公开(公告)号：WO02055059A3

公开(公告)日：2002-09-06

申请号：PCT/US0149737

申请日：2001-12-20

Applicant: BAXTER INT

Inventor： KIPP JAMES E ,  WONG JOSEPH CHUNG TAK ,  DOTY MARK J ,  REBBECK CHRISTINE L ,  BRYNJELSEN SEAN ,  WERLING JANE ,  SRIRAM RAJARAM

IPC: C07D407/14 ,  A61K9/10 ,  A61K9/14 ,  A61K9/16 ,  A61K31/495 ,  A61K31/496 ,  A61K47/12 ,  A61K47/14 ,  A61K47/18 ,  A61K47/20 ,  A61K47/24 ,  A61K47/28 ,  A61K47/34 ,  A61K47/36 ,  A61K47/38 ,  A61K47/42 ,  A61P31/10 ,  A61K9/20 ,  A61K9/51

CPC classification number: A61K31/495 ,  A61K9/10 ,  A61K9/14 ,  A61K9/145 ,  A61K9/146 ,  A61K9/1688 ,  A61K31/496

Abstract: The present invention provides a method for preparing a suspension of a pharmaceutically-active compound, the solubility of which is greater in a water-miscible first organic solvent than in a second solvent which is aqueous. The process includes the steps of : (i) dissolving a first quantity of the pharmaceutically-active compound in the water-miscible first organic solvent to form a first solution ; (ii) mixing the first solution with the second solvent to precipitate the pharmaceutically-active compound ; and (iii) seeding the first solution or the second solvent or the presuspension.

Abstract translation: 本发明提供了制备药物活性化合物的悬浮液的方法，所述药物活性化合物在水混溶性第一有机溶剂中的溶解度大于含水第二溶剂中的溶解度。 该方法包括以下步骤：（i）将第一数量的药学活性化合物溶解在可与水混溶的第一有机溶剂中以形成第一溶液; （ii）将第一溶液与第二溶剂混合以沉淀药物活性化合物; 和（iii）接种第一溶液或第二溶剂或预悬浮液。

公开(公告)号：WO2007059515A3

公开(公告)日：2007-11-01

申请号：PCT/US2006060939

申请日：2006-11-15

Applicant: BAXTER INT ,  BAXTER HEALTHCARE SA ,  KIPP JAMES E ,  WERLING JANE ,  GUPTA PRAMOD ,  BURESH RITA

Inventor： KIPP JAMES E ,  WERLING JANE ,  GUPTA PRAMOD ,  BURESH RITA

IPC: A61K9/14 ,  A61K9/10 ,  A61K9/19 ,  A61K31/38 ,  A61P1/00 ,  A61P9/10 ,  A61P11/06 ,  A61P17/06 ,  A61P17/10 ,  A61P29/00 ,  A61P35/00 ,  A61P37/08

CPC classification number: A61K9/10 ,  A61K9/0043 ,  A61K9/0048 ,  A61K9/19 ,  A61K9/5146 ,  A61K31/38 ,  A61K31/381

Abstract: Pharmaceutical compositions comprising particles of lipoxygenase inhibitor compounds having an effective average size of from about 10 nm to about 50 microns are provided. More particularly, pharmaceutical compositions of particle of a 5 -lipoxygenase inhibitor compound having an effective average size of from about 50 nm to about 5 microns are provided. The pharmaceutical compositions are in the form of aqueous suspensions with the particle of the 5-lipoxygenase-inhibitor compound present in concentrations of from about 5 to about 200 mg/ml. In addition, methods for making such pharmaceutical compositions are provided. In particular, microprecipitation and direct homogenization in the presence of at least one surfactant are disclosed for making the pharmaceutical compositions.

Abstract translation: 提供了包含有效平均尺寸为约10nm至约50微米的脂氧合酶抑制剂化合物颗粒的药物组合物。 更特别地，提供了具有约50nm至约5微米的有效平均尺寸的5-脂氧合酶抑制剂化合物颗粒的药物组合物。 药物组合物呈含水悬浮液的形式，其中5-脂氧合酶抑制剂化合物颗粒以约5至约200mg / ml的浓度存在。 另外，提供了制备这种药物组合物的方法。 具体而言，公开了用于制备药物组合物的微量沉淀和在至少一种表面活性剂存在下的直接均质化。

公开(公告)号：WO2005072706A3

公开(公告)日：2005-11-24

申请号：PCT/US2005001861

申请日：2005-01-21

Applicant: BAXTER INT ,  BAXTER HEALTHCARE SA ,  WERLING JANE ,  CHAUBAL MAHESH V ,  KIPP JAMES E ,  RABINOW BARRETT E

Inventor： WERLING JANE ,  CHAUBAL MAHESH V ,  KIPP JAMES E ,  RABINOW BARRETT E

IPC: A61K9/10 ,  A61K9/14 ,  A61K9/51 ,  A61K31/00 ,  A61K31/551 ,  A61K31/7072 ,  A61K31/7076

CPC classification number: A61K9/10 ,  A61K9/5123 ,  A61K31/00 ,  A61K31/551 ,  A61K31/7072 ,  A61K31/7076

Abstract: The present invention provides compositions comprising dispersions of anti-retroviral agents and methods of manufacture. The nanosuspensions are made by the process of microprecipitation and energy addition. Preferably, the nanosuspensions are made by the tandem process of microprecipitation-homogenization.

Abstract translation: 本发明提供了包含抗逆转录病毒剂分散体和制造方法的组合物。 纳米悬浮液是通过微量沉淀和能量添加过程制成的。 优选地，纳米悬浮液通过微量沉淀 - 均质化的串联过程制成。

公开(公告)号：WO2004103348A3

公开(公告)日：2005-01-06

申请号：PCT/US2004015621

申请日：2004-05-19

Applicant: BAXTER INT ,  BARRETT RABINOW E ,  WERLING JANE ,  KONKEL JAMIE TERESA ,  DOTY MARK J ,  REBBECK CHRISTINE L

Inventor： BARRETT RABINOW E ,  WERLING JANE ,  KONKEL JAMIE TERESA ,  DOTY MARK J ,  REBBECK CHRISTINE L

IPC: A61K9/107 ,  A61K9/14 ,  A61K31/00 ,  A61K31/55 ,  A61K38/13 ,  A61K9/16

CPC classification number: A61K31/00 ,  A61K9/1075 ,  A61K9/145 ,  A61K9/146 ,  A61K31/55 ,  A61K38/13

Abstract: This invention pertains to the formulation of small-particle suspensions of anticonvulsants, particularly carbamazepine, for pharmaceutical use. This invention also pertains to the formulation of a small-particle suspensions of immunosuppressive agents, particularly cyclosporin, for pharmaceutical use. The particles are coated with one or more surface modifiers.

Abstract translation: 本发明涉及用于药物用途的抗惊厥药，特别是卡马西平的小颗粒悬浮液的制剂。 本发明还涉及用于药物用途的免疫抑制剂，特别是环孢菌素的小颗粒悬浮液的制剂。 颗粒被一个或多个表面改性剂涂覆。

公开(公告)号：WO2004054500A3

公开(公告)日：2004-08-26

申请号：PCT/US0324353

申请日：2003-08-04

Applicant: BAXTER INT

Inventor： WERLING JANE ,  KIPP JAMES E ,  SRIRAM RAJARAM ,  DOTY MARK J ,  REBBECK CHRISTINE L ,  WONG JOSEPH CHUNG TAK

IPC: A61K9/00 ,  A61K31/495 ,  A61K9/127 ,  A61K9/14

CPC classification number: A61K9/14 ,  A61K9/0019 ,  A61K9/10 ,  A61K31/495

Abstract: The present invention provides a method of preparing particles with polymorph and size control of a pharmaceutical compound, the method including the steps of: (1) providing pharmaceutical compound in a first phase; (2) seeding the compound; (3) causing a phase change in the pharmaceutical compound to a second phase of a desired polymorphic form; and (4) wherein the mean particle size of the particles is less than 7µm. The present invention further provides a polymorphic form of itraconazole.

Abstract translation: 本发明提供一种制备具有药物化合物的多晶型物和粒度控制的颗粒的方法，所述方法包括以下步骤：（1）在第一相中提供药物化合物; （2）接种化合物; （3）引起药物化合物相变为所需多晶型物的第二相; 和（4）其中颗粒的平均粒度小于7μm。 本发明还提供了伊曲康唑的多晶型物。

公开(公告)号：BRPI0909780B1

公开(公告)日：2022-05-03

申请号：BRPI0909780

申请日：2009-03-05

Applicant: BAXTER HEALTHCARE SA ,  BAXTER INT ,  UNIV NEBRASKA

Inventor： BEDUNEAU ARNAUD ,  RABINOW BARRETT ,  GENDELMAN HOWARD ,  WERLING JANE

IPC: A61K9/51 ,  A61K31/337 ,  A61K39/44

Abstract: suspensão contendo uma partícula com superfície modificada, composição farmacêutica compreendendo a referida suspensão, método para aprimorar a absorção celular de um agente ativo, uso de partículas com superfície modificada, e método de preparação de uma partícula com superfície modificada. a presente invenção refere-se a partículas com superfície modificada e métodos para fabricar e usar a mesma. as partículas com superfície modificada compreendem um núcleo de partícula e um revestimento associado com o núcleo de partícula, em que o núcleo de partícula compreende um agente ativo, o revestimento compreende uma opsonina, e a partícula com superfície modificada tem um tamanho médio de aproximadamente 1 nm a aproximadamente 2.000 nm.

公开(公告)号：SG176055A1

公开(公告)日：2011-12-29

申请号：SG2011083789

申请日：2010-05-13

Applicant: BAXTER INT ,  BAXTER HEALTHCARE SA

Inventor： RABINOW BARRETT ,  BAIRSTOW SHAWN F ,  CHAUBAL MAHESH V ,  LEE SARAH ,  WERLING JANE

Abstract: The present disclosure is directed to surface-modified particles and to methods of making and using the same. The surface-modified particles comprise a particle core and a coating associated with the particle core, wherein the particle core comprises an active agent, the coating comprises a surfactant having formula (I) or a salt thereof, and the surface-modified particle has an average size from about 1 nm to about 2,000 nm:

公开(公告)号：CA2628630A1

公开(公告)日：2007-05-24

申请号：CA2628630

申请日：2006-11-15

Applicant: BAXTER HEALTHCARE SA ,  BAXTER INT

Inventor： BURESH RITA ,  GUPTA PRAMOD ,  WERLING JANE ,  KIPP JAMES E

IPC: A61K9/14 ,  A61K9/10 ,  A61K9/19 ,  A61K31/38 ,  A61P1/00 ,  A61P9/10 ,  A61P11/06 ,  A61P17/06 ,  A61P17/10 ,  A61P29/00 ,  A61P35/00 ,  A61P37/08

Abstract: Pharmaceutical compositions comprising particles of lipoxygenase inhibitor compounds having an effective average size of from about 10 nm to about 50 microns are provided. More particularly, pharmaceutical compositions of particle of a 5-lipoxygenase inhibitor compound having an effective average size of from about 50 nm to about 5 microns are provided. The pharmaceutical compositions are in the form of aqueous suspensions with the particle of the 5-lipoxygenase inhibitor compound present in concentrations of from about 5 to about 200 mg/ml. In addition, methods for making such pharmaceutical compositions are provided. In particular, microprecipitation and direct homogenization in the presence of at least one surfactant are disclosed for making the pharmaceutical compositions.

公开(公告)号：NZ526608A

公开(公告)日：2006-06-30

申请号：NZ52660801

申请日：2001-12-20

Applicant: BAXTER INT

Inventor： KIPP JAMES E ,  WONG JOSEPH CHUNG TAK ,  DOTY MARK J ,  REBBECK CHRISTINE L ,  BRYNJELSEN SEAN ,  WERLING JANE ,  SRIRAM RAJARAM

IPC: C07D407/14 ,  A61K9/10 ,  A61K9/14 ,  A61K9/16 ,  A61K31/495 ,  A61K31/496 ,  A61K47/12 ,  A61K47/14 ,  A61K47/18 ,  A61K47/20 ,  A61K47/24 ,  A61K47/28 ,  A61K47/34 ,  A61K47/36 ,  A61K47/38 ,  A61K47/42 ,  A61P31/10 ,  A61K9/20 ,  A61K9/51

Abstract: A method for preparing submicron sized particles of a pharmaceutically-active compound, the solubility of which is greater in a water-miscible first solvent than in a second solvent which is aqueous is disclosed, wherein the process comprises the steps of: (i) dissolving the pharmaceutically-active compound in the water-miscible first solvent to form a solution, the first solvent being selected from the group consisting of N methyl-2-pyrrolidinone, 2-pyrrolidone, dimethyl sulfoxide, dimethylacetamide, lactic acid, methanol, ethanol, isopropanol, 3-pentanol, n-propanol, glycerol, butylene glycol, ethylene glycol, polypropylene glycol, mono- and diacylated monoglycerides, dimethyl isosorbide, acetone, dimethylformamide, 1,4-dioxane, ethyl acetate, propyl acetate, polyethylene glycol, polyethylene glycol esters, polyethylene glycol sorbitans, polyethylene glycol monoalkyl ethers, polypolypropylene glycol, polypropylene alginate, polypolypropylene glycol-10 butanediol, polypolypropylene glycol-10 methyl glucose ether, polypolypropylene glycol-20 methyl glucose ether, polypolypropylene glycol-15 stearyl ether, polypolypropylene glycol dicaprylate, polypropylene glycol dicaprate, polypropylene glycol laurate; (ii) mixing the solution with the second solvent to define a pre-suspension; and (iii) adding energy to the pre-suspension to form particles having an average effective particle size of less than about 2 micron, and said adding energy step comprises homogenization, counter-current flow homogenization, microfluidization or sonication.

公开(公告)号：AU2004289233A1

公开(公告)日：2005-05-26

申请号：AU2004289233

申请日：2004-11-03

Applicant: BAXTER INT

Inventor： CHAUBAL MAHESH ,  RABINOW BARRETT E ,  WERLING JANE

IPC: A61K31/337 ,  A61K9/10 ,  A61K9/127 ,  A61K9/133 ,  A61K9/14 ,  A61K9/16 ,  A61K31/12 ,  A61K31/495 ,  A61K31/496 ,  A61K31/55 ,  A61K31/573

Abstract: The present invention is concerned with the formation of submicron particles of an antineoplastic agent, particularly paclitaxel, by precipitating the antineoplastic agent in an aqueous medium to form a pre-suspension followed by homogenization. Surfactants with phospholipids conjugated with a water soluble or hydrophilic polymer such as PEG are used as coating for the particles. The particles produced generally have an average particle size of less than about 1000 nm and are not rapidly soluble.