公开(公告)号：US4933431A

公开(公告)日：1990-06-12

申请号：US269448

申请日：1988-11-09

申请人： Abraham J. Domb ,  Robert S. Langer ,  Eyal Ron ,  Steven Giannos ,  Rohit Kothari ,  Edith Mathiowitz

发明人： Abraham J. Domb ,  Robert S. Langer ,  Eyal Ron ,  Steven Giannos ,  Rohit Kothari ,  Edith Mathiowitz

IPC分类号： C08G67/04 ,  C08G69/08 ,  C08G69/10

CPC分类号： C08G69/08 ,  C08G67/04 ,  C08G69/10

摘要： A method for synthetizing polyanhydrides in solution using coupling agents and a removable acid acceptor to effect a one-step polymerization of dicarboxylic acids. As used in the method, these coupling agents include phosgene, diphosgene, and acid chlorides. Insoluble acid acceptors include insoluble polyamines and crosslinked polyamines such as polyethyleneimine and polyvinylpyridine and inorganic bases such as K.sub.2 CO.sub.3, Na.sub.2 CO.sub.3, NaHCO.sub.3, and CaCO.sub.3. The only byproduct formed is a removable hydrochloric acid-acid acceptor.Examples are provided of the polymerization of highly pure polyanhydrides using phosgene, diphosgene or an acid chloride as the coupling agent, in combination with either an insoluble acid acceptor or a soluble acid acceptor in a solvent wherein the polymerizaiton byproduct or polymer is insoluble.A particularly important application of these polyanhydrides is in the formation of drug delivery devices containing bioactive compounds. The method is also useful in the polymerization of dicarboxylic acids including heat liable dipeptides of glutamic or aspartic acid.

摘要翻译： 使用偶联剂和可除去的酸受体在溶液中合成聚酐以实现二羧​​酸的一步聚合的方法。 如该方法所用，这些偶联剂包括光气，双光气和酰氯。 不溶性酸受体包括不溶性多胺和交联聚胺如聚乙烯亚胺和聚乙烯吡啶以及无机碱如K 2 CO 3，Na 2 CO 3，NaHCO 3和CaCO 3。 形成的唯一副产物是可除去的盐酸酸受体。 提供了使用光气，双光气或酰氯作为偶联剂的高纯度聚酐与在溶剂中的不溶性酸受体或可溶性酸受体组合的聚合反应，其中聚合物副产物或聚合物是不溶的。 这些多酸酐的特别重要的应用是形成含有生物活性化合物的药物递送装置。 该方法也可用于二羧酸的聚合，包括谷氨酸或天冬氨酸的热应答二肽。

公开(公告)号：US4916204A

公开(公告)日：1990-04-10

申请号：US80332

申请日：1987-07-31

申请人： Abraham J. Domb ,  Robert S. Langer ,  Eyal Ron ,  Steven Giannos ,  Rohit Kothari ,  Edith Mathiowitz

发明人： Abraham J. Domb ,  Robert S. Langer ,  Eyal Ron ,  Steven Giannos ,  Rohit Kothari ,  Edith Mathiowitz

IPC分类号： A61K31/335 ,  A61K31/365 ,  A61K31/39 ,  C08G67/04 ,  C08G69/08 ,  C08G69/10

CPC分类号： A61K31/335 ,  A61K31/365 ,  A61K31/39 ,  C08G67/04 ,  C08G69/08 ,  C08G69/10 ,  Y10S514/863

摘要： A method for synthesizing polyanhydrides in solution using coupling agents and a removable acid acceptor to effect a one-step polymerization of dicarboxylic acids. As used in the method, these coupling agents include phosgene, diphosgene, and acid chlorides. Insoluble acid acceptors include insoluble polyamines and crosslinked polyamines such as polyethyleneimine and polyvinylpyridine and inorganic bases such as K.sub.2 CO.sub.3, Na.sub.2 CO.sub.3, NaHCO.sub.3, and CaCO.sub.3. The only byproduct formed is a removable hydrochloric acid-acid acceptor.Examples are provided of the polymerization of highly pure polyanhydrides using phosgene, diphosgene or an acid chloride as the coupling agent, in combination with either an insoluble acid acceptor or a soluble acid acceptor in a solvent wherein the polymerization byproduct or polymer is insoluble.A particularly important application of these polyanhydrides is in the formation of drug delivery devices containing bioactive compounds. The method is also useful in the polymerization of dicarboxylic acids including heat liable dipeptides of glutamic or aspartic acid.

摘要翻译： 使用偶联剂和可除去的酸受体在溶液中合成聚酐以进行二羧酸的一步聚合的方法。 如该方法所用，这些偶联剂包括光气，双光气和酰氯。 不溶性酸受体包括不溶性多胺和交联聚胺如聚乙烯亚胺和聚乙烯吡啶以及无机碱如K 2 CO 3，Na 2 CO 3，NaHCO 3和CaCO 3。 形成的唯一副产物是可除去的盐酸酸受体。 提供了使用光气，双极光或酰氯作为偶联剂的高纯度聚酐与在溶剂中的不溶性酸受体或可溶性酸受体组合的聚合反应，其中聚合副产物或聚合物是不溶的。 这些多酸酐的特别重要的应用是形成含有生物活性化合物的药物递送装置。 该方法也可用于二羧酸的聚合，包括谷氨酸或天冬氨酸的热应答二肽。

公开(公告)号：US20060062838A1

公开(公告)日：2006-03-23

申请号：US11162525

申请日：2005-09-13

申请人： Guy DiPierro ,  Steven Giannos

发明人： Guy DiPierro ,  Steven Giannos

IPC分类号： A61N1/30 ,  A61K9/70

CPC分类号： A61M35/00 ,  A61K9/0009 ,  A61K9/0014 ,  A61K9/703 ,  A61K31/00 ,  A61K31/04 ,  A61K31/137 ,  A61K31/465 ,  A61M37/00 ,  A61M37/0015 ,  A61M37/0092 ,  A61M39/22 ,  A61M2037/0007 ,  A61M2037/0023 ,  A61M2037/0061 ,  A61M2205/0266 ,  A61M2205/3337 ,  A61M2205/50 ,  A61N1/30

摘要： Systems and methods for treating diseases, addictions and disorders in humans and animals involving synchronizing and tailoring the administration of drug compounds with the body's natural circadian rhythms, in order to counteract symptoms when they are likely to be at their worst. Automated and pre programmable transdermal drug administration system are used. This system can also utilize a pump or pressurized reservoir, and/or a system for removing depleted carrier solution, or other modulated dispensing actuator, in conjunction with micro-fabricated structures commonly referred to as Micro-needles, or heat, or iontophoresis, sonophoresis, or a wide range of chemical permeation enhancers.

摘要翻译： 用于治疗人类和动物中的疾病，成瘾症和疾病的系统和方法，其涉及使身体的天然昼夜节律同时和定制药物化合物的施用，以便当它们可能处于最坏状态时抵抗症状。 使用自动化和预先编程的透皮药物给药系统。 该系统还可以结合通常称为微针的微制造结构，或加热或离子电渗疗法，超声波引导，利用泵或加压储存器和/或用于去除耗尽的载体溶液或其它调制分配致动器的系统 ，或广泛的化学渗透增强剂。