公开(公告)号：JP2014114322A

公开(公告)日：2014-06-26

申请号：JP2014031168

申请日：2014-02-21

Applicant: Basf Se ,  ビーエーエスエフ ソシエタス・ヨーロピアBasf Se

Inventor： KOLTER KARL ,  MICHAEL SCHOENHERR ,  SILKE GEBERT ,  KATHRIN MEYER-BOHM ,  ANGELIKA MASCHKE

IPC: A61K9/26 ,  A61K47/10 ,  A61K47/20 ,  A61K47/32 ,  A61K47/38

CPC classification number: A61K9/2018 ,  A61K9/0056 ,  A61K9/2027 ,  A61K9/2054

Abstract: PROBLEM TO BE SOLVED: To provide tablets which disintegrate rapidly in the mouth, leave behind a pleasant sensation in the mouth, are mechanically very stable, and provide high content uniformity.SOLUTION: A pharmaceutical formulation in the form of agglomerates comprises the following components A) and B): A) an excipient consisting of a) 60-97% by weight of sugar or sugar alcohols, b) 1-25% by weight of a disintegration agent, c) 1-15% by weight of water-insoluble, film-forming polymers, d) 0-15% by weight of water-soluble polymers, and e) 0-15% by weight of another pharmaceutically customary excipients, wherein the sum of the components a) to e) is 100% by weight; and B) at least one active ingredient.

Abstract translation: 要解决的问题：提供在口中快速崩解的片剂，在口中留下愉快的感觉，机械上非常稳定，并提供高含量均匀性。溶解剂：附聚物形式的药物制剂包含以下组分A ）和B）：A）由a）60-97重量％的糖或糖醇组成的赋形剂，b）1-25重量％的崩解剂，c）1-15重量％的水不溶性 ，成膜聚合物，d）0-15重量％的水溶性聚合物，和e）0-15重量％的另一种药学上常规的赋形剂，其中组分a）至e）的总和为100％ 重量; 和B）至少一种活性成分。

公开(公告)号：WO2008080774A9

公开(公告)日：2009-11-12

申请号：PCT/EP2007063674

申请日：2007-12-11

Applicant: BASF SE ,  KOLTER KARL ,  MASCHKE ANGELIKA ,  DIETZEN FRANZ-JOSEF ,  SCHMELLER THORSTEN

Inventor： KOLTER KARL ,  MASCHKE ANGELIKA ,  DIETZEN FRANZ-JOSEF ,  SCHMELLER THORSTEN

IPC: A61K9/14

CPC classification number: A61K9/284

Abstract: The invention relates to solid particulate film coating agents consisting of: a) 40 - 90 % by weight, preferably 40 - 70 % by weight polyvinyl alcohol-polyether graft copolymers (component A), b) up to 60 % by weight, preferably between 20 and 45 % by weight of a coloured or achromatic colouring agent (component B), c) between 0 and 30 % by weight additional conventional auxiliary agents (component C). According to the invention, the quantities of components A to C total 100 % by weight. Said coating agents are obtained by the extrusion of a plastic mass of components A) to C) and by a subsequent shaping process.

Abstract translation: 固体颗粒薄膜包衣组合物，其包含：a）40 - 90重量％，b）由60重量％，优选为20〜45优选40〜70重量聚乙烯醇 - 聚醚接枝共聚物（组分A的％） .-有色或无色的着色剂（组分B），c）0至30重量的其它的常规辅助物质（组分C）％，其中组分A至C中的量合计为100重量％，由％ 获得挤出组分a）至C的塑性体），以及随后的成形。

公开(公告)号：WO2010130728A2

公开(公告)日：2010-11-18

申请号：PCT/EP2010056447

申请日：2010-05-11

Applicant: BASF SE ,  KOLTER KARL ,  DJURIC DEJAN ,  FISCHER STEFAN

Inventor： KOLTER KARL ,  DJURIC DEJAN ,  FISCHER STEFAN

IPC: A61K9/20 ,  C08F283/06

CPC classification number: A61K47/38 ,  A61K9/2027 ,  A61K9/2031 ,  A61K9/2054 ,  A61K9/2095 ,  A61K31/192 ,  A61K31/216 ,  A61K31/4164 ,  A61K31/4425 ,  A61K31/451 ,  A61K31/495 ,  A61K31/496 ,  A61K31/5415 ,  A61K31/55 ,  A61K31/635 ,  A61K47/32 ,  A61K47/34 ,  C08F283/06

Abstract: The invention relates to dosage forms which contain preparations of poorly water-soluble substances in a polymer matrix of polyether copolymers, said polyether copolymers being obtained by the radically initiated polymerization of a mixture from 30 to 80% by weight of N-vinyl lactam, 10 to 50% by weight of vinyl acetate and 10 to 50% by weight of a polyether, and at least one poorly water-soluble polymer, the poorly water-soluble substance being present in the polymer matrix as an amorphous substance.

Abstract translation: 剂型，包括在聚醚共聚物的聚合物基质的水溶性差的药物的制剂中，聚醚共聚物可通过30的混合物的自由基引发的聚合至80重量％的N-乙烯基内酰胺获得的，10至50重量％乙酸乙烯酯 和聚醚的10〜50重量％和至少一种微溶于水的聚合物，其中难溶于水的活性成分是在聚合物基质无定形的。

公开(公告)号：WO2011051155A3

公开(公告)日：2011-12-08

申请号：PCT/EP2010065848

申请日：2010-10-21

Applicant: BASF SE ,  KOLTER KARL ,  ANGEL MAXIMILIAN ,  BREINER THOMAS

Inventor： KOLTER KARL ,  ANGEL MAXIMILIAN ,  BREINER THOMAS

IPC: A61K9/16 ,  A61K9/20 ,  A61K9/50 ,  C08F2/12 ,  C08F2/22 ,  C08F220/14 ,  C08F220/24 ,  C08F220/34 ,  C09D5/02 ,  C09D133/14 ,  C09J133/14

CPC classification number: A61K47/32 ,  A61K9/10 ,  A61K9/2846 ,  C08F220/14 ,  C08F220/34 ,  C08K3/014 ,  C08K3/24 ,  C08K3/26 ,  C08K5/005 ,  C08K5/13 ,  C08K5/17 ,  C08K5/175 ,  C08K2003/262

Abstract: A coating material, containing a mixture of i) a polymer obtained by radical polymerization from a) N,N-diethylaminoethyl methacrylate, and b) at least one radically polymerizable compound, selected from esters of a,ß- ethylenically unsaturated mono- and dicarboxylic acids with C1-C18 alkanols, as component A, ii) one or more antioxidants as component B, iii) one or more plasticizers as component C, and iv) other excipients as components D, wherein the total amount of the mixture of components A-D is 100 wt.%.

Abstract translation: 一种涂料，它含有i）由a）N，N-二乙基氨基乙基甲基丙烯酸酯自由基聚合得到的聚合物，和b）至少一种可自由基聚合的化合物，该化合物选自β-烯键式不饱和单羧酸和二羧酸 作为组分A的一种或多种抗氧化剂，作为组分B的一种或多种抗氧化剂，作为组分C的一种或多种增塑剂，以及作为组分D的其他赋形剂，其中组分AD的混合物 是100重量％。

公开(公告)号：WO2010139654A3

公开(公告)日：2011-05-19

申请号：PCT/EP2010057515

申请日：2010-05-31

Applicant: BASF SE ,  KOLTER KARL ,  ANGEL MAXIMILIAN

Inventor： KOLTER KARL ,  ANGEL MAXIMILIAN

IPC: A61K9/32

CPC classification number: A61K9/0056 ,  A61K9/2081 ,  A61K9/5073 ,  A61K47/32

Abstract: The invention relates to orally disintegrating dosage forms of taste-masked active ingredients, which are provided with a coating of polymers containing N,N-diethylaminoethylmethacrylate (DEAEMA) that is polymerized therein for masking the taste, and in which the taste-masked active ingredients are embedded in an orally disintegrating matrix.

Abstract translation: 口腔崩解与聚合物的涂层共聚活性成分，其提供了用于味道掩盖，其包含N，N-二乙基氨基乙酯（DEAEMA）的掩味的剂型，并且其中所述掩味活性成分嵌入到口腔崩解基质。

公开(公告)号：WO2012085043A2

公开(公告)日：2012-06-28

申请号：PCT/EP2011073531

申请日：2011-12-21

Applicant: BASF SE ,  KOLTER KARL ,  GEBERT SILKE ,  KATSUNO YOSHITAKA

Inventor： KOLTER KARL ,  GEBERT SILKE ,  KATSUNO YOSHITAKA

IPC: A61K9/00

CPC classification number: A61K9/0056 ,  A61K9/2018 ,  A61K9/2027 ,  A61K9/2054 ,  A61K9/2072 ,  A61K9/2095 ,  A61K9/2813 ,  A61K9/284 ,  A61K9/2846

Abstract: Rapidly disintegrating, solid coated dosage form comprising a solid core consisting of at least 60% by weight of an auxiliary mixture, up to 40% by weight of at least one active ingredient, and optionally further auxiliaries, coated with at least one film coating comprising completely or partially hydrolyzed, rapidly water-soluble polyether-vinyl ester graft polymers, methods for the production thereof, and their use.

Abstract translation: 包含由至少60重量％的辅助混合物，至多40重量％的至少一种活性成分和任选的其它助剂组成的固体芯片的快速崩解的固体涂层剂型，涂覆有至少一种薄膜包衣，包括 完全或部分水解的快速水溶性聚醚 - 乙烯基酯接枝聚合物，其制备方法及其用途。

公开(公告)号：WO2010112489A3

公开(公告)日：2011-02-24

申请号：PCT/EP2010054167

申请日：2010-03-30

Applicant: BASF SE ,  MEYER-BOEHM KATHRIN ,  DOBRAWA RAINER ,  FISCHER STEFAN ,  KOLTER KARL

Inventor： MEYER-BOEHM KATHRIN ,  DOBRAWA RAINER ,  FISCHER STEFAN ,  KOLTER KARL

IPC: A61K9/14 ,  A23L1/03 ,  A61K8/81 ,  A61K8/86 ,  A61K9/20

CPC classification number: A61K9/2095 ,  A23L5/40 ,  A23L33/00 ,  A23L33/10 ,  A23P10/30 ,  A61K8/86 ,  A61K8/91 ,  A61K9/146 ,  A61K9/1641 ,  A61K9/1682 ,  A61K9/1694 ,  A61K47/34 ,  A61Q19/00 ,  C08F18/08 ,  C08F226/06 ,  C08F226/10 ,  C08F283/06

Abstract: The invention relates to a method for producing preparations of substances poorly soluble in water, wherein the poorly soluble substances are present amorphously embedded in a copolymer, and the copolymer is obtained by radically initiated polymerization of a mixture of i) 30 to 80 wt% N-vinyl lactam, ii) 10 to 50 wt% vinyl acetate, and iii) 10 to 50 wt% of a polyether, with the stipulation that the sum of the components i), ii), and iii) is equal to 100 wt%, wherein the embedding of the poorly soluble substance into the copolymer occurs at temperatures above the melting point of the poorly soluble substances.

Abstract translation: 本发明涉及一种用于微溶于水的物质，其特征在于，存在于无定形的微溶物质包埋在共聚物制剂的制备，并且通过我的从30的混合物）的自由基引发的聚合反应，80重量％N获得的共聚物 乙烯基内酰胺，ⅱ）10〜50重量％的乙酸乙烯酯，和iii）10至50重量的聚醚，条件的％各组分i）的总和，ii）和iii）等于100重量％ ，其中在所述共聚物中的微溶物质的嵌入是在温度的微溶物质的熔点以上进行。

公开(公告)号：WO2008065051A2

公开(公告)日：2008-06-05

申请号：PCT/EP2007062756

申请日：2007-11-23

Applicant: BASF SE ,  KOLTER KARL ,  SCHOENHERR MICHAEL ,  ASCHERL HERMANN ,  DIELEMAN CEDRIC ,  KNIERIEM TORSTEN ,  KOLTZENBURG SEBASTIAN ,  TUERK HOLGER

Inventor： KOLTER KARL ,  SCHOENHERR MICHAEL ,  ASCHERL HERMANN ,  DIELEMAN CEDRIC ,  KNIERIEM TORSTEN ,  KOLTZENBURG SEBASTIAN ,  TUERK HOLGER

IPC: A01N25/12 ,  A01N25/10 ,  A01N43/653 ,  A01N47/24

CPC classification number: A01N25/12 ,  A01N25/10 ,  A01N47/24 ,  A01N43/653 ,  A01N2300/00

Abstract: The invention relates to a method for production of solid solutions of poorly soluble pesticides, power products obtained by such a method and the use thereof for pesticide formulations.

Abstract translation: 本发明涉及一种用于其通过这样的方法和它们的杀虫制剂中的用途获得的微溶性农药，粉状产品固体溶液的制备方法。

公开(公告)号：WO2011107466A3

公开(公告)日：2011-12-15

申请号：PCT/EP2011053012

申请日：2011-03-01

Applicant: BASF SE ,  KOLTER KARL ,  DJURIC DEJAN

Inventor： KOLTER KARL ,  DJURIC DEJAN

IPC: A61K9/14 ,  A61K9/16 ,  A61K31/00 ,  A61K47/10 ,  A61K47/34

CPC classification number: A61K9/1676 ,  A61K31/216 ,  A61K31/4174 ,  A61K31/495 ,  A61K31/496 ,  A61K31/5415

Abstract: The invention relates to preparations of active agents not easily soluble in water, consisting of carrier particles having active agent-containing coatings, wherein the active agents not easily soluble in water are embedded in coatings made of amphiphilic copolymers and the coatings are applied in the form of a solvent-free melt.

Abstract translation: 由活性成分涂层载体颗粒组成的微溶于水活性成分的制剂，将微溶性活性成分嵌入两亲共聚物的涂层中，并且涂层以无溶剂熔体的形式施用。

公开(公告)号：WO2010034688A3

公开(公告)日：2011-02-24

申请号：PCT/EP2009062199

申请日：2009-09-21

Applicant: BASF SE ,  MEYER-BOEHM KATHRIN ,  DOBRAWA RAINER ,  MASCHKE ANGELIKA ,  KOLTER KARL

Inventor： MEYER-BOEHM KATHRIN ,  DOBRAWA RAINER ,  MASCHKE ANGELIKA ,  KOLTER KARL

IPC: A61K9/16 ,  A61K9/20

CPC classification number: A61K47/34 ,  A61K9/1641 ,  A61K9/2031 ,  A61K9/2095

Abstract: Use of water-soluble or water-dispersible copolymers obtained through radically-initiated polymerization of a mixture of i) 30 to 80 wt.-% of N-vinyl lactam, ii) 10 to 50 wt.-% of vinyl acetate and iii) 10 to 50 wt.-% of a polyether as a binder for the manufacture of dosing forms comprising solid active ingredients, said copolymers being conditioned in that the total of i), ii) and iii) is equal to 100 wt.-%.

Abstract translation: 其通过我的从30的混合物）的自由基引发的聚合至80重量％的N-乙烯基内酰胺得到的水溶性或水分散性共聚物，ⅱ）10至50重量％的乙酸乙烯酯，和iii）10至50重量％的使用 聚醚，条件是i的总和），ii）和iii）等于100重量％，作为固体含活性成分的剂型的制备的粘合剂。