PH-dependent controlled release pharmaceutical opioid composition with resistance against the influence of ethanol

    公开(公告)号:US09757343B2

    公开(公告)日:2017-09-12

    申请号:US13062591

    申请日:2008-09-24

    IPC分类号: A61K9/50

    CPC分类号: A61K9/5078

    摘要: The invention relates to a pH-dependent controlled release pharmaceutical composition, comprising a core, and an opioid, wherein the core is coated at least by one coating layer, controlling the release of the pharmaceutical composition, wherein the coating layer comprises a polymer mixture of i) 40-95% by weight, based on dry weight of the polymer mixture, of at least one water insoluble essentially neutral vinyl polymer, and ii) 5-60% by weight, based on dry weight of the polymer mixture, of at least one anionic polymer or copolymer, which is insoluble in a buffered medium below pH 4.0 and soluble at least in the range from pH 7.0 to pH 8.0, characterized in that the coating layer further comprises 110 to 250% by weight of a non-porous inert lubricant, 1 to 35% by weight of a neutral cellulosic compound and 1 to 25% by weight of an emulsifier, each calculated on dry weight of the polymer mixture.

    PH-DEPENDENT CONTROLLED RELEASE PHARMACEUTICAL OPIOID COMPOSITION WITH RESISTANCE AGAINST THE INFLUENCE OF ETHANOL
    3.
    发明申请
    PH-DEPENDENT CONTROLLED RELEASE PHARMACEUTICAL OPIOID COMPOSITION WITH RESISTANCE AGAINST THE INFLUENCE OF ETHANOL 有权
    PH依赖性控释药物抗药性组合物对乙醇的影响

    公开(公告)号:US20110217383A1

    公开(公告)日:2011-09-08

    申请号:US13062591

    申请日:2008-09-24

    CPC分类号: A61K9/5078

    摘要: The invention relates to a pH-dependent controlled release pharmaceutical composition, comprising a core, and an opioid, wherein the core is coated at least by one coating layer, controlling the release of the pharmaceutical composition, wherein the coating layer comprises a polymer mixture of i) 40 95% by weight, based on dry weight of the polymer mixture, of at least one water insoluble essentially neutral vinyl polymer, and ii) 5 60% by weight, based on dry weight of the polymer mixture, of at least one anionic polymer or copolymer, which is insoluble in a buffered medium below pH 4.0 and soluble at least in the range from pH 7.0 to pH 8.0, characterized in that the coating layer further comprises 110 to 250 % by weight of a non-porous inert lubricant, 1 to 35 % by weight of a neutral cellulosic compound and 1 to 25 % by weight of an emulsifier, each calculated on dry weight of the polymer mixture.

    摘要翻译: 本发明涉及一种pH依赖性控释药物组合物,其包含核心和阿片样物质,其中所述核心至少涂覆一层涂层,以控制药物组合物的释放,其中所述涂层包含: i)40 95重量%,基于聚合物混合物的干重,至少一种水不溶性基本上中性的乙烯基聚合物,和ii)基于聚合物混合物的干重计,60重量%的至少一种 阴离子聚合物或共聚物,其不溶于低于pH 4.0的缓冲介质,并且至少可溶于pH 7.0至pH 8.0,其特征在于,所述涂层还包含110至250重量%的无孔惰性润滑剂 ,1至35重量%的中性纤维素化合物和1至25重量%的乳化剂,其各自以聚合物混合物的干重计算。

    PH-DEPENDENT CONTROLLED RELEASE PHARMACEUTICAL COMPOSITION FOR NON-OPIOIDS WITH RESISTANCE AGAINST THE INFLUENCE OF ETHANOL
    4.
    发明申请
    PH-DEPENDENT CONTROLLED RELEASE PHARMACEUTICAL COMPOSITION FOR NON-OPIOIDS WITH RESISTANCE AGAINST THE INFLUENCE OF ETHANOL 审中-公开
    对依赖于乙醇的影响的非依赖性药物的PH依赖性控制释放药物组合物

    公开(公告)号:US20110229562A1

    公开(公告)日:2011-09-22

    申请号:US13120112

    申请日:2008-09-24

    CPC分类号: A61K9/5078

    摘要: The invention relates to a pH-dependent controlled release pharmaceutical composition, comprising at least one pharmaceutical active ingredient, with the exception of opioids, wherein the core is coated at least by one coating layer, controlling the release of the pharmaceutical composition, wherein the coating layer comprises a polymer mixture of i) 40-95% by weight, based on dry weight of the polymer mixture, of at least one water insoluble essentially neutral vinyl polymer or copolymer, and ii) 5-60% by weight, based on dry weight of the polymer mixture, of at least one anionic polymer or copolymer, which is insoluble in a buffered medium below pH 4.0 and soluble at least in the range from pH 7.0 to pH 8.0, characterized in that the coating layer further comprises 110 to 250% by weight of a non-porous inert lubricant, 1 to 35% by weight of at least one neutral cellulosic compound and 1 to 25% by weight of at least one emulsifier, each calculated on dry weight of the polymer mixture.

    摘要翻译: 本发明涉及pH依赖性控释药物组合物,其包含除阿片样物质以外的至少一种药物活性成分,其中核心至少涂覆一层涂层,以控制药物组合物的释放,其中涂层 至少一种不溶于水的基本上中性的乙烯基聚合物或共聚物,和ii)5-60重量%,基于干燥的聚合物混合物,i)40-95重量%,基于聚合物混合物的干重, 聚合物混合物的重量,至少一种阴离子聚合物或共聚物,其不溶于低于pH 4.0的缓冲介质中并且可溶于至少在7.0至8.0的范围内,其特征在于所述涂层还包含110至250 重量%的无孔惰性润滑剂,1至35重量%的至少一种中性纤维素化合物和1至25重量%的至少一种乳化剂,其各自以聚合物混合物的干重计算。

    PH-dependent controlled release pharmaceutical composition for non-opioids with resistance against the influence of ethanol

    公开(公告)号:US10933024B2

    公开(公告)日:2021-03-02

    申请号:US13120112

    申请日:2008-09-24

    摘要: The invention relates to a pH-dependent controlled release pharmaceutical composition, comprising at least one pharmaceutical active ingredient, with the exception of opioids, wherein the core is coated at least by one coating layer, controlling the release of the pharmaceutical composition, wherein the coating layer comprises a polymer mixture of i) 40-95% by weight, based on dry weight of the polymer mixture, of at least one water insoluble essentially neutral vinyl polymer or copolymer, and ii) 5-60% by weight, based on dry weight of the polymer mixture, of at least one anionic polymer or copolymer, which is insoluble in a buffered medium below pH 4.0 and soluble at least in the range from pH 7.0 to pH 8.0, characterized in that the coating layer further comprises 110 to 250% by weight of a non-porous inert lubricant, 1 to 35% by weight of at least one neutral cellulosic compound and 1 to 25% by weight of at least one emulsifier, each calculated on dry weight of the polymer mixture.

    CONTROLLED RELEASE PHARMACEUTICAL COMPOSITION WITH RESISTANCE AGAINST THE INFLUENCE OF ETHANOL EMPLOYING A COATING COMPRISING NEUTRAL VINYL POLYMERS AND EXCIPIENTS
    6.
    发明申请
    CONTROLLED RELEASE PHARMACEUTICAL COMPOSITION WITH RESISTANCE AGAINST THE INFLUENCE OF ETHANOL EMPLOYING A COATING COMPRISING NEUTRAL VINYL POLYMERS AND EXCIPIENTS 有权
    控制释放的药物组合物具有抵抗乙酸乙酯对包含中性乙烯基聚合物和其特性的涂料的影响

    公开(公告)号:US20120045506A1

    公开(公告)日:2012-02-23

    申请号:US13256694

    申请日:2009-03-18

    CPC分类号: A61K9/5078

    摘要: The invention relates to a controlled release pharmaceutical composition, comprising a core, comprising a pharmaceutical active ingredient, whereby the core is coated by an ethanol resistance conferring coating layer which has the effect of conferring the release profile of the pharmaceutical active ingredient to be resistant against the influence of ethanol, whereby the ethanol resistance conferring coating layer comprises at least 70% by weight of a mixture of a polymeric portion a) and an excipients portion b), with the polymeric portion a) is consisting of a water insoluble essentially neutral vinyl polymer or vinyl copolymer and the excipients portion b) is consisting of the excipients b1) 100 to 250% by weight of a non-porous inert lubricant, b2) 1 to 35% by weight of a cellulosic compound, b3) 0.1 to 25% by weight of an emulsifier and additionally or alternatively to b3), b4) 0.1 to 30% by weight of a plasticizer whereby the excipients of the excipients portion b) are each calculated on the dry weight of the polymer portion a).

    摘要翻译: 本发明涉及一种控释药物组合物,其包含核心,其包含药物活性成分,由此核心由赋予乙醇抗性的涂层涂覆,其具有赋予药物活性成分的释放特性以抵抗 乙醇的影响,其中赋予涂料的乙醇抗性包含至少70重量%的聚合物部分a)和赋形剂部分b)的混合物,聚合物部分a)由不溶于水的基本上为中性的乙烯基 聚合物或乙烯基共聚物和赋形剂部分b)由赋形剂b1)100-250重量%的无孔惰性润滑剂组成,b2)1至35重量%的纤维素化合物,b3)0.1至25重量% 的b),b4)0.1〜30重量%的增塑剂,其中赋形剂部分b)的赋形剂各自计算 以聚合物部分a)的干重计。

    Leucine aminopeptidases produced recombinantly from Aspergillus soyae
    9.
    发明授权
    Leucine aminopeptidases produced recombinantly from Aspergillus soyae 失效
    亮氨酸氨基肽酶由大豆曲霉重组产生

    公开(公告)号:US06228632B1

    公开(公告)日:2001-05-08

    申请号:US09011540

    申请日:1998-04-20

    IPC分类号: C12N948

    CPC分类号: C12N9/48

    摘要: This invention relates to a recombinant deoxyribonucleic acid (DNA) which can be isolated from Aspergillus soyae, characterised in that it codes for a leucine aminopeptidase (LAP) and comprises a nucleotide sequence corresponding to the nucleotide sequence given in SEQ ID NO: 1 for the mature LAP or to a nucleotide sequence derived therefrom which hybridises under stringent conditions with the nucleotide sequence given in SEQ ID NO: 1 for the mature LAP. The invention further relates to vectors and transformed host organisms, and also relates to methods of producing LAP. Enzyme products for the production of protein hydrolysates, as well as protein hydrolysates which are produced correspondingly, also form part of the invention.

    摘要翻译: 本发明涉及可从大豆粉中分离的重组脱氧核糖核酸(DNA),其特征在于其编码亮氨酸氨基肽酶(LAP),其包含对应于SEQ ID NO:1中给出的核苷酸序列的核苷酸序列,用于 成熟LAP或衍生自其的核苷酸序列,其在严格条件下与成熟LAP的SEQ ID NO:1中给出的核苷酸序列杂交。 本发明进一步涉及载体和转化的宿主生物,并且还涉及产生LAP的方法。 用于生产蛋白质水解产物的酶产物以及相应生产的蛋白质水解产物也构成本发明的一部分。