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    Long-acting solid formulation comprising triptorelin acetate
    5.
    发明申请
    Long-acting solid formulation comprising triptorelin acetate 审中-公开
    长效固体制剂，包括醋酸曲普瑞林

    公开(公告)号：US20070031500A1

    公开(公告)日：2007-02-08

    申请号：US11499777

    申请日：2006-08-07

    Applicant: Roland Cherif-Cheikh ,  Francesc Navarro Pujol

    Inventor： Roland Cherif-Cheikh ,  Francesc Navarro Pujol

    IPC: A61K9/14 ,  A61K31/4439

    CPC classification number: A61K9/0024 ,  A61K9/204 ,  A61K9/2095 ,  A61K38/09

    Abstract: The invention relates to a long-acting solid formulation for parenteral administration, comprising a) triptorelin acetate and b) one or more excipients comprising a polymer or copolymer of lactic and/or glycolic acid or a mixture of polymers and/or copolymers of lactic acid and/or glycolic acid, said formulation containing 10 to 99% of triptorelin acetate by weight with relation to the total weight of the formulation. Said formulation is obtained by means of a method comprising the fusion of a mixture of triptorelin acetate and the excipient(s) on the fusion/extrusion of the triptorelin acetate with the excipient(s), said formulation being embodied such as to release the triptorelin acetate over a duration of at least one week, once administered parenterally to a patient.

    Abstract translation: 本发明涉及用于肠胃外给药的长效固体制剂，其包含a）醋酸曲普瑞林和b）一种或多种赋形剂，其包含乳酸和/或乙醇酸的聚合物或共聚物或乳酸的聚合物和/或共聚物的混合物 和/或乙醇酸，所述制剂含有10至99％的醋酸曲普瑞林，其重量与制剂的总重量相关。 所述制剂通过包括将醋酸曲普瑞林与赋形剂的混合物在醋酸曲普瑞司酯与赋形剂的融合/挤出物上融合的方法获得，所述制剂被实施为释放曲普瑞林 乙酸盐，持续至少一周，一次胃肠外给予患者。

    Method for preparing an injectable preparation and device for implementing same
    6.
    发明授权
    Method for preparing an injectable preparation and device for implementing same 有权
    注射用制剂的制备方法及其制造方法

    公开(公告)号：US06349850B1

    公开(公告)日：2002-02-26

    申请号：US09194918

    申请日：1999-02-18

    Applicant: Roland Cherif Cheikh

    Inventor： Roland Cherif Cheikh

    IPC: A61J100

    CPC classification number: A61J1/2096 ,  A61J1/062 ,  A61J1/201 ,  A61J1/2041 ,  A61J1/2055 ,  A61J1/2065 ,  A61J1/2089 ,  A61J1/2093 ,  A61M5/002 ,  A61M5/284 ,  A61M5/31596 ,  A61M2005/31598

    Abstract: A method comprising the following steps: preparing in a vacuum a dry form (18) of an active principle, as well as a liquid (22), and drawing this liquid into the dry form, by the action of the vacuum to obtain an injectable preparation. The device comprises a gastight syringe (19) to condition under vacuum the dry form, a reservoir (12) containing the liquid (22) and a cap (29) forming a connector between the syringe and the liquid reservoir, the injection needle (25) of the syringe being driven into the septum (24) of the cap (29). The invention enables a preparation which is directly injectable by an automatic rehydration step to be obtained; indeed, after activation, the extemporaneous preparation is automatic since the device elements move by themselves under the action of the liquid which is drawn by suction into the volume under vacuum containing the solid formulation (18).

    Abstract translation: 一种包括以下步骤的方法：在真空中制备具有活性成分的干燥形式（18）以及液体（22），并通过真空作用将该液体拉成干燥形式，以获得可注射的 制备。 该装置包括气密注射器（19），用于在真空下干燥形式，容纳液体（22）的储存器（12）和在注射器和液体储存器之间形成连接器的盖（29），注射针 ）被驱动进入盖（29）的隔膜（24）中。 本发明能够通过自动补液步骤直接注射的制剂; 事实上，在活化之后，临时制剂是自动的，因为装置元件在由含有固体制剂（18）的真空吸入体积的液体作用下自身移动。

    Apparatus for the delivery of elongate solid drug compositions
    7.
    发明授权
    Apparatus for the delivery of elongate solid drug compositions 失效
    用于递送细长固体药物组合物的装置

    公开(公告)号：US5837276A

    公开(公告)日：1998-11-17

    申请号：US300138

    申请日：1994-09-02

    Applicant: Roland Cherif Cheikh

    Inventor： Roland Cherif Cheikh

    IPC: A61F2/00 ,  A61J1/00 ,  A61J1/20 ,  A61K9/00 ,  A61K9/06 ,  A61K9/20 ,  A61K9/22 ,  A61K9/70 ,  A61K38/22 ,  A61K38/25 ,  A61K38/28 ,  A61K38/29 ,  A61K38/31 ,  A61K47/26 ,  A61L9/00 ,  A61L15/44 ,  A61M5/00 ,  A61M5/14 ,  A61M5/142 ,  A61M5/152 ,  A61M31/00 ,  B65D83/00

    CPC classification number: A61K9/0024 ,  A61K38/28 ,  A61K9/0019 ,  A61K9/06 ,  A61K9/2018 ,  A61K9/70 ,  A61M31/002 ,  A61M37/0069 ,  A61J1/201 ,  A61K47/26

    Abstract: The invention features an implantable device for the automatic delivery of an active ingredient according to an adjustable delivery profile. The device includes a housing; a reservoir operatively connected to the housing and arranged to store an elongate solid composition including the active ingredient, such as a filament of tape; an actuator arranged within the housing to move the solid composition from the reservoir to a transit assembly, providing a water-tight seal wherein the solid composition exits the housing at the transit assembly; a controller that acts on the actuator to adjust movement of the solid composition out of the housing according to the adjustable delivery profile; and a power source arranged to provide energy to the actuator and the controller. The solid composition can be an elongate, solid composition comprising a drug, and up to 90% of a carrier, wherein the composition has a cross-section of less than 0.5 mm, and wherein the drug and the carrier are selected and compounded in a proportion such that the drug is immediately released from the carrier upon contact with a liquid.

    Abstract translation: 本发明的特征在于一种可植入装置，用于根据可调输送轮廓自动递送活性成分。 该装置包括壳体; 储存器，其操作地连接到所述壳体并且布置成存储包括所述活性成分的细长固体组合物，例如带状丝; 布置在壳体内的致动器，用于将固体组合物从储存器移动到运输组件，提供水密封，其中固体组合物在运输组件处离开壳体; 作用在致动器上的控制器，以根据可调输送轮廓来调节固体组合物离开壳体的运动; 以及布置成向致动器和控制器提供能量的电源。 固体组合物可以是细长的固体组合物，其包含药物和至多90％的载体，其中所述组合物具有小于0.5mm的横截面，并且其中所述药物和载体被选择并复合于 使得药物在与液体接触时立即从载体释放。

    Osmotic pumps
    9.
    发明授权
    Osmotic pumps 失效
    渗透泵

    公开(公告)号：US5279608A

    公开(公告)日：1994-01-18

    申请号：US802326

    申请日：1991-12-04

    Applicant: Roland Cherif Cheikh

    Inventor： Roland Cherif Cheikh

    IPC: A61M5/148 ,  A61M5/00 ,  A61M5/14 ,  A61M5/145

    CPC classification number: A61M5/145 ,  A61M2005/14513

    Abstract: An osmotic pump comprises a housing (2) within which is a delivery chamber (5) separated from an osmotic salt chamber (7) by impermeable moveable pressure responsive means such as a piston (6) or a flexible membrane. The osmotic salt chamber (7) is separated from a source of osmotic fluid, e.g. an osmotic fluid chamber (12), by a semipermeable membrane (96,36), optionally mounted in a piston (9,23). A fluid barrier isolates the osmotic salt chamber (7) from the source of osmotic fluid for storage of the pump, and may be inactivated when the pump is to be used. The fluid barrier may be a foil sheet (10), inactivatable by rupture, or a piston and a fluid bypass arrangement (21,23). Activation of the osmotic pump may be effected in some embodiments by loading the discharge chamber (5) with the agent to be delivered and in other embodiments by movement of a plunger (16), under manual control or, if the plunger is pre-biassed, by release of a locking means (18) which holds it in position.

    Abstract translation: 渗透泵包括壳体（2），在其中是通过不可渗透的可移动压力响应装置例如活塞（6）或柔性膜与渗透盐室（7）分离的输送室（5）。 渗透盐室（7）与渗透液源（例如， 通过半透膜（96,36），可选地安装在活塞（9,23）中的渗透液室（12）。 流体屏障将渗透盐室（7）与渗透液源隔离，以便储存泵，并且当使用泵时可以使其失活。 流体屏障可以是通过破裂而不活动的箔片（10），或活塞和流体旁路装置（21,23）。 渗透泵的活化可以在一些实施方案中通过将放电室（5）与待递送的药剂装载在一起，并且在其它实施方案中通过在手动控制下的柱塞（16）的运动来实现，或者如果柱塞是预先偏置的 通过释放将其保持在适当位置的锁定装置（18）。

    METHOD FOR THE PREPARATION OF PLYMERS WITH VARIED ARCHTECTURE AND AMIDE INITIATION
    10.
    发明申请
    METHOD FOR THE PREPARATION OF PLYMERS WITH VARIED ARCHTECTURE AND AMIDE INITIATION 审中-公开
    用于制备具有变化的结构和氨基酸启动的聚合物的方法

    公开(公告)号：US20130317121A1

    公开(公告)日：2013-11-28

    申请号：US13885654

    申请日：2011-11-14

    Applicant: Didier Bourissou ,  Blanca Martin-Vaca ,  Aurélie Alba ,  Roland Cherif-Cheikh ,  Anne-Paula De Sousa Delgado

    Inventor： Didier Bourissou ,  Blanca Martin-Vaca ,  Aurélie Alba ,  Roland Cherif-Cheikh ,  Anne-Paula De Sousa Delgado

    IPC: A61K47/34

    CPC classification number: A61K47/34 ,  C08G63/08 ,  C08G63/6852 ,  C08G63/81 ,  C08G63/823

    Abstract: The invention relates to a method for preparing linear polymers having an amide end or having a star architecture comprising an amide core, by means of a ring opening using lactide and glycolide monomers or a lactide monomer ring in the presence of a catalyst, wherein the method includes the steps of: (i) reacting the excess monomer(s) with an initiator in a solvent, said initiator being selected from among an amine and an amino alcohol, given that the initiator has at least one primary or secondary amine function; (ii) adding a catalyst, said catalyst being a non-nucleophilic base and including at least one neutral sp2 nitrogen atom; and (iii) neutralizing the reaction mixture. Said novel method is particularly advantageous in that it can be easily monitored and enables better modulation of the polymers, and thus of the properties thereof, than the methods of the prior art. The invention also relates to novel polymers that are obtainable by means of said method.

    Abstract translation: 本发明涉及一种通过在催化剂存在下通过使用丙交酯和乙交酯单体或丙交酯单体环的开环制备具有酰胺末端或具有包含酰胺核心的星型结构的线性聚合物的方法，其中所述方法 包括以下步骤：（i）使多余的单体与引发剂在溶剂中反应，所述引发剂选自胺和氨基醇，假定引发剂具有至少一个伯或仲胺官能团; （ii）加入催化剂，所述催化剂是非亲核碱，并包括至少一个中性sp2氮原子; 和（iii）中和反应混合物。 所述新颖的方法特别有利的是，与现有技术的方法相比，其可以容易地被监测并且能够更好地调节聚合物，并因此实现其性质。 本发明还涉及通过所述方法可获得的新型聚合物。

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