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1. 发明申请

WO2005084639A2 POLYMERIC DRUG DELIVERY SYSTEM FOR HYDROPHOBIC DRUGS 审中-公开
标题翻译：用于疏水性药物的聚合物药物递送系统
公开(公告)号：WO2005084639A2
公开(公告)日：2005-09-15
申请号：PCT/US2005/007525
申请日：2005-03-03
申请人： SPHERICS, INC. , JACOB, Jules, S. , BASSETT, Michael , SCHESTOPOL, Marcus, A. , MATHIOWITZ, Edith , NANGIA, Avinash , CARTER, Bennett , MOSLEMY, Peyman , SHAKED, Ze'ev , ENSCORE, David , SIKES, Courtney
发明人： JACOB, Jules, S. , BASSETT, Michael , SCHESTOPOL, Marcus, A. , MATHIOWITZ, Edith , NANGIA, Avinash , CARTER, Bennett , MOSLEMY, Peyman , SHAKED, Ze'ev , ENSCORE, David , SIKES, Courtney
IPC分类号： A61K9/00
CPC分类号： A61K9/209 , A61K9/0065 , A61K9/1635 , A61K9/1641 , A61K9/1647 , A61K9/1652 , A61K9/1676 , A61K9/2054 , A61K9/2077 , A61K9/2086 , A61K9/2853
摘要： An oral delivery system for Class II drugs that have low oral bioavailability due to their insolubility in water and slow dissolution kinetics and method for making such a drug delivery system are disclosed herein. The formulation may be a controlled release or immediate release formulation. The immediate release formulation contains a Class II drug, together with a hydrophobic polymer, preferably a bioadhesive polymer. In one embodiment, the drug and polymer are co-dissolved in a common solvent. The solution is formed into small solid particles by any convenient method, particularly by spray drying. The resulting particles contain drug dispersed as small particles in a polymeric matrix. The particles are stable against aggregation, and can be put into capsules or tableted for administration. The controlled release formulations contain a BCS Class II drug and a bioadhesive polymer. The controlled release formulations may be in the form of a tablet, capsules, mini-tab, microparticulate, or osmotic pump. Enhancement of oral uptake of the drug from use of bioadhesive polymers occurs through (1) increased dissolution kinetics due to stable micronization of the drug, (2) rapid release of the drug from the polymer in the GI tract; and (3) prolonged GI transit due to bioadhesive properties of the polymers. The combination of these effects allows the preparation of a compact, stable dosage form suitable for oral administration of many class II drugs.
摘要翻译：本文公开了由于其不溶于水且缓慢溶出动力学而具有低口服生物利用度的II类药物的口服递送系统以及制备此类药物递送系统的方法。该制剂可以是控释或速释制剂。速释制剂含有II类药物以及疏水聚合物，优选生物粘附聚合物。在一个实施方案中，药物和聚合物共溶于普通溶剂中。通过任何方便的方法，特别是通过喷雾干燥，溶液形成小的固体颗粒。所得颗粒含有作为小颗粒分散在聚合物基质中的药物。颗粒对于聚集是稳定的，并且可以放入胶囊或制成片剂给药。控释制剂含有BCS II类药物和生物粘附聚合物。控释制剂可以是片剂，胶囊剂，小片，微粒或渗透泵的形式。（1）由于药物的稳定微粉化，溶解动力学增加，（2）药物从胃肠道中的聚合物中快速释放，因此通过使用生物粘附聚合物增强药物的口服摄取。和（3）由于聚合物的生物粘附性而延长的GI运输。这些效果的结合使得可以制备适用于许多II类药物的口服给药的致密稳定的剂型。

2. 发明申请

WO2011097103A1 STENT AND STENT DELIVERY SYSTEM WITH IMPROVED DELIVERABILITY 审中-公开
标题翻译：具有改进的可交付性的STENT和STENT交付系统
公开(公告)号：WO2011097103A1
公开(公告)日：2011-08-11
申请号：PCT/US2011/022623
申请日：2011-01-26
申请人： MICELL TECHNOLOGIES, INC. , MCCLAIN, James, B. , TAYLOR, Douglas , ENSCORE, David
发明人： MCCLAIN, James, B. , TAYLOR, Douglas , ENSCORE, David
IPC分类号： A61F2/06
CPC分类号： A61F2/958 , A61F2/0077 , A61F2002/826 , A61F2250/003
摘要： Stent delivery systems having improved deliverability comprising an elongate member having an inflation lumen and a guidewire lumen therein; a balloon having an interior that is in fluid communication with the inflation lumen; and a stent comprising a coating mounted on the balloon. Methods for making stent delivery systems having improved deliverability. Methods for delivering two stent delivery systems concurrently through a guiding catheter, each stent delivery system comprising elongate member having an inflation lumen and a guidewire lumen therein, a balloon having an interior that is in fluid communication with the inflation lumen, and a stent comprising a coating mounted on the balloon. Stent coatings may comprise a pharmaceutical agent at least a portion of which is in crystalline form.
摘要翻译：具有改善的输送能力的支架输送系统包括具有膨胀腔和其中的导丝管腔的细长构件; 具有与所述充气腔流体连通的内部的气囊; 以及包括安装在气囊上的涂层的支架。用于制造具有改善的输送性的支架输送系统的方法。用于通过引导导管同时输送两个支架输送系统的方法，每个支架输送系统包括具有充气腔和其中的导丝腔的细长构件，具有与膨胀腔流体连通的内部的球囊，以及支架，涂层安装在气球上。支架涂层可以包含至少一部分为结晶形式的药剂。

3. 发明申请

WO2003051304A2 BIOADHESIVE DRUG DELIVERY SYSTEM WITH ENHANCED GASTRIC RETENTION 审中-公开
标题翻译：具有增强气体保持力的生物药物输送系统
公开(公告)号：WO2003051304A2
公开(公告)日：2003-06-26
申请号：PCT/US2002/040025
申请日：2002-12-13
申请人： SPHERICS, INC. , JACOB, Jules , MATHIOWITZ, Edith , ENSCORE, David , SCHESTOPOL, Marcus
发明人： JACOB, Jules , MATHIOWITZ, Edith , ENSCORE, David , SCHESTOPOL, Marcus
IPC分类号： A61K
CPC分类号： A61K9/0065 , A61K9/501 , A61K9/5026 , A61K9/5031 , A61K9/5073
摘要： Bioadhesive macrosphere delivery systems ("BDDS") having prolonged gastric retention time due to bioadhesion rather than physical density or size are described. In general, the macrospheres have diameters that are greater than 200 microns, more preferably greater than 500 microns. The bioadhesive macrospheres are released in the stomach where they reside in close proximity to the gastric mucosa for a prolonged period of time. Increased residence of BDDS in the upper GI can lead to increased systemic absorption of drug in the preferred site of systemic absorption, namely the upper GI tract (upper to mid-jejunum). The BDDS may be engineered either as a capsule with drug delivery controlled by a diffusion-limited membrane or degradable shell, or as a solid matrix system with drug delivery controlled by a combination of diffusion and polymer degradation kinetics.
摘要翻译：描述了由于生物粘附而不是物理密度或大小而具有延长的胃停留时间的生物粘附大球传递系统（“BDDS”）。通常，大球的直径大于200微米，更优选大于500微米。生物粘附的大球在胃中被释放，其中它们靠近胃粘膜存在一段较长的时间。增加BDDS在上GI中的居住可导致药物在全身吸收的优选部位，即上胃肠道上（上至中空）中的全身吸收增加。 BDDS可以被设计为具有通过扩散限制膜或可降解壳控制的药物递送的胶囊，或者作为具有由扩散和聚合物降解动力学的组合控制的药物递送的固体基质体系。

4. 发明申请

WO2009124096A1 PERMEANT DELIVERY SYSTEM AND METHODS FOR USE THEREOF 审中-公开
标题翻译：渗透剂输送系统及其使用方法
公开(公告)号：WO2009124096A1
公开(公告)日：2009-10-08
申请号：PCT/US2009/039045
申请日：2009-03-31
申请人： ALTEA THERAPEUTICS CORPORATION , TAGLIFERRI, Frank , SMITH, Alan , ENSCORE, David , TOLIA, Gaurav , BAUDYS, Mirek
发明人： TAGLIFERRI, Frank , SMITH, Alan , ENSCORE, David , TOLIA, Gaurav , BAUDYS, Mirek
IPC分类号： A61F13/00
CPC分类号： A61M37/00 , A61K9/7053 , A61K31/4468 , A61K31/485 , A61K47/12 , A61K47/183 , A61K47/38 , A61P5/50 , A61P23/02
摘要： Disclosed are a patch, system, and method for delivery of a permeant composition into a subject via at least one formed pathway through a biological membrane of the subject. The patch comprises a matrix, at least one hydrophilic permeant disposed within the matrix, wherein at least a portion of the permeant can dissolve in biological moisture received from the subject, and at least one permeability enhancer disposed within the matrix. Also disclosed are systems and methods for delivery of a permeant composition into a subject via at least one formed pathway through a skin layer of the subject.
摘要翻译：公开了一种用于通过穿过受试者的生物膜的至少一个形成的途径将渗透组合物递送至受试者的贴剂，系统和方法。所述贴剂包含基质，至少一个亲水性渗透物，其设置在所述基质内，其中所述渗透剂的至少一部分可以溶解在从所述受试者接收的生物水分中，以及至少一种渗透性增强剂。还公开了用于通过穿过受试者的皮肤层的至少一个形成的途径将渗透组合物递送至受试者的系统和方法。

5. 发明申请

WO1992007555A1 DRUG DELIVERY SYSTEM AND METHOD 审中-公开
标题翻译：药物递送系统和方法
公开(公告)号：WO1992007555A1
公开(公告)日：1992-05-14
申请号：PCT/US1991007922
申请日：1991-10-25
申请人： ALZA CORPORATION , BERGGREN, Randall, G. , ENSCORE, David, James , MARKS, Susan, M. , OSBORNE, James, L. , WONG, Patrick, S.-L. , ROORDA, Wouter, Erik
发明人： ALZA CORPORATION
IPC分类号： A61K09/22
CPC分类号： A61C19/063 , A61K6/0067 , A61K9/0063 , A61K47/34
摘要： The present invention is directed to a material (10) which can be used to deliver a drug, such as an antibiotic, into a diseased tissue pocket (12), such as a periodontal pocket. The material (10) is preferably a bioerodible polymer such as a poly(orthoester), a polylactic acid, a polyglycolic acid or a copolymer or mixture thereof. The polymer containing the drug is heated to a physiologically compatible elevated temperature prior to injection into the tissue pocket (12). Once the bioerodible material (10) is injected into the pocket (12), the material (10) cools to the body temperature of the pocket (12). As it cools, the material (10) hardens and remains in place in the tissue pocket (12). The hardened material (10) bioerodes in the pocket (12) and releases the drug over a period of several days.
摘要翻译：本发明涉及可用于将诸如抗生素的药物递送到诸如牙周袋的患病组织袋（12）中的材料（10）。材料（10）优选为生物可腐蚀聚合物，例如聚（原酸酯），聚乳酸，聚乙醇酸或其共聚物或混合物。将含有药物的聚合物在注入组织袋（12）之前被加热至生理上相容的升高的温度。一旦将生物可蚀解材料（10）注入到口袋（12）中，材料（10）冷却到口袋（12）的体温。当它冷却时，材料（10）硬化并保持在组织袋（12）中的适当位置。硬化材料（10）在口袋（12）中生物代谢并在几天的时间内释放药物。

6. 发明申请

WO2006138658A3 PERMEANT DELIVERY SYSTEM AND METHODS FOR USE THEREOF 审中-公开
公开(公告)号：WO2006138658A3
公开(公告)日：2006-12-28
申请号：PCT/US2006/023640
申请日：2006-06-19
申请人： ALTEA THERAPEUTICS CORP. , EPPSTEIN, Jonathan , ENSCORE, David , TAGLIAFERRI, Frank , TOLIA, Gaurav , CHANG, Shulun , SMITH, Alan , PATEL, Yogi , MCRAE, Stuart
发明人： EPPSTEIN, Jonathan , ENSCORE, David , TAGLIAFERRI, Frank , TOLIA, Gaurav , CHANG, Shulun , SMITH, Alan , PATEL, Yogi , MCRAE, Stuart
IPC分类号： A61B17/20
摘要： Disclosed is a device for causing the transdermal flux of a permeant into a subject via at least one formed pathway through a skin layer of the subject. The device comprises a delivery reservoir comprising: i) a non-biodegradable matrix having a bottom surface and defining a plurality of conduits therein the matrix, at least a portion of the plurality of conduits being in communication with the bottom surface; and ii) an undissolved hydrophilic permeant disposed therein at least a portion of the plurality of conduits of the matrix, wherein the hydrophilic permeant can come in contact with subcutaneous fluid from the subject when the bottom surface of the matrix is positioned in fluid communication with the at least one formed pathway. Also disclosed are systems and methods for causing the transdermal flux of a permeant into a subject via at least one formed pathway through a skin layer of the subject.

7. 发明申请

WO2005084639A3 POLYMERIC DRUG DELIVERY SYSTEM FOR HYDROPHOBIC DRUGS 审中-公开
标题翻译：用于疏水药物的聚合物药物递送系统
公开(公告)号：WO2005084639A3
公开(公告)日：2005-10-20
申请号：PCT/US2005007525
申请日：2005-03-03
申请人： SPHERICS INC , JACOB JULES S , BASSETT MICHAEL , SCHESTOPOL MARCUS A , MATHIOWITZ EDITH , NANGIA AVINASH , CARTER BENNETT , MOSLEMY PEYMAN , SHAKED ZE EV , ENSCORE DAVID , SIKES COURTNEY
发明人： JACOB JULES S , BASSETT MICHAEL , SCHESTOPOL MARCUS A , MATHIOWITZ EDITH , NANGIA AVINASH , CARTER BENNETT , MOSLEMY PEYMAN , SHAKED ZE EV , ENSCORE DAVID , SIKES COURTNEY
IPC分类号： A61K9/00 , A61K9/14 , A61K9/16 , A61K9/20 , A61K9/24 , A61K9/28 , A61K9/48
CPC分类号： A61K9/209 , A61K9/0065 , A61K9/1635 , A61K9/1641 , A61K9/1647 , A61K9/1652 , A61K9/1676 , A61K9/2054 , A61K9/2077 , A61K9/2086 , A61K9/2853
摘要： An oral delivery system for Class II drugs that have low oral bioavailability due to their insolubility in water and slow dissolution kinetics and method for making such a drug delivery system are disclosed herein. The formulation may be a controlled release or immediate release formulation. The immediate release formulation contains a Class II drug, together with a hydrophobic polymer, preferably a bioadhesive polymer. In one embodiment, the drug and polymer are co-dissolved in a common solvent. The solution is formed into small solid particles by any convenient method, particularly by spray drying. The resulting particles contain drug dispersed as small particles in a polymeric matrix. The particles are stable against aggregation, and can be put into capsules or tableted for administration. The controlled release formulations contain a BCS Class II drug and a bioadhesive polymer. The controlled release formulations may be in the form of a tablet, capsules, mini-tab, microparticulate, or osmotic pump. Enhancement of oral uptake of the drug from use of bioadhesive polymers occurs through (1) increased dissolution kinetics due to stable micronization of the drug, (2) rapid release of the drug from the polymer in the GI tract; and (3) prolonged GI transit due to bioadhesive properties of the polymers. The combination of these effects allows the preparation of a compact, stable dosage form suitable for oral administration of many class II drugs.
摘要翻译：本文公开了由于其在水中的不溶性和缓慢的溶解动力学以及制备这种药物递送系统的方法而具有低口服生物利用度的II类药物的口服递送系统。制剂可以是控释或即时释放制剂。立即释放制剂含有II类药物，以及疏水性聚合物，优选生物粘附性聚合物。在一个实施方案中，将药物和聚合物共溶于常用溶剂。通过任何方便的方法，特别是通过喷雾干燥，将溶液形成小的固体颗粒。所得到的颗粒含有作为小颗粒分散在聚合物基质中的药物。颗粒对聚集是稳定的，并且可以放入胶囊或压片以供给药。控释制剂含有BCS II类药物和生物粘附性聚合物。控制释放制剂可以是片剂，胶囊，迷你片，微粒或渗透泵的形式。通过（1）由于药物的稳定的微粉化引起的溶出动力学增加，（2）药物从胃肠道中的聚合物快速释放，增加了使用生物粘附性聚合物对药物的口服摄取。和（3）由于聚合物的生物粘合性质而延长GI运输。这些作用的组合允许制备适于口服多种II类药物的紧凑，稳定的剂型。

8. 发明申请

WO2006138658A2 PERMEANT DELIVERY SYSTEM AND METHODS FOR USE THEREOF 审中-公开
标题翻译：渗透剂输送系统及其使用方法
公开(公告)号：WO2006138658A2
公开(公告)日：2006-12-28
申请号：PCT/US2006023640
申请日：2006-06-19
申请人： ALTEA THERAPEUTICS CORP , EPPSTEIN JONATHAN , ENSCORE DAVID , TAGLIAFERRI FRANK , TOLIA GAURAV , CHANG SHULUN , SMITH ALAN , PATEL YOGI , MCRAE STUART
发明人： EPPSTEIN JONATHAN , ENSCORE DAVID , TAGLIAFERRI FRANK , TOLIA GAURAV , CHANG SHULUN , SMITH ALAN , PATEL YOGI , MCRAE STUART
IPC分类号： A61K9/24
CPC分类号： A61K9/7053 , A61K9/0009
摘要： Disclosed is a device for causing the transdermal flux of a permeant into a subject via at least one formed pathway through a skin layer of the subject. The device comprises a delivery reservoir comprising: i) a non-biodegradable matrix having a bottom surface and defining a plurality of conduits therein the matrix, at least a portion of the plurality of conduits being in communication with the bottom surface; and ii) an undissolved hydrophilic permeant disposed therein at least a portion of the plurality of conduits of the matrix, wherein the hydrophilic permeant can come in contact with subcutaneous fluid from the subject when the bottom surface of the matrix is positioned in fluid communication with the at least one formed pathway. Also disclosed are systems and methods for causing the transdermal flux of a permeant into a subject via at least one formed pathway through a skin layer of the subject.
摘要翻译：公开了一种用于通过穿过受试者的皮肤层的至少一个形成的途径使得渗透物经皮通流入受试者的装置。所述装置包括输送储存器，其包括：i）具有底表面并且在其中限定所述基质中的多个导管的不可生物降解的基质，所述多个导管的至少一部分与所述底表面连通; 和ii）在所述基质的所述多个导管的至少一部分中设置未溶解的亲水性渗透物，其中当所述基质的底表面位于与所述基质的流体连通时，所述亲水性透过物可与来自所述受试者的皮下流体接触至少一个形成的途径。还公开了一种系统和方法，用于通过穿过受试者的皮肤层的至少一个形成的途径使渗透物的经皮通流进入受试者。

9. 发明申请

WO2005084639A9 POLYMERIC DRUG DELIVERY SYSTEM FOR HYDROPHOBIC DRUGS 审中-公开
标题翻译：用于疏水性药物的聚合物药物递送系统
公开(公告)号：WO2005084639A9
公开(公告)日：2005-11-17
申请号：PCT/US2005007525
申请日：2005-03-03
申请人： SPHERICS INC , JACOB JULES S , BASSETT MICHAEL , SCHESTOPOL MARCUS A , MATHIOWITZ EDITH , NANGIA AVINASH , CARTER BENNETT , MOSLEMY PEYMAN , SHAKED ZE EV , ENSCORE DAVID , SIKES COURTNEY
发明人： JACOB JULES S , BASSETT MICHAEL , SCHESTOPOL MARCUS A , MATHIOWITZ EDITH , NANGIA AVINASH , CARTER BENNETT , MOSLEMY PEYMAN , SHAKED ZE EV , ENSCORE DAVID , SIKES COURTNEY
IPC分类号： A61K9/00 , A61K9/14 , A61K9/16 , A61K9/20 , A61K9/24 , A61K9/28 , A61K9/48
CPC分类号： A61K9/209 , A61K9/0065 , A61K9/1635 , A61K9/1641 , A61K9/1647 , A61K9/1652 , A61K9/1676 , A61K9/2054 , A61K9/2077 , A61K9/2086 , A61K9/2853
摘要： An oral delivery system for Class II drugs that have low oral bioavailability due to their insolubility in water and slow dissolution kinetics and method for making such a drug delivery system are disclosed herein. The formulation may be a controlled release or immediate release formulation. The immediate release formulation contains a Class II drug, together with a hydrophobic polymer, preferably a bioadhesive polymer. In one embodiment, the drug and polymer are co-dissolved in a common solvent. The solution is formed into small solid particles by any convenient method, particularly by spray drying. The resulting particles contain drug dispersed as small particles in a polymeric matrix. The particles are stable against aggregation, and can be put into capsules or tableted for administration. The controlled release formulations contain a BCS Class II drug and a bioadhesive polymer. The controlled release formulations may be in the form of a tablet, capsules, mini-tab, microparticulate, or osmotic pump. Enhancement of oral uptake of the drug from use of bioadhesive polymers occurs through (1) increased dissolution kinetics due to stable micronization of the drug, (2) rapid release of the drug from the polymer in the GI tract; and (3) prolonged GI transit due to bioadhesive properties of the polymers. The combination of these effects allows the preparation of a compact, stable dosage form suitable for oral administration of many class II drugs.
摘要翻译：本文公开了由于不溶于水而具有低口服生物利用度和缓慢溶出动力学的II类药物的口服递送系统以及制备这种药物递送系统的方法。该制剂可以是控释或速释制剂。速释制剂含有II类药物以及疏水聚合物，优选生物粘附聚合物。在一个实施方案中，药物和聚合物共溶于普通溶剂中。通过任何方便的方法，特别是通过喷雾干燥，溶液形成小的固体颗粒。所得颗粒含有作为小颗粒分散在聚合物基质中的药物。颗粒对于聚集是稳定的，并且可以放入胶囊或制成片剂给药。控释制剂含有BCS II类药物和生物粘附聚合物。控释制剂可以是片剂，胶囊剂，小片，微粒或渗透泵的形式。（1）由于药物的稳定微粉化，溶解动力学增加，（2）药物从胃肠道中的聚合物中快速释放，因此通过使用生物粘附聚合物增强药物的口服摄取。和（3）由于聚合物的生物粘附性而延长的GI运输。这些效果的组合允许制备适用于许多II类药物口服给药的紧凑稳定剂型。

10. 发明申请

WO2003051304A3 BIOADHESIVE DRUG DELIVERY SYSTEM WITH ENHANCED GASTRIC RETENTION 审中-公开
公开(公告)号：WO2003051304A3
公开(公告)日：2003-06-26
申请号：PCT/US2002/040025
申请日：2002-12-13
申请人： SPHERICS, INC. , JACOB, Jules , MATHIOWITZ, Edith , ENSCORE, David , SCHESTOPOL, Marcus
发明人： JACOB, Jules , MATHIOWITZ, Edith , ENSCORE, David , SCHESTOPOL, Marcus
IPC分类号： A61K9/48
摘要： Bioadhesive macrosphere delivery systems ("BDDS") having prolonged gastric retention time due to bioadhesion rather than physical density or size are described. In general, the macrospheres have diameters that are greater than 200 microns, more preferably greater than 500 microns. The bioadhesive macrospheres are released in the stomach where they reside in close proximity to the gastric mucosa for a prolonged period of time. Increased residence of BDDS in the upper GI can lead to increased systemic absorption of drug in the preferred site of systemic absorption, namely the upper GI tract (upper to mid-jejunum). The BDDS may be engineered either as a capsule with drug delivery controlled by a diffusion-limited membrane or degradable shell, or as a solid matrix system with drug delivery controlled by a combination of diffusion and polymer degradation kinetics.

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