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1. 发明授权

US08821938B2 Porous drug matrices and methods of manufacture thereof 有权
标题翻译：多孔药物基质及其制造方法
公开(公告)号：US08821938B2
公开(公告)日：2014-09-02
申请号：US13022776
申请日：2011-02-08
申请人： Julie Straub , David Altreuter , Howard Bernstein , Donald E. Chickering, III , Sarwat Khattak , Greg Randall
发明人： Julie Straub , David Altreuter , Howard Bernstein , Donald E. Chickering, III , Sarwat Khattak , Greg Randall
IPC分类号： A61K9/14 , A61K9/00 , A61K31/335 , A01N43/02
CPC分类号： A61K9/1635 , A61K9/1611 , A61K9/1623 , A61K9/1688 , A61K9/1694
摘要： Drugs, especially low aqueous solubility drugs, are provided in a porous matrix form, preferably microparticles, which enhances dissolution of the drug in aqueous media. The drug matrices preferably are made using a process that includes (i) dissolving a drug, preferably a drug having low aqueous solubility, in a volatile solvent to form a drug solution, (ii) combining at least one pore forming agent with the drug solution to form an emulsion, suspension, or second solution and hydrophilic or hydrophobic excipients that stabilize the drug and inhibit crystallization, and (iii) removing the volatile solvent and pore forming agent from the emulsion, suspension, or second solution to yield the porous matrix of drug. Hydrophobic or hydrophilic excipients may be selected to stabilize the drug in crystalline form by inhibiting crystal growth or to stabilize the drug in amorphous form by preventing crystallization. The pore forming agent can be either a volatile liquid that is immiscible with the drug solvent or a volatile solid compound, preferably a volatile salt. In a preferred embodiment, spray drying is used to remove the solvents and the pore forming agent. The resulting porous matrix has a faster rate of dissolution following administration to a patient, as compared to non-porous matrix forms of the drug. In a preferred embodiment, microparticles of the porous drug matrix are reconstituted with an aqueous medium and administered parenterally, or processed using standard techniques into tablets or capsules for oral administration.
摘要翻译：药物，特别是低含水溶性药物以多孔基质形式提供，优选微粒，其增强药物在水性介质中的溶解。药物基质优选使用以下方法制备，所述方法包括（i）将挥发性溶剂中的药物（优选为低溶解度的药物）溶解以形成药物溶液，（ii）将至少一种成孔剂与药物溶液以形成稳定药物并抑制结晶的乳液，悬浮液或第二溶液和亲水或疏水赋形剂，和（iii）从乳液，悬浮液或第二溶液中除去挥发性溶剂和成孔剂以产生多孔基质药物。可以选择疏水性或亲水性赋形剂，以通过抑制晶体生长来稳定药物的结晶形式，或者通过防止结晶来稳定药物的无定形形式。成孔剂可以是与药物溶剂或挥发性固体化合物，优选挥发性盐不混溶的挥发性液体。在优选的实施方案中，使用喷雾干燥来除去溶剂和成孔剂。与药物的无孔基质形式相比，得到的多孔基质在给予患者后具有更快的溶解速率。在优选的实施方案中，多孔药物基质的微粒用水性介质重新配制，并肠胃外给药，或使用标准技术加工成用于口服给药的片剂或胶囊。

2. 发明授权

US06610317B2 Porous paclitaxel matrices and methods of manufacture thereof 有权
公开(公告)号：US06610317B2
公开(公告)日：2003-08-26
申请号：US09798824
申请日：2001-03-02
申请人： Julie Straub , Howard Bernstein , Donald E. Chickering, III , Sarwat Khattak , Greg Randall
发明人： Julie Straub , Howard Bernstein , Donald E. Chickering, III , Sarwat Khattak , Greg Randall
IPC分类号： A61F200
CPC分类号： A61K9/1623 , A61K9/1611 , A61K9/1635 , A61K9/1694 , Y10S977/906
摘要： Paclitaxel is provided in a porous matrix form, which allows the drug to be formulated without Cremophor and administered as a bolus. The paclitaxel matrices preferably are made using a process that includes (i) dissolving paclitaxel in a volatile solvent to form a paclitaxel solution, (ii) combining at least one pore forming agent with the paclitaxel solution to form an emulsion, suspension, or second solution, and (iii) removing the volatile solvent and pore forming agent from the emulsion, suspension, or second solution to yield the porous matrix of paclitaxel. The pore forming agent can be either a volatile liquid that is immiscible with the paclitaxel solvent or a volatile solid compound, preferably a volatile salt. In a preferred embodiment, spray drying is used to remove the solvents and the pore forming agent. In a preferred embodiment, microparticles of the porous paclitaxel matrix are reconstituted with an aqueous medium and administered parenterally, or processed using standard techniques into tablets or capsules for oral administration.

3. 发明授权

US06560897B2 Spray drying apparatus and methods of use 有权
标题翻译：喷雾干燥装置及使用方法
公开(公告)号：US06560897B2
公开(公告)日：2003-05-13
申请号：US10045419
申请日：2001-10-26
申请人： Donald E. Chickering, III , Mark J. Keegan , Greg Randall , Howard Bernstein , Julie Straub
发明人： Donald E. Chickering, III , Mark J. Keegan , Greg Randall , Howard Bernstein , Julie Straub
IPC分类号： F26B1700
CPC分类号： B01J2/04 , B01D1/18
摘要： Improved spray drying apparati, and methods of use thereof, have been developed. The spray drying equipment includes a primary drying chamber and a secondary drying apparatus which includes tubing having a length sufficient to increase the contact time between the drying gas and the droplets/particles to dry the particles to the extent desired, at a drying rate and temperature which would be too low to provide adequate drying without the secondary drying apparatus. The secondary drying apparatus increases the drying efficiency of the spray dryer system without increasing the drying rate, while minimizing loss in yield. Te secondary drying apparatus can include multiple secondary apparati, which are independently controlled for temperature and/or have different dimensions (cross-sectional areas and/or lengths), to allow for optimization of drying conditions. For example, in one embodiment, the temperatures of the secondary appararati are set to gradually increase, or decrease, enabling the particles to be dried at multiple temperatures and drying conditions. In another embodiment, the apparati have different dimensions to alter the velocity at which the particles are dried, to accommodate changes in particle aggregation or other properties affecting product yield. A preferred application for the spray drying process and equipment is in the production of microparticles, between about 1 and 200 &mgr;m in diameter, which can be used to deliver therapeutic and diagnostic agents.
摘要翻译：已经开发了改进的喷雾干燥装置及其使用方法。喷雾干燥设备包括初级干燥室和次级干燥设备，其包括具有足以增加干燥气体和液滴/颗粒之间的接触时间的长度的管道，以将干燥颗粒以期望的程度以干燥速率和温度这不足以在没有二次干燥装置的情况下提供足够的干燥。二次干燥装置提高喷雾干燥器系统的干燥效率，而不增加干燥速率，同时最小化产率损失。 Te二次干燥装置可以包括多个二次装置，其独立地控制温度和/或具有不同的尺寸（横截面积和/或长度），以允许优化干燥条件。例如，在一个实施方案中，二次装置的温度被设定为逐渐增加或降低，使颗粒能够在多个温度和干燥条件下干燥。在另一个实施方案中，所述装置具有不同的尺寸以改变颗粒干燥的速度，以适应颗粒聚集的变化或影响产品产率的其它性质。用于喷雾干燥方法和设备的优选应用是生产直径约1-200μm的微粒，其可用于递送治疗和诊断剂。

4. 发明授权

US06395300B1 Porous drug matrices and methods of manufacture thereof 有权
标题翻译：多孔药物基质及其制造方法
公开(公告)号：US06395300B1
公开(公告)日：2002-05-28
申请号：US09433486
申请日：1999-11-04
申请人： Julie Straub , Howard Bernstein , Donald E. Chickering, III , Sarwat Khattak , Greg Randall
发明人： Julie Straub , Howard Bernstein , Donald E. Chickering, III , Sarwat Khattak , Greg Randall
IPC分类号： A61K914
CPC分类号： A61K9/1688 , A61K9/1611 , A61K9/1623 , A61K9/1635 , A61K9/1694 , Y10S514/951 , Y10S977/906 , Y10S977/923
摘要： Drugs, especially low aqueous solubility drugs, are provided in a porous matrix form, preferably microparticles, which enhances dissolution of the drug in aqueous media. The drug matrices preferably are made using a process that includes (i) dissolving a drug, preferably a drug having low aqueous solubility, in a volatile solvent to form a drug solution, (ii) combining at least one pore forming agent with the drug solution to form an emulsion, suspension, or second solution, and (iii) removing the volatile solvent and pore forming agent from the emulsion, suspension, or second solution to yield the porous matrix of drug. The pore forming agent can be either a volatile liquid that is immiscible with the drug solvent or a volatile solid compound, preferably a volatile salt. In a preferred embodiment, spray drying is used to remove the solvents and the pore forming agent. The resulting porous matrix has a faster rate of dissolution following administration to a patient, as compared to non-porous matrix forms of the drug. In a preferred embodiment, microparticles of the porous drug matrix are reconstituted with an aqueous medium and administered parenterally, or processed using standard techniques into tablets or capsules for oral administration.
摘要翻译：药物，特别是低含水溶性药物以多孔基质形式提供，优选微粒，其增强药物在水性介质中的溶解。药物基质优选使用以下方法制备，所述方法包括（i）将挥发性溶剂中的药物（优选为低溶解度的药物）溶解以形成药物溶液，（ii）将至少一种成孔剂与药物溶液以形成乳液，悬浮液或第二溶液，和（iii）从乳液，悬浮液或第二溶液中除去挥发性溶剂和成孔剂以产生药物的多孔基质。成孔剂可以是与药物溶剂或挥发性固体化合物，优选挥发性盐不混溶的挥发性液体。在优选的实施方案中，使用喷雾干燥来除去溶剂和成孔剂。与药物的无孔基质形式相比，得到的多孔基质在给予患者后具有更快的溶解速率。在优选的实施方案中，多孔药物基质的微粒用水性介质重新配制，并肠胃外给药，或使用标准技术加工成用于口服给药的片剂或胶囊。

5. 发明授权

US07919119B2 Porous drug matrices and methods of manufacture thereof 有权
标题翻译：多孔药物基质及其制造方法
公开(公告)号：US07919119B2
公开(公告)日：2011-04-05
申请号：US10053929
申请日：2002-01-22
申请人： Julie Straub , David Altreuter , Howard Bernstein , Donald E. Chickering, III , Sarwat Khattak , Greg Randall
发明人： Julie Straub , David Altreuter , Howard Bernstein , Donald E. Chickering, III , Sarwat Khattak , Greg Randall
IPC分类号： A61K9/14 , A61K9/50 , B29B9/00
CPC分类号： A61K9/1635 , A61K9/1611 , A61K9/1623 , A61K9/1688 , A61K9/1694
摘要： Drugs, especially low aqueous solubility drugs, are provided in a porous matrix form, preferably microparticles, which enhances dissolution of the drug in aqueous media. The drug matrices preferably are made using a process that includes (i) dissolving a drug, preferably a drug having low aqueous solubility, in a volatile solvent to form a drug solution, (ii) combining at least one pore forming agent with the drug solution to form an emulsion, suspension, or second solution and hydrophilic or hydrophobic excipients that stabilize the drug and inhibit crystallization, and (iii) removing the volatile solvent and pore forming agent from the emulsion, suspension, or second solution to yield the porous matrix of drug. Hydrophobic or hydrophilic excipients may be selected to stabilize the drug in crystalline form by inhibiting crystal growth or to stabilize the drug in amorphous form by preventing crystallization. The pore forming agent can be either a volatile liquid that is immiscible with the drug solvent or a volatile solid compound, preferably a volatile salt. In a preferred embodiment, spray drying is used to remove the solvents and the pore forming agent. The resulting porous matrix has a faster rate of dissolution following administration to a patient, as compared to non-porous matrix forms of the drug. In a preferred embodiment, microparticles of the porous drug matrix are reconstituted with an aqueous medium and administered parenterally, or processed using standard techniques into tablets or capsules for oral administration.
摘要翻译：药物，特别是低含水溶性药物以多孔基质形式提供，优选微粒，其增强药物在水性介质中的溶解。药物基质优选使用以下方法制备，所述方法包括（i）将挥发性溶剂中的药物（优选为低溶解度的药物）溶解以形成药物溶液，（ii）将至少一种成孔剂与药物溶液以形成稳定药物并抑制结晶的乳液，悬浮液或第二溶液和亲水或疏水赋形剂，和（iii）从乳液，悬浮液或第二溶液中除去挥发性溶剂和成孔剂以产生多孔基质药物。可以选择疏水性或亲水性赋形剂，以通过抑制晶体生长来稳定药物的结晶形式，或者通过防止结晶来稳定药物的无定形形式。成孔剂可以是与药物溶剂或挥发性固体化合物，优选挥发性盐不混溶的挥发性液体。在优选的实施方案中，使用喷雾干燥来除去溶剂和成孔剂。与药物的无孔基质形式相比，得到的多孔基质在给予患者后具有更快的溶解速率。在优选的实施方案中，多孔药物基质的微粒用水性介质重新配制，并肠胃外给药，或使用标准技术加工成用于口服给药的片剂或胶囊。

6. 发明授权

US06800297B2 Porous COX-2 inhibitor matrices and methods of manufacture thereof 失效
公开(公告)号：US06800297B2
公开(公告)日：2004-10-05
申请号：US10441440
申请日：2003-05-19
申请人： David Altreuter , Julie Straub , Howard Bernstein , Donald E. Chickering, III , Paul Kopesky , Greg Randall
发明人： David Altreuter , Julie Straub , Howard Bernstein , Donald E. Chickering, III , Paul Kopesky , Greg Randall
IPC分类号： A51K914
CPC分类号： A61K9/0019 , A61K9/2095 , A61K47/02
摘要： One or more COX-2 inhibitors are provided in a porous matrix form wherein the dissolution rate of the drug is enhanced when the matrix is contacted with an aqueous medium. The porous matrix yields upon contact with an aqueous medium nanoparticles and microparticles of COX-2 inhibitors having a mean diameter between about 0.01 and 5 &mgr;m and a total surface area greater than about 0.5 m2/mL. The dry porous matrix preferably is in a dry powder form having a TAP density less than or equal to 1.0 g/mL. The porous COX-2 inhibitor matrices preferably are made using a process that includes (i) dissolving one or more COX-2 inhibitors in a volatile solvent to form a drug solution, (ii) combining at least one pore forming agent with the drug solution to form an emulsion, suspension, or second solution, and (iii) removing the volatile solvent and pore forming agent from the emulsion, suspension, or second solution to yield the dry porous matrix of COX-2 inhibitors. The resulting porous matrix has a faster rate of dissolution following administration to a patient, as compared to non-porous matrix forms of the drug.

7. 发明授权

US06645528B1 Porous drug matrices and methods of manufacture thereof 有权
公开(公告)号：US06645528B1
公开(公告)日：2003-11-11
申请号：US09694407
申请日：2000-10-23
申请人： Julie Straub , Howard Bernstein , Donald E. Chickering, III , Sarwat Khattak , Greg Randall
发明人： Julie Straub , Howard Bernstein , Donald E. Chickering, III , Sarwat Khattak , Greg Randall
IPC分类号： A61K914
CPC分类号： A61K9/1688 , A61K9/1611 , A61K9/1623 , A61K9/1635 , A61K9/1694 , Y10S514/951 , Y10S977/906 , Y10S977/923
摘要： Drugs, especially low aqueous solubility drugs, are provided in a porous matrix form, preferably microparticles, which enhances dissolution of the drug in aqueous media. The drug matrices preferably are made using a process that includes (i) dissolving a drug, preferably a drug having low aqueous solubility, in a volatile solvent to form a drug solution, (ii) combining at least one pore forming agent with the drug solution to form an emulsion, suspension, or second solution, and (iii) removing the volatile solvent and pore forming agent from the emulsion, suspension, or second solution to yield the porous matrix of drug. The pore forming agent can be either a volatile liquid that is immiscible with the drug solvent or a volatile solid compound, preferably a volatile salt. In a preferred embodiment, spray drying is used to remove the solvents and the pore forming agent. The resulting porous matrix has a faster rate of dissolution following administration to a patient, as compared to non-porous matrix forms of the drug. In a preferred embodiment, microparticles of the porous drug matrix are reconstituted with an aqueous medium and administered parenterally, or processed using standard techniques into tablets or capsules for oral administration.

8. 发明申请

US20110129533A1 POROUS DRUG MATRICES AND METHODS OF MANUFACTURE THEREOF 有权
标题翻译：多糖药物及其制造方法
公开(公告)号：US20110129533A1
公开(公告)日：2011-06-02
申请号：US13022776
申请日：2011-02-08
申请人： Julie Straub , David Altreuter , Howard Bernstein , Donald E. Chickering, III , Sarwat Khattak , Greg Randall
发明人： Julie Straub , David Altreuter , Howard Bernstein , Donald E. Chickering, III , Sarwat Khattak , Greg Randall
IPC分类号： A61K31/337 , A61K9/10 , A61P35/00
CPC分类号： A61K9/1635 , A61K9/1611 , A61K9/1623 , A61K9/1688 , A61K9/1694
摘要： Drugs, especially low aqueous solubility drugs, are provided in a porous matrix form, preferably microparticles, which enhances dissolution of the drug in aqueous media. The drug matrices preferably are made using a process that includes (i) dissolving a drug, preferably a drug having low aqueous solubility, in a volatile solvent to form a drug solution, (ii) combining at least one pore forming agent with the drug solution to form an emulsion, suspension, or second solution and hydrophilic or hydrophobic excipients that stabilize the drug and inhibit crystallization, and (iii) removing the volatile solvent and pore forming agent from the emulsion, suspension, or second solution to yield the porous matrix of drug. Hydrophobic or hydrophilic excipients may be selected to stabilize the drug in crystalline form by inhibiting crystal growth or to stabilize the drug in amorphous form by preventing crystallization. The pore forming agent can be either a volatile liquid that is immiscible with the drug solvent or a volatile solid compound, preferably a volatile salt. In a preferred embodiment, spray drying is used to remove the solvents and the pore forming agent. The resulting porous matrix has a faster rate of dissolution following administration to a patient, as compared to non-porous matrix forms of the drug. In a preferred embodiment, microparticles of the porous drug matrix are reconstituted with an aqueous medium and administered parenterally, or processed using standard techniques into tablets or capsules for oral administration.
摘要翻译：药物，特别是低含水溶性药物以多孔基质形式提供，优选微粒，其增强药物在水性介质中的溶解。药物基质优选使用以下方法制备，所述方法包括（i）将挥发性溶剂中的药物（优选为低溶解度的药物）溶解以形成药物溶液，（ii）将至少一种成孔剂与药物溶液以形成稳定药物并抑制结晶的乳液，悬浮液或第二溶液和亲水或疏水赋形剂，和（iii）从乳液，悬浮液或第二溶液中除去挥发性溶剂和成孔剂以产生多孔基质药物。可以选择疏水性或亲水性赋形剂，以通过抑制晶体生长来稳定药物的结晶形式，或者通过防止结晶来稳定药物的无定形形式。成孔剂可以是与药物溶剂或挥发性固体化合物，优选挥发性盐不混溶的挥发性液体。在优选的实施方案中，使用喷雾干燥来除去溶剂和成孔剂。与药物的无孔基质形式相比，得到的多孔基质在给予患者后具有更快的溶解速率。在优选的实施方案中，多孔药物基质的微粒用水性介质重新配制，并肠胃外给药，或使用标准技术加工成用于口服给药的片剂或胶囊。

9. 发明授权

US06589557B2 Porous celecoxib matrices and methods of manufacture thereof 有权
公开(公告)号：US06589557B2
公开(公告)日：2003-07-08
申请号：US09881289
申请日：2001-06-14
申请人： Julie Straub , Howard Bernstein , Donald E. Chickering, III , Greg Randall
发明人： Julie Straub , Howard Bernstein , Donald E. Chickering, III , Greg Randall
IPC分类号： A61K914
CPC分类号： A61K47/02 , A61K9/0019 , A61K9/2095
摘要： Celecoxib is provided in a porous matrix form wherein the dissolution rate of the drug is enhanced when the matrix is contacted with an aqueous medium. The porous matrix yields upon contact with an aqueous medium nanoparticles and microparticles of celecoxib having a mean diameter between about 0.01 and 5 &mgr;m and a total surface area greater than about 0.5 m2/mL. The dry porous matrix preferably is in a dry powder form having a TAP density less than or equal to 1.0 g/mL. The porous celecoxib matrices preferably are made using a process that includes (i) dissolving celecoxib in a volatile solvent to form a drug solution, (ii) combining at least one pore forming agent with the drug solution to form an emulsion, suspension, or second solution, and (iii) removing the volatile solvent and pore forming agent from the emulsion, suspension, or second solution to yield the dry porous matrix of celecoxib. The resulting porous matrix has a faster rate of dissolution following administration to a patient, as compared to non-porous matrix forms of the drug.

10. 发明授权

US06308434B1 Spray drying method 有权
标题翻译：喷雾干燥法
公开(公告)号：US06308434B1
公开(公告)日：2001-10-30
申请号：US09756950
申请日：2001-01-09
申请人： Donald E. Chickering, III , Mark J. Keegan , Greg Randall , Howard Bernstein , Julie Straub
发明人： Donald E. Chickering, III , Mark J. Keegan , Greg Randall , Howard Bernstein , Julie Straub
IPC分类号： F26B308
CPC分类号： B01J2/04 , B01D1/18
摘要： Improved spray drying methods of have been developed. The spray drying method includes use of a primary drying chamber and a secondary drying apparatus which includes tubing having a length sufficient to increase the contact time between the drying gas and the droplets/particles to dry the particles to the extent desired, at a drying rate and temperature which would be too low to provide adequate drying without the secondary drying apparatus. The secondary drying apparatus increases the drying efficiency of the spray dryer system without increasing the drying rate, while minimizing loss in yield. The ratio of the length of tubing to the length of the primary drying chamber is at least 2:1. The tubing diameter is substantially smaller than the diameter of the primary drying chamber, such that the particles move at higher velocity through the tubing to minimize product losses. The ratio of the cross-sectional area of the primary drying chamber to the cross-sectional area of the tubing most preferably is about 16:1. The tubing preferably is in a compact coil design, which can more easily be transported and which has minimum space requirements, and may optionally include a jacket to control the temperature of the secondary drying process. A preferred application for the spray drying process and equipment is in the production of microparticles, between about 1 and 200 &mgr;m in diameter, which can be used to deliver therapeutic and diagnostic agents.
摘要翻译：已经开发出改进的喷雾干燥方法。喷雾干燥方法包括使用初级干燥室和二次干燥设备，其包括具有足以增加干燥气体和液滴/颗粒之间的接触时间的长度的管道，以将颗粒干燥至所需的程度，干燥速率温度太低，无法在没有二次干燥装置的情况下提供足够的干燥。二次干燥装置提高喷雾干燥器系统的干燥效率，而不增加干燥速率，同时最小化产率损失。管道长度与初级干燥室长度之比至少为2：1。管道直径基本上小于初级干燥室的直径，使得颗粒以更高的速度移动通过管道以最小化产品损失。初级干燥室的横截面积与管道的横截面面积的比率最优选为约16:1。管道优选地处于紧凑的线圈设计中，其可以更容易地被输送并且具有最小的空间要求，并且可以可选地包括用于控制二次干燥过程的温度的护套。用于喷雾干燥方法和设备的优选应用是生产直径约1-200μm的微粒，其可用于递送治疗和诊断剂。

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