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    Method of preparation and isolation of betulin diacetate from birch bark from paper mills and its optical processing to betulin
    1.
    发明授权
    Method of preparation and isolation of betulin diacetate from birch bark from paper mills and its optical processing to betulin 有权
    从桦木树皮制备和分离桦木双乙酸酯的方法，并将其光学加工与桦木醇分离

    公开(公告)号：US08093413B2

    公开(公告)日：2012-01-10

    申请号：US12522339

    申请日：2008-01-09

    申请人： Jan Sarek ,  Michal Svoboda ,  Marian Hajduch

    发明人： Jan Sarek ,  Michal Svoboda ,  Marian Hajduch

    IPC分类号： C07J53/00

    CPC分类号： C07J63/008 ,  Y02P20/544

    摘要： The invention relates to a method of preparation and isolation of betulin diacetate from birch bark from paper mills and its optional processing to betulin, wherein the birch bark is ground, mixed with two- to twenty-fold excess volume of water and is stirred so that all birch bark is dipped, then the fraction of the birch bark which floats on the surface is collected, said collected fraction is dried at the temperature in the range of from 50 to 85° C. and the betulin contained in the dried birch bark is then subjected to an acetylation reaction, after the acetylation the birch bark is dried at the temperature of from 50 to 100° C. and the formed betulin diacetate is then isolated from the birch bark by supercritical extraction of the birch bark with carbon dioxide at the pressure of 28-35 MPa and the temperature of from 50 to 100° C. and subsequently, the supercritical extract is recrystallized for direct use or for further processing. The further processing can be basic hydrolysis of the re-crystallized betulin diacetate to betulin.

    摘要翻译： 本发明涉及从造纸厂的桦树皮制备和分离桦木二乙酸酯的方法及其对桦木醇的任选加工，其中将桦树皮研磨，与二至二十倍体积的水混合并搅拌，使得 将所有桦树皮浸渍，然后收集漂浮在表面上的桦树皮的部分，收集的部分在50至85℃的温度范围内干燥，干燥的桦树皮中含有的桦木糖是 然后进行乙酰化反应，乙酰化后，桦木树皮在50〜100℃的温度下干燥，然后通过超临界萃取桦树皮与二氧化碳从桦树皮中分离形成的桦木酸二乙酸酯 压力为28-35MPa，温度为50-100℃，然后将超临界萃取物重结晶直接使用或进一步加工。 进一步的处理可以是重结晶的桦木醇二乙酸酯至桦木醇的碱性水解。

    METHOD OF PREPARATION AND ISOLATION OF BETULIN DIACETATE FROM BIRCH BARK FROM PAPER MILLS AND ITS OPTIONAL PROCESSING TO BETULIN
    3.
    发明申请
    METHOD OF PREPARATION AND ISOLATION OF BETULIN DIACETATE FROM BIRCH BARK FROM PAPER MILLS AND ITS OPTIONAL PROCESSING TO BETULIN 有权
    制备和分离来自纸浆的BIRCH BARK的白芥子酸酯的方法及其对BETULIN的可选处理

    公开(公告)号：US20090318719A1

    公开(公告)日：2009-12-24

    申请号：US12522339

    申请日：2008-01-09

    申请人： Jan Sarek ,  Michal Svoboda ,  Marian Hajduch

    发明人： Jan Sarek ,  Michal Svoboda ,  Marian Hajduch

    IPC分类号： C07J53/00

    CPC分类号： C07J63/008 ,  Y02P20/544

    摘要： The invention relates to a method of preparation and isolation of betulin diacetate from birch bark from paper mills and its optional processing to betulin, wherein the birch bark is ground, mixed with two- to twenty-fold excess volume of water and is stirred so that all birch bark is dipped, then the fraction of the birch bark which floats on the surface is collected, said collected fraction is dried at the temperature in the range of from 50 to 85° C. and the betulin contained in the dried birch bark is then subjected to an acetylation reaction, after the acetylation the birch bark is dried at the temperature of from 50 to 100° C. and the formed betulin diacetate is then isolated from the birch bark by supercritical extraction of the birch bark with carbon dioxide at the pressure of 28-35 MPa and the temperature of from 50 to 100° C. and subsequently, the supercritical extract is recrystallized for direct use or for further processing. The further processing can be basic hydrolysis of the re-crystallized betulin diacetate to betulin.

    摘要翻译： 本发明涉及从造纸厂的桦树皮制备和分离桦木二乙酸酯的方法及其对桦木醇的任选加工，其中将桦树皮研磨，与二至二十倍体积的水混合并搅拌，使得 将所有桦树皮浸渍，然后收集漂浮在表面上的桦树皮的部分，收集的部分在50至85℃的温度范围内干燥，干燥的桦树皮中含有的桦木糖是 然后进行乙酰化反应，乙酰化后，桦木树皮在50〜100℃的温度下干燥，然后通过超临界萃取桦树皮与二氧化碳从桦树皮中分离形成的桦木酸二乙酸酯 压力为28-35MPa，温度为50-100℃，然后将超临界萃取物重结晶直接使用或进一步加工。 进一步的处理可以是重结晶的桦木醇二乙酸酯至桦木醇的碱性水解。

    PHARMACEUTICAL COMPOSITION CONTAINING TAXANE DERIVATIVE DESTINED FOR THE PREPARATION OF AN INFUSION SOLUTION, METHOD OF PREPARATION THEREOF AND USE THEREOF
    4.
    发明申请
    PHARMACEUTICAL COMPOSITION CONTAINING TAXANE DERIVATIVE DESTINED FOR THE PREPARATION OF AN INFUSION SOLUTION, METHOD OF PREPARATION THEREOF AND USE THEREOF 审中-公开
    含有衍生物的药物组合物，用于制备输注溶液，其制备方法及其用途

    公开(公告)号：US20090156660A1

    公开(公告)日：2009-06-18

    申请号：US12299230

    申请日：2007-03-26

    申请人： Michal Svoboda ,  Xenia Svobodova ,  Martin Potucek ,  Vieroslav Kratky ,  Pavel Hanzlik

    发明人： Michal Svoboda ,  Xenia Svobodova ,  Martin Potucek ,  Vieroslav Kratky ,  Pavel Hanzlik

    IPC分类号： A61K31/337

    CPC分类号： C07D305/14 ,  A61K9/0019 ,  A61K31/337 ,  A61K47/10 ,  A61K47/12 ,  A61K47/26

    摘要： A pharmaceutical composition containing a taxane derivative, destined for the preparation of an infusion solution for administration to patients, containing a concentrate consisting of a pharmaceutically effective amount of docetaxel, a suitable solvent, which is preferably ethanol, a surfactant, which is polysorbate 80 and a pharmaceutically effective amount of an appropriate buffer; and optionally a co-solvent, consisting of an aqueous solution of a pharmaceutically effective amount of polysorbate 80 and optionally suitable organic solvent and/or a pharmaceutically effective amount of an appropriate buffer. This composition shows an excellent chemical and physical stability. The invention includes also a method of preparation of the pharmaceutical composition and the use thereof.

    摘要翻译： 一种含有紫杉烷衍生物的药物组合物，其用于制备用于给予患者的输注溶液，其含有由药学有效量的多西他赛组成的浓缩物，优选为乙醇的合适溶剂，作为聚山梨醇酯80的表面活性剂和 药学有效量的适当缓冲液; 和任选的共溶剂，由药学有效量的聚山梨酯80的水溶液和任选合适的有机溶剂和/或药学有效量的适当的缓冲剂组成。 该组合物显示出优异的化学和物理稳定性。 本发明还包括制备药物组合物的方法及其用途。

    Method of Production of Fine-Crystalline Mixture Containing Non-Steroid Anti-Inflammatory Drug, Fine-Crystalline Mixture Obtainable by this Method and Solid Pharmaceutical Composition Containing this Mixture
    6.
    发明申请
    Method of Production of Fine-Crystalline Mixture Containing Non-Steroid Anti-Inflammatory Drug, Fine-Crystalline Mixture Obtainable by this Method and Solid Pharmaceutical Composition Containing this Mixture 审中-公开
    包含非类固醇抗炎药物的微晶混合物的制造方法，该方法可获得的微晶混合物和含有该混合物的固体药物组合物

    公开(公告)号：US20080233187A1

    公开(公告)日：2008-09-25

    申请号：US12063845

    申请日：2006-08-10

    申请人： Michal Svoboda ,  Xenia Svobodova

    发明人： Michal Svoboda ,  Xenia Svobodova

    IPC分类号： A61K31/192 ,  A61K9/28 ,  A61K9/48 ,  A61P29/00

    CPC分类号： A61K9/19 ,  A61K9/1611 ,  A61K9/1635 ,  A61K9/1652 ,  A61K9/167 ,  A61K9/1688 ,  A61K9/2054 ,  A61K31/192

    摘要： The invention concerns a method of production of a fine-crystalline mixture containing a non-steroid anti-inflammatory drug and an auxiliary substance, wherein a coarse-crystalline substance from the group of non-steroid anti-inflammatory drugs is dissolved in a solvent at an increased temperature, the solution is subsequently distributed at rapid chilling into a cooling liquid containing the auxiliary substance, said cooling liquid being placed in an ice bath, and the product is then filtered off and dried. It further concerns the fine-crystalline mixture of the non-steroid anti-inflammatory drug and the auxiliary substance that can be obtained by the said method. The invention further concerns a solid pharmaceutical composition, having substantially improved dissolution properties, which contains 60 to 78% w/w of the fine-crystalline mixture, 17 to 40% w/w of microcrystalline cellulose, colloidal silicon dioxide in an amount of up to 0.3% w/w, a disintegrant in an amount of up to 4% w/w and optionally a surface active compound in an amount of up to 0.1% w/w. This solid pharmaceutical composition can be filled into capsules or used for the preparation of tablets.

    摘要翻译： 本发明涉及一种生产含有非类固醇抗炎药物和辅助物质的细晶混合物的方法，其中来自非类固醇抗炎药物组的粗结晶物质溶于溶剂中 温度升高，随后将溶液快速冷却分配到含有辅助物质的冷却液中，将所述冷却液置于冰浴中，然后将产物过滤并干燥。 还涉及可以通过所述方法获得的非类固醇抗炎药物和辅助物质的微晶混合物。 本发明还涉及具有显着改善的溶解性质的固体药物组合物，其含有60至78％w / w的细晶混合物，17至40％w / w的微晶纤维素，胶体二氧化硅的量为上 至0.3％w / w，高达4％w / w的崩解剂和任选的表面活性化合物，其量为至多0.1％w / w。 该固体药物组合物可以填充到胶囊中或用于制备片剂。

    Stable, palatable syrup containing ibuprofen and method of its preparation
    8.
    发明申请
    Stable, palatable syrup containing ibuprofen and method of its preparation 审中-公开
    稳定，可口的糖浆含布洛芬及其制备方法

    公开(公告)号：US20070154497A1

    公开(公告)日：2007-07-05

    申请号：US10588870

    申请日：2005-02-15

    申请人： Michal Svoboda ,  Xenia Svobodova

    发明人： Michal Svoboda ,  Xenia Svobodova

    IPC分类号： A61K31/724 ,  A61K31/192 ,  A61K9/00

    CPC分类号： B82Y5/00 ,  A61K9/0095 ,  A61K31/19 ,  A61K47/6951

    摘要： The invention concerns stable, palatable syrups for oral administration, containing S(+)-ibuprofen, hydroxypropyl beta-cyclodextrin, at least one sweetener and water, optionally essential oils. It also includes methods of preparation of the syrups of the invention, wherein crystalline S(+)-ibuprofen is dissolved in a hydroxypropyl beta-cyclodextrin aqueous solution and the final concentration of S(+)-ibuprofen is adjusted as desired by addition of an aqueous solution of sweeteners or a mixture of sweeteners and optionally of water. If the syrup of the invention contains essential oils, it is prepared by dissolving of crystalline S(+)-ibuprofen in a hydroxypropyl beta-cyclodextrin aqueous solution, combining the resulting solution with an essential oil solution in sweetener/mixture of sweeteners, preferably in a mixture of glycerin and 70% sorbitol aqueous solution, and adjusting the final concentration as desired by addition of aqueous solution of sweeteners or mixture of sweeteners and optionally of water.

    摘要翻译： 本发明涉及用于口服给药的稳定可口的糖浆，其含有S（+） - 布洛芬，羟丙基β-环糊精，至少一种甜味剂和水，任选的精油。 它还包括制备本发明糖浆的方法，其中将结晶S（+） - 布洛芬溶解在羟丙基β-环糊精水溶液中，并根据需要通过加入S（+） - 布洛芬来调节最终浓度的S（+） - 布洛芬 甜味剂的水溶液或甜味剂和任选的水的混合物。 如果本发明的糖浆含有精油，则通过将结晶S（+） - 布洛芬溶解在羟丙基β-环糊精水溶液中制备，将所得溶液与甜味剂/甜味剂混合物中的精油溶液 甘油和70％山梨糖醇水溶液的混合物，并通过加入甜味剂或甜味剂和任选的水混合物的水溶液来调节最终浓度。