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1. 发明申请

WO2021110127A1 METHOD OF TREATING INFLAMMATORY BOWEL DISEASE 审中-公开
公开(公告)号：WO2021110127A1
公开(公告)日：2021-06-10
申请号：PCT/CN2020/133825
申请日：2020-12-04
申请人： CHEER GLOBAL LIMITED
发明人： KWOK, Sui Yi , WAI, Norman Fung Man , TAI, Chi Shing
IPC分类号： A61K31/606 , A61K35/74 , A61K33/24 , A61K31/635 , A61K31/352 , A61P7/00
摘要： A method for treating an inflammatory bowel disease in a subject in need thereof, the method comprising administering a therapeutically effective amount of a hemoglobin to the subject.

2. 发明申请

WO2020245382A1 IRSOGLADINE FOR THE TREATMENT OF EOSINOPHILIC GASTROINTESTINAL DISEASES 审中-公开
公开(公告)号：WO2020245382A1
公开(公告)日：2020-12-10
申请号：PCT/EP2020/065660
申请日：2020-06-05
申请人： EPITHELION SCIENCE BIOTECH, S.L.
发明人： GASSULL PALLÀS, Daniel , GASSULL DURÓ, Miquel Àngel
IPC分类号： A61K31/53 , A61P1/00 , A61P37/08 , A61K31/52 , A61K31/56 , A61K31/573 , A61K31/58 , A61K31/606
摘要： The present invention provides Irsogladine or a pharmaceutically acceptable salt thereof for use in the treatment and/or prevention of eosinophilic gastrointestinal diseases in mammals. The invention is useful in the treatment of eosinophilic gastritis, eosinophilic gastroenteritis, eosinophilic duodenitis, eosinophilic enteritis, eosinophilic colitis, and in particular, eosinophilic esophagitis. The invention is particularly useful for inducing disease remission in acute inflammatory activity and long-term maintenance of remission as well. The Irsogladine of the invention can be administered in the form of a pharmaceutical composition, or more specifically, in the form of an oral and rectal pharmaceutical composition.

3. 发明申请

WO2020121231A1 SOLID ORAL PHARMACEUTICAL COMPOSITIONS FOR CHRONOTROPIC ADMINISTRATION OF DIPEPTIDYL PEPTIDASE IV INHIBITORS 审中-公开
公开(公告)号：WO2020121231A1
公开(公告)日：2020-06-18
申请号：PCT/IB2019/060688
申请日：2019-12-12
申请人： DPL PHARMA S.P.A.
发明人： PEDRANI, Massimo , CONTI, Chiara , GIAMMILLARI, Salvatore Agostino , MACCARI, Giuseppe
IPC分类号： A61K9/20 , A61K9/28 , A61K31/606 , A61K31/4985
摘要： The present invention relates to solid oral pharmaceutical compositions for chronotropic administration of dipeptidyl peptidase IV inhibitors consisting of a monolithic matrix core comprising at least one low/medium viscosity hydroxypropyl methylcellulose, at least one medium/high viscosity hydroxypropyl methylcellulose, one or more methacrylic polymers or copolymers and/or cellulose acetate phthalate or shellac and an outer coating of said core consisting of a layer comprising ethylcellulose, a gastroresistant layer, or a layer comprising ethylcellulose coated in turn with gastroresistant polymers.

4. 发明申请

WO2020115256A1 SOLID COMPOSITION COMPRISING MESALAZINE 审中-公开
公开(公告)号：WO2020115256A1
公开(公告)日：2020-06-11
申请号：PCT/EP2019/083911
申请日：2019-12-05
申请人： TILLOTTS PHARMA AG
发明人： BUSER, Thomas , CETINKAYA-COSKUN, Yalcin , BRAVO GONZÁLEZ, Roberto Carlos
IPC分类号： A61K9/20 , A61K9/28 , A61K31/606
摘要： A method of producing a coatable core for a modified release drug formulation for oral administration. The coatable core has a high drug load of at least 70 wt % based on the total weight of the coatable core. The method comprises the steps of granulating a composition comprising a drug and at least one binder to form granules; blending the granules with a pharmacologically acceptable disintegrant and optionally one or more additional pharmacologically acceptable excipients to form a compression blend, wherein the disintegrant is present in an amount from about 0.5 wt % to about 5 wt %, based on the total weight of the coatable core; and compressing the compression blend using an external lubrication compression method to form a coatable core.

5. 发明申请

WO2017175123A1 PROCESS FOR MESALAZINE SOLID FORMULATIONS 审中-公开
标题翻译：哒嗪固体制剂的工艺
公开(公告)号：WO2017175123A1
公开(公告)日：2017-10-12
申请号：PCT/IB2017/051907
申请日：2017-04-04
申请人： SOFAR S.P.A.
发明人： LABRUZZO, Carla
IPC分类号： A61K9/16 , A61K9/20 , A61K31/606
CPC分类号： A61K9/1694 , A61K9/1623 , A61K9/1635 , A61K9/1652 , A61K9/2013 , A61K9/2018 , A61K9/2027 , A61K9/2054 , A61K9/2059 , A61K9/2095 , A61K9/2846 , A61K31/606
摘要： The present invention relates to a process to prepare solid pharmaceutical forms comprising a quantity of mesalazine comprised between 75 and 95%, i.e. between 1000 and 1600 mg of drug per dosage unit. Furthermore, the present invention relates to a granulate and/or tablets obtained/obtainable with the process according to the invention, preferably coated to allow the controlled release of the drug. Finally, the present invention relates to the use of the granulate and/or the tablets as a medicament, preferably for the treatment of chronic inflammatory pathologies that preferably affect the intestinal tract.
摘要翻译：制备固体药物剂型的方法本发明涉及一种制备固体药物剂型的方法，所述固体药物剂型包含75-95％，即每剂量单位1000-1600mg药物的美沙拉嗪。此外，本发明涉及用本发明方法获得/可获得的颗粒和/或片剂，优选包衣以允许药物的控制释放。最后，本发明涉及颗粒和/或片剂作为药物的用途，优选用于治疗优选影响肠道的慢性炎症病理学。

6. 发明申请

WO2015159302A3 PROCESS FOR PREPARATION OF MESALAMINE COMPOSITION AND MESALAMINE COMPOSITION THEREOF 审中-公开
标题翻译：木质素组合物的制备方法及其组合物
公开(公告)号：WO2015159302A3
公开(公告)日：2016-01-14
申请号：PCT/IN2015000143
申请日：2015-03-26
申请人： ATHENA DRUG DELIVERY SOLUTIONS PVT LTD
发明人： B CHAUDHARI MAHENDRA , S WADHWANI JAGDISH , P NEHETE NITIN
IPC分类号： A61K9/56 , A61K31/205 , A61K31/606
CPC分类号： A61K31/196 , A61K9/5047 , A61K9/5078 , A61K31/606
摘要： A process for preparation of a mesalamine composition, comprising: preparing a first drug layering suspension comprising mesalamine; performing a first drug layering in the fluid bed coater to form first drug layered pellets; preparing a seal coating suspension; performing the seal coating in the fluid bed coater on the first drug layered pellets to form seal coated pellets; preparing a second drug layering suspension comprising mesalamine; performing the second drug layering in the fluid bed coater on seal coated pellets to form second drug layered pellets; preparing an extended release coating suspension; performing the extended release coating in the fluid bed coater on the second drug layered pellets to form extended release pellets; preparing a color coating suspension; performing the color coating in the fluid bed coater on the extended release pellets to form color coated pellets; and lubricating the color coated pellets to form mesalamine pellets.
摘要翻译：美沙拉坦组合物的制备方法，包括：制备包含美沙拉嗪的第一药物分层悬浮液; 在流化床涂布机中进行第一次药物分层以形成第一药物分层丸; 制备密封涂层悬浮液; 在第一药物分层颗粒上的流化床涂布机中进行密封涂层以形成密封涂覆的颗粒; 制备包含美沙拉嗪的第二药物分层悬浮液; 在流化床涂布机中对密封涂覆的颗粒进行第二次药物分层以形成第二药物分层颗粒; 制备延长释放涂层悬浮液; 在第二药物分层颗粒上的流化床涂布机中进行延长释放涂层以形成延长释放颗粒; 制备彩色涂层悬浮液; 在延伸释放颗粒上的流化床涂布机中进行彩色涂层以形成涂有彩色的颗粒; 并润滑着色的颗粒以形成美沙拉嗪颗粒。

7. 发明申请

WO2015104414A1 COMPOSITIONS FOR USE IN THE TREATMENT OF ULCERATIVE COLITIS 审中-公开
标题翻译：用于治疗精神病院的组合物
公开(公告)号：WO2015104414A1
公开(公告)日：2015-07-16
申请号：PCT/EP2015/050423
申请日：2015-01-12
申请人： SIGMOID PHARMA LIMITED
发明人： COULTER, Ivan
IPC分类号： A61K9/50 , A61K38/13 , A61K31/606 , A61K31/56 , A61K45/06
CPC分类号： A61K38/13 , A61K9/0053 , A61K9/4858 , A61K9/4866 , A61K9/5026 , A61K9/5036 , A61K9/5047 , A61K9/5073 , A61K31/573 , A61K31/606 , A61K45/06 , A61K2300/00
摘要： An oral modified release composition comprising cyclosporin, wherein the composition is for use in the treatment of ulcerative colitis in a patient, wherein the composition is for use in the concurrent treatment of the patient with an active agent selected from an aminosalicylate and a steroid, and a fixed or free combination thereof. Also claimed are kits comprising the oral modified release composition and the active agent. Also disclosed are methods for the treatment of ulcerative colitis using the oral modified release composition.
摘要翻译：一种包含环孢菌素的口腔释放组合物，其中所述组合物用于治疗患者的溃疡性结肠炎，其中所述组合物用于同时使用选自氨基水杨酸酯和类固醇的活性剂治疗患者，以及其固定或自由组合。还要求保护的是包含口服缓释组合物和活性剂的试剂盒。还公开了使用口腔改良释放组合物治疗溃疡性结肠炎的方法。

8. 发明申请

WO2013164315A1 A DELAYED RELEASE DRUG FORMULATION 审中-公开
标题翻译：延迟释放药物配方
公开(公告)号：WO2013164315A1
公开(公告)日：2013-11-07
申请号：PCT/EP2013/058921
申请日：2013-04-29
申请人： TILLOTTS PHARMA AG
发明人： BRAVO GONZÁLEZ, Roberto Carlos , BUSER, Thomas , GOUTTE, Frédéric Jean-Claude
IPC分类号： A61K9/00 , A61K9/28 , A61K31/606 , A61K47/32 , A61K47/36
CPC分类号： A61K9/2886 , A61K9/0053 , A61K9/2013 , A61K9/2054 , A61K9/284 , A61K9/2846 , A61K9/2853 , A61K9/286 , A61K9/2866 , A61K9/288 , A61K9/2893 , A61K31/196 , A61K31/606 , A61K31/616 , A61K47/32 , A61K47/36 , A61K47/38
摘要： Delayed release of a drug to the colon is achieved from a delayed release formulation comprising a core and a coating for the core. The core comprises a drug and the coating comprises an inner layer and an outer layer. The outer layer comprises a mixture of a first polymeric material which is susceptible to attack by colonic bacteria, and a second polymeric material which has a pH threshold at about pH 5 or above. The inner layer comprises a third polymeric material which is soluble in intestinal fluid or gastrointestinal fluid, said third polymeric material being selected from an at least partially neutralised polycarboxylic acid and a non-ionic polymer. In embodiments in which the third polymeric material is a non-ionic polymer, the inner layer comprises at least one of a buffer agent and a base. Advantages of formulations according to the present invention include accelerated release of the drug when exposed to colonic conditions and reduction or elimination of a food and/or alcohol effect on drug release after administration.
摘要翻译：将药物延迟释放到结肠是由包含核心和核心涂层的延迟释放制剂实现的。核心包括药物，涂层包括内层和外层。外层包含易受结肠细菌攻击的第一聚合物材料和pH值约为pH5或更高的第二聚合物质的混合物。内层包括可溶于肠液或胃肠液的第三聚合物材料，所述第三聚合物材料选自至少部分中和的多元羧酸和非离子聚合物。在第三聚合物材料是非离子聚合物的实施方案中，内层包括缓冲剂和碱的至少一种。根据本发明的制剂的优点包括当暴露于结肠状况时药物的加速释放和给药后药物释放的食物和/或酒精作用的降低或消除。

9. 发明申请

WO2013134348A1 CONTROLLED-RELEASE SOLID DOSAGE FORMS OF MESALAMINE 审中-公开
标题翻译：受控释放的马来西亚的固体剂量形式
公开(公告)号：WO2013134348A1
公开(公告)日：2013-09-12
申请号：PCT/US2013/029291
申请日：2013-03-06
申请人： SANTARUS, INC.
发明人： BOWE, Craig, Michael , CARTER, John, Christopher , MOSESON, Dana, Elaine , LEVINE, Stephen, Paul
IPC分类号： A61K9/20 , A61K9/28 , A61K9/48 , A61K31/606 , A61P29/00
CPC分类号： A61K9/2077 , A61K9/2018 , A61K9/2846 , A61K9/2866 , A61K9/2886 , A61K9/4808 , A61K31/58 , A61K31/606 , A61K2300/00
摘要： Described are controlled-release solid dosage forms of mesalamine. In one aspect of the invention the controlled-release solid dosage forms of mesalamine are capsules comprising a plurality of coated mini-tablets. Another aspect of the invention relates to a method of treating a patient suffering from inflammatory bowel disease, comprising the step of administering to the patient a therapeutically effective amount of the solid dosage form. The invention also relates to methods of inducing remission of inflammatory bowel disease and maintaining remission of inflammatory bowel disease. In certain aspects, the inflammatory bowel disease is ulcerative colitis or Crohn's disease.
摘要翻译：描述的是美沙拉嗪的控释固体剂型。在本发明的一个方面，美沙拉嗪的控释固体剂型是包含多个包被的微型片剂的胶囊。本发明的另一方面涉及一种治疗患有炎症性肠病的患者的方法，包括向患者施用治疗有效量的固体剂型的步骤。本发明还涉及诱导炎症性肠病缓解和维持炎症性肠病缓解的方法。在某些方面，炎性肠病是溃疡性结肠炎或克罗恩病。

10. 发明申请

WO2011084638A3 MESALAMINE SUPPOSITORY 审中-公开
公开(公告)号：WO2011084638A3
公开(公告)日：2011-07-14
申请号：PCT/US2010/060849
申请日：2010-12-16
申请人： APTALIS PHARMA CANADA INC. , POWEL, David
发明人： POWEL, David , DUMOULIN, Yves , GAUTHIER, Carl , MOREAU, Hugues
IPC分类号： A61K9/00 , A61K9/02 , A61K47/44 , A61K31/606
摘要： The present invention relates to a mesalamine rectal suppository designed to provide improved comfort of use. One embodiment of the invention is a mesalamine rectal suppository comprising mesalamine and one or more pharmaceutically acceptable excipients, wherein the drug load of the suppository ranges from 35% to 50%. Yet another embodiment of the invention is a mesalamine rectal suppository comprising mesalamine having a tap density ranging from about 600 to about 800 g/L (as measured by USP ) and a hard fat having an ascending melting point of 32 to 35.5° C. Yet another embodiment is a mesalamine rectal suppository comprising mesalamine particles and one or more pharmaceutically acceptable excipients, where the mesalamine particles have a surface area of from about 0.1 m 2 /g to about 2.8 m 2 /g (e.g., from about 0.1 m 2 /g to about 1.3 m 2 /g). Methods of preparing and methods of treatment with mesalamine suppositories are also provided. The invention further provides a method of determining a dissolution parameter (such as dissolution rate) of a mesalamine rectal suppository, such as a 1 g mesalamine suppository, by measuring its dissolution with USP Apparatus #2 at 40° C and a paddle rotation speed of 125 rpm in 0.2 M phosphate buffer at a pH of 7.5.

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