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    PHARMACEUTICAL COMPOSITIONS FOR GASTROINTESTINAL DRUG DELIVERY
    1.
    发明申请
    PHARMACEUTICAL COMPOSITIONS FOR GASTROINTESTINAL DRUG DELIVERY 有权
    用于胃肠道给药的药物组合物

    公开(公告)号：US20090011019A1

    公开(公告)日：2009-01-08

    申请号：US12144894

    申请日：2008-06-24

    申请人： Harshal Anil Jahagirdar ,  Rajesh Kulkarni ,  Shirishkumar Kulkarni

    发明人： Harshal Anil Jahagirdar ,  Rajesh Kulkarni ,  Shirishkumar Kulkarni

    IPC分类号： A61K9/24 ,  A61K9/20

    CPC分类号： A61K47/44 ,  A61K9/0065 ,  A61K9/0095 ,  A61K9/1611 ,  A61K9/1617 ,  A61K9/1623 ,  A61K9/1635 ,  A61K9/1641 ,  A61K9/1652 ,  A61K9/2009 ,  A61K9/2013 ,  A61K9/2018 ,  A61K9/2027 ,  A61K9/2031 ,  A61K9/205 ,  A61K9/2054 ,  A61K9/2086 ,  A61K9/209 ,  A61K31/196 ,  A61K31/197 ,  A61K31/437 ,  A61K31/4402 ,  A61K31/606 ,  A61K31/635 ,  A61K31/655 ,  A61K31/785 ,  A61K38/12 ,  A61K47/32 ,  A61K47/34 ,  A61K47/38

    摘要： A novel pharmaceutical composition, which comprises a therapeutically effective amount of active principle(s) or a pharmaceutically acceptable salt or enantiomer or polymorph thereof, optionally one or more release controlling agent(s) and pharmaceutical acceptable excipient(s) thereof, wherein the composition is formulated to increase the residence time of the said pharmaceutical composition and/or active principle(s) in the gastrointestinal tract. A novel pharmaceutical composition comprising at least two entities wherein one entity is an immediate release/fast release and the other is controlled release. A pharmaceutical composition comprising at least two entities wherein one entity is an immediate release/fast release and the other is bioadhesive. A pharmaceutical composition comprising: at least two entities wherein one entity is controlled release and the other is bioadhesive All the three compositions are formulated to increase the residence time of active principle(s) in the gastrointestinal tract. A multilayered composition with active in a layer which provides immediate release or controlled release of active principles and layer providing increased residence time in the GI tract.

    摘要翻译： 一种新型药物组合物，其包含治疗有效量的活性成分或其药学上可接受的盐或对映体或多晶型物，任选的一种或多种释放控制剂及其药学上可接受的赋形剂，其中所述组合物 配制成增加所述药物组合物和/或活性成分在胃肠道中的停留时间。 一种新型药物组合物，其包含至少两个实体，其中一个实体是即时释放/快速释放，另一个实体是控制释放的。 包含至少两个实体的药物组合物，其中一个实体是立即释放/快速释放，另一个是生物粘附的。 一种药物组合物，其包含：至少两个实体，其中一个实体被控制释放，另一个实体是生物粘附剂。所有三种组合物被配制以增加活性成分在胃肠道中的停留时间。 在层中具有活性的多层组合物，其提供活性成分和层的即时释放或控制释放，从而在GI道中提供增加的停留时间。

    Herbal extract comprising a mixture of saponins obtained from sapindus trifoliatus for anticonvulsant activity
    3.
    发明申请
    Herbal extract comprising a mixture of saponins obtained from sapindus trifoliatus for anticonvulsant activity 审中-公开
    草药提取物包含从三叶皂甙获得的皂苷混合物，用于抗惊厥活性

    公开(公告)号：US20050249831A1

    公开(公告)日：2005-11-10

    申请号：US10525992

    申请日：2003-08-27

    申请人： Sudershan Arora ,  Vandita Srivastava ,  Veeranjaneyulu Addepalli ,  Sridhar Natesan ,  Rajan Goel

    发明人： Sudershan Arora ,  Vandita Srivastava ,  Veeranjaneyulu Addepalli ,  Sridhar Natesan ,  Rajan Goel

    IPC分类号： A61K20060101 ,  A61K31/704 ,  A61K35/00 ,  A61K36/77 ,  A61P20060101 ,  A61P25/06 ,  A61K35/78

    CPC分类号： A61K36/77

    摘要： A pharmaceutical composition comprising a herbal extract, comprising a mixture of saponins prepared from the pericarp of Sapindus trifoliatus, with binding affinities for the receptor sites viz. GABA-A agonist site, Glutamate-AMPA site, Glutamate-Kainate site, Glutamate-NMDA agonistic site, Glutamate-NMDA glycine (strychnine insensitive) site and Sodium channel (site 2), having major mediatory role in anticonvulsant activity. A process for preparation of the herbal extract; isolation of six pure compounds from the mixture of saponins in the aqueous extract; and a pharmaceutical composition comprising the said extract in combination with pharmaceutically acceptable additives. A method of prophylactic treatment of migraine through anticonvulsant activity of the composition by its administration through intranasal route.

    摘要翻译： 包含草药提取物的药物组合物，其包含由Sapindus trifoliatus的果皮制备的皂苷的混合物，对受体位点的结合亲和力。 GABA-A激动剂位点，谷氨酸 - AMPA位点，谷氨酸 - 红藻酸酯位点，谷氨酸-N NMDA激动位点，谷氨酸-N NMDA甘氨酸（士的宁不敏感）位点和钠通道（位点2），在抗惊厥活性中具有主要的介导作用。 制备草药提取物的方法 在水提取物中从皂甙混合物中分离出六种纯化合物; 以及包含所述提取物与药学上可接受的添加剂组合的药物组合物。 一种通过鼻内途径施用组合物的抗惊厥活性来预防性治疗偏头痛的方法。

    Process for preparation of duloxetine hydrochloride
    6.
    发明授权
    Process for preparation of duloxetine hydrochloride 失效
    盐酸度洛西汀的制备方法

    公开(公告)号：US08269023B2

    公开(公告)日：2012-09-18

    申请号：US12530214

    申请日：2008-03-05

    申请人： Rajinder Singh Siyan ,  Sunil Kumar Vinubhai Gohel ,  Girij Pal Singh

    发明人： Rajinder Singh Siyan ,  Sunil Kumar Vinubhai Gohel ,  Girij Pal Singh

    IPC分类号： C07D333/16

    CPC分类号： C07D333/20

    摘要： An improved process for synthesis of duloxetine hydrochloride (1) having chiral purity greater than 99.9% that is characterized by the following: (i) preparation of racemic condensed compound (RS)—N,N-di methyl-3-(1-naphthyloxy)-3-(2-thienyl)propanamine (4) by reaction of racemic hydroxy compound (2) with 1-fluoronaphthalene (3) in presence of a base such as sodamide, potassium amide or potassium bis(trimethylsilyl)amide (KHDMS) in polar aprotic solvent, (ii) optical resolution of racemic condensed compound (5a+5b) with di-benzoyl-L-tartaric acid (7, DBTA, R=H) or di-para-anisoyl-L-tartaric acid (7, DATA, R=OCH3) to obtain crude (S)—N.N-dimethyl-3-(1-naphthyloxy)-3-(2-thienyl)propanamine dibenzoyl tartarate salt (8a) or (S)—N.N-dimethyl-3-(1-naphthyloxy)-3-(2-thienyl)propanamine di-p-anisoyl tartarate salt (9a) respectively, (iii) optionally purification of crude tartarate salts (8a or 9a) by crystallization, (iv) optionally purification of duloxetine hydrochloride (1) by crystallization and (v) racemization of undesired (R)—N,N-di methyl-3-(1-naphthyloxy)-3-(2-thienyl)propanamine (5b) by treatment with base potassium bis(trimethylsilyl)amide (KHDMS) to obtain racemic mixture of condensed compounds (5a and 5b).

    摘要翻译： 具有手性纯度大于99.9％的改进的度洛西汀盐酸盐（1）的改进方法，其特征在于：（i）制备外消旋缩合化合物（RS）-N，N-二甲基-3-（1-萘氧基 ）3-（2-噻吩基）丙胺（4），通过外消旋羟基化合物（2）与1-氟萘（3）在碱如Sodamide，氨基化钾或双（三甲基甲硅烷基）氨基钾（KHDMS）的存在下反应， 在极性非质子溶剂中，（ii）用二苯甲酰基-L-酒石酸（7，DBTA，R = H）或二对甲氧基苯甲酰基-L-酒石酸（7）的外消旋缩合化合物（5a + 5b） ，DATA，R = OCH 3），得到粗（S）-N'-二甲基-3-（1-萘氧基）-3-（2-噻吩基）丙胺二苯甲酰酒石酸盐（8a）或（S）-N'-二甲基-3 - （1-萘氧基）-3-（2-噻吩基）丙胺二对茴香酰酒石酸盐（9a），（iii）任选地通过结晶纯化粗酒石酸盐（8a或9a），（iv） 盐酸度洛西汀（1）通过晶体 （R）-N，N-二甲基-3-（1-萘氧基）-3-（2-噻吩基）丙胺（5b）通过用双（三甲基甲硅烷基）氨基钾酰胺（KHDMS）处理而外消旋化 ），得到缩合化合物（5a和5b）的外消旋混合物。

    Method for manufacture of 4-hydroxy pyran-2-one derivatives
    7.
    发明授权
    Method for manufacture of 4-hydroxy pyran-2-one derivatives 有权
    4-羟基吡喃-2-酮衍生物的制备方法

    公开(公告)号：US07777056B2

    公开(公告)日：2010-08-17

    申请号：US11547533

    申请日：2004-03-30

    申请人： Milind Moreshwar Gharpure ,  Swapnil Panditrao Sonawane ,  Srihari Shivaji Mane ,  Rajendra Dagesing Mahale

    发明人： Milind Moreshwar Gharpure ,  Swapnil Panditrao Sonawane ,  Srihari Shivaji Mane ,  Rajendra Dagesing Mahale

    IPC分类号： C07D311/02

    CPC分类号： C07D309/30

    摘要： A process for preparation of 4-hydroxy-pyran-2-one derivative of formula (I), wherein R is, and wherein R1 and R2 are methyl and R3 is hydrogen or methyl, comprising the steps of, heating a compound of formula (II), wherein R is as defined before, and R4 is hydrogen, NH4+ or an alkali metal, in a solvent mixture consisting of an aromatic hydrocarbon and a ketone in an inert atmosphere at a temperature of between 60° C. to 92° C. in the absence or presence of orthophosphoric acid or its alkali dihydrogen salts or alkali hydrogen salts of a dibasic acid, followed by optional neutralization of the reaction mixture with an organic base and obtaining compound of formula (I) in high purity and substantially free of impurities through a step of isolation and crystallization. The process leads to formation of derivatives of formula I in high purity with dimmer impurity (III) less than 0.1% and anhydro impurity (IV) below 0.15%.

    摘要翻译： 一种制备式（I）的4-羟基 - 吡喃-2-酮衍生物的方法，其中R为，并且其中R 1和R 2为甲基且R 3为氢或甲基，包括以下步骤：加热式 II），其中R如前所定义，并且R 4是氢，NH 4 +或碱金属，在惰性气氛中，在60℃至92℃的温度下在由芳族烃和酮组成的溶剂混合物中 在不存在或存在正磷酸或其二氢酸的碱式二氢盐或碱式氢盐的情况下，随后将有机碱任选地中和反应混合物，得到高纯度且基本上不含 杂质通过分离和结晶的步骤。 该方法导致以高纯度形成式I的衍生物，其中较少的杂质（III）小于0.1％，而脱水杂质（IV）低于0.15％。

    PHARMACEUTICAL COMPOSITIONS OF RIFAXIMIN
    9.
    发明申请
    PHARMACEUTICAL COMPOSITIONS OF RIFAXIMIN 有权
    RIFAXIMIN的药物组合物

    公开(公告)号：US20090028940A1

    公开(公告)日：2009-01-29

    申请号：US12144453

    申请日：2008-06-23

    申请人： Harshal Anil Jahagirdar ,  Rajesh Kulkarni ,  Shirishkumar Kulkarni

    发明人： Harshal Anil Jahagirdar ,  Rajesh Kulkarni ,  Shirishkumar Kulkarni

    IPC分类号： A61K9/22 ,  A61K31/439 ,  A61P1/12 ,  A61K9/20 ,  A61K9/00

    CPC分类号： A61K31/44 ,  A61K9/1623 ,  A61K9/1652 ,  A61K9/2086 ,  A61K9/2846 ,  A61K9/2866 ,  A61K9/4808 ,  Y02A50/473 ,  Y02A50/475

    摘要： A pharmaceutical composition comprising therapeutically effective amount of rifaximin or pharmaceutically acceptable salt or enantiomer or polymorph thereof, pharmaceutically acceptable excipient(s) and release controlling agent(s). Pharmaceutical composition of rifaximin comprising: at least two entities wherein one entity is an immediate release or fast release and the other is controlled release. The pharmaceutical composition in the form of multilayer tablet comprising, at least one layer comprising, therapeutically effective amount of rifaximin or pharmaceutically acceptable salt or enantiomer or polymorph thereof, pharmaceutically acceptable excipient(s); said layer providing controlled release rifaximin; and at least one layer which provides increased residence time of the dosage form in the gastrointestinal tract. The pharmaceutical formulation comprising rifaximin having an in vitro dissolution profile, wherein about 70% of rifaximin is released in about 24 hours. The composition comprising therapeutically effective amount of rifaximin or pharmaceutically acceptable salt(s) or enantiomer(s) or polymorph(s) thereof, one or more release controlling agent(s) and pharmaceutically acceptable excipient(s) causing pathogenic eradication.

    摘要翻译： 一种药物组合物，其包含治疗有效量的利福昔明或其药学上可接受的盐或对映异构体或其多晶型物，药学上可接受的赋形剂和释放控制剂。 利福昔明的药物组合物包括：至少两个实体，其中一个实体是立即释放或快速释放，另一个实体是控制释放的。 多层片剂形式的药物组合物，包含至少一层，其包含治疗有效量的利福昔明或其药学上可接受的盐或对映体或其多晶型物，药学上可接受的赋形剂; 所述层提供受控释放的利福昔明; 以及提供剂型在胃肠道中的延长停留时间的至少一个层。 包含具有体外溶出曲线的利福昔明的药物制剂，其中约70％的利福昔明在约24小时内释放。 所述组合物包含治疗有效量的利福昔明或其药学上可接受的盐或对映异构体或多晶型物，一种或多种释放控制剂和引起致病根除的药学上可接受的赋形剂。

    Method for preparation of crystalline perindopril erbumine
    10.
    发明授权
    Method for preparation of crystalline perindopril erbumine 失效
    制备结晶培哚普利埃布胆碱的方法

    公开(公告)号：US07456296B2

    公开(公告)日：2008-11-25

    申请号：US10576386

    申请日：2003-10-21

    申请人： Girij Pal Singh ,  Himanshu Madhav Godbole ,  Sagar Purushottam Nehate

    发明人： Girij Pal Singh ,  Himanshu Madhav Godbole ,  Sagar Purushottam Nehate

    IPC分类号： A61K31/405 ,  C07D209/42

    CPC分类号： C07D209/42

    摘要： A process for preparation of crystalline perindopril erbumine of formula (II) which exhibits the X-ray (powder) diffraction pattern like that shown in FIG. 2 The process comprises reacting a solution of perindopril of formula (I), in a solvent selected from N,N-dimethylformamide, dimethyl acetals of lower aliphatic aldehydes, dimethyl ketals of lower aliphatic ketones and 1,2-dialkoxyethane with tertiary butylamine and crystallization of the erbumine salt thus obtained by heating the reaction mixture to reflux, filtering hot, cooling gradually to 20° C. to 30° C., and further cooling to 0° C. to 15° C. for 30 minutes to 1 hour and finally filtering off and drying the crystals.

    摘要翻译： 制备式（II）的结晶培哚普利埃布林的方法，其显示如图1所示的X射线（粉末）衍射图案。 2该方法包括使式（I）培哚普利溶液在选自N，N-二甲基甲酰胺，低级脂族醛的二甲基缩醛，低级脂族酮和1,2-二烷氧基乙烷的二甲基缩酮与叔丁胺的溶剂和结晶 通过将反应混合物加热回流，从而过滤热，逐渐冷却至20℃至30℃，并进一步冷却至0℃至15℃，持续30分钟至1小时，从而获得 最后过滤并干燥晶体。