公开(公告)号：US06558957B1

公开(公告)日：2003-05-06

申请号：US09707498

申请日：2000-11-07

申请人： Kurt Roinestad ,  Frank S. Cheng ,  Philip J. Palermo ,  Kevin Bynum

发明人： Kurt Roinestad ,  Frank S. Cheng ,  Philip J. Palermo ,  Kevin Bynum

IPC分类号： G01N2101

CPC分类号： G01N21/33 ,  G01N13/00 ,  G01N21/01 ,  G01N21/05 ,  G01N21/359 ,  G01N21/65 ,  G01N21/8507 ,  G01N33/15 ,  G01N2013/006 ,  G01N2021/6484 ,  G01N2021/651 ,  G01N2021/8521 ,  G01N2021/8528 ,  Y10T436/24 ,  Y10T436/25875

摘要： The present invention relates to an improvement in a detection system used for continuously measuring the release of a drug from a pharmaceutical dosage form comprising a singular dissolution vessel or multiple dissolution vessels containing a dissolution medium and a measuring device for detecting the amount of drug released at a given time, the improvement comprising a mixing shaft and a probe placed within the mixing shaft or outside the individual dissolution vessels, the probe capable of measuring the dissolution characteristics using UV, IR, near-IR, fluorescence, electrochemical, and Raman spectroscopy techniques. The present invention also relates to a method for predicting the dissolution curve provided by a controlled release pharmaceutical dosage form comprising taking continuous measurements of the amount of drug released from a dosage form for a portion of the time over which the drug is expected to be released and predicting the remainder of the dissolution curve based on the values obtained.

摘要翻译： 本发明涉及一种检测系统的改进，所述检测系统用于连续地测量药物从包含溶解介质的单一溶出容器或多个溶解容器的药物剂型中释放的检测系统，所述检测系统包括用于检测药物释放量的测量装置 在一定时间内，改进包括混合轴和放置在混合轴内或各个溶解容器外部的探针，该探针能够使用UV，IR，近红外，荧光，电化学和拉曼光谱技术测量溶解特性 。 本发明还涉及一种用于预测由控释药物剂型提供的溶出曲线的方法，包括连续测量药物预期释放的一段时间内从剂型中释放的药物的量 并基于获得的值预测溶出曲线的剩余部分。

公开(公告)号：US06174497B1

公开(公告)日：2001-01-16

申请号：US08915785

申请日：1997-08-21

申请人： Kurt Roinestad ,  Frank S. Cheng ,  Philip J. Palermo ,  Kevin Bynum

发明人： Kurt Roinestad ,  Frank S. Cheng ,  Philip J. Palermo ,  Kevin Bynum

IPC分类号： G01N2101

CPC分类号： G01N21/33 ,  G01N13/00 ,  G01N21/01 ,  G01N21/05 ,  G01N21/359 ,  G01N21/65 ,  G01N21/8507 ,  G01N33/15 ,  G01N2013/006 ,  G01N2021/6484 ,  G01N2021/651 ,  G01N2021/8521 ,  G01N2021/8528 ,  Y10T436/24 ,  Y10T436/25875

摘要： The present invention relates to an improvement in a detection system used for continuously measuring the release of a drug from a pharmaceutical dosage form having a singular dissolution vessel or multiple dissolution vessels containing a dissolution medium and a measuring device for detecting the amount of drug released at a given time, the improvement being a mixing shaft and a probe placed within the mixing shaft or outside the individual dissolution vessels, the probe capable of measuring the dissolution characteristics using UV, IR, near-IR, fluorescence, electrochemical, and Raman spectroscopy techniques. The present invention also relates to a method for predicting the dissolution curve provided by a controlled release pharmaceutical dosage form by taking continuous measurements of the amount of drug released from a dosage form for a portion of the time over which the drug is expected to be released and predicting the remainder of the dissolution curve based on the values obtained.

摘要翻译： 本发明涉及一种检测系统的改进，该检测系统用于从具有单一溶出容器或含有溶出介质的多个溶解容器的药物剂型连续测量药物的释放，以及用于检测药物释放量的测量装置 给定的时间，改进是混合轴和放置在混合轴内或在各个溶解容器之外的探针，该探针能够使用UV，IR，近红外，荧光，电化学和拉曼光谱技术测量溶解特性 。 本发明还涉及一种用于通过连续测量药物预期释放的一段时间内从剂型中释放的药物的量来预测由控释药物剂型提供的溶出曲线的方法 并基于获得的值预测溶出曲线的剩余部分。

公开(公告)号：US6130434A

公开(公告)日：2000-10-10

申请号：US316862

申请日：1999-05-21

申请人： James A. Mitchell ,  Philip J. Palermo

发明人： James A. Mitchell ,  Philip J. Palermo

IPC分类号： G01Q30/04 ,  G01Q30/08 ,  H01J37/00 ,  H01J37/18 ,  H01J37/20 ,  H01J37/252 ,  H01J37/26 ,  H01J37/28

CPC分类号： G01N23/2204 ,  H01J37/20 ,  H01J37/28 ,  H01J2237/2001 ,  H01J2237/2002 ,  H01J2237/2003 ,  H01J2237/2005 ,  H01J2237/204 ,  H01J2237/206 ,  H01J2237/2605

摘要： A system is provided for imaging, in an ESE microscope or other variable pressure microscope, a single sample at various time intervals during dissolution of the sample in a liquid. The system includes a sample chamber having a sample well. The sample well includes an first fluid port and a second fluid port for forming a dissolution bath in the sample well. In accordance with the system according to the present invention, the sample chamber is placed into the specimen chamber of the ESE microscope and a sample is deposited into the sample well of the sample chamber. The sample is immersed in a liquid which flows through the sample well via the first and second fluid ports during a dissolution cycle. The liquid is then drained from the sample well via one of the first and second fluid ports during a draining cycle, and then, during an imaging cycle, the sample is imaged by the ESE microscope. The dissolution cycle, the draining cycle, and the imaging cycle all occur while the sample well is inside the specimen chamber of the ESE microscope.

公开(公告)号：US06627635B2

公开(公告)日：2003-09-30

申请号：US09815162

申请日：2001-03-22

申请人： Philip J. Palermo ,  Robert F. Kaiko ,  Robert D. Colucci

发明人： Philip J. Palermo ,  Robert F. Kaiko ,  Robert D. Colucci

IPC分类号： A61K3144

CPC分类号： A61K31/44 ,  A61K31/485 ,  Y10S514/81 ,  Y10S514/812 ,  A61K2300/00

摘要： The invention relates in part to a method of reducing the abuse potential of an oral dosage form of an opioid analgesic, wherein an analgesically effective amount of an orally active opioid agonist is combined with an opioid antagonist into an oral dosage form which would require at least a two-step extraction process to be separated from the opioid agonist, the amount of opioid antagonist including being sufficient to counteract opioid effects if extracted together with the opioid agonist and administered parenterally.

公开(公告)号：US06444982B1

公开(公告)日：2002-09-03

申请号：US09599325

申请日：2000-06-22

申请人： James A. Mitchell ,  Philip J. Palermo

发明人： James A. Mitchell ,  Philip J. Palermo

IPC分类号： H01J3700

CPC分类号： G01N23/2204 ,  H01J37/20 ,  H01J37/28 ,  H01J2237/2001 ,  H01J2237/2002 ,  H01J2237/2003 ,  H01J2237/2005 ,  H01J2237/204 ,  H01J2237/206 ,  H01J2237/2605

摘要： A system is provided for imaging, in an ESE microscope or other variable pressure microscope, a single sample at various time intervals during dissolution of the sample in a liquid. The system includes a sample chamber having a sample well. The sample well includes an first fluid port and a second fluid port for forming a dissolution bath in the sample well. In accordance with the system according to the present invention, the sample chamber is placed into the specimen chamber of the ESE microscope and a sample is deposited into the sample well of the sample chamber. The sample is immersed in a liquid which flows through the sample well via the first and second fluid ports during a dissolution cycle. The liquid is then drained from the sample well via one of the first and second fluid ports during a draining cycle, and then, during an imaging cycle, the sample is imaged by the ESE microscope. The dissolution cycle, the draining cycle, and the imaging cycle all occur while the sample well is inside the specimen chamber of the ESE microscope.

摘要翻译： 提供了一种系统，用于在ESE显微镜或其它可变压力显微镜下，将样品溶解在液体中，以不同的时间间隔对单个样品进行成像。 该系统包括具有样品阱的样品室。 样品阱包括用于在样品阱中形成溶解浴的第一流体端口和第二流体端口。 根据本发明的系统，将样品室放置在ESE显微镜的样品室中，并将样品沉积到样品室的样品孔中。 在溶解循环期间，将样品浸入通过第一和第二流体端口流经样品的液体中。 然后在排液循环期间，通过第一和第二流体端口之一从样品阱中排出液体，然后在成像周期期间，通过ESE显微镜对样品进行成像。 当样品孔在ESE显微镜的样品室内时，溶解循环，排水循环和成像循环都会发生。

公开(公告)号：US06228863B1

公开(公告)日：2001-05-08

申请号：US09218663

申请日：1998-12-22

申请人： Philip J. Palermo ,  Robert D. Colucci ,  Robert F. Kaiko

发明人： Philip J. Palermo ,  Robert D. Colucci ,  Robert F. Kaiko

IPC分类号： A61K3144

CPC分类号： A61K31/44 ,  A61K31/485 ,  Y10S514/81 ,  Y10S514/812 ,  A61K2300/00

摘要： The invention relates in part to a method of reducing the abuse potential of an oral dosage form of an opioid analgesic, wherein an analgesically effective amount of an orally active opioid agonist is combined with an opioid antagonist into an oral dosage form which would require at least a two-step extraction process to be separated from the opioid agonist, the amount of opioid antagonist including being sufficient to counteract opioid effects if extracted together with the opioid agonist and administered parenterally.

摘要翻译： 本发明部分地涉及减少口服剂型阿片类止痛剂的滥用潜力的方法，其中止痛有效量的口服活性阿片样物质激动剂与阿片样物质拮抗剂组合成口服剂型，其至少需要 与阿片样物质激动剂分离的两步提取过程，阿片样物质拮抗剂的量如果与阿片样物质激动剂一起提取并肠胃外给药，则其量足以抵消阿片样物质的影响。