公开(公告)号：WO2004012711A1

公开(公告)日：2004-02-12

申请号：PCT/US2003/021884

申请日：2003-07-14

Applicant: DOW GLOBAL TECHNOLOGIES INC. ,  TUCKER, Christopher, J. ,  SVENSON, Sonke ,  HITT, James, E. ,  CURTIS, Cathy, A.

Inventor： TUCKER, Christopher, J. ,  SVENSON, Sonke ,  HITT, James, E. ,  CURTIS, Cathy, A.

IPC: A61K9/14

CPC classification number: A61K9/146

Abstract: Drug particles which are essentially crystalline and have a mean particle size below 2 microns, when dispersed in water, are described. When added to an aqueous medium at 25-95% of the equilibrium solubility of the drug substance, the drug particles show complete dissolution, as characterized by a 95% reduction in turbidity, in less than 5 minutes. Using a controlled precipitation process to prepare such drug particles is also described. Such drug particles exhibit an enhanced dissolution rate and better stability as compared to particles prepared according to processes described in the prior art.

Abstract translation: 描述了当分散在水中时基本上是结晶的并且具有低于2微米的平均粒度的药物颗粒。 当以25-95％的药物物质的平衡溶解度加入到水性介质中时，药物颗粒显示完全溶解，其特征在于在不到5分钟内95％的浊度降低。 还描述了使用受控沉淀法制备这种药物颗粒。 与根据现有技术中描述的方法制备的颗粒相比，这样的药物颗粒显示出增强的溶解速率和更好的稳定性。

公开(公告)号：WO2008067028A2

公开(公告)日：2008-06-05

申请号：PCT/US2007/080152

申请日：2007-10-02

Applicant: DOW GLOBAL TECHNOLOGIES INC. ,  BUSBY, Molly, I-chin ,  TUCKER, Christopher, J.

Inventor： BUSBY, Molly, I-chin ,  TUCKER, Christopher, J.

CPC classification number: A61Q19/10 ,  A61K8/046 ,  A61K8/70 ,  A61K8/731 ,  A61K2800/5426 ,  A61Q17/005

Abstract: A foamable aqueous composition having alcohol and at least one water soluble polymer.

Abstract translation: 可发泡的含有醇和至少一种水溶性聚合物的含水组合物。

公开(公告)号：WO2004012710A1

公开(公告)日：2004-02-12

申请号：PCT/US2003/021882

申请日：2003-07-14

Applicant: DOW GLOBAL TECHNOLOGIES INC. ,  SVENSON, Sonke ,  TUCKER, Christopher, J. ,  HITT, James, E.

Inventor： SVENSON, Sonke ,  TUCKER, Christopher, J. ,  HITT, James, E.

IPC: A61K9/14

CPC classification number: A61K9/146 ,  A61K9/145

Abstract: Particles having a plurality of crystalline domains are described. Each crystalline domain is oriented differently than any of the adjacent domains and comprises a drug substance. A plurality of interfacial regions surround the crystalline domains, each interfacial region comprising at least one stabilizer. A process used to prepare the particles of the present invention is also described. The particles of the present invention exhibit relatively fast dissolution times as compared to particles prepared by processes described in the prior art.

Abstract translation: 描述具有多个结晶域的颗粒。 每个结晶结构域的取向与任何相邻的结构域不同，并且包含药物物质。 多个界面区域围绕结晶域，每个界面区域包括至少一个稳定剂。 还描述了用于制备本发明的颗粒的方法。 与通过现有技术中描述的方法制备的颗粒相比，本发明的颗粒表现出相对较快的溶解时间。

公开(公告)号：WO2003059319A1

公开(公告)日：2003-07-24

申请号：PCT/US2003/000726

申请日：2003-01-10

Applicant: DOW GLOBAL TECHNOLOGIES INC.

Inventor： SVENSON, Sonke ,  TUCKER, Christopher, J. ,  LUBETKIN, Steven, D. ,  EVANS, Jonathan, C. ,  ROSENBERG, Steven, S.

IPC: A61K9/107

CPC classification number: A61K9/14

Abstract: A method for producing micron-sized or submicron-sized drugs is disclosed, which comprises preparing a template emulsion comprising water and a templating agent; preparing a drug-containing mixture comprising a drug substance; and combining the template emulsion with the drug-containing mixture to form a template emulsion loaded with drug particles. Drug particles prepared from this process are also disclosed. The resulting drug particles demonstrate faster dissolution rates and enhanced bioavailability as compared to unprocessed drug particles and particles prepared using other processes.

Abstract translation: 公开了一种制备微米级或亚微米级药物的方法，其包括制备包含水的模板乳液和制备包含药物物质的药物混合物的模板剂，并将模板乳剂与含药物混合物组合以形成 装载有药物颗粒的模板乳液。 还公开了从该方法制备的药物颗粒。 与未处理的药物颗粒和使用其它方法制备的颗粒相比，所得药物颗粒显示更快的溶解速率和增强的生物利用度。

公开(公告)号：WO2006017391A2

公开(公告)日：2006-02-16

申请号：PCT/US2005/027008

申请日：2005-08-01

Applicant: DOW GLOBAL TECHNOLOGIES INC. ,  BISCOGLIO, Michael, B. ,  KLIER, John ,  CHAUDHARY, Bharat, I. ,  MULLINS, Michael, J. ,  TUCKER, Christopher, J.

Inventor： BISCOGLIO, Michael, B. ,  KLIER, John ,  CHAUDHARY, Bharat, I. ,  MULLINS, Michael, J. ,  TUCKER, Christopher, J.

IPC: C08L23/00 ,  C08L51/06

CPC classification number: C08K5/42 ,  C08F255/00 ,  C08F255/02 ,  C08L23/0892 ,  C08L2312/08 ,  C08F230/08 ,  C08L43/04

Abstract: Silane crosslinkable polymer compositions comprise (i) at least one silane crosslinkable polymer, e.g., ethylene-silane copolymer, and (ii) a catalytic amount of at least one polysubstituted aromatic sulfonic acid (PASA). The PASA catalysts are of the formula: HSO 3 Ar-R 1 (R x ) m Where: m is 0 to 3; R 1 is (CH 2 ) n CH 3 , and n is 0 to 3 or greater than 20; Each R x is the same or different than R 1 ; and Ar is an aromatic moiety.

Abstract translation: 硅烷交联聚合物组合物包含（i）至少一种硅烷可交联聚合物，例如乙烯 - 硅烷共聚物，和（ii）催化量的至少一种多取代芳族磺酸（PASA）。 PASA催化剂具有下式：HSO 3 Ar-R 1（R x x）m其中：m 是0到3; R 1是（CH 2 CH 2）n CH 3 CH 3，n是0至3或大于20; 每个R x X相同或不同于R 1; 并且Ar是芳族部分。

公开(公告)号：WO2004013618A1

公开(公告)日：2004-02-12

申请号：PCT/US2003/021883

申请日：2003-07-14

Applicant: DOW GLOBAL TECHNOLOGIES INC. ,  TUCKER, Christopher, J.

Inventor： TUCKER, Christopher, J.

IPC: G01N21/51

CPC classification number: G01N33/15 ,  G01N15/0205 ,  G01N21/51 ,  G01N2013/006 ,  G01N2015/0693

Abstract: A method for determining the percent of a solid material dissolved into a liquid medium is disclosed. The method comprises the steps of combining the solid material and the liquid medium; determining the initial solid concentration (i); determining the dynamic solid concentration (d) using a light scattering technique; and calculating the percent dissolved material according to the formula: [(i - d)/i] x 100 . Methods for determining dissolution rate and particle size using turbidity measurements are also disclosed.

Abstract translation: 公开了一种确定溶解在液体介质中的固体材料的百分比的方法。 该方法包括将固体材料与液体介质结合的步骤; 确定初始固体浓度（i）; 使用光散射技术确定动态固体浓度（d）; 并根据以下公式计算溶解的百分比：[（i-d）/ i]×100。 还公开了使用浊度测量来确定溶解速率和粒径的方法。

公开(公告)号：WO2003037837A2

公开(公告)日：2003-05-08

申请号：PCT/US2002/033672

申请日：2002-10-22

Applicant: DOW GLOBAL TECHNOLOGIES INC. ,  TUCKER, Christopher, J. ,  KALANTAR, Thomas, H. ,  KUMAR, Promod ,  STRANDBURG, Gary, M.

Inventor： TUCKER, Christopher, J. ,  KALANTAR, Thomas, H. ,  KUMAR, Promod ,  STRANDBURG, Gary, M.

IPC: C07C43/11

CPC classification number: C11D1/72 ,  C07C43/11 ,  C07C305/10 ,  C11D1/29

Abstract: This invention is for di-substituted surfactant precursors, surfactants prepared from them, methods of making the di-substituted surfactant precursors and derived surfactants, and to surfactants having the properties of the described surfactants. The di-substituted surfactant precursors and surfactants are derived from admixing water, surfactant, a hydrolysis catalyst, and an initial quantity of a substituted three-membered heterocycle (a substituted l-oxacyclopropane, a substituted 1-thiacyclopropane, or a substituted l-azacyclopropane) and sustaining an emulsion admixture of the di-substituted surfactant precursor, the water, the heterocycle, the surfactant, and the catalyst to yield the di-substituted surfactant precursor. The di-substituted surfactant precursor is further functionalized to achieve desired hydrophilic properties. A new surfactant product is ultimately provided affording a new combination of (in aqueous admixture) critical micelle concentration, viscosity, and clarity properties.

Abstract translation: 本发明涉及二取代的表面活性剂前体，由它们制备的表面活性剂，制备二取代的表面活性剂前体和衍生的表面活性剂的方法以及具有所述表面活性剂性质的表面活性剂。 二取代的表面活性剂前体和表面活性剂来自混合水，表面活性剂，水解催化剂和初始量的取代的三元杂环（取代的1-氧杂环丙烷，取代的1-硫杂环丙烷或取代的1-氮杂环丙烷 ）并保持二取代的表面活性剂前体，水，杂环，表面活性剂和催化剂的乳液混合物，得到二取代的表面活性剂前体。 二取代的表面活性剂前体进一步官能化以获得所需的亲水性质。 最终提供新的表面活性剂产物，提供（水性混合物）临界胶束浓度，粘度和透明度性质的新组合。

公开(公告)号：WO2003032951A1

公开(公告)日：2003-04-24

申请号：PCT/US2002/027444

申请日：2002-08-27

Applicant: DOW GLOBAL TECHNOLOGIES INC. ,  HITT, James, E. ,  TUCKER, Christopher, J. ,  EVANS, Jonathan, C. ,  CURTIS, Cathy, A. ,  SVENSON, Sonke

Inventor： HITT, James, E. ,  TUCKER, Christopher, J. ,  EVANS, Jonathan, C. ,  CURTIS, Cathy, A. ,  SVENSON, Sonke

IPC: A61K9/14

CPC classification number: A61K9/5146 ,  A61K9/1635 ,  A61K9/1688 ,  B01D9/005 ,  B82Y5/00

Abstract: A process for preparing crystalline particles of a drug substance is disclosed, said process comprising recirculating an anti-solvent through a mixing zone, dissolving the drug substance in a solvent to form a solution, adding the solution to the mixing zone to form a article slurry in the anti-solvent, and recirculating at least a portion of the particle slurry back through the mixing zone. Particles produced from the process are also disclosed. The present invention has the ability to be operated in a continuous fashion, resulting in a more efficient process and a more uniform product. The present invention has the additional advantage of having the ability to operate at a relatively low solvent ratio, thereby increasing the drug to excipient ratio.

Abstract translation: 公开了一种制备药物结晶颗粒的方法，所述方法包括通过混合区使反溶剂再循环，将药物溶解在溶剂中以形成溶液，将溶液加入混合区以形成制品浆料 在反溶剂中，并且将至少一部分颗粒浆料再循环通过混合区。 还公开了从该方法生产的颗粒。 本发明具有以连续方式操作的能力，从而产生更有效的工艺和更均匀的产品。 本发明具有能够以相对低的溶剂比操作的能力的另外的优点，从而将药物增加到赋形剂比例。

公开(公告)号：WO2003070777A1

公开(公告)日：2003-08-28

申请号：PCT/US2003/004668

申请日：2003-02-12

Applicant: DOW GLOBAL TECHNOLOGIES INC. ,  KALANTAR, Thomas, H. ,  NIU, Qing Shan, J. ,  TUCKER, Christopher, J. ,  DOMKE, Christopher, H.

Inventor： KALANTAR, Thomas, H. ,  NIU, Qing Shan, J. ,  TUCKER, Christopher, J. ,  DOMKE, Christopher, H.

IPC: C08F2/30

CPC classification number: C08F2/24

Abstract: This invention is cross-linked, polymerized hydrocarbon particles which composition is characterized in that the particles have an average diameter of less than 30 nm, the particles exhibit a volume swell factor of no greater than 3.0; the composition is essentially free of metal ions; the particles have a polydispersity (polystyrene relative Mw/Mn) of less than 3.0, and the particles are characterized by a Mark-Houwink plot having a slope with an absolute value of less than 0.4 for the peak molecular weight range. The invention is also a method of making nanoparticles having a weight average diameter less than 30 nm by emulsion polymerization in the substantial absence of ionic components. Finally, the invention is a method of using such particles as thermally degradable components in making porous films.

Abstract translation: 本发明是交联的聚合烃颗粒，其组成特征在于颗粒的平均直径小于30nm，颗粒的体积溶胀因子不大于3.0; 该组合物基本上不含金属离子; 颗粒具有小于3.0的多分散性（聚苯乙烯相对Mw / Mn），并且该颗粒的特征在于在峰值分子量范围内具有绝对值小于0.4的斜率的Mark-Houwink图。 本发明也是通过基本上没有离子组分的乳液聚合制备重均粒径小于30nm的纳米颗粒的方法。 最后，本发明是在制造多孔膜时使用这种颗粒作为可热降解组分的方法。

公开(公告)号：WO2003037837A3

公开(公告)日：2003-05-08

申请号：PCT/US2002/033672

申请日：2002-10-22

Applicant: DOW GLOBAL TECHNOLOGIES INC. ,  TUCKER, Christopher, J. ,  KALANTAR, Thomas, H. ,  KUMAR, Promod ,  STRANDBURG, Gary, M.

Inventor： TUCKER, Christopher, J. ,  KALANTAR, Thomas, H. ,  KUMAR, Promod ,  STRANDBURG, Gary, M.

IPC: C07C43/11 ,  C07C305/10 ,  C08G65/00 ,  B01F17/00 ,  C11D1/72 ,  C11D1/29

Abstract: This invention is for di-substituted surfactant precursors, surfactants prepared from them, methods of making the di-substituted surfactant precursors and derived surfactants, and to surfactants having the properties of the described surfactants. The di-substituted surfactant precursors and surfactants are derived from admixing water, surfactant, a hydrolysis catalyst, and an initial quantity of a substituted three-membered heterocycle (a substituted l-oxacyclopropane, a substituted 1-thiacyclopropane, or a substituted l-azacyclopropane) and sustaining an emulsion admixture of the di-substituted surfactant precursor, the water, the heterocycle, the surfactant, and the catalyst to yield the di-substituted surfactant precursor. The di-substituted surfactant precursor is further functionalized to achieve desired hydrophilic properties. A new surfactant product is ultimately provided affording a new combination of (in aqueous admixture) critical micelle concentration, viscosity, and clarity properties.