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1. 发明授权

EP1663216B1 MODIFIED RELEASE COMPOSITIONS COMPRISING TACROLIMUS 有权转让
标题翻译：与修饰释放他克莫司组合物
公开(公告)号：EP1663216B1
公开(公告)日：2011-11-02
申请号：EP04762794.8
申请日：2004-08-30
申请人： Veloxis Pharmaceuticals A/S
发明人： HOLM, Per , NORLING, Tomas
IPC分类号： A61K31/436 , A61K9/16 , A61K9/14 , A61P37/06
CPC分类号： A61K31/436 , A61K9/0053 , A61K9/10 , A61K9/1611 , A61K9/1617 , A61K9/1623 , A61K9/1641 , A61K9/1652 , A61K9/2009 , A61K9/2013 , A61K9/2018 , A61K9/2027 , A61K9/2031 , A61K9/2054 , A61K9/2077 , A61K9/2095 , A61K9/2846 , A61K9/2893 , A61K31/00 , A61K31/439 , A61K31/4745 , Y10S514/885
摘要： A modified release composition comprising tacrolimus releases less than 20% w/w of the active ingredient within 0.5 hours when subjected to an in vitro dissolution test using USP Paddle method and using 0.1 N HCl as dissolution medium and has increased bioavailability by effectively reducing or even avoiding the effects of CYP3A4 metabolism. The modified composition may be coated with an enteric coating; and/or may comprise a solid dispersion or a solid solution of tacrolimus in a hydrophilic or water-miscible vehicle and one or more modifying release agents; and/or may comprise a solid dispersion or a solid solution of tacrolimus in an amphiphilic or hydrophobic vehicle and optionally one or more modifying release agents.

2. 发明公开

EP1663216A1 MODIFIED RELEASE COMPOSITIONS COMPRISING TACROLIMUS 有权转让
标题翻译： TACROLIMUS ENTHALTENDE ZUSAMMENSETZUNGEN MIT MODIFIZIERTER FREISETZUNG
公开(公告)号：EP1663216A1
公开(公告)日：2006-06-07
申请号：EP04762794.8
申请日：2004-08-30
申请人： LifeCycle Pharma A/S
发明人： HOLM, Per , NORLING, Tomas
IPC分类号： A61K31/436 , A61K9/16 , A61K9/14 , A61P37/06
CPC分类号： A61K31/436 , A61K9/0053 , A61K9/10 , A61K9/1611 , A61K9/1617 , A61K9/1623 , A61K9/1641 , A61K9/1652 , A61K9/2009 , A61K9/2013 , A61K9/2018 , A61K9/2027 , A61K9/2031 , A61K9/2054 , A61K9/2077 , A61K9/2095 , A61K9/2846 , A61K9/2893 , A61K31/00 , A61K31/439 , A61K31/4745 , Y10S514/885
摘要： A modified release composition comprising tacrolimus releases less than 20% w/w of the active ingredient within 0.5 hours when subjected to an in vitro dissolution test using USP Paddle method and using 0.1 N HCl as dissolution medium and has increased bioavailability by effectively reducing or even avoiding the effects of CYP3A4 metabolism. The modified composition may be coated with an enteric coating; and/or may comprise a solid dispersion or a solid solution of tacrolimus in a hydrophilic or water-miscible vehicle and one or more modifying release agents; and/or may comprise a solid dispersion or a solid solution of tacrolimus in an amphiphilic or hydrophobic vehicle and optionally one or more modifying release agents.
摘要翻译：溶解和/或分散在亲水或水混溶媒介物中的他克莫司（FK-506）的药物组合物在环境温度下形成固体分散体或固体溶液具有改善的生物利用度。

3. 发明授权

US11141408B2 Regimen for suppressing organ rejection 有权
公开(公告)号：US11141408B2
公开(公告)日：2021-10-12
申请号：US16678527
申请日：2019-11-08
申请人： Veloxis Pharmaceuticals A/S
发明人： William J. Polvino
IPC分类号： A61K31/436 , A61K31/5377 , A61K39/395 , A61P43/00 , A61K45/06 , A61K39/00 , A61K9/20 , A61K9/00
摘要： The present invention relates to a method of suppressing organ rejection in a patient receiving an organ transplant by initiating oral treatment with a once-daily extended release tacrolimus dosage form, for example, at an initial dose of from about 0.15 to about 0.20 mg/kg/day within 24 or 48 hours following transplantation. The once-daily extended release tacrolimus dosage form (i) provides low fluctuation and/or swing of tacrolimus, (ii) provides a significantly lower Cmax than an immediate release formulation of tacrolimus while providing the same or greater area under the curve (AUC), (iii) releases the tacrolimus substantially in the colon and/or the lower ileum, (iv) releases at most 63.5% of the tacrolimus in the dosage form at the 12 hour time point, or (v) any combination of any of the foregoing.

4. 发明授权

US11123331B2 Tacrolimus for improved treatment of transplant patients 有权
公开(公告)号：US11123331B2
公开(公告)日：2021-09-21
申请号：US17085379
申请日：2020-10-30
申请人： Veloxis Pharmaceuticals A/S
发明人： Robert D. Gordon , Per Holm , Anne-Marie Lademann , Tomas Norling
IPC分类号： A61K31/436 , A61K9/20 , A61K9/28 , A61K9/16 , A61K9/48 , A61K9/00 , A61K47/10
摘要： An extended release oral dosage form comprising as active substance tacrolimus or a pharmaceutically active analogue thereof for a once daily immunosuppressive treatment of a patient in need thereof, preferable a kidney or liver transplant patient. The dosage form releases the active substance over an extended period of time. It also provides improved pharmacokinetic parameters due to an extended and constant in vivo release including substantial decreased peak concentrations, despite increased bioavailability, substantial extended times for maximal concentration, and higher minimal concentrations when compared with conventional immediate release dosage forms and a recent modified release tacrolimus dosage form.

5. 发明授权

US11077096B2 Modified release compositions comprising tacrolimus 有权
公开(公告)号：US11077096B2
公开(公告)日：2021-08-03
申请号：US15677938
申请日：2017-08-15
申请人： Veloxis Pharmaceuticals A/S
发明人： Per Holm , Tomas Norling
IPC分类号： A61K9/16 , A61K31/436 , A61K9/20 , A61K9/28 , A61K31/00 , A61K31/4745 , A61K9/10 , A61K31/439 , A61K9/00
摘要： A modified release composition comprising tacrolimus releases less than 20% w/w of the active ingredient within 0.5 hours when subjected to an in vitro dissolution test using USP Paddle method and using 0.1 N HCl as dissolution medium and has increased bioavailability by effectively reducing or even avoiding the effects of CYP3A4 metabolism. The modified composition may be coated with an enteric coating; and/or may comprise a solid dispersion or a solid solution of tacrolimus in a hydrophilic or water-miscible vehicle and one or more modifying release agents; and/or may comprise a solid dispersion or a solid solution of tacrolimus in an amphiphilic or hydrophobic vehicle and optionally one or more modifying release agents.

6. 发明申请

US20210046054A1 Tacrolimus For Improved Treatment Of Transplant Patients 有权
公开(公告)号：US20210046054A1
公开(公告)日：2021-02-18
申请号：US17085291
申请日：2020-10-30
申请人： Veloxis Pharmaceuticals A/S
发明人： Robert D. GORDON , Per HOLM , Anne-Marie LADEMANN , Tomas NORLING
IPC分类号： A61K31/436 , A61K9/20 , A61K9/28 , A61K9/16 , A61K9/48 , A61K9/00 , A61K47/10
摘要： An extended release oral dosage form comprising as active substance tacrolimus or a pharmaceutically active analogue thereof for a once daily immunosuppressive treatment of a patient in need thereof, preferable a kidney or liver transplant patient. The dosage form releases the active substance over an extended period of time. It also provides improved pharmacokinetic parameters due to an extended and constant in vivo release including substantial decreased peak concentrations, despite increased bioavailability, substantial extended times for maximal concentration, and higher minimal concentrations when compared with conventional immediate release dosage forms and a recent modified release tacrolimus dosage form.

7. 发明授权

US09173847B2 Tablet comprising a fibrate 有权
标题翻译：片剂包含贝特类
公开(公告)号：US09173847B2
公开(公告)日：2015-11-03
申请号：US11449918
申请日：2006-06-09
申请人： Per Holm , Tomas Norling
发明人： Per Holm , Tomas Norling
IPC分类号： A61K9/20 , A61K9/16 , A61K31/192
CPC分类号： A61K9/2077 , A61K9/1623 , A61K31/192
摘要： Stable tablets and pharmaceutical compositions in particulate form comprising a fibrate, for example fenofibrate, dissolved or dispersed in an non-aqueous vehicle with improved bioavailability, thereby eliminating the food effect so that the tablet or composition can be administered to a patient irrespective of being in fed or fasted state.
摘要翻译：稳定的片剂和药物组合物，其包含溶解或分散在具有改善的生物利用度的非水性载体中的贝特类贝特类，例如非诺贝特，从而消除食物效应，使得片剂或组合物可以施用于患者，而不管喂食或禁食状态。

8. 发明授权

EP1406594B1 CONTROLLED AGGLOMERATION 有权转让
公开(公告)号：EP1406594B1
公开(公告)日：2019-06-05
申请号：EP02758174.3
申请日：2002-07-05
申请人： Veloxis Pharmaceuticals A/S
发明人： HOLM, Per , BUUR, Anders , ELEMA, Michiel, Onne , MULLGAARD, Birgitte , HOLM, Jannie, Egeskov , SCHULTZ, Kirsten
IPC分类号： A61K9/16 , A61K9/20 , B01J2/16

9. 发明授权

EP1973529B1 DISINTEGRATING LOADABLE TABLETS 有权转让
标题翻译： ZERFALLENDEBEFÜLBARETABLETTEN
公开(公告)号：EP1973529B1
公开(公告)日：2011-05-25
申请号：EP07700149.3
申请日：2007-01-05
申请人： LifeCycle Pharma A/S
发明人： HOLM, Per , SLOT, Lillian
IPC分类号： A61K9/20
CPC分类号： A61K9/2095 , A61K9/2009 , A61K9/2013 , A61K9/2018 , A61K9/2027 , A61K9/2031 , A61K9/205 , A61K9/2054
摘要： A disintegrating loadable tablet product in compressed form comprising i) at least 60% w/w of a sorbent material having a specific surface area (BET surface area) of at least 50 m2/g as measured by gas adsorption or mixtures of such sorbent materials, and ii) a disintegrant or a mixture of disintegrants wherein the tablet in compressed form has a) a porosity of 45% v/v or more, b) a hardness of at least 20 Newton, and c) a loading capacity of at least 30% of a liquid. The tablet is suitable for the preparation of a tablet containing an active substance by e.g. immersing the tablet in a liquid containing the active substance. The invention thus provides a safe and reproducible new method of preparing pharmaceutical tablets.
摘要翻译：一种压缩形式的崩解性可装载片剂，其包含：i）通过气体吸附测定的至少60％w / w的具有至少50m 2 / g的比表面积（BET表面积）的吸附剂材料或这些吸附剂材料的混合物，和ii）崩解剂或崩解剂的混合物，其中压缩形式的片剂具有a）45％v / v以上的孔隙率，b）至少20牛顿的硬度，和c）至少负载能力 30％的液体。片剂适用于制备含有活性物质的片剂。将片剂浸入含有活性物质的液体中。因此，本发明提供了制备药物片剂的安全且可重现的新方法。

10. 发明公开

EP1406594A1 CONTROLLED AGGLOMERATION 有权转让
标题翻译： KONTROLLIERTE AGGLOMERATION
公开(公告)号：EP1406594A1
公开(公告)日：2004-04-14
申请号：EP02758174.3
申请日：2002-07-05
申请人： LifeCycle Pharma A/S
发明人： HOLM, Per , BUUR, Anders , ELEMA, Michiel, Onne , MULLGAARD, Birgitte , HOLM, Jannie, Egeskov , SCHULTZ, Kirsten
IPC分类号： A61K9/16 , A61K9/20 , B01J2/16
CPC分类号： A61K9/1682 , A61K9/1611 , A61K9/1623 , A61K9/1641 , A61K9/1652 , A61K9/1694 , A61K9/2009 , A61K9/2018 , A61K9/2031 , B01J2/006 , B01J2/02 , Y10T428/24868 , Y10T428/24901 , Y10T428/29 , Y10T428/2982 , Y10T428/2991 , Y10T428/2998
摘要： A process for the preparation of a particulate material by a controlled agglomeration method, i.e. a method that enables a controlled growth in particle size. The method is especially suitable for use in the preparation of pharmaceutical compositions containing a therapeutically and/or prophylactically active substance which has a relatively low aqueous solubility and/or which is subject to chemical decomposition. By employment of the novel process, compositions can be prepared that have improved properties with respect to release of the active substance from the composition as evidenced by in vitro dissolution test and/or with respect to improved shelf life of the compositions upon storage. The process comprising i) spraying a first composition comprising a carrier, which has a melting point of about 5 °C or more such as, e.g., about 10 °C or more, about 20°C or more or about 25 °C or more and which is present in the first composition in liquid form, on a second composition comprising a material in solid form, the second composition having a temperature of at the most a temperature corresponding to the melting point of the carrier and/or of the carrier composition such as, e.g., a temperature of at least about 2 °C, at least about 5 °C or at least about 10°C lower than the melting point of the carrier and/or of the carrier composition, and ii) mixing or other means of mechanical working the second composition onto which the first composition is sprayed to obtain the particulate material. The invention also relates to a particulate material obtained by the novel process and to pharmaceutical compositions containing such particulate material. The particulate material obtained exhibits excellent flowability and compactability and possess excellent tabletting properties.
摘要翻译：用于通过受控的团聚法制备颗粒材料的方法，即能够控制粒度增长的方法。该方法特别适用于制备含有较低水溶性和/或经受化学分解的治疗和/或预防活性物质的药物组合物。通过使用该新方法，可以制备组合物，其相对于组合物释放活性物质具有改善的性质，如通过体外溶出试验和/或关于储存时组合物的保质期的改善所证明的。该方法包括：i）喷涂包含载体的第一组合物，所述载体的熔点为约5℃或更高，例如约10℃或更高，约20℃或更高或约25℃或更高并且其以液体形式存在于包含固体形式的材料的第二组合物上，第二组合物的温度最高为对应于载体和/或载体组合物的熔点的温度例如比载体和/或载体组合物的熔点低至少约2℃，至少约5℃或至少约10℃的温度，以及ii）混合或其它对第二组合物进行机械加工以对其喷射第一组合物以获得颗粒材料的装置。本发明还涉及通过新方法获得的颗粒材料和含有这种颗粒材料的药物组合物。获得的颗粒材料表现出优异的流动性和紧实性，并且具有优异的压片性能。

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