Cross-linked collagenic peptide for preventing post-surgical adhesions
    1.
    发明授权
    Cross-linked collagenic peptide for preventing post-surgical adhesions 失效
    交联胶原肽用于预防手术后粘连

    公开(公告)号:US06790438B1

    公开(公告)日:2004-09-14

    申请号:US09914424

    申请日:2002-01-14

    IPC分类号: A61L3106

    摘要: The aim of the invention is to provide a modified collagen peptide for preventing post-operative adhesions that is non-toxic, economic, in addition to being easy to obtain, sterilize, manipulate and implement, having controlled biodegradability and presenting a sufficiently strong initial mechanical resistance in situ (cohesion). This is achieved in the case of the modified collagen peptide for preventing post-operative adhesions according to the invention which is characterized in that it comprises at least one collagen peptide that is modified by grafting thiol functions that are free or substituted, cross-linkable and/or at least partly cross-linked, whereby the thiol functions are provided by mercaptoamine radicals that are exclusively grafted on the aspartic and glutamic acids of the collagen chains by means of amide bonds. The modified collagen peptide can exist in the form of a homogeneous or composite film, as a gel or in as a liquid which can be applied and cross-linked per se as on in vivo tissue.

    摘要翻译: 本发明的目的是提供一种改进的胶原肽,用于防止术后粘连,除了易于获得,消毒,操作和实施之外,还具有无毒的,经济的,具有受控的生物降解性并具有足够强的初始机械 原位抵抗力(内聚力)。 在用于预防根据本发明的术后粘连的改性胶原肽的情况下实现,其特征在于其包含至少一种胶原肽,所述胶原肽通过接枝游离或取代,可交联的硫醇官能团和 /或至少部分交联,由此巯基功能由巯基胺基团提供,其通过酰胺键专门接枝在胶原链的天冬氨酸和谷氨酸上。 修饰的胶原肽可以以均匀或复合膜的形式存在,如凝胶或以液体形式存在,其本身可作为体内组织施用和交联。

    Long-acting colloidal insulin formulation and its preparation
    2.
    发明申请
    Long-acting colloidal insulin formulation and its preparation 失效
    长效胶体胰岛素制剂及其制备

    公开(公告)号:US20090110742A1

    公开(公告)日:2009-04-30

    申请号:US11632992

    申请日:2005-06-09

    IPC分类号: A61K9/14 A61K38/28 A61P3/10

    摘要: The invention relates to injectable long-acting insulin formulations for the treatment of types I and II diabetes in humans and animals.The essential object of the invention is to provide an injectable long-acting insulin formulation in the form of a colloidal suspension which is stable, which has a good local tolerance and toxicity compatible with the chronic treatment of diabetics, and which maintains a substantial hypoglycemic effect extending over at least 24 hours after a single administration, e.g. by the subcutaneous route.To achieve this object, the invention relates to a stable aqueous colloidal formulation of insulin-laden nanoparticles of at least one poly(Leu-block-Glu) in which the pH is between 5.8 and 7.0, the osmolarity O (in mOsmol) . . . : 270≦O≦800, and the viscosity v (in mPa.s) is low, namely v≦40. The nanoparticles of poly(Leu-block-Glu) have a mean hydrodynamic diameter Dh such that: 15≦Dh≦40.The invention relates to an antidiabetic drug based on this long-acting insulin formulation and injectable using needles of gauge 29G, 30G or 31G.

    摘要翻译: 本发明涉及用于治疗人和动物中I型和II型糖尿病的可注射长效胰岛素制剂。 本发明的基本目的是提供一种稳定的胶体悬浮液形式的可注射的长效胰岛素制剂,其具有与糖尿病患者的慢性治疗相适应的良好的局部耐受性和毒性,并且其保持显着的降血糖效应 在单次给药后延长至少24小时,例如 通过皮下途径。 为了实现这个目的,本发明涉及至少一种pH(在5.8至7.0之间),渗透压浓度O(以mOsmol计)的至少一种聚(Leu-block-Glu)的含胰岛素的纳米颗粒的稳定水性胶体制剂。 。 。 :270 <= 0 <= 800,粘度v(mPa.s)低,即v <= 40。 聚(Leu-block-Glu)的纳米颗粒具有平均流体动力学直径Dh,使得:15 <= Dh <= 40。 本发明涉及基于该长效胰岛素制剂的抗糖尿病药物,并使用量规29G,30G或31G的针头进行注射。

    Oral ribavirin pharmaceutical compositions
    3.
    发明申请

    公开(公告)号:US20070166378A1

    公开(公告)日:2007-07-19

    申请号:US11449675

    申请日:2006-06-09

    IPC分类号: A61K31/7056 A61K9/22

    摘要: The invention relates to oral pharmaceutical compositions for the prevention and/or the treatment of viral diseases. This invention also addresses methods of prevention and/or treatment of these viral diseases, using these oral compositions. One of the main problems considered in the present invention is to enhance the efficiency of anti-viral treatments, especially against Hepatitis C virus by means of ribavirin, for example in combination with interferon. The oral ribavirin antiviral composition according to the invention increases the bio-absorption time of ribavirin, and thus improves the treatment of patients. Said composition comprises at least one modified release form of ribavirin, the bio-absorption time BAT of which is greater than the bio-absorption time BAT* of a reference* immediate release form of ribavirin administered at the same dose; BAT being preferably comprised between 2 and 15 h and more preferably between 4 and 12 h. Said composition is a reservoir type form or a matrix type form. Said composition is a gastric retentive system or a multiparticulate form.

    Oral pharmaceutical formulation in the form of aqueous suspension of microcapsules for modified release of amoxicillin
    4.
    发明申请
    Oral pharmaceutical formulation in the form of aqueous suspension of microcapsules for modified release of amoxicillin 失效
    用于阿莫西林改性释放的微胶囊水性悬浮液形式的口服药物制剂

    公开(公告)号:US20060110463A1

    公开(公告)日:2006-05-25

    申请号:US10510621

    申请日:2003-04-07

    IPC分类号: A61K31/43 A61K9/50 A61K9/16

    摘要: The invention relates to liquid pharmaceutical formulations for oral administration with the modified release of amoxicillin, said formulations consisting of suspensions of coated particles of amoxicillin (microcapsules). According to the invention, the microcapsules constituting the disperse phase of the suspension are designed to allow the modified release of the amoxicillin according to a profile that does not change during the storage of the liquid suspension. To do this the inventors propose the selection of a specific coating composition for the microcapsules which consists of at least four components that allow these microcapsules to be stored in water without modifying their properties of modified release of the amoxicillin, this liquid phase furthermore being saturated with amoxicillin.

    摘要翻译: 本发明涉及用于阿莫西林的改性释放的口服给药的液体药物制剂,所述制剂由阿莫西林(微胶囊)的包衣颗粒的悬浮液组成。 根据本发明,构成悬浮液分散相的微胶囊被设计成允许根据在液体悬浮液储存过程中不变化的分布来改变阿莫西林的释放。 为了做到这一点,发明人提出了选择用于微胶囊的特定涂料组合物,其由至少四种组分组成,这些组分允许这些微胶囊储存在水中而不改变其改性释放的阿莫西林的性质,此液相还饱和 阿莫西林

    Process and compositions promoting biological effectiveness of exogenous
chemical substances in plants
    5.
    发明授权
    Process and compositions promoting biological effectiveness of exogenous chemical substances in plants 失效
    促进植物中外源化学物质生物有效性的方法和成分

    公开(公告)号:US6133199A

    公开(公告)日:2000-10-17

    申请号:US124318

    申请日:1998-07-29

    摘要: A plant treatment composition for application of an anionic exogenous chemical substance such as glyphosate herbicide to foliage of a plant is provided. The composition is a colloidal dispersion having supramolecular aggregates dispersed in an aqueous application medium. The supramolecular aggregates comprise one or more amphiphilic salt(s) having anions of the exogenous chemical substance and cations derived by protonation of one or more polyamine(s) or polyamine derivative(s) each having (a) at least two nitrogen-containing groups, of which a number n not less than 1 are amino groups that can be protonated to form cationic primary, secondary or tertiary ammonium groups, and (b) at least one hydrocarbyl or acyl group having about 6 to about 30 carbon atoms. The composition contains (i) a molar amount X in total of the exogenous chemical substance, in all salt and acid forms thereof present, sufficient to elicit a biological response when the composition is applied to the foliage of the plant at a rate of about 10 to about 1000 l/ha, (ii) a molar amount A in total of said polyamine(s) and derivative(s) thereof and cations derived therefrom, and (iii) a zero or molar amount B in total of one or more monovalent base(s) and cations derived therefrom, said base(s) being other than a polyamine or derivative thereof, such that nA/(nA+B) is about 0.01 to 1, and (nA+B)/X is about 0.5 to about 10.Also provided are a liquid concentrate composition which, upon dilution with water, forms a plant treatment composition as described above, and a process for making such a liquid concentrate composition. Plant treatment compositions of the invention are useful for eliciting a biological activity, for example herbicidal activity, in a plant when applied to foliage thereof.

    摘要翻译: 提供了一种用于将阴离子外源化学物质如草甘膦除草剂施用于植物叶子的植物处理组合物。 该组合物是具有分散在水溶液介质中的超分子聚集体的胶态分散体。 超分子聚集体包含一种或多种具有外源化学物质的阴离子的两亲盐和通过一种或多种多胺或多胺衍生物的质子化产生的阳离子,每个多胺或多胺衍生物各自具有(a)至少两个含氮基团 其数n为不小于1的氨基可以被质子化形成阳离子伯,仲或叔铵基团,和(b)至少一个具有约6至约30个碳原子的烃基或酰基。 所述组合物包含(i)外源化学物质的总量X,其存在的所有盐和酸形式,足以引起组合物以约10的速率施用于植物的叶子时的生物反应 至约1000l / ha,(ii)所述多胺及其衍生物的总摩尔量A和由其衍生的阳离子,和(iii)零或摩尔量B总计为一种或多种一价 碱和其衍生的阳离子,所述碱不是多胺或其衍生物,使得nA /(nA + B)为约0.01至1,和(nA + B)/ X为约0.5至 还提供了液体浓缩组合物,其在用水稀释时形成如上所述的植物处理组合物,以及制备这种液体浓缩组合物的方法。 本发明的植物处理组合物可用于在施用于其叶面时在植物中引发生物活性,例如除草活性。

    Anti-Misuse Microparticulate Oral Drug Form
    8.
    发明申请
    Anti-Misuse Microparticulate Oral Drug Form 审中-公开
    反滥用微量口服药物形式

    公开(公告)号:US20090041838A1

    公开(公告)日:2009-02-12

    申请号:US11883935

    申请日:2006-02-08

    IPC分类号: A61K9/50 A61K9/14 A61K9/22

    摘要: The invention relates to solid microparticulate oral dosage forms having a composition that prevents the misuse of the active pharmaceutical ingredient (API) contained therein. The aim of the invention is to prevent the improper use of solid oral drugs for any use other than the therapeutic use(s) officially approved by the appropriate public health authorities. Another aim of the invention is to provide novel analgesic drugs which can be used to: prevent the misuse of, and addiction to certain analgesics and/or to control plasma concentration variability and/or to facilitate oral; administration; and/or to combine analgesics with one another and/or with one or more active ingredients in the same oral form. More specifically, the invention relates to a solid oral drug form comprising anti-misuse means and at least one active ingredient, which is characterized in that: at least part of the active ingredient is contained in microparticles; and the anti-misuse means comprise anti-crushing means (a) which enable the microparticles of the active ingredient to resist crushing, such as to prevent the misuse thereof. According to the invention, the drug form can also comprise means (b) for preventing the misuse of the active ingredient following a possible liquid extraction process.

    摘要翻译: 本发明涉及具有防止滥用其中所含的活性药物成分(API)的组合物的固体微粒口服剂型。 本发明的目的是防止不适当地使用固体口服药物以用于由适当的公共卫生当局正式批准的治疗用途以外的任何用途。 本发明的另一个目的是提供新的止痛药,其可用于:防止某些止痛剂的滥用和成瘾和/或控制血浆浓度变异性和/或促进口服; 行政; 和/或将镇痛药彼此和/或以相同口服形式的一种或多种活性成分组合。 更具体地,本发明涉及包含抗滥用手段和至少一种活性成分的固体口服药物形式,其特征在于:至少部分活性成分包含在微粒中; 并且防误用手段包括能够使活性成分的微粒抵抗破碎的抗破碎装置(a),以防止其误用。 根据本发明,药物形式还可以包括用于防止在可能的液体提取过程后滥用活性成分的装置(b)。

    Pharmaceutical Formulations For The Prolonged Release Of Interleukins And Their Therapeutic Applications
    9.
    发明申请
    Pharmaceutical Formulations For The Prolonged Release Of Interleukins And Their Therapeutic Applications 审中-公开
    长期释放白介素及其治疗应用的药物制剂

    公开(公告)号:US20070218142A1

    公开(公告)日:2007-09-20

    申请号:US10580035

    申请日:2004-11-19

    IPC分类号: A61K9/14

    摘要: The present invention relates to novel pharmaceutical formulations based on stable, fluid aqueous colloidal suspensions for the prolonged release of an interleukin (IL) (and one or more other possible active principles), and to the applications, especially therapeutic applications, of these formulations. The object of the invention is to propose a fluid pharmaceutical formulation for the prolonged release of interleukin(s) (and one or more other possible active principles) that makes it possible, after parenteral injection, significantly to increase the in vivo release time of the IL while at the same time reducing the plasma concentration peak of this IL, said formulation furthermore being stable on storage and also being biocompatible, biodegradable, non-toxic and non-immunogenic and having a good local tolerance. The formulation according to the invention is an aqueous colloidal suspension of low viscosity based on submicronic particles of water-soluble biodegradable polymer PO carrying hydrophobic groups (HG), said particles being non-covalently associated with at least one interleukin (and one or more other possible active principles) and forming a gelled deposit at the injection site, this gelling being caused by a protein present in the physiological medium.

    摘要翻译: 本发明涉及基于用于延长释放白介素(IL)(和一种或多种其它可能的活性成分)的稳定的流体水性胶体悬浮液以及这些制剂的应用,特别是治疗应用的新型药物制剂。 本发明的目的是提出用于延长释放白细胞介素(和一种或多种其它可能的活性成分)的流体药物制剂,其使得在胃肠外注射后可显着地增加体内释放时间 IL,同时降低该IL的血浆浓度峰值,所述制剂还在储存时稳定,并且也是生物相容的,可生物降解的,无毒的和非免疫原性的并且具有良好的局部耐受性。 根据本发明的制剂是基于具有疏水基团(HG)的水溶性生物可降解聚合物PO的亚微米颗粒的低粘度水性胶态悬浮液,所述颗粒与至少一种白细胞介素(和一种或多种其它物质)非共价结合 可能的活性成分),并在注射部位形成凝胶沉积物,该胶凝是由存在于生理介质中的蛋白质引起的。

    Oral pharmaceutical compositions with controlled release and prolonged absorption
    10.
    发明申请
    Oral pharmaceutical compositions with controlled release and prolonged absorption 有权
    具有控制释放和延长吸收的口服药物组合物

    公开(公告)号:US20070207214A1

    公开(公告)日:2007-09-06

    申请号:US11723553

    申请日:2007-03-21

    IPC分类号: A61K9/14

    摘要: The invention concerns a galenic system with prolonged/controlled release of the medicinal and/or nutritional active principle, for oral administration. The aim is to provide a system enabling to obtain with one single tolerable and acceptable dose of active principle, efficient therapeutic protection over 24 hours (increasing the bioabsorption time without affecting bioavailability). To achieve this, the invention provides a composition comprising two controlled release systems associated in series, namely: individualised coated particles (microcapsules) of active principle forming an internal phase, the coating comprising a film-forming polymer P1 (ethylcellulose), a nitrogenous polymer (polyvinylpyrrolidone), a softener (castor oil) and a lubricant (magnesium stearate), and an external phase of functional carriers: polyelectrolytic hydrophilic polymer: (alginate), neutral hydrophilic polymer (hydroxypropylmethylcellulose) and a gelling additive (calcium acetate), said composition spontaneously forming in the presence of water, a cohesive and stable composite macroscopic solid, wherein the external continuous phase is a gelled matrix including the active principle microcapsules. The invention is useful for delayed oral galenic formulation of metformin.

    摘要翻译: 本发明涉及用于口服给药的药物和/或营养活性成分的延长/受控释放的盖仑系统。 目的是提供一种能够以一个单一可耐受和可接受剂量的活性成分获得的系统,24小时以上的有效治疗保护(增加生物吸收时间而不影响生物利用度)。 为了实现这一目的,本发明提供了包含两个串联相关的控制释放系统的组合物,即形成内相的活性成分的单独的涂覆颗粒(微胶囊),该涂层包含成膜聚合物P 1 (乙基纤维素),含氮聚合物(聚乙烯吡咯烷酮),软化剂(蓖麻油)和润滑剂(硬脂酸镁)和功能性载体的外相:聚电解亲水性聚合物:(藻酸盐),中性亲水性聚合物(羟丙基甲基纤维素)和 凝胶添加剂(乙酸钙),所述组合物在水的存在下自发形成,粘性和稳定的复合宏观固体,其中外部连续相是包含活性成分微胶囊的凝胶基质。 本发明可用于二甲双胍延迟口服盖仑制剂。