KR20150131070A - 개질된 구아 검을 갖는 제약 연질 젤라틴 캡슐 투여 형태 - Google Patents
개질된 구아 검을 갖는 제약 연질 젤라틴 캡슐 투여 형태 Download PDFInfo
- Publication number
- KR20150131070A KR20150131070A KR1020157026413A KR20157026413A KR20150131070A KR 20150131070 A KR20150131070 A KR 20150131070A KR 1020157026413 A KR1020157026413 A KR 1020157026413A KR 20157026413 A KR20157026413 A KR 20157026413A KR 20150131070 A KR20150131070 A KR 20150131070A
- Authority
- KR
- South Korea
- Prior art keywords
- dosage form
- soft gelatin
- gelatin capsule
- capsule dosage
- guar gum
- 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.)
- Ceased
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- 239000000665 guar gum Substances 0.000 title claims abstract description 35
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Applications Claiming Priority (3)
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| US201361794906P | 2013-03-15 | 2013-03-15 | |
| US61/794,906 | 2013-03-15 | ||
| PCT/US2014/027145 WO2014152269A1 (en) | 2013-03-15 | 2014-03-14 | Pharmaceutical soft gelatin capsule dosage form with modified guar gum |
Publications (1)
| Publication Number | Publication Date |
|---|---|
| KR20150131070A true KR20150131070A (ko) | 2015-11-24 |
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| KR1020157026413A Ceased KR20150131070A (ko) | 2013-03-15 | 2014-03-14 | 개질된 구아 검을 갖는 제약 연질 젤라틴 캡슐 투여 형태 |
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| EP (2) | EP3187170A1 (enExample) |
| JP (3) | JP6335270B2 (enExample) |
| KR (1) | KR20150131070A (enExample) |
| CN (2) | CN111374959A (enExample) |
| AU (2) | AU2014239994B2 (enExample) |
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| CA (1) | CA2906633C (enExample) |
| ES (1) | ES2619121T3 (enExample) |
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| RU (1) | RU2676480C2 (enExample) |
| WO (1) | WO2014152269A1 (enExample) |
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| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| MX364440B (es) * | 2013-03-15 | 2019-04-26 | Warner Chilcott Co Llc | Forma de dosis farmacéutica de cápsula de gelatina blanda con goma guar modificada. |
| CA2980165C (en) * | 2015-03-26 | 2021-06-15 | Patheon Softgels Inc. | Liquisoft capsules |
| JP2017214299A (ja) * | 2016-05-30 | 2017-12-07 | ライオン株式会社 | 半固形製剤及びその製造方法 |
| CN116916895A (zh) * | 2020-11-13 | 2023-10-20 | 辉瑞公司 | 他拉唑帕尼软明胶胶囊剂型 |
| KR20230107647A (ko) * | 2020-11-13 | 2023-07-17 | 화이자 인코포레이티드 | 탈라조파립 연질 젤라틴 캡슐 투여 형태 |
| CN116531444B (zh) * | 2023-07-06 | 2023-10-10 | 健码制药（广东）有限公司 | 镇咳清肺软胶囊及其制备工艺 |
Family Cites Families (38)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US4708834A (en) | 1986-05-01 | 1987-11-24 | Pharmacaps, Inc. | Preparation of gelatin-encapsulated controlled release composition |
| US5102666A (en) | 1990-09-11 | 1992-04-07 | Oramed, Inc. | Calcium polycarbophil controlled release composition and method |
| FR2739558B1 (fr) * | 1995-10-05 | 1997-11-28 | Innothera Lab Sa | Forme galenique unitaire pour hormonotherapie locale de la secheresse vaginale |
| IT1275816B1 (it) * | 1995-10-27 | 1997-10-17 | Montefarmaco Spa | Composizioni farmaceutiche solide per uso vaginale |
| WO1997033568A1 (en) | 1996-03-12 | 1997-09-18 | Novartis Ag | Filled gelatin capsules having a reduced degree of cross-linking |
| US6024980A (en) * | 1996-06-28 | 2000-02-15 | Mcneil-Ppc, Inc. | Multiphase soft gelatin dosage form |
| US5919481A (en) * | 1996-06-28 | 1999-07-06 | Ncneil-Ppc, Inc. | Fill material for soft gelatin pharmaceutical dosage form |
| US5989535A (en) | 1997-08-15 | 1999-11-23 | Soma Technologies | Polymeric bioadhesive emulsions and suspensions and methods of treatment |
| IN188719B (enExample) * | 1997-09-08 | 2002-11-02 | Panacea Biotec Ltd | |
| US6187747B1 (en) * | 1997-09-08 | 2001-02-13 | Panacea Biotech Limited | Pharmaceutical composition comprising cyclosporin |
| US7374779B2 (en) * | 1999-02-26 | 2008-05-20 | Lipocine, Inc. | Pharmaceutical formulations and systems for improved absorption and multistage release of active agents |
| US6251426B1 (en) * | 1999-09-02 | 2001-06-26 | Banner Pharmacaps, Inc. | Ibuprofen-containing softgels |
| US20040131670A1 (en) * | 2001-04-17 | 2004-07-08 | Ping Gao | Pellicle-resistant gelatin capsule |
| FR2843304B1 (fr) * | 2002-08-07 | 2005-12-16 | Ricarimpex | Extraits de sangsues pour stents |
| EP1599485A2 (en) | 2003-02-18 | 2005-11-30 | Ranbaxy Laboratories, Ltd. | Podophyllotoxin derivatives as antitumor agents |
| KR100570450B1 (ko) * | 2003-09-25 | 2006-04-12 | 한국유나이티드제약 주식회사 | 가용성 로바스타틴의 연질캡슐제 조성물 및 그의 제조방법 |
| US20050142185A1 (en) * | 2003-12-29 | 2005-06-30 | Beleno Alfredo B. | Softgel formulations of bisphosphonates bone resorption inhibitors |
| WO2005070949A1 (en) | 2004-01-15 | 2005-08-04 | Warner Chilcott Company, Inc. | Di-steroidal prodrugs of estradiol |
| EP1709061A1 (en) | 2004-01-15 | 2006-10-11 | Warner Chilcott Company Inc. | Di-steroidal prodrugs of ethinyl estradiol |
| US20060110415A1 (en) * | 2004-11-22 | 2006-05-25 | Bioderm Research | Topical Delivery System for Cosmetic and Pharmaceutical Agents |
| US7485323B2 (en) | 2005-05-31 | 2009-02-03 | Gelita Ag | Process for making a low molecular weight gelatine hydrolysate and gelatine hydrolysate compositions |
| US10016442B2 (en) | 2005-06-16 | 2018-07-10 | Allergan Pharmaceuticals International Limited | Estrogen compositions for vaginal administration |
| CA2610481A1 (en) | 2005-07-12 | 2007-01-18 | Warner Chilcott Company, Inc. | 3-ester prodrugs of estradiol |
| CN101218245B (zh) | 2005-07-12 | 2011-08-17 | 沃纳奇尔科特有限责任公司 | 炔雌醇的3-酯前药 |
| US7468970B2 (en) | 2005-10-24 | 2008-12-23 | Honeywell International Inc. | Routing of mobile agents in a network |
| CN101360485B (zh) * | 2005-10-26 | 2013-04-17 | 班纳制药公司 | 作为胶囊填充物的基于亲水性载体的双重控释基质系统 |
| US20070104778A1 (en) | 2005-11-07 | 2007-05-10 | Hongxia Zeng | Controlled-release emulsion compositions |
| WO2007066837A1 (en) | 2005-12-06 | 2007-06-14 | Lg Household & Health Care Ltd. | Delivery system for tooth whitening component using in situ gelling |
| EP1986591A1 (en) | 2006-02-10 | 2008-11-05 | LG Household & Health Care Ltd. | In-situ melting and gelling tablet composition for oral care |
| US20080090569A1 (en) | 2006-10-13 | 2008-04-17 | At&T Knowledge Ventures, L.P. | Method and apparatus for performing signal processing in an ip multimedia subsystem network |
| US20080122993A1 (en) | 2006-11-29 | 2008-05-29 | Sanyo Electric Co., Ltd. | Television image receiver |
| EP2114380A1 (en) | 2007-01-25 | 2009-11-11 | Panacea Biotec Ltd. | Modified release pharmaceutical composition and a process of making the same |
| WO2008122993A1 (en) | 2007-04-09 | 2008-10-16 | Panacea Biotec Limited | Controlled release formulation of coated microparticles |
| EP2264574A2 (en) | 2008-03-26 | 2010-12-22 | Crucialtec Co., Ltd. | Optical pointing apparatus and portable electronic apparatus with the same |
| CN101474167A (zh) * | 2009-01-23 | 2009-07-08 | 西安德天药业股份有限公司 | 雌二醇阴道用胶囊的制备方法 |
| US20110003000A1 (en) | 2009-07-06 | 2011-01-06 | Femmepharma Holding Company, Inc. | Transvaginal Delivery of Drugs |
| WO2011018800A2 (en) | 2009-08-13 | 2011-02-17 | Fdc Limited | A novel in-situ gel forming solution for ocular drug delivery |
| MX364440B (es) * | 2013-03-15 | 2019-04-26 | Warner Chilcott Co Llc | Forma de dosis farmacéutica de cápsula de gelatina blanda con goma guar modificada. |
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