TW201815383A - 用於藥學用途之多層珠粒 - Google Patents
用於藥學用途之多層珠粒 Download PDFInfo
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- TW201815383A TW201815383A TW106134584A TW106134584A TW201815383A TW 201815383 A TW201815383 A TW 201815383A TW 106134584 A TW106134584 A TW 106134584A TW 106134584 A TW106134584 A TW 106134584A TW 201815383 A TW201815383 A TW 201815383A
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- polymer
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- layer
- lubiprostone
- bead
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| US201662405131P | 2016-10-06 | 2016-10-06 | |
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| JP6957610B2 (ja) | 2016-10-06 | 2021-11-02 | スキャンポ・アーゲーSucampo AG | 医薬品用途のための多層ビーズ |
| CN110022862B (zh) * | 2016-12-09 | 2022-05-24 | 拜耳动物保健有限责任公司 | 药物制剂及其制造方法 |
| WO2019221215A1 (ja) * | 2018-05-18 | 2019-11-21 | ニプロ株式会社 | ルビプロストン含有粒子状医薬組成物 |
| CN109701461B (zh) * | 2018-10-25 | 2021-06-08 | 西南交通大学 | 一种基于PEG/Dex双水相的碳酸钙/海藻酸钙复合微囊的制备及其应用 |
| JP2020075874A (ja) * | 2018-11-06 | 2020-05-21 | ニプロ株式会社 | ルビプロストン含有フィルム状医薬組成物 |
| US20220331257A1 (en) * | 2019-03-01 | 2022-10-20 | Avadel Legacy Pharmaceuticals, Llc | Liquid pharmaceutical compositions with stable drug release profiles |
| JP7518661B2 (ja) * | 2020-05-14 | 2024-07-18 | 沢井製薬株式会社 | ルビプロストン含有整粒物、ルビプロストン含有錠剤およびそれらの製造方法 |
Family Cites Families (24)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| JPS5942313A (ja) * | 1982-09-01 | 1984-03-08 | Teijin Ltd | ポリビニルポリピロリドンを用いた製剤 |
| JPS6377821A (ja) * | 1986-09-19 | 1988-04-08 | Teikoku Seiyaku Kk | 安定なプロスタグランジンe組成物 |
| US5317032A (en) | 1987-10-02 | 1994-05-31 | Kabushiki Kaisha Ueno Seiyaku Oyo Kenkyujo | Prostaglandin cathartic |
| EP0503887B1 (en) | 1991-03-14 | 1996-08-28 | R-Tech Ueno Ltd. | Promotion of wound-healing with 15-keto-prostaglandin compounds |
| RU2695274C3 (ru) | 1999-10-15 | 2020-11-09 | Сукампо Аг | Новые композиции и способы их стабилизации |
| DE19962544A1 (de) | 1999-12-23 | 2001-07-19 | Degussa | Verfahren zum Beschichten eines keramischen Wabenkörpers |
| NZ521784A (en) * | 2000-04-06 | 2005-04-29 | Sucampo Ag | Bile secretion promoting composition |
| US6414016B1 (en) | 2000-09-05 | 2002-07-02 | Sucampo, A.G. | Anti-constipation composition |
| TWI302100B (en) | 2001-05-02 | 2008-10-21 | Sucampo Ag | Composition for treating drug-induced constipation |
| WO2002094274A1 (en) | 2001-05-18 | 2002-11-28 | Sucampo Ag | Cathartic composition |
| EP1420794B1 (en) | 2001-08-31 | 2017-12-27 | Sucampo AG | Prostaglandin analogs as chloride channel openers |
| JP2005139085A (ja) * | 2003-11-04 | 2005-06-02 | Ono Pharmaceut Co Ltd | 顆粒 |
| US20080220080A1 (en) * | 2005-03-29 | 2008-09-11 | Röhm Gmbh | Multiparticulate Pharmaceutical form Comprising Pellets with a Substance Having a Modular Effect in Relation to Active Ingredient Release |
| CA2637274C (en) * | 2006-01-24 | 2013-06-04 | R-Tech Ueno, Ltd. | Soft-gelatin capsule formulation |
| JP2010502591A (ja) * | 2006-09-04 | 2010-01-28 | パナセア バイオテック リミテッド | プログラム可能な浮揚性送達技術 |
| CN101318948B (zh) * | 2008-04-01 | 2011-04-27 | 上海天伟生物制药有限公司 | 鲁比前列酮晶体、其制备方法及用途 |
| US20120208773A1 (en) * | 2008-08-12 | 2012-08-16 | Valeant International (Barbados) Srl | Pharmaceutical compositions with tetrabenazine |
| WO2011019956A2 (en) * | 2009-08-12 | 2011-02-17 | Biovail Laboratories International (Barbados) S.R.L. | Pharmaceutical compositions |
| JP4706785B2 (ja) * | 2008-09-30 | 2011-06-22 | アステラス製薬株式会社 | 経口投与用粒子状医薬組成物 |
| CA2757979A1 (en) * | 2009-04-09 | 2010-10-14 | Alkermes Pharma Ireland Limited | Controlled-release clozapine compositions |
| UA119335C2 (uk) * | 2013-12-11 | 2019-06-10 | Айронвуд Фармасьютикалз, Інк. | Композиції лінаклотиду з затриманим вивільненням |
| US20160120840A1 (en) | 2014-10-30 | 2016-05-05 | Sucampo Ag | Method and composition for treating nonerosive reflux disease |
| EP3463307A4 (en) * | 2016-06-03 | 2020-01-15 | Velicept Therapeutics, Inc. | COMPOSITIONS AND METHODS FOR USE OF SOLABEGRON WITH MODIFIED RELEASE FOR SYMPTOMS OF THE LOWER URINARY PATHWAYS |
| JP6957610B2 (ja) | 2016-10-06 | 2021-11-02 | スキャンポ・アーゲーSucampo AG | 医薬品用途のための多層ビーズ |
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- 2017-10-05 WO PCT/IB2017/001383 patent/WO2018065826A1/en not_active Ceased
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- 2017-10-06 AR ARP170102802A patent/AR109898A1/es unknown
- 2017-10-06 TW TW106134584A patent/TW201815383A/zh unknown
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| US11534404B2 (en) | 2022-12-27 |
| JP2019529467A (ja) | 2019-10-17 |
| AR109898A1 (es) | 2019-02-06 |
| US20200390708A1 (en) | 2020-12-17 |
| JP6957610B2 (ja) | 2021-11-02 |
| WO2018065826A1 (en) | 2018-04-12 |
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