Diffusion-osmotic controlled drug-release pharmaceutical composition and
process for preparing same
    2.
    发明授权
    Diffusion-osmotic controlled drug-release pharmaceutical composition and process for preparing same 失效
    扩散渗透控制药物释放药物组合物及其制备方法

    公开(公告)号:US5543155A

    公开(公告)日:1996-08-06

    申请号:US341209

    申请日:1994-12-05

    CPC分类号: A61K9/0004 Y10S514/96

    摘要: The invention relates to a novel diffusion-osmotic controlled drug-release pharmaceutical composition containing a one-layer tablet core including a polymeric film-coat, a therapeutically active agent and a hydrophilic polymer; if desired, a two-layer tablet core including active agent and hydrophilic polymer in the first layer thereof and a hydrophilic polymer in the second layer thereof; at least one bore on the part of film-coat in contact with the core or core layer containing the active agent; and, if desired, containing one or more bore(s) in the part thereof in contact with the second layer containing the hydrophilic polymer, which comprises an ammonium methacrylate copolymer as coating material and hydroxypropyl-methylcellulose as hydrophilic polymer. The composition according to the invention is useful for preparing controlled drug-release tablets containing as active agents e.g. .beta.-adrenergic inhibitors (e.g. propranolol) calcium-antagonists (e.g. nifedipine), angiotensin convertase enzyme (ACE) inhibitors (e.g. captopril); prazosin; or nitroglycerol, all used in heart and circulation diseases; vasodilatory active agents (e.g. pentoxyfylline), nonsteroidal antiinflammatory agents (e.g. naproxene), analgetic drugs (e.g. morphine) and drugs acting on the central nervous system (e.g. amitriptyline, buspiron). The invention furthermore relates to a process for the preparation of the above compositions.

    摘要翻译: 本发明涉及一种新颖的扩散渗透控制药物释放药物组合物,其含有包含聚合物膜包衣,治疗活性剂和亲水性聚合物的单层片芯; 如果需要,在其第一层中包含活性剂和亲水性聚合物的两层片芯和其第二层中的亲水性聚合物; 膜包衣部分的至少一个孔与含有活性剂的芯层或芯层接触; 并且如果需要,在其部分中含有与包含亲水性聚合物的第二层接触的一个或多个孔,其包含作为涂层材料的甲基丙烯酸铵共聚物和作为亲水性聚合物的羟丙基甲基纤维素。 根据本发明的组合物可用于制备包含作为活性剂的受控药物释放片剂,例如, β-肾上腺素能抑制剂(如普萘洛尔)钙拮抗剂(如硝苯地平),血管紧张素转化酶(ACE)抑制剂(如卡托普利); 哌唑嗪 或硝酸甘油,均用于心脏和循环疾病; 血管舒张活性剂(例如戊氧基线),非甾体抗炎剂(例如萘普生),止痛药(例如吗啡)和作用于中枢神经系统的药物(例如阿米替林,buspiron)。 本发明还涉及制备上述组合物的方法。

    Fodder additive and a process for the preparation
    8.
    发明授权
    Fodder additive and a process for the preparation 失效
    饲料添加剂和制备方法

    公开(公告)号:US4659712A

    公开(公告)日:1987-04-21

    申请号:US790856

    申请日:1985-10-24

    CPC分类号: A23K50/30 A23K20/111

    摘要: The invention relates to fodder additives comprising a compound inducing the microsomal enzyme system of the liver, preferably a compound of the formula (I) ##STR1## wherein R.sub.1, R.sub.2 and R.sub.3 are identical or different and stand for hydrogen, halogen, trihalomethyl, or alkyl or alkoxy each containing from 1 to 6 carbon atoms;R.sub.4 is phenyl, dialkylaminocarbonyl or alkoxycarbonyl having from 1 to 6 carbon atoms in the alkyl and alkoxy moieties, respectively;R.sub.5 is hydrogen or methyl, or together with R.sub.4 and the adjacent nitrogen atom forms a hetero-ring having up to 8 members;n is 1, 2, 3, 4 or 5;m is 0 or 1;a is 0 or 1,with the proviso that if a=0, R.sub.1 is trihalomethyl and R.sub.2 and R.sub.3 both are hydrogen, preferably in amount of 0.5 to 99% by weight, in an admixture with conventional carriers and/or additives and optionally at least one further active ingredient conventionally used in the animal husbandry.The enzyme inducing compounds used according to the invention accelerate the elimination of various xenobiotics metabolizing in the liver.

    摘要翻译: 本发明涉及包含诱导肝脏微粒体酶系统的化合物的饲料添加剂,优选式(I)化合物其中R 1,R 2和R 3相同或不同,代表氢,卤素, 三卤甲基或各自含有1至6个碳原子的烷基或烷氧基; R4分别是苯基,二烷基氨基羰基或在烷基和烷氧基部分具有1-6个碳原子的烷氧基羰基; R 5是氢或甲基,或与R 4一起并且相邻的氮原子形成具有至多8个成员的杂环; n为1,2,3,4或5; m为0或1; a为0或1,条件是如果a = 0,则R1为三卤甲基,R2和R3均为氢,优选为0.5至99重量%,与常规载体和/或添加剂混合,并且任选地 至少一种常规用于畜牧业的活性成分。 根据本发明使用的酶诱导化合物加速了在肝脏中代谢的各种异种生物的消除。