公开(公告)号：WO2006031420A3

公开(公告)日：2006-03-23

申请号：PCT/US2005/030651

申请日：2005-08-29

Applicant: SPHERICS, INC. ,  NANGIA, Avinash ,  JACOB, Jules ,  MATHIOWITZ, Edith ,  RICKETTS, Thomas, L. ,  KREITZ, Mark, R.

Inventor： NANGIA, Avinash ,  JACOB, Jules ,  MATHIOWITZ, Edith ,  RICKETTS, Thomas, L. ,  KREITZ, Mark, R.

IPC: A61K9/28

Abstract: Bioadhesives coatings increase the gastrointestinal retention time of orally-ingested medicaments. Certain bioadhesive coatings producing a fracture strength of at least 100 N/m 2 , as measured on rat intestine, when applied to at least one surface of a pharmaceutical dosage form for oral delivery of a drug, result in a gastrointestinal retention time of at least 4 hours in a fed beagle dog model, during which the drug is released from the dosage form. Multi-layer tablets, particularly those including hydrophobic excipients, are useful in administering hygroscopic and/or deliquescent drugs. In addition, varying the amount of drug in multi-layer tablets allows the release rate of the drug to be controlled.

公开(公告)号：WO2006031420A2

公开(公告)日：2006-03-23

申请号：PCT/US2005030651

申请日：2005-08-29

Applicant: SPHERICS INC ,  NANGIA AVINASH ,  JACOB JULES ,  MATHIOWITZ EDITH ,  RICKETTS THOMAS L ,  KREITZ MARK R

Inventor： NANGIA AVINASH ,  JACOB JULES ,  MATHIOWITZ EDITH ,  RICKETTS THOMAS L ,  KREITZ MARK R

IPC: A61K9/28

CPC classification number: A61K9/209 ,  A61K9/2027 ,  A61K9/2031 ,  A61K9/2054 ,  A61K9/2086

Abstract: Bioadhesives coatings increase the gastrointestinal retention time of orally-ingested medicaments. Certain bioadhesive coatings producing a fracture strength of at least 100 N/m 2 , as measured on rat intestine, when applied to at least one surface of a pharmaceutical dosage form for oral delivery of a drug, result in a gastrointestinal retention time of at least 4 hours in a fed beagle dog model, during which the drug is released from the dosage form. Multi-layer tablets, particularly those including hydrophobic excipients, are useful in administering hygroscopic and/or deliquescent drugs. In addition, varying the amount of drug in multi-layer tablets allows the release rate of the drug to be controlled.

Abstract translation: 生物粘附剂涂层增加口服药物的胃肠道停留时间。 当在大鼠肠道上测量时，产生至少100N / m 2的断裂强度的某些生物粘附涂层在应用于用于口服递送药物的药物剂型的至少一个表面时导致 在喂养比格犬模型中至少4小时的胃肠道停留时间，在此期间药物从剂型释放。 多层片剂，特别是那些包括疏水性赋形剂的片剂可用于施用吸湿性和/或潮解性药物。 另外，改变多层片剂中药物的量可以控制药物的释放速率。

公开(公告)号：WO2005056708A2

公开(公告)日：2005-06-23

申请号：PCT/US2004/041783

申请日：2004-12-09

Applicant: SPHERICS, INC. ,  SCHESTOPOL, Marcus, A. ,  JACOB, Jules, S. ,  DONNELY, Ryan ,  RICKETTS, Thomas, L. ,  NANGIA, Avinash ,  MATHIOWITZ, Edith ,  SHAKED, Ze'ev

Inventor： SCHESTOPOL, Marcus, A. ,  JACOB, Jules, S. ,  DONNELY, Ryan ,  RICKETTS, Thomas, L. ,  NANGIA, Avinash ,  MATHIOWITZ, Edith ,  SHAKED, Ze'ev

IPC: C09J129/00

CPC classification number: 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

Abstract: 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 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.

Abstract translation: 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，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。

公开(公告)号：WO2005056708A3

公开(公告)日：2005-07-28

申请号：PCT/US2004041783

申请日：2004-12-09

Applicant: SPHERICS INC ,  SCHESTOPOL MARCUS A ,  JACOB JULES S ,  DONNELY RYAN ,  RICKETTS THOMAS L ,  NANGIA AVINASH ,  MATHIOWITZ EDITH ,  SHAKED ZE EV

Inventor： SCHESTOPOL MARCUS A ,  JACOB JULES S ,  DONNELY RYAN ,  RICKETTS THOMAS L ,  NANGIA AVINASH ,  MATHIOWITZ EDITH ,  SHAKED ZE EV

IPC: A61K9/00 ,  A61K9/20 ,  A61K31/74 ,  C08F8/32 ,  C08G63/91 ,  C09J135/00 ,  C09J167/00 ,  C09J167/04 ,  C09J201/06 ,  C08F222/06 ,  C08G67/04

CPC classification number: 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

Abstract: 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 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.

Abstract translation: 已经开发出具有改善的生物粘附性质的聚合物和用于改善聚合物的生物粘附性的方法。 含有含一个或多个羟基的芳族基团的化合物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。 在一些实施例中，聚合物是疏水性聚合物。 在优选的实施方案中，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，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。 这些材料的生物粘附性能优于用于治疗和诊断应用的常规生物粘附剂。 这些生物粘附材料可用于制造在组织表面处具有增加的停留时间的新型药物递送或诊断系统，并因此增加药物或诊断剂的生物利用度。 在一个优选的实施方案中，生物粘附材料是控释口服剂型中的包衣和/或在口服剂型中形成基质。