公开(公告)号：US20080193543A1

公开(公告)日：2008-08-14

申请号：US11914394

申请日：2006-05-17

Applicant: Arthur Peter Morello, III ,  Joshua Reineke ,  Peter Matthew Cheifetz ,  Bryan Laulicht ,  Edith Mathiowitz

Inventor： Arthur Peter Morello, III ,  Joshua Reineke ,  Peter Matthew Cheifetz ,  Bryan Laulicht ,  Edith Mathiowitz

IPC: A61K9/16 ,  A61N2/00

CPC classification number: A61K9/0004 ,  A61K9/0009

Abstract: The size and location of microsphere uptake/delivery are important determinants of the final biodistribution of oral microsphere systems. Formulations, kits, methods of administering the formulations, and using the kits are described herein. The formulations are oral dosage formulations. In one embodiment, the formulations contain microparticles and/or nanoparticles having a homogenous size range selected to optimize uptake in a specific region of the GI tract and target drug delivery to specific organs. In some embodiments, the dosage formulation contains an enteric coating and/or a magnetic material. In a preferred embodiment, the formulation contains a magnetic material and an active agent to be delivered, optionally the active agent is in the form of micro- or nano-particles. In some embodiments metallomucoadhesive materials and/or magnetic materials are employed as magnetic and/or mucoadhesive sources. Formulations containing magnetic materials can be localized using the kits and methods disclosed herein. In one embodiment, the method includes orally administering the formulation and applying an extracorporeal magnet to a site on the outside surface of the patient's body in an area that closely apposes the location in the gastrointestinal tract to which delivery of the formulation is desired. The extracorporeal magnet is applied for a suitable time period to allow for the drug to be released from the formulation and/or to allow for the formulation to adhere to the site. Both magnetic and mucoadhesive forces may be utilized to site-direct and retain the dosage form in the region of the gastrointestinal (GI) tract most suitable for the desired delivery.

Abstract translation: 微球吸收/释放的大小和位置是口腔微球系统最终生物分布的重要决定因素。 本文描述了制剂，试剂盒，施用制剂的方法和使用试剂盒。 制剂是口服剂型。 在一个实施方案中，制剂含有选择的均匀尺寸范围的微粒和/或纳米颗粒，以优化GI道的特定区域中的摄取并将靶向药物递送至特定器官。 在一些实施方案中，剂量制剂含有肠溶衣和/或磁性材料。 在优选的实施方案中，制剂含有磁性材料和待递送的活性剂，任选的活性剂是微粒或纳米颗粒的形式。 在一些实施方案中，金属粘着粘附材料和/或磁性材料用作磁性和/或粘膜粘附源。 可以使用本文公开的试剂盒和方法将含有磁性材料的制剂定位。 在一个实施方案中，该方法包括口服施用该制剂并将一个体外磁体施加到患者身体的外表面上的一个位置，该区域紧密地形成需要递送制剂的胃肠道中的位置。 将体外磁体施加合适的时间段以允许药物从制剂中释放和/或允许制剂粘附到部位。 可以利用磁性和粘膜粘附力来定位直接并将剂型保留在最适合于所需递送的胃肠道（GI）区域中。