公开(公告)号：US4062831A

公开(公告)日：1977-12-13

申请号：US568777

申请日：1975-04-17

申请人： Jinrich Kopecek ,  Karel Ulbrich ,  Jiri Vacik ,  Jiri Strohalm ,  Vladimir Chytry ,  Jaroslav Drobnik ,  Jaroslav Kalal

发明人： Jinrich Kopecek ,  Karel Ulbrich ,  Jiri Vacik ,  Jiri Strohalm ,  Vladimir Chytry ,  Jaroslav Drobnik ,  Jaroslav Kalal

IPC分类号： C08F2/00 ,  B01J39/20 ,  C08F2/04 ,  C08F2/18 ,  C08F20/00 ,  C08F20/34 ,  C08F20/52 ,  C08F220/54 ,  C08F222/12 ,  C08G69/44 ,  C08G73/16 ,  C08J5/20

CPC分类号： C08F220/54

摘要： The invention relates to copolymers based on N-substituted acrylamides, N-substituted methacrylamides and N,N-disubstituted acrylamides and to a method for their manufacturing, which copolymers are prepared under conditions when the phase separation takes place. The resulting copolymer contains reactive groups and serves as the intermediate for preparation of biologically active compounds (enzymes, hormones, drugs, etc.) bonded to the polymer. The procedure according to the invention enables to prepare porous polymers suitable as separation barriers (membranes) or column packings for gel or affinity chromatography, if the polymerization is carried out in the presence of a divinyl component.

摘要翻译： 本发明涉及基于N-取代的丙烯酰胺，N-取代的甲基丙烯酰胺和N，N-二取代的丙烯酰胺的共聚物及其制备方法，该共聚物是在发生相分离的条件下制备的。 所得共聚物含有反应性基团，并且用作制备与聚合物结合的生物活性化合物（酶，激素，药物等）的中间体。 如果聚合是在二乙烯基组分的存在下进行的，根据本发明的方法能够制备适合作为凝胶或亲和色谱法的分离屏障（膜）或柱填料的多孔聚合物。

公开(公告)号：US4427808A

公开(公告)日：1984-01-24

申请号：US283424

申请日：1981-07-15

申请人： Miroslav Stol ,  Miroslav Tolar ,  Milan Adam ,  Pavel Cefelin ,  Jaroslav Kalal

发明人： Miroslav Stol ,  Miroslav Tolar ,  Milan Adam ,  Pavel Cefelin ,  Jaroslav Kalal

IPC分类号： A61L15/16 ,  A61L15/22 ,  A61L27/00 ,  A61L27/26 ,  A61L29/00 ,  A61L33/00 ,  C08L33/08 ,  C08L89/04 ,  C12N5/00 ,  C07G7/00 ,  C08L89/06 ,  G02C7/04

CPC分类号： C12N5/0068 ,  A61L15/225 ,  A61L27/26 ,  A61L33/0011 ,  C08L33/08 ,  C08L89/04 ,  C12N2533/30 ,  C12N2533/54 ,  Y10S128/08 ,  Y10S525/937

摘要： The invention relates to a composite polymeric material suitable for biological and medical applications and to the method for preparation thereof. The composite material consists of 1-99 wt. % of hydrophilic polymer or copolymer based on methacrylic or acrylic esters, 1-99 wt. % of fibrillar collagen, and up to 2.5 wt. % of a crosslinking agent, based on both polymeric components. The composite material may further comprise biologically active compounds and other auxiliary materials, as fillers and/or plasticizers. The composite material is prepared by dispersing the fibrillar collagen in a solution or a highly swollen dispersion of the synthetic hydrophilic polymer or copolymer in a lyotropic agent and the subsequent removal of the lyotropic agent, thus forming a matrix of the synthetic polymer or copolymer penetrated by fibrillar collagen or vice versa. The composite material may be applied on a solid support or reinforced with glass, plastics, cellulose, or metallic materials.A method for the preparation of the composite material consists in dispersing of fibrillar collagen in a solution or a highly swollen dispersion of the synthetic hydrophilic polymer or copolymer in a lyotropic agent, e.g. in water diluted carboxylic acids, strongly acidified aqueous mixtures of ethanol and methanol, high-concentrated aqueous solutions of lyotropic salts, and high-concentrated aqueous solutions of urea or guanidinium chloride, at temperature not exceeding 37.degree. C., and the subsequent removing of the lyotropic agent from the viscous dispersion at temperature not exceeding 37.degree. C. using the known methods.The crosslinking agent, e.g. trimethylolurea, formaldehyde, acetaldehyde, glutaraldehyde, starch dialdehyde, glyoxal, or Cr(III) salts, may be added in the course of preparation of the dispersion or after removal of the lyotropic agent.

摘要翻译： 本发明涉及适用于生物和医学应用的复合聚合物材料及其制备方法。 复合材料由1-99wt。 基于甲基丙烯酸或丙烯酸酯的亲水性聚合物或共聚物的％，1-99重量％ ％的原纤维胶原蛋白，高达2.5wt。 基于两种聚合物组分的交联剂的％。 复合材料可以进一步包含生物活性化合物和其它辅助材料，作为填料和/或增塑剂。 复合材料通过将原纤维胶原分散在合成的亲水性聚合物或共聚物的溶液或高度溶胀的分散体中的溶液中并随后除去溶致剂来制备，从而形成合成聚合物或共聚物的基体， 纤维胶原蛋白或反之亦然。 复合材料可以施加在固体支撑物上或用玻璃，塑料，纤维素或金属材料增强。 用于制备复合材料的方法在于将原纤维胶原蛋白分散在合成亲水性聚合物或共聚物的溶液或高度溶胀的分散体中的溶解剂中，例如溶于水。 在水中稀释的羧酸，乙醇和甲醇的强酸化水溶液，高浓度的溶致盐水溶液，以及尿素或氯化胍的高浓度水溶液，温度不超过37℃，随后除去 使用已知方法在不超过37℃的粘稠分散体中的溶致剂。 交联剂，例如 三羟甲基脲，甲醛，乙醛，戊二醛，淀粉二醛，乙二醛或Cr（III）盐可以在制备分散体或除去溶解剂后加入。

公开(公告)号：US4332694A

公开(公告)日：1982-06-01

申请号：US98343

申请日：1979-11-29

申请人： Jaroslav Kalal ,  Marie Tlustakova

发明人： Jaroslav Kalal ,  Marie Tlustakova

IPC分类号： C08K9/00 ,  B01J20/32 ,  C08F2/44 ,  C08G83/00 ,  C08K7/24 ,  C08K9/04 ,  C12N11/08 ,  B32B17/10

CPC分类号： C08G83/001 ,  B01J20/10 ,  B01J20/261 ,  B01J20/265 ,  B01J20/267 ,  B01J20/28004 ,  B01J20/28078 ,  B01J20/3021 ,  B01J20/3204 ,  B01J20/327 ,  B01J20/328 ,  B01J20/3282 ,  B01J2220/54 ,  Y10T428/2991 ,  Y10T428/2993 ,  Y10T428/2998 ,  Y10T428/31525

摘要： The invention relates to three-dimensional carriers consisting of inorganic porous material and 0.001-95% of unextractably sorbed reactive polymer of the general formula I: ##STR1## where R.sub.1, R.sub.2, R.sub.4 respectively are hydrogen atom, alkyl with 1-5 carbon atoms, or aryl, and R.sub.3 is the group --COO--(CH.sub.2).sub.n --, and to a method for its preparation. The three-dimensional carriers may be prepared by coating the inorganic porous material with a monomer, which is left to polymerize under the conditions of solution polymerization, while the soluble polymer, which is not bound on the surface of the inorganic material, is removed by extraction.The three-dimensional carrier may also be prepared by depositing a solution of a polymer of general formula I and with a degree of polymerization lower than 10.sup.3 on the inorganic porous material, leaving the two materials in contact with each other, and separating the unbound polymer by extraction.The carriers of inorganic porous material-reactive polymer combine good properties of the inorganic material with the high reactivity of the polymeric coating. An advantage of the carrier is not only the combining of inorganic porous materials with a polymer containing epoxy groups, but also an ample opportunity of modifying the carrier by chemical reactions of the epoxy group. This opportunity may be employed in bonding biologically active compounds, dyes, complex-forming compounds and other low-molecular and high-molecular weight compounds to the carrier.

摘要翻译： 本发明涉及由无机多孔材料组成的三维载体和通式I的不可萃取吸附反应性聚合物的0.001-95％：其中R1，R2，R4分别是氢原子，具有1-5个 碳原子或芳基，并且R 3是基团-COO-（CH 2）n - ，以及其制备方法。 三维载体可以通过用单体涂覆无机多孔材料来制备，该单体在溶液聚合条件下聚合，而不结合在无机材料表面上的可溶性聚合物通过 萃取。 三维载体也可以通过在无机多孔材料上沉积通式I的聚合物和聚合度低于103的聚合物，使两种材料彼此接触并分离出未结合的聚合物 通过提取。 无机多孔材料反应性聚合物的载体将无机材料的良好性能与聚合物涂层的高反应性相结合。 载体的优点不仅在于无机多孔材料与含有环氧基团的聚合物的组合，而且还具有通过环氧基化学反应改性载体的充分机会。 这种机会可以用于将生物活性化合物，染料，络合物形成化合物和其它低分子量和高分子量化合物键合到载体上。

公开(公告)号：US4097470A

公开(公告)日：1978-06-27

申请号：US584887

申请日：1975-06-09

申请人： Jaroslav Drobnik ,  Jindrich Kopecek ,  Jiri Labsky ,  Pavla Rejmanova ,  Josef Exner ,  Jaroslav Kalal

发明人： Jaroslav Drobnik ,  Jindrich Kopecek ,  Jiri Labsky ,  Pavla Rejmanova ,  Josef Exner ,  Jaroslav Kalal

IPC分类号： C08F220/36 ,  C08F220/60 ,  C08F16/28 ,  C08F24/00 ,  C08F210/00

CPC分类号： C08F220/36 ,  C08F220/60 ,  Y10S260/47

摘要： Polymeric form of a biologically active compound containing at least one -NH.sub.2 group in its molecule, adapted for the protracted release of said biologically active compound by enzymatic cleavage of the polymer in vivo in the organism. The active compound is bonded by its -NH.sub.2 group to the carboxylic group of an L-amino acid as for instance, .beta.-phenylalanine, tyrosine, tryptophane, lysine, arginine, glycine, alanine, leucine, citruline or ornithine, which latter is in twin bonded by its amino group to the terminal carboxylic group of the side chain of a substituted amide or ester of acrylic or methacrylic acid, said side chain constituting a linear moiety containing at least 3 carbon atoms. The latter compound or monomer is copolymerized with a hydrophilic monomer such as, N-alkylmethacrylamide, N-alkylacrylamide, N,N-dialkylacrylamide, wherein alkyl has 1-6 carbon atoms and may contain 1 to 3 OH groups, or glycol acrylate or methacrylate alone or in admixture, and which copolymer may contain further monomeric components, for example, cross-linking agents. It is the copolymer which constitutes the subject matter of the invention, i.e., the biologically active substance bearing -NH.sub.2 groups in a form releasable by enzymatic cleavage. The copolymer can also be prepared using as the monomer a compound containing the bonded L-amino acid and in which the terminal carboxylic group has been converted to the reactive ester. The active compound is then bonded to the thusly prepared reactive polymer. The enzymatic release of the active compound bearing -NH.sub.2 groups can be controlled, i.e., regulated by the size of the side chain carrying the L-amino acid.

摘要翻译： 在其分子中含有至少一个-NH 2基团的生物活性化合物的聚合形式，适于通过生物体内的体内酶的裂解来延长所述生物活性化合物的释放。 活性化合物通过其-NH 2基团与L-氨基酸的羧基键合，例如β-苯丙氨酸，酪氨酸，色氨酸，赖氨酸，精氨酸，甘氨酸，丙氨酸，亮氨酸，柠檬酸或鸟氨酸，后者位于 双键通过其氨基键合至取代酰胺或丙烯酸或甲基丙烯酸酯的侧链的末端羧基，所述侧链构成含有至少3个碳原子的直链部分。 后一种化合物或单体与亲水性单体如N-烷基甲基丙烯酰胺，N-烷基丙烯酰胺，N，N-二烷基丙烯酰胺共聚合，其中烷基具有1-6个碳原子并且可以含有1至3个OH基团，或二醇丙烯酸酯或甲基丙烯酸酯 单独或混合，并且哪种共聚物可以含有其它单体组分，例如交联剂。 构成本发明主题的共聚物，即具有可通过酶裂解释放形式的-NH 2基团的生物活性物质。 共聚物也可以使用含有键合的L-氨基酸的化合物作为单体制备，并且其中末端羧基已经转化成反应性酯。 然后将活性化合物与如此制备的反应性聚合物结合。 可以控制带有-NH 2基团的活性化合物的酶促释放，即通过携带L-氨基酸的侧链的大小来调节。

公开(公告)号：US4563490A

公开(公告)日：1986-01-07

申请号：US553859

申请日：1983-11-18

申请人： Miroslav Stol ,  Miroslav Tolar ,  Milan Adam ,  Pavel Cefelin ,  Jaroslav Kalal

发明人： Miroslav Stol ,  Miroslav Tolar ,  Milan Adam ,  Pavel Cefelin ,  Jaroslav Kalal

IPC分类号： A61L15/16 ,  A61L15/22 ,  A61L27/00 ,  A61L27/26 ,  A61L29/00 ,  A61L33/00 ,  C08L33/08 ,  C08L89/04 ,  C12N5/00 ,  C08L89/06

CPC分类号： C12N5/0068 ,  A61L15/225 ,  A61L27/26 ,  A61L33/0011 ,  C08L33/08 ,  C08L89/04 ,  C12N2533/30 ,  C12N2533/54 ,  Y10S128/08 ,  Y10S525/937

摘要： The invention relates to a composite polymeric material suitable for biological and medical applications and to the method for preparation thereof. The composite material consists of 1-99 wt. % of hydrophilic polymer or copolymer based on methacrylic or acrylic esters, 1-99 wt. % of fibrillar collagen, and up to 2.5 wt. % of a crosslinking agent, based on both polymeric components. The composite material may further comprise biologically active compounds and other auxiliary materials, as fillers and/or plasticizers. The composite material is prepared by dispersing the fibrillar collagen in a solution or a highly swollen dispersion of the synthetic hydrophilic polymer or copolymer in a lytropic agent and the subsequent removal of the lyotropic agent, thus forming a matrix of the synthetic polymer or copolymer penetrated by fibrillar collagen or vice versa. The composite material may be applied on a solid support or reinforced with glass, plastics, cellulose, or metallic materials.

摘要翻译： 本发明涉及适用于生物和医学应用的复合聚合物材料及其制备方法。 复合材料由1-99wt。 基于甲基丙烯酸或丙烯酸酯的亲水性聚合物或共聚物的％，1-99重量％ ％的原纤维胶原蛋白，高达2.5wt。 基于两种聚合物组分的交联剂的％。 复合材料可以进一步包含生物活性化合物和其它辅助材料，作为填料和/或增塑剂。 复合材料通过将原纤维胶原分散在合成亲水性聚合物或共聚物的溶液或高度溶胀的分散体中的溶剂中制备，随后除去溶致剂，从而形成合成聚合物或共聚物的基质， 纤维胶原蛋白或反之亦然。 复合材料可以施加在固体支撑物上或用玻璃，塑料，纤维素或金属材料增强。

公开(公告)号：US4166804A

公开(公告)日：1979-09-04

申请号：US842273

申请日：1977-10-14

申请人： Miroslav Bleha ,  Zdenek Plichta ,  Eva Votavova ,  Jaroslav Kalal

发明人： Miroslav Bleha ,  Zdenek Plichta ,  Eva Votavova ,  Jaroslav Kalal

IPC分类号： G01N31/22 ,  G01N21/08 ,  C08F8/30 ,  C08J9/00

CPC分类号： G01N31/221

摘要： Polymeric color pH indicators are prepared which are insoluble in the measured aqueous medium and show a certain range of color change. These polymeric indicators are the product of copolymerization of a hydrophilic comonomer, selected from esters, amides and N-substituted amides of acrylic and methacrylic acid, with 0.1- 30 wt.% of a comonomer. The comonomer forms the pH-indicating color center by a subsequent coupling with a suitable diazonium salt or a passive component. Vinylic monomers comprising an aromatic system in the molecule are suitable as the functional comonomers. The indicators are prepared by radical copolymerization of the comonomers either in a suspension or in a solution, followed by the subsequent coupling with a diazonium compound, or diazotizing and coupling with a passive component, to obtain the pH-indicating sites of polymer. The product is in the form of small spherical macroporous particles suitable for pH indication in flow-through column processes, in small volumes, or on a microscope stage, or in the form of a solution applicable as a paint and indicating the pH of vessels, reactors, etc. coated therewith, or useful for application to inert carriers.

摘要翻译： 制备聚合物颜色pH指示剂，其不溶于测量的水性介质并显示一定范围的颜色变化。 这些聚合物指示剂是选自丙烯酸和甲基丙烯酸的酯，酰胺和N-取代的酰胺的亲水共聚单体与0.1-30重量％的共聚单体共聚的产物。 共聚单体通过与合适的重氮盐或无源组分的后续偶联形成pH-指示颜色中心。 分子中包含芳族体系的乙烯基单体适用作为功能性共聚单体。 指示剂通过在悬浮液或溶液中共聚单体的自由基共聚制备，随后与重氮化合物偶联，或与无源组分重氮化并偶联，得到聚合物的pH指示位点。 该产品是适于在流通柱方法中以小体积或在显微镜载物台上的pH指示的小球形大孔颗粒的形式，或以可用作涂料的溶液形式并指示血管的pH值， 反应器等，或者可用于惰性载体。

公开(公告)号：US4093602A

公开(公告)日：1978-06-06

申请号：US623964

申请日：1975-10-20

申请人： Jaroslav Kalal ,  Eva Zurkova ,  Frantisek Svec

发明人： Jaroslav Kalal ,  Eva Zurkova ,  Frantisek Svec

IPC分类号： C08F2/00 ,  C08F2/18 ,  C08F12/00 ,  C08F16/00 ,  C08F16/34 ,  C08F16/38 ,  C08F20/00 ,  C08F20/10 ,  C08F20/42 ,  C08F24/00 ,  C08F216/34 ,  C08G2/00 ,  C08G2/26 ,  C08G12/04

CPC分类号： C08F216/34 ,  Y10T428/2982

摘要： Three-dimensional polymeric material in the form of spherical particles of diameter .ltoreq.3 mm and containing up to 40% of free aldehyde groups which exhibits a measurable specific surface area is prepared by copolymerization of an aldehyde monomer R.sub.1 CH.dbd.C(CH.dbd.O)R.sub.2, where R.sub.1 is H, C.sub.1-5 alkyl, aryl or furyl and R.sub.2 is H, C.sub.1-5 alkyl, halogen, CN, phenyl or furyl, with a crosslinking agent in the aqueous dispersion phase. The dispersion contains 1 - 25% of a component reducing the monomer solubility in water, which is either an inorganic salt of alkali metal or alkaline earth metal or a water-soluble alcohol. The crosslinking agent used as comonomer is divinylbenzene, diester CH.sub.2 .dbd.C(R.sub.1)COOR.sub.2 OCOC(R.sub.1).dbd.CH.sub.2 (R.sub.1 .dbd. H, C.sub.1-10 alkyl or halogen; R.sub.2 .dbd. C.sub.1-10 alkylene or hydroxyalkylene), or diamide CH.sub.2 .dbd.C(R.sub.1)CONHR.sub.2 NHCOC(R.sub.1).dbd.CH.sub.2 (R.sub.1 .dbd. H, C.sub.1-10 alkyl or halogen; R.sub.2 .dbd. C.sub.1-10 alkylene or phenylene). The material may be used in continuous column processes, e.g. in catalysis of organic syntheses, separation of amines, and immobilization of compounds which contain primary amino groups.

摘要翻译： 通过醛单体R 1 CH = C（CH = O）的共聚制备具有直径≤3mm并且含有高达40％表现出可测量比表面积的游离醛基的直链形式的三维聚合物材料 ）R2，其中R1是H，C1-5烷基，芳基或呋喃基，R2是H，C1-5烷基，卤素，CN，苯基或呋喃基，在水分散相中与交联剂反应。 分散体含有1-25％的降低单体在水中的溶解度的组分，其是碱金属或碱土金属的无机盐或水溶性醇。 用作共聚单体的交联剂是二乙烯基苯，二酯CH2 = C（R1）COOR2OCOC（R1）= CH2（R1 = H，C1-10烷基或卤素; R2 = C1-10亚烷基或羟基亚烷基）或二酰胺CH2 = C（ R1）CONHR2NHCOC（R1）= CH2（R1 = H，C1-10烷基或卤素; R2 = C1-10亚烷基或亚苯基）。 该材料可以用于连续柱方法，例如。 在有机合成的催化，胺的分离和含有伯氨基的化合物的固定化。

公开(公告)号：US4634604A

公开(公告)日：1987-01-06

申请号：US622671

申请日：1984-06-20

申请人： Marie Tlustakova ,  Jiri Horak ,  Josef Vavrouch ,  Jiri Kulisek ,  Jaroslav Kalal

发明人： Marie Tlustakova ,  Jiri Horak ,  Josef Vavrouch ,  Jiri Kulisek ,  Jaroslav Kalal

IPC分类号： B01J20/32 ,  B01J13/02

CPC分类号： B01J20/261 ,  B01J20/264 ,  B01J20/267 ,  B01J20/28004 ,  B01J20/28047 ,  B01J20/3092 ,  B01J20/321 ,  B01J20/327 ,  B01J20/3276 ,  B01J20/3282 ,  B01J2220/58 ,  Y10T428/2987 ,  Y10T428/2998

摘要： The invention pertains to the method for producing a biocompatible layer on the surface of particles of porous synthetic sorbents.An object of the invention consists in the method for producing a biocompatible layer on the surface of particles of porous synthetic sorbents by action of a solution of biocompatible polymer of acrylate or methacrylate type, or of its monomer in the presence of polymerization initiators, on a suspension of sorbent, which is agitated with steam.The method according to the invention renders a material, the sorption capacity of which is entirely retained. This is due to water, which remains enclosed in the pores of sorbent and enables the sorption of toxins also inside the gel particles. In addition, steam can be prepared completely apyrogenic and thus to secure that the sorbents remain clean inside. Clinical tests reveal that the sorbents coated by the method according to the invention have an excellent hemocompatibility.

摘要翻译： 本发明涉及在多孔合成吸附剂颗粒表面上生产生物相容层的方法。 本发明的目的在于通过在聚合引发剂存在下，通过丙烯酸酯或甲基丙烯酸酯类或其单体的生物相容性聚合物溶液的作用，在多孔合成吸附剂颗粒的表面上生产生物相容层的方法， 用蒸汽搅拌的吸附剂的悬浮液。 根据本发明的方法使得材料的吸附能力被完全保留。 这是由于水，其保持封闭在吸附剂的孔中，并且能够将毒素吸附在凝胶颗粒内。 此外，蒸汽可以完全制备成apyrogenic，从而确保吸附剂在内部保持清洁。 临床试验表明，通过本发明方法包被的吸附剂具有优异的血液相容性。

公开(公告)号：US4031037A

公开(公告)日：1977-06-21

申请号：US551271

申请日：1975-02-20

申请人： Jaroslav Kalal ,  Jiri Coupek ,  Svatopluk Pokorny ,  Frantisek Svec ,  Karel Bouchal

发明人： Jaroslav Kalal ,  Jiri Coupek ,  Svatopluk Pokorny ,  Frantisek Svec ,  Karel Bouchal

IPC分类号： B01J39/12 ,  C08F8/40 ,  C08G59/40

CPC分类号： C08G59/4071 ,  B01J39/12 ,  C08F8/40

摘要： Organic three-dimensional polymeric gel-like materials containing covalently bonded phosphoric acid or a derivative thereof and a method for their manufacture. The bonding is accomplished by the reaction of the free hydroxy or epoxide groups in the homogeneous or macroporous gel-like matrix with the H.sub.3 PO.sub.4, P.sub.2 O.sub.5, phosphorus pentahalide and oxyhalide. The halide containing groups may then be hydrolyzed to form acid groups which then may be modified to form complex compounds by reaction with Lewis acids. The gel material may serve as a strongly acidic cation exchanger, catalyst or polymer reagent.

摘要翻译： 含有共价键合的磷酸或其衍生物的有机三维聚合物凝胶状材料及其制造方法。 通过均相或大孔凝胶状基质中的游离羟基或环氧基团与H 3 PO 4，P 2 O 5，五卤化磷和卤氧化物的反应来实现键合。 然后可以将含卤化物基团水解形成酸基团，然后可以通过与路易斯酸反应来改性以形成络合物。 凝胶材料可以用作强酸性阳离子交换剂，催化剂或聚合物试剂。

公开(公告)号：US4622367A

公开(公告)日：1986-11-11

申请号：US807281

申请日：1985-12-10

申请人： Daniel Horak ,  Marie Metalova ,  Frantisek Svec ,  Jaroslav Drobnik ,  Jaroslav Kalal ,  Michail I. Kuzin ,  Arnold A. Adamian ,  Jurij V. Moiseiev ,  Klara Z. Gumargalieva

发明人： Daniel Horak ,  Marie Metalova ,  Frantisek Svec ,  Jaroslav Drobnik ,  Jaroslav Kalal ,  Michail I. Kuzin ,  Arnold A. Adamian ,  Jurij V. Moiseiev ,  Klara Z. Gumargalieva

IPC分类号： C08F8/00 ,  A61B19/00 ,  A61K49/04 ,  C08F8/30 ,  C08F8/32

CPC分类号： C08F8/30 ,  A61B90/39 ,  Y10T428/2982

摘要： The invention pertains to X-ray contrast spherical hydrogel particles based on polymers and copolymers of acrylates and methacrylates and to a method of their preparation.The subject of this invention are X-ray contrast spherical hydrogel particles based on polymers and copolymers of acrylates and methacrylates characterized by the particles of spherical form with diameter 0.2 to 2 mm, which strongly swell in water and contain a derivative of amino-triiodobenzoic acid of general formula I, ##STR1## where R.sup.1,R.sup.2 is hydrogen, acyl group with 1 to 3 carbon atoms or alkyl with 1 to 10 carbon atoms and X is halogen, --OH or --NH(CH.sub.2).sub.n NH.sub.2, where n=1-6, covalently bonded to the polymer skeleton.A method for preparation of X-ray contrast hydrogel particles according to the invention in which hydrogel particles, containing hydroxyl or epoxide groups localized on side chains of the polymer skeleton, are allowed to swell in an excess of a solvent chosen from the group comprising dioxane, dimethylacetamide, dimethylformamide, tetrahydrofuran and dimethylsulfoxide, which contains the dissolved derivative of amino-triiodobenzoic acid of the general formula I, optionally together with a compound reacting with hydrogen halogenide formed, which is selected, for example, from the group comprising tertiary amines, the dispersion is heated to 100.degree. C. at utmost and allowed to react for 150 hours at utmost, the solid phase is separated and freed of soluble substances by washing.The procedure according to the invention provides spherical hydrogels with X-ray contrast properties without changing their other properties substantial for application in medical practice.

摘要翻译： 本发明涉及基于丙烯酸酯和甲基丙烯酸酯的聚合物和共聚物的X射线对比球形水凝胶颗粒及其制备方法。 本发明的主题是基于丙烯酸酯和甲基丙烯酸酯的聚合物和共聚物的X射线对比球形水凝胶颗粒，其特征在于直径为0.2至2mm的球形颗粒，其在水中强烈溶胀并含有氨基 - 三碘苯甲酸的衍生物 通式I，其中R 1，R 2是氢，具有1至3个碳原子的酰基或具有1至10个碳原子的烷基，X是卤素，-OH或-NH（CH 2）n NH 2，其中n = 共价键合到聚合物骨架上。 制备根据本发明的X射线对比度水凝胶颗粒的方法，其中将含有位于聚合物骨架的侧链上的羟基或环氧基团的水凝胶颗粒在过量的溶剂中溶胀，所述溶剂选自二恶烷 ，二甲基乙酰胺，二甲基甲酰胺，四氢呋喃和二甲基亚砜，其含有溶解的通式I的氨基 - 三碘苯甲酸的衍生物，任选地与形成的卤化氢反应的化合物，其选自例如叔胺， 将分散体最大程度地加热至100℃，最大限度地反应150小时，分离固相并通过洗涤除去可溶性物质。 根据本发明的方法提供具有X射线对比性质的球形水凝胶，而不改变其在医学实践中应用的实质性的其他性质。