Polyalkoxylated alcohols as excipients for pharmaceutical compositions
    12.
    发明授权
    Polyalkoxylated alcohols as excipients for pharmaceutical compositions 有权
    聚烷氧基化醇作为药物组合物的赋形剂

    公开(公告)号:US09592294B2

    公开(公告)日:2017-03-14

    申请号:US14649721

    申请日:2014-01-13

    Abstract: The present invention relates to the use of polyalkoxylated alcohols of the formula R—O-(AO)—H, wherein R is a substituted or unsubstituted alkyl, alkenyl, alkynyl, aryl, aralkyl or heterocyclic group having 7 to 25 carbon atoms, (AO) is a polyoxyalkylene moiety of the composition (BO)m(EO)n(DO)r with random or blockwise arrangement of the constituting oxyalkylene units, wherein m, n and r represent the average number of oxybutylene (BO) units, oxyethylene (EO) units and oxyalkylene units derived from at least one epoxide selected from styrene oxide and alkylene oxides having from 5 to 10 carbon atoms (DO) per molecule of the polyalkoxylated alcohol, respectively, m being a number greater than or equal to 1, n being a number greater than or equal to 1 and r being a number in the range from 0 to 50 under the proviso that (m+n+r) is less than or equal to 200 and the ratio n/(m+r) is in the range of 1 to 20, as excipients in pharmaceutical compositions. Said polyalkoxylated alcohols enable very effective solubilization of poorly soluble active pharmaceutical ingredients in aqueous media. Solid or semi-solid pharmaceutical compositions comprising one or more such polyalkoxylated alcohol combined with at least one active pharmaceutical ingredient are further long term stable under typical storage conditions and can be readily provided in various dosage forms such as tablets and filled capsules.

    Abstract translation: 本发明涉及式R-O-(AO)-H的聚烷氧基化醇的用途,其中R是具有7至25个碳原子的取代或未取代的烷基,烯基,炔基,芳基,芳烷基或杂环基,( AO)是组成(BO)m(EO)n(DO)r的聚氧化烯部分,其具有构成的氧化烯单元的无规或块状排列,其中m,n和r表示氧化丁烯(BO)单元的平均数,氧化乙烯 (EO)单元和衍生自至少一种选自氧化苯乙烯和每分子聚烷氧基化醇具有5至10个碳原子的氧化烯(DO)的环氧化物的氧化烯单元,m分别大于或等于1, n是大于或等于1的数,r是0至50的数,条件是(m + n + r)小于或等于200,并且比率n /(m + r) 在1至20的范围内,作为药物组合物中的赋形剂。 所述聚烷氧基化的醇使得难溶性活性药物成分非常有效地溶解在水性介质中。 包含一种或多种这样的多烷氧基化醇与至少一种活性药物成分组合的固体或半固体药物组合物在典型的储存条件下进一步长期稳定,并且可以容易地以各种剂型例如片剂和填充的胶囊提供。

    Dispersion comprising an esterified cellulose ether

    公开(公告)号:US10383944B2

    公开(公告)日:2019-08-20

    申请号:US15129505

    申请日:2015-03-03

    Abstract: An aqueous composition useful for producing capsules shells comprises a) at least one dispersed esterified cellulose ether comprising (i) groups of the formula —C(O)—R—COOA or (ii) a combination of aliphatic monovalent acyl groups and groups of the formula —C(O)—R—COOA, wherein R is a divalent aliphatic or aromatic hydrocarbon group and A is hydrogen or a cation, and b) from 0.05 to 20 percent of at least one salt of a fatty acid, based on the weight of the dispersed esterified cellulose ether, wherein the median particle size, d50, of the dispersed esterified cellulose ether particles is up to 7 micrometers, such median particle size (d50) being the size at which 50 mass percent of the particles have a smaller equivalent diameter and 50 mass percent have a larger equivalent diameter.

    Dispersion comprising a partially neutralized esterified cellulose ether

    公开(公告)号:US10179110B2

    公开(公告)日:2019-01-15

    申请号:US15308792

    申请日:2015-04-28

    Abstract: An aqueous composition comprising at least 10 weight percent of a dispersed esterified cellulose ether, based on the total weight of the aqueous composition, wherein the esterified cellulose ether comprises (i) groups of the formula —C(O)—R—COOH or (ii) a combination of aliphatic monovalent acyl groups and groups of the formula —C(O)—R—COOH, R being a divalent aliphatic or aromatic hydrocarbon group, and at least a part of the groups —C(O)—R—COOH are neutralized with an ammonium salt of carbonic acid, formic acid or acetic acid, and wherein d90 of the dispersed esterified cellulose ether particles is up to 10 micrometers, d90 being the diameter where 90 mass percent of the particles have a smaller equivalent diameter and the other 10 mass percent have a larger equivalent diameter, is useful for preparing coating dosage forms including tablets, capsules and others, or for the formation of capsules shells.

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