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1. 发明申请

US20050249799A1 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：US20050249799A1
公开(公告)日：2005-11-10
申请号：US11072098
申请日：2005-03-03
申请人： Jules Jacob , Michael Bassett , Marcus Schestopol , Edith Mathlowitz , Avinash Nangia , Bennett Carter , Peyman Moslemy , Ze'ev Shaked , David Enscore , Courtney Sikes
发明人： Jules Jacob , Michael Bassett , Marcus Schestopol , Edith Mathlowitz , Avinash Nangia , Bennett Carter , Peyman Moslemy , Ze'ev Shaked , David Enscore , Courtney Sikes
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。

2. 发明申请

US20050201974A1 Bioadhesive polymers with catechol functionality 审中-公开
标题翻译：具有儿茶酚功能的生物粘合剂聚合物
公开(公告)号：US20050201974A1
公开(公告)日：2005-09-15
申请号：US11009327
申请日：2004-12-09
申请人： Marcus Schestopol , Jules Jacob , Ryan Donnelly , Thomas Ricketts , Avinash Nangia , Edith Mathiowitz , Ze'ev Shaked
发明人： Marcus Schestopol , Jules Jacob , Ryan Donnelly , Thomas Ricketts , Avinash Nangia , Edith Mathiowitz , Ze'ev Shaked
IPC分类号： A61K9/00 , A61K9/20 , A61K31/74 , C08F8/32 , C08G63/91 , C09J135/00 , C09J167/00 , C09J167/04 , C09J201/06
CPC分类号： C08F8/32 , A61K9/0004 , A61K9/006 , A61K9/0065 , A61K9/204 , A61K9/2077 , A61K9/2081 , A61K9/2086 , C08G63/91 , C08G63/912 , C09J167/00 , C09J167/04 , C08F222/06
摘要： Polymers with improved bioadhesive properties and methods for improving bioadhesion of polymers have been developed. A compound containing an aromatic group which contains one or more hydroxyl groups is grafted onto a polymer or coupled to individual monomers. In one embodiment, the polymer is a biodegradable polymer. In another embodiment, the monomers may be polymerized to form any type of polymer, including biodegradable and non-biodegradable polymers. In some embodiments, the polymer is a hydrophobic polymer. In the preferred embodiment, the aromatic compound is catechol or a derivative thereof and the polymer contains reactive functional groups. In the most preferred embodiment, the polymer is a polyanhydride and the aromatic compound is the catechol derivative, DOPA. These materials display bioadhesive properties superior to conventional bioadhesives used in therapeutic and diagnostic applications. These bioadhesive materials can be used to fabricate new drug delivery or diagnostic systems with increased residence time at tissue surfaces, and consequently increase the bioavailability of a drug or a diagnostic agent. In a preferred embodiment, the bioadhesive material is a coating on a controlled release oral dosage formulation and/or forms a matrix in an oral dosage formulation.
摘要翻译：已经开发了具有改进的生物粘附性质的聚合物和改善聚合物生物粘附的方法。含有含有一个或多个羟基的芳族基团的化合物被接枝到聚合物上或与单独的单体偶联。在一个实施方案中，聚合物是可生物降解的聚合物。在另一个实施方案中，单体可以聚合以形成任何类型的聚合物，包括可生物降解和不可生物降解的聚合物。在一些实施方案中，聚合物是疏水性聚合物。在优选的实施方案中，芳族化合物是儿茶酚或其衍生物，并且聚合物含有反应性官能团。在最优选的实施方案中，聚合物是聚酐，芳族化合物是邻苯二酚衍生物DOPA。这些材料显示出比用于治疗和诊断应用的常规生物粘合剂优越的生物粘附性。这些生物粘附材料可用于制造具有增加的组织表面停留时间的新药物递送或诊断系统，并因此提高药物或诊断剂的生物利用度。在优选的实施方案中，生物粘附材料是在控释口服剂量制剂上的涂层和/或在口服剂量制剂中形成基质。

3. 发明申请

US20050064027A1 Bioadhesive drug delivery system with enhanced gastric retention 审中-公开
标题翻译：生物粘附药物递送系统具有增强的胃滞留
公开(公告)号：US20050064027A1
公开(公告)日：2005-03-24
申请号：US10498661
申请日：2002-12-13
申请人： Jules Jacob , Edith Mathiowitz , David Enscore , Marcus Schestopol
发明人： Jules Jacob , Edith Mathiowitz , David Enscore , Marcus Schestopol
IPC分类号： A61K9/30 , A61K9/00 , A61K9/16 , A61K9/20 , A61K9/48 , A61K9/50 , A61K9/52 , A61K31/522 , A61K45/00 , A61K47/04 , A61K47/36 , A61K47/42 , A61P31/12 , A61P31/20 , A61P33/00 , A61P35/00
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可以被设计为具有由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

US20070154547A1 Gastric release pulse system for drug delivery 有权
标题翻译：用于药物输送的胃释放脉冲系统
公开(公告)号：US20070154547A1
公开(公告)日：2007-07-05
申请号：US11644707
申请日：2006-12-22
申请人： Henry H. Flanner , Donald Treacy , Sanna Tolle-Sander , Scott Ibrahim , Marcus Schestopol , Beth A. Burnside
发明人： Henry H. Flanner , Donald Treacy , Sanna Tolle-Sander , Scott Ibrahim , Marcus Schestopol , Beth A. Burnside
IPC分类号： A61K9/22
CPC分类号： A61K9/0004 , A61K9/0065 , A61K9/1623 , A61K9/1635 , A61K9/1652 , A61K9/2027 , A61K9/2054 , A61K9/2077 , A61K9/2081 , A61K9/2086 , A61K9/209 , A61K9/501 , A61K9/5015 , A61K9/5026 , A61K9/5042 , A61K9/5073 , A61K9/5084
摘要： Disclosed are pharmaceutical products for providing pulses of at least one pharmaceutically active ingredient from a patient's stomach, or from a subsequent gastrointestinal site proximal thereto, for absorption thereof at a site(s) more distal in the gastrointestinal tract than the patient's stomach, or than the subsequent gastrointestinal site proximal thereto. The product comprises first, second, and third pharmaceutical dosage forms, each of which comprises at least one pharmaceutically active agent and a pharmaceutically acceptable carrier. The product is formulated such that at least two of the first, second, and third pharmaceutical dosage forms further comprise means for providing temporary gastric-retention of the at least two of the first, second, and third pharmaceutical dosage forms within the patient's stomach, or at the subsequent gastrointestinal site proximal thereto.
摘要翻译：公开了用于从患者的胃或其后接近的胃肠部位提供至少一种药物活性成分的脉冲的药物产品，用于在胃肠道比患者的胃更远的部位吸收它们，或比随后的胃肠部位近端。该产品包含第一，第二和第三药物剂型，其各自包含至少一种药物活性剂和药学上可接受的载体。该产品被配制成使得第一，第二和第三药物剂型中的至少两个进一步包括用于在患者的胃内提供至少两种第一，第二和第三药物剂型的临时胃滞留的装置，或在其后的胃肠部位。

5. 发明授权

US09125803B2 Gastric release pulse system for drug delivery 有权
标题翻译：用于药物输送的胃释放脉冲系统
公开(公告)号：US09125803B2
公开(公告)日：2015-09-08
申请号：US11644707
申请日：2006-12-22
申请人： Henry H. Flanner , Donald Treacy , Sanna Tolle-Sander , Scott Ibrahim , Marcus Schestopol , Beth A. Burnside
发明人： Henry H. Flanner , Donald Treacy , Sanna Tolle-Sander , Scott Ibrahim , Marcus Schestopol , Beth A. Burnside
IPC分类号： A61K9/22 , A61K9/00 , A61K9/16 , A61K9/20 , A61K9/24 , A61K9/50
CPC分类号： A61K9/0004 , A61K9/0065 , A61K9/1623 , A61K9/1635 , A61K9/1652 , A61K9/2027 , A61K9/2054 , A61K9/2077 , A61K9/2081 , A61K9/2086 , A61K9/209 , A61K9/501 , A61K9/5015 , A61K9/5026 , A61K9/5042 , A61K9/5073 , A61K9/5084
摘要： Disclosed are pharmaceutical products for providing pulses of at least one pharmaceutically active ingredient from a patient's stomach, or from a subsequent gastrointestinal site proximal thereto, for absorption thereof at a site(s) more distal in the gastrointestinal tract than the patient's stomach, or than the subsequent gastrointestinal site proximal thereto. The product comprises first, second, and third pharmaceutical dosage forms, each of which comprises at least one pharmaceutically active agent and a pharmaceutically acceptable carrier. The product is formulated such that at least two of the first, second, and third pharmaceutical dosage forms further comprise means for providing temporary gastric-retention of the at least two of the first, second, and third pharmaceutical dosage forms within the patient's stomach, or at the subsequent gastrointestinal site proximal thereto.
摘要翻译：公开了用于从患者的胃或其后接近的胃肠部位提供至少一种药物活性成分的脉冲的药物产品，用于在胃肠道比患者的胃更远的部位吸收它们，或比随后的胃肠部位近端。该产品包含第一，第二和第三药物剂型，其各自包含至少一种药物活性剂和药学上可接受的载体。该产品被配制成使得第一，第二和第三药物剂型中的至少两个进一步包括用于在患者的胃内提供至少两种第一，第二和第三药物剂型的临时胃滞留的装置，或在其后的胃肠部位。

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