公开(公告)号：US20020173467A1

公开(公告)日：2002-11-21

申请号：US10127558

申请日：2002-04-23

申请人： Takeda Chemical Industries, Ltd.

发明人： Shigeru Kamei ,  Yasutaka Igari ,  Yasuaki Ogawa

IPC分类号： A61K038/10 ,  A61K009/22 ,  A61K009/14

CPC分类号： C07K7/23 ,  A61K9/1647 ,  A61K38/00 ,  A61K38/09

摘要： A sustained-release preparation which comprises a physiologically active peptide of general formula 1 wherein X represents an acyl group; R1, R2 and R4 each represents an aromatic cyclic group; R3 represents a D-amino acid residue or a group of the formula 2 wherein R3null is a heterocyclic group; R5 represents a group of the formula null(CH2)nnullR5null wherein n is 2 or 3, and R5null is an amino group which may optionally be substituted, an aromatic cyclic group or an O-glycosyl group; R6 represents a group of the formula null(CH2)nnullR6null wherein n is 2 or 3, and R6null is an amino group which may optionally be substituted; R7 represents a D-amino acid residue or an azaglycyl residue; and Q represents hydrogen or a lower alkyl group, or a salt thereof and a biodegradable polymer having a terminal carboxyl group. The sustained-release preparation shows a constant release of the peptide over a long time and is substantially free from an initial burst.

摘要翻译： 一种持续释放制剂，其包含通式的生理活性肽，其中X表示酰基; R1，R2和R4各自表示芳族环状基团; R3表示D-氨基酸残基或下式的基团其中R3'是杂环基; R5表示式 - （CH2）n-R5'的基团，其中n为2或3，R5'为任选取代的氨基，芳族环基或O-糖基; R6表示式 - （CH2）n-R6'的基团，其中n为2或3，R6'为可任意取代的氨基; R7表示D-氨基酸残基或氮杂十八烷基残基; Q表示氢或低级烷基，或其盐和具有末端羧基的生物降解性聚合物。 持续释放制剂显示长时间的肽的恒定释放并且基本上没有初始爆发。

公开(公告)号：US20020165248A1

公开(公告)日：2002-11-07

申请号：US10128632

申请日：2002-04-23

发明人： Walter Wimmer ,  Bianca Brogmann ,  Udo Hahn ,  Christof Spitzley

IPC分类号： A61K009/22 ,  A61K031/485

CPC分类号： A61K31/485 ,  A61K9/209 ,  A61K31/135 ,  A61K31/137

摘要： The invention is relative to a pharmaceutical preparation, especially for oral administration, with at least one active substance and with formulation components influencing the release of active substance, which preparation comprises at least one opiod analgesic as active substance that is formulated proportionally on the one hand for rapid release and on the other hand for delayed release in such a manner that the in vitro release rate from the preparation according to the Ph. Eur. paddle test shows a mean value of above 40% by weight after one hour and that the in vitro release rate shows a mean value that is still below 80% by weight after four hours.

摘要翻译： 本发明相对于药物制剂，特别是用于口服给药，具有至少一种活性物质和影响活性物质释放的制剂组分，该制剂包含至少一种作为活性物质的阿司匹林止痛剂，一方面按比例配制 用于快速释放，另一方面用于延迟释放，使得从根据Ph.Eur。的制剂的体外释放速率。 桨试验在1小时后显示出高于40重量％的平均值，体外释放速率显示出在4小时后仍低于80重量％的平均值。

公开(公告)号：US20020161354A1

公开(公告)日：2002-10-31

申请号：US09925598

申请日：2001-08-09

发明人： Chris C. Christiansen ,  James M. Olsen

IPC分类号： A61K009/22

CPC分类号： A61M5/14276

摘要： A human body implantable drug delivery pump comprises a housing including at least a first shield and a second shield. The housing defines an interior within the shields. The pump further includes a fluid reservoir within the housing, a fluid conduit also within the housing from the reservoir, an outlet from the fluid conduit to the exterior of the housing, and a pump member in the housing adapted to move fluid through the fluid conduit to the outlet. The fluid in the reservoir and fluid conduit is isolated from the pump interior. The pump further comprises a desiccant in the pump interior, the desiccant absorbent of moisture in the pump interior, and preferably absorbent of substantially all the moisture in the pump interior. The desiccant also preferably has a moisture absorbent property dependent on temperature, being lessened at higher temperatures, the desiccant being pre-baked to improve its moisture absorbent property before being placed in the pump. Most preferably, the desiccant is still further absorbent of moisture, whereby the desiccant may be placed within the housing during final assembly of the pump when the pump housing is not completely sealed, and the desiccant is absorbent during a time period of final assembly, and remains absorbent of substantially all the moisture within the housing after complete sealing of the housing. The desiccant may be molded to fit free space within the housing, and the desiccant may comprise liquid silicon rubber and aluminum oxide. A prior art, time consuming, baking of the whole pump and creation and sealing of a tig hole, is avoided.

摘要翻译： 人体可植入药物输送泵包括至少包括第一屏蔽和第二屏蔽的壳体。 壳体限定了屏蔽内的内部。 所述泵还包括在所述壳体内的流体贮存器，还存在从所述容器的壳体内的流体导管，从所述流体导管到所述壳体的外部的出口以及所述壳体中的泵构件，其适于将流体移动通过所述流体导管 到出口。 储存器和流体导管中的流体与泵内部隔离。 泵还包括泵内部的干燥剂，泵内部的湿气的干燥剂吸收剂，并且优选地在泵内部基本上吸收所有的水分。 干燥剂还优选具有取决于温度的吸湿性，在较高温度下减弱，干燥剂被预烘烤以在放入泵之前改善其吸湿性能。 最优选地，干燥剂仍然是更多的吸湿剂，其中当泵壳体未被完全密封时，干燥剂在泵的最终组装期间可以放置在壳体内，并且干燥剂在最终组装的时间段内是吸收性的，以及 在壳体完全密封之后仍然保持壳体内几乎全部水分的吸收。 干燥剂可以被模制以在壳体内配合自由空间，并且干燥剂可以包括液体硅橡胶和氧化铝。 避免了现有技术，耗时，整个泵的烘烤和丝绒孔的产生和密封。

公开(公告)号：US20020142033A1

公开(公告)日：2002-10-03

申请号：US09801469

申请日：2001-03-07

发明人： Suneel K. Gupta ,  Gayatri Sathyan ,  Samuel R. Saks

IPC分类号： A61K009/22

CPC分类号： A61K9/0004 ,  A61K31/216

摘要： A method is disclosed for the management of dry mouth associated with the administration of an anticholinergic drug to a patient. Also, a composition and a device are disclosed comprising an anticholinergic drug administered for anticholinergic therapy.

摘要翻译： 公开了一种用于管理与向患者施用抗胆碱能药物相关的干口的方法。 此外，公开了组合物和装置，其包含用于抗胆碱能治疗的抗胆碱能药物。

公开(公告)号：US20020137765A1

公开(公告)日：2002-09-26

申请号：US09940097

申请日：2001-08-27

发明人： Mary T. Am Ende ,  William J. Curatolo ,  Scott M. Herbig

IPC分类号： A61K009/22 ,  A61K031/4745

CPC分类号： A61K9/0004 ,  A61K9/2054 ,  A61K9/2059 ,  A61K9/2866

摘要： The present invention relates to formulations for administering a growth hormone secretagogue. More specifically, the present invention relates to sustained release formulations for administering a growth hormone secretagogue and formulations for administering a growth hormone secretagogue that provide for a part of the dose of the growth hormone secretagogue to be administered using an immediate release formulation and part of the dose of the growth hormone secretagogue to be administered using a sustained release formulation.

摘要翻译： 本发明涉及用于施用生长激素促分泌素的制剂。 更具体地，本发明涉及用于施用生长激素促分泌素的缓释制剂和用于施用生长激素促分泌素的制剂，所述制剂提供使用立即释放制剂施用的一部分生长激素促分泌素的剂量， 使用持续释放制剂来施用生长激素促分泌素的剂量。

公开(公告)号：US20020132001A1

公开(公告)日：2002-09-19

申请号：US09854264

申请日：2001-05-11

发明人： Susan M. Garthwaite ,  Leo K. Mathur

IPC分类号： A61K009/22

CPC分类号： A61K45/06 ,  A61K9/2018 ,  A61K9/2054 ,  A61K9/2846 ,  A61K9/4858 ,  A61K9/4866 ,  A61K9/4891 ,  A61K31/00 ,  A61K31/57 ,  A61K31/585 ,  A61K2300/00

摘要： A pharmaceutical composition is provided for administration to a subject mammal such as a human exhibiting a diurnal cycle of plasma aldosterone concentration, the composition comprising a delayed-release formulation of an aldosterone antagonist drug, e.g., eplerenone, in a therapeutically effective amount. The delayed-release formulation, when administered about 6 hours to about 12 hours prior to the acrophase, results in a profile of plasma drug concentration that corresponds substantially to the diurnal cycle of plasma aldosterone concentration.

摘要翻译： 提供药物组合物用于给予受试哺乳动物例如表现出血浆醛固酮浓度的昼夜循环的人，该组合物包含治疗有效量的醛固酮拮抗剂药物例如依普利酮的延迟释放制剂。 延迟释放制剂当在该亲水合酶之前约6小时至约12小时施用时，导致等离子体药物浓度的曲线，其基本上对应于血浆醛固酮浓度的昼夜循环。

公开(公告)号：US20020110635A1

公开(公告)日：2002-08-15

申请号：US10055584

申请日：2002-01-23

发明人： Michael J. Brubaker ,  Pavlos Papadopoulos ,  Ramesh Krishnamoorthy

IPC分类号： A61K009/22

CPC分类号： A61K9/0051

摘要： Disclosed is an improved sustained release drug delivery device and method of producing such device. The device comprises a drug core in an impermeable cup or impermeable coating layer that is adhered to an uncured suture tab and covered with a permeable polymer coating layer that is similar to the makeup of the suture tab. The permeable polymer coating layer that covers the device, covering the impermeable coating layer and at least a portion of the drug core, is cured (after drying) along with the uncured suture tab. The nullcocuringnull or one step curing process forms a very strong bond between the outer coating layer to the suture tab preventing leaks.

摘要翻译： 公开了一种改进的缓释药物递送装置及其制造方法。 该装置包括不渗透杯或不渗透涂层中的药物核心，其粘附到未固化的缝合片上，并覆盖有类似于缝合片的组成的可渗透的聚合物涂层。 覆盖该装置的可渗透聚合物涂层覆盖该不透水涂层和该药芯的至少一部分，与未固化的缝合片一起被固化（干燥后）。 “共固化”或一步固化过程在外涂层与缝合线片之间形成非常牢固的粘结，防止泄漏。

公开(公告)号：US20020103475A1

公开(公告)日：2002-08-01

申请号：US09772702

申请日：2001-01-30

发明人： John M. Bartha ,  Lehel Balint ,  Gregory Zeltser ,  Arthur Bunzel ,  Yin S. Tang

IPC分类号： A61K009/22

CPC分类号： A61M5/14276 ,  A61K35/12 ,  A61K2035/126 ,  C12N5/0677

摘要： An implantable bioartificial active secretion system for providing a physiological secretion such as insulin necessary for functionality of a physiologic activity such as glucose metabolism of a living-being host. The system includes a housing implantable within the host in fluidic communication with tissue fluid indicative of secretion need. A chamber within the housing contains a plurality of physiologically active, autonomously functioning, live secretory cells for producing the physiological secretion. A periodically operating pump apparatus moves tissue fluid into contact with the secretory cells for pick up of the regulating physiological secretion for subsequent physiologically-effective dispensing into the host while avoiding immunorejection of the host body or of the host to the secretory cells.

摘要翻译： 一种可植入的生物人工活性分泌系统，用于提供诸如活体宿主的生理活性如葡萄糖代谢功能的必需的生理分泌物，例如胰岛素。 该系统包括可植入主体内的壳体，其与指示分泌需要的组织液体流体连通。 壳体内的腔室包含多个生理活性的，自主功能的活分泌细胞，用于产生生理分泌。 周期性操作的泵装置使组织液与分泌细胞接触，用于拾取调节生理分泌物，用于随后的生理有效分配到宿主中，同时避免宿主体或宿主免疫分泌到分泌细胞。

公开(公告)号：US20020102302A1

公开(公告)日：2002-08-01

申请号：US10052844

申请日：2001-10-19

发明人： Benjamin Oshlack ,  Hua-Pin Huang ,  Mark Chasin ,  Paul Goldenheim

IPC分类号： A61K009/22 ,  A61K031/137

CPC分类号： A61K9/2054 ,  A61K9/2013 ,  A61K9/2095

摘要： A stabilized sustained release oral solid dosage form which includes an effective amount of tramadol or a pharmaceutically acceptable salt thereof dispersed in a matrix of a hydrophobic material comprising a wax-like substance which was melted or softened during the preparation of the matrix, is cured at a temperature from about 35null C. to about 65null C. for a time period from about 4 to about 72 hours, such that the formulation, when subjected to in-vitro dissolution after exposure to accelerated storage conditions of at least one month at 40null C./75% RH, releases an amount of tramadol which does not vary at any given dissolution time point by more than about 20% of the total amount of tramadol released when compared to in-vitro dissolution conducted prior to subjecting the dosage form to the accelerated storage conditions.

摘要翻译： 稳定的持续释放口服固体剂型，其包含分散在疏水性材料的基质中的有效量的曲马朵或其药学上可接受的盐，其包含在制备基质期间熔融或软化的蜡状物质，其在 温度为约35℃至约65℃，时间为约4至约72小时，使得当暴露于至少一个月的加速储存条件后经受体外溶解时，该制剂 40℃/ 75％RH时，释放一定量的曲马多，与任何给定的溶解时间点相比，在与给药剂量之前进行的体外溶出相比，释放曲马多总量的大约20％ 形成加速存储条件。

公开(公告)号：US20020095138A1

公开(公告)日：2002-07-18

申请号：US09896149

申请日：2001-06-29

发明人： George R. Lynch ,  Andrew Nelson ,  Gilles Petitjean

IPC分类号： A61K009/22

CPC分类号： A61M39/02 ,  A61M5/14244 ,  A61M5/14248 ,  A61M5/158 ,  A61M2005/14252 ,  A61M2005/1581 ,  A61M2005/1587

摘要： System for the subcutaneous delivery into the body of a patient of a fluid from a remote vessel. The system includes a main assembly and placement member with a needle. A delivery tube for carrying the fluid is attached at a near end to the remote reservoir or vessel. At removed end, the delivery tube has a needle for engagement with the main assembly. The main assembly includes a rotating member that when the rotating is perpendicular to the main assembly, it will accept the handle and needle for emplacement of the body onto a patient. After the handle and needle are removed, the delivery tube can be attached to the rotating member which can then be rotated down to a position along to and adjacent the skin of the patient. This provides for a flush mounted infusion device.

摘要翻译： 用于从远程血管皮下递送到患者体液的系统。 该系统包括具有针的主组件和放置构件。 用于承载流体的输送管在近端附接到远程储存器或容器。 在移除端，输送管具有用于与主组件接合的针。 主组件包括旋转构件，当旋转垂直于主组件时，旋转构件将接收用于将身体放置到患者身上的手柄和针。 在手柄和针被移除之后，输送管可以附接到旋转构件，然后可以向下旋转到沿着和邻近患者皮肤的位置。 这提供了一种嵌入式灌注装置。