3)C(O)=O)O)[C@H](O)[C@@H](CO)O2)NC(C)=O)[C@@H](C(O)=O)O1 KIUKXJAPPMFGSW-DNGZLQJQSA-N 0.000 claims 10
- 229920002674 hyaluronan Polymers 0.000 claims 10
- 229960003160 hyaluronic acid Drugs 0.000 claims 10
- 239000000203 mixture Substances 0.000 claims 9
- -1 C 1- C 6 hydroxyalkyl β-cyclodextrin Chemical compound 0.000 claims 8
- PEDCQBHIVMGVHV-UHFFFAOYSA-N Glycerine Chemical compound OCC(O)CO PEDCQBHIVMGVHV-UHFFFAOYSA-N 0.000 claims 8
- 208000037265 diseases, disorders, signs and symptoms Diseases 0.000 claims 7
- RTZKZFJDLAIYFH-UHFFFAOYSA-N Diethyl ether Chemical compound CCOCC RTZKZFJDLAIYFH-UHFFFAOYSA-N 0.000 claims 6
- HEBKCHPVOIAQTA-UHFFFAOYSA-N meso ribitol Natural products OCC(O)C(O)C(O)CO HEBKCHPVOIAQTA-UHFFFAOYSA-N 0.000 claims 6
- 208000035475 disorder Diseases 0.000 claims 4
- 235000011187 glycerol Nutrition 0.000 claims 4
- 102000000543 Histamine Receptors Human genes 0.000 claims 3
- 108010002059 Histamine Receptors Proteins 0.000 claims 3
- 208000002205 allergic conjunctivitis Diseases 0.000 claims 3
- 230000008485 antagonism Effects 0.000 claims 3
- 201000010099 disease Diseases 0.000 claims 3
- 239000000832 lactitol Substances 0.000 claims 3
- 235000010448 lactitol Nutrition 0.000 claims 3
- VQHSOMBJVWLPSR-JVCRWLNRSA-N lactitol Chemical compound OC[C@H](O)[C@@H](O)[C@@H]([C@H](O)CO)O[C@@H]1O[C@H](CO)[C@H](O)[C@H](O)[C@H]1O VQHSOMBJVWLPSR-JVCRWLNRSA-N 0.000 claims 3
- 229960003451 lactitol Drugs 0.000 claims 3
- 125000004964 sulfoalkyl group Chemical group 0.000 claims 3
- ODLHGICHYURWBS-LKONHMLTSA-N trappsol cyclo Chemical compound CC(O)COC[C@H]([C@H]([C@@H]([C@H]1O)O)O[C@H]2O[C@@H]([C@@H](O[C@H]3O[C@H](COCC(C)O)[C@H]([C@@H]([C@H]3O)O)O[C@H]3O[C@H](COCC(C)O)[C@H]([C@@H]([C@H]3O)O)O[C@H]3O[C@H](COCC(C)O)[C@H]([C@@H]([C@H]3O)O)O[C@H]3O[C@H](COCC(C)O)[C@H]([C@@H]([C@H]3O)O)O3)[C@H](O)[C@H]2O)COCC(O)C)O[C@@H]1O[C@H]1[C@H](O)[C@@H](O)[C@@H]3O[C@@H]1COCC(C)O ODLHGICHYURWBS-LKONHMLTSA-N 0.000 claims 3
- PCWPQSDFNIFUPO-VDQKLNDWSA-N (1S,3R,5R,6S,8R,10R,11S,13R,15R,16S,18R,20R,21S,23R,25R,26S,28R,30R,31S,33R,35R,36R,37S,38R,39S,40R,41S,42R,43S,44R,45S,46R,47S,48R,49S)-37,39,41,43,45,47,49-heptakis(2-hydroxyethoxy)-5,10,15,20,25,30,35-heptakis(hydroxymethyl)-2,4,7,9,12,14,17,19,22,24,27,29,32,34-tetradecaoxaoctacyclo[31.2.2.23,6.28,11.213,16.218,21.223,26.228,31]nonatetracontane-36,38,40,42,44,46,48-heptol Chemical compound OCCO[C@H]1[C@H](O)[C@@H]2O[C@H]3O[C@H](CO)[C@@H](O[C@H]4O[C@H](CO)[C@@H](O[C@H]5O[C@H](CO)[C@@H](O[C@H]6O[C@H](CO)[C@@H](O[C@H]7O[C@H](CO)[C@@H](O[C@H]8O[C@H](CO)[C@@H](O[C@H]1O[C@@H]2CO)[C@@H](O)[C@@H]8OCCO)[C@@H](O)[C@@H]7OCCO)[C@@H](O)[C@@H]6OCCO)[C@@H](O)[C@@H]5OCCO)[C@@H](O)[C@@H]4OCCO)[C@@H](O)[C@@H]3OCCO PCWPQSDFNIFUPO-VDQKLNDWSA-N 0.000 claims 2
- 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 2
- FBPFZTCFMRRESA-KVTDHHQDSA-N D-Mannitol Chemical compound OC[C@@H](O)[C@@H](O)[C@H](O)[C@H](O)CO FBPFZTCFMRRESA-KVTDHHQDSA-N 0.000 claims 2
- HEBKCHPVOIAQTA-QWWZWVQMSA-N D-arabinitol Chemical compound OC[C@@H](O)C(O)[C@H](O)CO HEBKCHPVOIAQTA-QWWZWVQMSA-N 0.000 claims 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 2
- LYCAIKOWRPUZTN-UHFFFAOYSA-N Ethylene glycol Chemical compound OCCO LYCAIKOWRPUZTN-UHFFFAOYSA-N 0.000 claims 2
- 229930195725 Mannitol Natural products 0.000 claims 2
- JVWLUVNSQYXYBE-UHFFFAOYSA-N Ribitol Natural products OCC(C)C(O)C(O)CO JVWLUVNSQYXYBE-UHFFFAOYSA-N 0.000 claims 2
- TVXBFESIOXBWNM-UHFFFAOYSA-N Xylitol Natural products OCCC(O)C(O)C(O)CCO TVXBFESIOXBWNM-UHFFFAOYSA-N 0.000 claims 2
- 230000000172 allergic effect Effects 0.000 claims 2
- 208000010668 atopic eczema Diseases 0.000 claims 2
- 239000001913 cellulose Substances 0.000 claims 2
- 229920002678 cellulose Polymers 0.000 claims 2
- 150000002170 ethers Chemical class 0.000 claims 2
- 229960003511 macrogol Drugs 0.000 claims 2
- 239000000594 mannitol Substances 0.000 claims 2
- 235000010355 mannitol Nutrition 0.000 claims 2
- HEBKCHPVOIAQTA-ZXFHETKHSA-N ribitol Chemical compound OC[C@H](O)[C@H](O)[C@H](O)CO HEBKCHPVOIAQTA-ZXFHETKHSA-N 0.000 claims 2
- 239000000600 sorbitol Substances 0.000 claims 2
- 235000010356 sorbitol Nutrition 0.000 claims 2
- 239000012929 tonicity agent Substances 0.000 claims 2
- XLYOFNOQVPJJNP-UHFFFAOYSA-N water Substances O XLYOFNOQVPJJNP-UHFFFAOYSA-N 0.000 claims 2
- 239000000811 xylitol Substances 0.000 claims 2
- 235000010447 xylitol Nutrition 0.000 claims 2
- HEBKCHPVOIAQTA-SCDXWVJYSA-N xylitol Chemical compound OC[C@H](O)[C@@H](O)[C@H](O)CO HEBKCHPVOIAQTA-SCDXWVJYSA-N 0.000 claims 2
- 229960002675 xylitol Drugs 0.000 claims 2
- 206010010726 Conjunctival oedema Diseases 0.000 claims 1
- 206010010741 Conjunctivitis Diseases 0.000 claims 1
- 206010010744 Conjunctivitis allergic Diseases 0.000 claims 1
- 208000003556 Dry Eye Syndromes Diseases 0.000 claims 1
- 206010013774 Dry eye Diseases 0.000 claims 1
- 206010015150 Erythema Diseases 0.000 claims 1
- 239000004386 Erythritol Substances 0.000 claims 1
- UNXHWFMMPAWVPI-UHFFFAOYSA-N Erythritol Natural products OCC(O)C(O)CO UNXHWFMMPAWVPI-UHFFFAOYSA-N 0.000 claims 1
- 206010015946 Eye irritation Diseases 0.000 claims 1
- 206010018258 Giant papillary conjunctivitis Diseases 0.000 claims 1
- 208000009319 Keratoconjunctivitis Sicca Diseases 0.000 claims 1
- 206010023644 Lacrimation increased Diseases 0.000 claims 1
- 239000002202 Polyethylene glycol Substances 0.000 claims 1
- 239000004372 Polyvinyl alcohol Substances 0.000 claims 1
- 208000003251 Pruritus Diseases 0.000 claims 1
- 125000000217 alkyl group Chemical group 0.000 claims 1
- 208000026935 allergic disease Diseases 0.000 claims 1
- 208000024998 atopic conjunctivitis Diseases 0.000 claims 1
- 206010069664 atopic keratoconjunctivitis Diseases 0.000 claims 1
- 230000004064 dysfunction Effects 0.000 claims 1
- 235000019414 erythritol Nutrition 0.000 claims 1
- UNXHWFMMPAWVPI-ZXZARUISSA-N erythritol Chemical compound OC[C@H](O)[C@H](O)CO UNXHWFMMPAWVPI-ZXZARUISSA-N 0.000 claims 1
- 229940009714 erythritol Drugs 0.000 claims 1
- 231100000013 eye irritation Toxicity 0.000 claims 1
- FBPFZTCFMRRESA-GUCUJZIJSA-N galactitol Chemical compound OC[C@H](O)[C@@H](O)[C@@H](O)[C@H](O)CO FBPFZTCFMRRESA-GUCUJZIJSA-N 0.000 claims 1
- 239000003349 gelling agent Substances 0.000 claims 1
- 230000007803 itching Effects 0.000 claims 1
- 206010023332 keratitis Diseases 0.000 claims 1
- 230000004317 lacrimation Effects 0.000 claims 1
- 239000000845 maltitol Substances 0.000 claims 1
- VQHSOMBJVWLPSR-WUJBLJFYSA-N maltitol Chemical compound OC[C@H](O)[C@@H](O)[C@@H]([C@H](O)CO)O[C@H]1O[C@H](CO)[C@@H](O)[C@H](O)[C@H]1O VQHSOMBJVWLPSR-WUJBLJFYSA-N 0.000 claims 1
- 235000010449 maltitol Nutrition 0.000 claims 1
- 229940035436 maltitol Drugs 0.000 claims 1
- 229920000609 methyl cellulose Polymers 0.000 claims 1
- 239000001923 methylcellulose Substances 0.000 claims 1
- 230000003204 osmotic effect Effects 0.000 claims 1
- 229920001223 polyethylene glycol Polymers 0.000 claims 1
- 229920002451 polyvinyl alcohol Polymers 0.000 claims 1
- 230000000069 prophylactic effect Effects 0.000 claims 1
- 206010039083 rhinitis Diseases 0.000 claims 1
- 208000024891 symptom Diseases 0.000 claims 1
- 208000011580 syndromic disease Diseases 0.000 claims 1
- 230000001225 therapeutic effect Effects 0.000 claims 1
- 208000018464 vernal keratoconjunctivitis Diseases 0.000 claims 1
- 229920003169 water-soluble polymer Polymers 0.000 claims 1
Applications Claiming Priority (3)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| EP18382021 | 2018-01-18 | ||
| EP18382021.6 | 2018-01-18 | ||
| PCT/EP2019/050433 WO2019141563A1 (en) | 2018-01-18 | 2019-01-09 | Ophthalmic compositions comprising bilastine, a beta-cyclodextrin and at least one gelling agent |
Publications (3)
| Publication Number | Publication Date |
|---|---|
| JP2021511317A JP2021511317A (ja) | 2021-05-06 |
| JP2021511317A5 true JP2021511317A5 (cg-RX-API-DMAC7.html) | 2021-09-09 |
| JP7309729B2 JP7309729B2 (ja) | 2023-07-18 |
Family
ID=61017875
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2020539288A Active JP7309729B2 (ja) | 2018-01-18 | 2019-01-09 | ビラスチン、β－シクロデキストリンおよび少なくとも１種のゲル化剤を含有する眼科用組成物 |
Country Status (28)
Families Citing this family (6)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| JP2025508704A (ja) * | 2022-02-17 | 2025-04-10 | ファエス・ファルマ・ソシエダッド・アノニマ | １日１回非経口投与のためのビラスチン組成物 |
| CN116211795B (zh) * | 2022-12-26 | 2025-09-26 | 深圳市贝美药业有限公司 | 一种比拉斯汀口服液体制剂及其制备方法 |
| CN115970066B (zh) * | 2022-12-29 | 2024-09-27 | 成都爱睿康乐医疗器械有限公司 | 基于主客体相互作用的载药纳米凝胶生物润滑剂及其制备方法和应用 |
| WO2024224326A1 (en) * | 2023-04-27 | 2024-10-31 | Leiutis Pharmaceuticals Llp | Liquid parenteral formulations of bilastine |
| WO2024224308A1 (en) * | 2023-04-27 | 2024-10-31 | Leiutis Pharmaceuticals Llp | Liquid parenteral formulations of bilastine free of cyclodextrins |
| WO2024256956A1 (en) * | 2023-06-13 | 2024-12-19 | Leiutis Pharmaceuticals Llp | Stable formulations of bilastine for nasal and ophthalmic use |
Family Cites Families (19)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| IT1229075B (it) * | 1985-04-05 | 1991-07-17 | Fidia Farmaceutici | Medicamenti per uso topico, ottenuti tramite l'impiego dell'acido ialuronico |
| ES2048109B1 (es) | 1992-07-20 | 1994-12-16 | Espanola Prod Quimicos | Procedimiento de preparacion de nuevos derivados piperidicos del bencimidazol. |
| JP3527256B2 (ja) | 1992-12-09 | 2004-05-17 | ロート製薬株式会社 | 抗アレルギー点眼剤 |
| TW401300B (en) * | 1992-12-25 | 2000-08-11 | Senju Pharma Co | Antiallergic composition for ophthalmic or nasal use |
| ES2124167B1 (es) | 1996-06-04 | 1999-09-16 | Espanola Prod Quimicos | Nuevos derivados del bencimidazol con actividad antihistaminica. |
| DE10161149B4 (de) * | 2001-12-12 | 2007-03-08 | Ursapharm Arzneimittel Gmbh & Co. Kg | Verwendung von Heparin-haltigem Ophthalmikum |
| CA2484460C (en) | 2002-04-19 | 2009-09-29 | Faes Farma, S.A. | Polymorph of 4-[2-[4-[1-(2-ethoxyethyl)-1h-benzimidazole-2-yl]-1-piperidinyl]ethyl]-.alpha..alpha. dimethyl-benzeneacetic acid |
| US20050239745A1 (en) * | 2004-03-03 | 2005-10-27 | Ophthalmic Research Associates, Inc. | Novel topical ophthalmic formulations |
| US7247623B2 (en) | 2005-08-19 | 2007-07-24 | Inspire Pharmaceuticals, Inc. | Method of treating dry eye disease with non-drying antihistamines |
| WO2007047253A2 (en) | 2005-10-11 | 2007-04-26 | Eastman Chemical Company | Pharmaceutical formulations of cyclodextrins and antifungal azole compounds |
| UA94938C2 (ru) * | 2006-03-31 | 2011-06-25 | ВИСТЕКОН ФАРМАСЬЮТИКАЛС, ЭлЭлСи | Офтальмическая композиция для лечения клинических симптомов глазной аллергии, которая содержит алкафтадин или его производное (варианты) |
| SG170044A1 (en) * | 2006-03-31 | 2011-04-29 | Vistakon Pharmaceuticals Llc | Ocular allergy treatments |
| JP2010531898A (ja) | 2007-06-28 | 2010-09-30 | サイデックス・ファーマシューティカルズ・インコーポレイテッド | 鼻および眼へのコルチコステロイド水溶液送達 |
| JP2012520880A (ja) * | 2009-03-17 | 2012-09-10 | アーシエックス セラピューティックス， インコーポレイテッド | ケトチフェンの眼科用製剤および使用方法 |
| TWI544922B (zh) | 2011-05-19 | 2016-08-11 | 愛爾康研究有限公司 | 高濃度歐羅派特錠（ｏｌｏｐａｔａｄｉｎｅ）眼用組成物 |
| CN103110575B (zh) * | 2013-03-07 | 2014-11-05 | 宁夏康亚药业有限公司 | 一种美洛昔康滴眼液及其制备方法和应用 |
| WO2014150899A1 (en) * | 2013-03-15 | 2014-09-25 | Chapin Matthew J | Topical ophthalmic formulations for treating migraine |
| CN103784462A (zh) * | 2014-02-25 | 2014-05-14 | 宋俊智 | 包含比拉斯汀及甾族化合物的药物制剂 |
| EP3040334A1 (en) | 2014-12-29 | 2016-07-06 | Faes Farma, S.A. | New benzimidazole derivatives as antihistamine agents |
-
2019
- 2019-01-09 EA EA202091725A patent/EA202091725A1/ru unknown
- 2019-01-09 DK DK19701154.7T patent/DK3740191T3/da active
- 2019-01-09 ES ES19701154T patent/ES2878107T3/es active Active
- 2019-01-09 CA CA3088740A patent/CA3088740A1/en not_active Abandoned
- 2019-01-09 MA MA51612A patent/MA51612B1/fr unknown
- 2019-01-09 SI SI201930076T patent/SI3740191T1/sl unknown
- 2019-01-09 EP EP19701154.7A patent/EP3740191B1/en active Active
- 2019-01-09 HR HRP20211037TT patent/HRP20211037T1/hr unknown
- 2019-01-09 HU HUE19701154A patent/HUE054594T2/hu unknown
- 2019-01-09 JP JP2020539288A patent/JP7309729B2/ja active Active
- 2019-01-09 KR KR1020207023573A patent/KR102695627B1/ko active Active
- 2019-01-09 LT LTEP19701154.7T patent/LT3740191T/lt unknown
- 2019-01-09 MX MX2020007692A patent/MX2020007692A/es unknown
- 2019-01-09 PT PT197011547T patent/PT3740191T/pt unknown
- 2019-01-09 CN CN201980009293.0A patent/CN111727035B/zh active Active
- 2019-01-09 US US16/963,219 patent/US20210128544A1/en not_active Abandoned
- 2019-01-09 EP EP21169956.6A patent/EP3915539A1/en not_active Withdrawn
- 2019-01-09 AU AU2019209214A patent/AU2019209214B2/en active Active
- 2019-01-09 PL PL19701154T patent/PL3740191T3/pl unknown
- 2019-01-09 WO PCT/EP2019/050433 patent/WO2019141563A1/en not_active Ceased
- 2019-01-17 PY PY201901903392A patent/PY1903392A/es unknown
- 2019-01-17 AR ARP190100094A patent/AR114216A1/es not_active Application Discontinuation
- 2019-01-17 TW TW108101861A patent/TWI833727B/zh active
- 2019-01-18 UY UY38055A patent/UY38055A/es not_active Application Discontinuation
-
2020
- 2020-07-15 SA SA520412443A patent/SA520412443B1/ar unknown
- 2020-07-17 CL CL2020001895A patent/CL2020001895A1/es unknown
- 2020-08-13 CO CONC2020/0009992A patent/CO2020009992A2/es unknown
- 2020-08-17 ZA ZA2020/05077A patent/ZA202005077B/en unknown
-
2021
- 2021-06-25 CY CY20211100569T patent/CY1124270T1/el unknown
-
2025
- 2025-10-02 US US19/347,880 patent/US20260027099A1/en active Pending
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