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1.发明申请Matrices Formed of Polymer and Hydrophobic Compounds For Use in Drug Delivery 审中-公开用于药物输送的聚合物和疏水性化合物形成的基质公开(公告)号：US20070104656A1
公开(公告)日：2007-05-10
申请号：US11617935
申请日：2006-12-29
IPC分类号： A61K9/14
CPC分类号： A61K9/1617 , A61K9/1647 , Y10S514/951 , Y10S514/952
摘要： A lipid or other hydrophobic or amphiphilic compound (collectively referred to herein as “hydrophobic compounds”) is integrated into a polymeric matrix for drug delivery to alter drug release kinetics. In embodiments where the drug is water soluble, the drug is released over longer periods of time as compared to release from the polymeric matrix not incorporating the hydrophobic compound into the polymeric material. In contrast to methods in which a surfactant or lipid is added as an excipient, the hydrophobic compound is actually integrated into the polymeric matrix, thereby modifying the diffusion of water into the microparticle and diffusion of solubilized drug out of the matrix. The integrated hydrophobic compound also prolongs degradation of hydrolytically unstable polymers forming the matrix, further delaying release of encapsulated drug.
摘要翻译： 将脂质或其它疏水性或两亲性化合物（本文统称为“疏水化合物”）整合到用于药物递送的聚合物基质中以改变药物释放动力学。 在药物是水溶性的实施方案中，与不将疏水化合物掺入聚合物材料的聚合物基质的释放相比，药物在更长的时间内释放。 与其中加入表面活性剂或脂质作为赋形剂的方法相反，疏水化合物实际上整合到聚合物基质中，从而改变水进入微粒的扩散并将溶解的药物扩散出基质。 整合的疏水化合物还延长了形成基质的水解不稳定聚合物的降解，进一步延缓了包封药物的释放。
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公开(公告)号：US07052719B2
公开(公告)日：2006-05-30
申请号：US09731412
申请日：2000-12-06
CPC分类号： A61K9/1617 , A61K9/1647 , Y10S514/951 , Y10S514/952
摘要： A lipid or other hydrophobic or amphiphilic compound (collectively referred to herein as “hydrophobic compounds”) is integrated into a polymeric matrix for drug delivery to alter drug release kinetics. In embodiments where the drug is water soluble, the drug is released over longer periods of time as compared to release from the polymeric matrix not incorporating the hydrophobic compound into the polymeric material. In contrast to methods in which a surfactant or lipid is added as an excipient, the hydrophobic compound is actually integrated into the polymeric matrix, thereby modifying the diffusion of water into the microparticle and diffusion of solubilized drug out of the matrix. The integrated hydrophobic compound also prolongs degradation of hydrolytically unstable polymers forming the matrix, further delaying release of encapsulated drug.
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公开(公告)号：US20050058710A1
公开(公告)日：2005-03-17
申请号：US10928886
申请日：2004-08-27
申请人： Julie Straub , David Altreuter , Howard Bernstein , Donald Chickering , Sarwat Khattak , Greg Randall
发明人： Julie Straub , David Altreuter , Howard Bernstein , Donald Chickering , Sarwat Khattak , Greg Randall
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。
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公开(公告)号：US20050048116A1
公开(公告)日：2005-03-03
申请号：US10924642
申请日：2004-08-24
申请人： Julie Straub , David Altreuter , Howard Bernstein , Donald Chickering , Sarwat Khattak , Greg Randall
发明人： Julie Straub , David Altreuter , Howard Bernstein , Donald Chickering , Sarwat Khattak , Greg Randall
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。
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公开(公告)号：US06689390B2
公开(公告)日：2004-02-10
申请号：US10383264
申请日：2003-03-05
IPC分类号： A61K950
CPC分类号： A61K9/1617 , A61K9/1647 , Y10S514/951 , Y10S514/952
摘要： A lipid or other hydrophobic or amphiphilic compound (collectively referred to herein as “hydrophobic compounds”) is integrated into a polymeric matrix for drug delivery to alter drug release kinetics. In embodiments where the drug is water soluble, the drug is released over longer periods of time as compared to release from the polymeric matrix not incorporating the hydrophobic compound into the polymeric material. In contrast to methods in which a surfactant or lipid is added as an excipient, the hydrophobic compound is actually integrated into the polymeric matrix, thereby modifying the diffusion of water into the microparticle and diffusion of solubilized drug out of the matrix. The integrated hydrophobic compound also prolongs degradation of hydrolytically unstable polymers forming the matrix, further delaying release of encapsulated drug.
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6.发明授权Matrices formed of polymer and hydrophobic compounds for use in drug delivery 有权由聚合物和疏水化合物形成的矩阵用于药物递送公开(公告)号：US07160557B2
公开(公告)日：2007-01-09
申请号：US09730694
申请日：2000-12-06
CPC分类号： A61K9/1617 , A61K9/1647 , Y10S514/951 , Y10S514/952
摘要： A lipid or other hydrophobic or amphiphilic compound (collectively referred to herein as “hydrophobic compounds”) is integrated into a polymeric matrix for drug delivery to alter drug release kinetics. In embodiments where the drug is water soluble, the drug is released over longer periods of time as compared to release from the polymeric matrix not incorporating the hydrophobic compound into the polymeric material. In contrast to methods in which a surfactant or lipid is added as an excipient, the hydrophobic compound is actually integrated into the polymeric matrix, thereby modifying the diffusion of water into the microparticle and diffusion of solubilized drug out of the matrix. The integrated hydrophobic compound also prolongs degradation of hydrolytically unstable polymers forming the matrix, further delaying release of encapsulated drug.
摘要翻译： 将脂质或其它疏水性或两亲性化合物（本文统称为“疏水性化合物”）整合到用于药物递送的聚合物基质中以改变药物释放动力学。 在药物是水溶性的实施方案中，与不将疏水化合物掺入聚合物材料的聚合物基质的释放相比，药物在更长的时间内释放。 与其中加入表面活性剂或脂质作为赋形剂的方法相反，疏水化合物实际上整合到聚合物基质中，从而改变水进入微粒的扩散并将溶解的药物扩散出基质。 整合的疏水化合物还延长了形成基质的水解不稳定聚合物的降解，进一步延缓了包封药物的释放。
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7.发明授权Matrices formed of polymer and hydrophobic compounds for use in drug delivery 失效由聚合物和疏水化合物形成的矩阵用于药物递送公开(公告)号：US06730322B1
公开(公告)日：2004-05-04
申请号：US10384902
申请日：2003-03-06
IPC分类号： A61K910
CPC分类号： A61K9/1647 , A61K9/1617
摘要： A lipid or other hydrophobic or amphiphilic compound (collectively referred to herein as “hydrophobic compounds”) is integrated into a polymeric matrix for drug delivery to alter drug release kinetics. In embodiments where the drug is water soluble, the drug is released over longer periods of time as compared to release from the polymeric matrix not incorporating the hydrophobic compound into the polymeric material. In contrast to methods in which a surfactant or lipid is added as an excipient, the hydrophobic compound is actually integrated into the polymeric matrix, thereby modifying the diffusion of water into the microparticle and diffusion of solubilized drug out of the matrix. The integrated hydrophobic compound also prolongs degradation of hydrolytically unstable polymers forming the matrix, further delaying release of encapsulated drug.
摘要翻译： 将脂质或其它疏水性或两亲性化合物（本文统称为“疏水化合物”）整合到用于药物递送的聚合物基质中以改变药物释放动力学。 在药物是水溶性的实施方案中，与不将疏水化合物掺入聚合物材料的聚合物基质的释放相比，药物在更长的时间内释放。 与其中加入表面活性剂或脂质作为赋形剂的方法相反，疏水化合物实际上整合到聚合物基质中，从而改变水进入微粒的扩散并将溶解的药物扩散出基质。 整合的疏水化合物还延长了形成基质的水解不稳定聚合物的降解，进一步延缓了包封药物的释放。
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公开(公告)号：US06423345B1
公开(公告)日：2002-07-23
申请号：US09255179
申请日：1999-02-22
IPC分类号： A61K910
摘要： A lipid or other hydrophobic or amphiphilic compound (collectively referred to herein as “hydrophobic compounds”) is integrated into a polymeric matrix for drug delivery to alter drug release kinetics. In embodiments where the drug is water soluble, the drug is released over longer periods of time as compared to release from the polymeric matrix not incorporating the hydrophobic compound into the polymeric material. In contrast to methods in which a surfactant or lipid is added as an excipient, the hydrophobic compound is actually integrated into the polymeric matrix, thereby modifying the diffusion of water into the microparticle and diffusion of solubilized drug out of the matrix. The integrated hydrophobic compound also prolongs degradation of hydrolytically unstable polymers forming the matrix, further delaying release of encapsulated drug.
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9.发明申请PROCESSES FOR MAKING PARTICLE-BASED PHARMACEUTICAL FORMULATIONS FOR ORAL ADMINISTRATION 审中-公开制造基于粒子的药物制剂进行口腔管理的方法公开(公告)号：US20070148211A1
公开(公告)日：2007-06-28
申请号：US11610802
申请日：2006-12-14
申请人： David Altreuter , Howard Bernstein , Luis Brito , Shaina Brito , Donald Chickering , Eric Huang , Rajeev Jain , Sridhar Narasimhan , Julie Straub
发明人： David Altreuter , Howard Bernstein , Luis Brito , Shaina Brito , Donald Chickering , Eric Huang , Rajeev Jain , Sridhar Narasimhan , Julie Straub
CPC分类号： A61K9/145 , A61K9/0056 , A61K9/0095 , A61K9/2072 , A61K9/2077 , A61K9/2095
摘要： A method is provided for making an oral dosage form of a pharmaceutical agent which includes the steps of (a) providing particles which include a pharmaceutical agent; (b) blending the particles with particles of a pre-processed excipient to form a primary blend, wherein the pre-processed excipient is prepared by (i) dissolving a bulking agent (e.g., a sugar) and at least one non-friable excipient (e.g., a waxy or liquid surfactant) in a solvent to form an excipient solution, and (ii) removing the solvent from the excipient solution to form the pre-processed excipient in dry powder form; (c) milling the primary blend to form a milled pharmaceutical formulation blend that includes microparticles or nanoparticles of the pharmaceutical agent; and (d) processing the milled pharmaceutical formulation blend into a solid oral dosage form or liquid suspension for oral administration. The process yields formulations having improved wettability or dispersibility.
摘要翻译： 提供了制备药剂口服剂型的方法，其包括以下步骤：（a）提供包含药剂的颗粒; （b）将颗粒与预处理的赋形剂的颗粒混合以形成初级共混物，其中预处理的赋形剂通过以下步骤制备：（i）将填充剂（例如糖）和至少一种不易碎的赋形剂 （例如，蜡状或液体表面活性剂）在溶剂中形成赋形剂溶液，和（ii）从赋形剂溶液中除去溶剂以形成干粉末形式的预处理赋形剂; （c）研磨初级共混物以形成包含药剂的微粒或纳米颗粒的研磨的药物配制物混合物; 和（d）将经研磨的药物制剂混合物加工成固体口服剂型或用于口服给药的液体悬浮液。 该方法产生具有改善的润湿性或分散性的制剂。
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公开(公告)号：US20050271591A1
公开(公告)日：2005-12-08
申请号：US11143170
申请日：2005-06-02
CPC分类号： A61K49/223
摘要： Clinical studies have been conducted and specific dosage formulations developed using polymeric microparticles having incorporated therein perfluorocarbon gases that provide significantly enhanced images of long duration. The dosage formulation includes microparticles formed of a biocompatible polymer, preferably including a lipid incorporated therein, and containing a perfluorocarbon that is a gas at body temperature. The microparticles are provided to a patient in an amount effective to enhance ultrasound imaging in the ventricular chambers for more than 5 minutes or in the mycocardium for more than a minute, in a dose ranging from 0.025 to 8.0 mg microparticles/kg body weight. Preferably the dose ranges from 0.05 to 4.0 mg microparticles/kg body weight. The dosage formulation typically is provided in a vial. A typical formulation is in the form of a dry powder that is reconstituted with sterile water prior to use by adding the water to the vial or syringe of the dry powder and shaking to yield an isosmotic or isotonic suspension of microparticles.
摘要翻译： 已经进行了临床研究，并且使用其中结合有全氟化碳气体的聚合物微粒开发特定的剂型，其提供了长时间显着增强的图像。 剂量制剂包括由生物相容性聚合物形成的微粒，其优选包括掺入其中的脂质，并且含有在体温下作为气体的全氟化碳。 将微粒以有效量的方式提供给患者，剂量范围为0.025至8.0mg微粒/ kg体重的剂量，以有效增强心室中的超声成像超过5分钟或在心肌中超过一分钟。 剂量优选为0.05至4.0mg微粒/ kg体重。 剂型通常提供在小瓶中。 典型的制剂是干粉的形式，其在使用前通过将水添加到干粉末的小瓶或注射器中并且摇动以产生微粒的等渗或等渗悬浮液而在使用前用无菌水重构。
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