公开(公告)号：US20100063084A1

公开(公告)日：2010-03-11

申请号：US12620794

申请日：2009-11-18

申请人： Matthew F. Heil ,  Glynn Wilson

发明人： Matthew F. Heil ,  Glynn Wilson

IPC分类号： A61K31/439 ,  C07D491/08 ,  A61P25/00

CPC分类号： A61K31/537 ,  A61K9/5084 ,  C07D451/10 ,  Y02A50/478

摘要： Formulations have been developed administering methscopolamine in multi-phases. In a preferred embodiment, the formulation contains methscopolamine in an immediate release. (“IR”) form and a sustained or delayed release (“DR”) form and/or poised release (“PR”) form. In another embodiment, the methscopolamine is released in a gradient, decreasing the side effects associated with rapidly elevated blood levels. In another embodiment the drug is bound to an ion-exchange resin, which can be suspended in a liquid or incorporated into a matrix for delayed, sustained and/or pulsed release. Dosage unit forms may be tablets, gels, liquids, capsules, beads, microparticles, films or lozenges. Multi-phase delivery can also be achieved through the use of a kit that provides for dosage escalation. This kit can be a blister pack or equivalent, wherein the drug is packaged so that a first dosage is taken, then sequentially larger dosages. The dosages can be the same in each unit, and instructions provided so that the correct dosage is obtained through the number of units and the time of administration or the dosages may be different, and the units ordered so dial the desired dosage administration profile is obtained when the patient takes the units in order as instructed.

摘要翻译： 已经开发了多阶段施用甲泊泊胺的制剂。 在优选的实施方案中，制剂在立即释放中含有甲基东莨菪碱。 （“IR”）形式和持续或延迟释放（“DR”）形式和/或准备释放（“PR”）形式。 在另一个实施方案中，甲基东莨菪碱以梯度释放，减少与快速升高的血液水平相关的副作用。 在另一个实施方案中，药物结合于离子交换树脂，其可以悬浮在液体中或并入基质中用于延迟，持续和/或脉冲释放。 剂量单位形式可以是片剂，凝胶，液体，胶囊，珠粒，微粒，薄膜或锭剂。 多相递送也可以通过使用提供剂量递增的试剂盒来实现。 该试剂盒可以是泡罩包装或等同物，其中药物被包装以便服用第一剂量，然后顺序地更大剂量。 每个单位的剂量可以相同，并且提供说明书，以便通过单位数量和给药时间获得正确的剂量或剂量可以不同，并且获得所选择的单位，从而拨出所需的剂量给药谱 当患者按照指示按顺序接受单位时。

公开(公告)号：US20080085312A1

公开(公告)日：2008-04-10

申请号：US11680355

申请日：2007-02-28

申请人： Glynn Wilson ,  Matthew F. Heil

发明人： Glynn Wilson ,  Matthew F. Heil

IPC分类号： A61K31/075 ,  A61K9/22

CPC分类号： A61K31/075 ,  A61K9/209 ,  Y02A50/401

摘要： Formulations have been developed administering a guaiacolsulfonate salt, preferably potassium salt, in multi-phases. In a preferred embodiment, the formulation contains potassium guaiacolsulfonate in an immediate release (“IR”) form and a sustained or delayed release (“DR”) form and/or pulsed release (“PR”) form. In another embodiment, the potassium guaiacolsulfonate is released in a gradient, decreasing the side effects associated with rapidly elevated blood levels. In another embodiment, the drug is bound to an ion-exchange resin, which can be suspended in a liquid or incorporated into a matrix for delayed, sustained and/or pulsed release. Dosage unit forms may be tablets, gels, liquids, capsules, beads, microparticles, films or lozenges. Multi-phase delivery can also be achieved through the use of a kit that provides for dosage escalation. The formulations are useful in the treatment of one or more symptoms of coughs, colds, sinusitis and other respiratory illnesses. The formulations are also useful in the treatment or relief of fibromyalgia, pain, and Irritable Bowel Syndrome

摘要翻译： 已经开发出多次施用愈创木酚磺酸盐，优选钾盐的制剂。 在优选的实施方案中，制剂含有立即释放（“IR”）形式的愈创木酚磺酸钾和持续或延迟释放（“DR”）形式和/或脉冲释放（“PR”）形式。 在另一个实施方案中，愈创木酚磺酸钾以梯度释放，减少与快速升高的血液水平相关的副作用。 在另一个实施方案中，药物与离子交换树脂结合，离子交换树脂可以悬浮在液体中或并入基质中用于延迟，持续和/或脉冲释放。 剂量单位形式可以是片剂，凝胶，液体，胶囊，珠粒，微粒，薄膜或锭剂。 多相递送也可以通过使用提供剂量递增的试剂盒来实现。 该制剂可用于治疗一种或多种咳嗽，感冒，鼻窦炎和其它呼吸系统疾病的症状。 制剂也可用于治疗或缓解纤维肌痛，疼痛和肠易激综合征

公开(公告)号：US20080081070A1

公开(公告)日：2008-04-03

申请号：US11680276

申请日：2007-02-28

申请人： Glynn Wilson ,  Gerhard Renner ,  Hema Ravishankar ,  Preeti Patil

发明人： Glynn Wilson ,  Gerhard Renner ,  Hema Ravishankar ,  Preeti Patil

IPC分类号： A61K9/32 ,  A61K31/56 ,  A61P1/00

CPC分类号： A61K9/5073 ,  A61K9/5078 ,  A61K31/56

摘要： Formulations have been developed to improve the solubility of corticosteroids such as fluticasone proprionate in a composition designed to achieve localized release of the drug in the small intestine and/or colon. In one embodiment, solid dispersions of fluticasone are prepared wherein the drug is blended with or coated onto a highly water soluble substrate such as nonpareil (sugar beads) then coated with a layer of polymer soluble in small intestinal fluid, then coated with an enteric coating. The inner polymer layer controls release of the drug, and the enteric coating, a pH sensitive polymer that is broken down in the ileum and colon, controls localized release of drug at various sites within the gastrointestinal tract. The multilayer pharmaceutical composition can be in the form of pellets, tablets compressed from pellets or pellets packed into capsules. The release profile of the drug can be manipulated by (1) altering size or shape (i.e., surface area) and solubility of the inert substrate; (2) the ratio of drug to polymer, the polymer composition and solubility, the porosity of the polymer; (3) the drug form (i.e., free base or salt, or which salt); and the thickness and/or surface area of the drug/polymer and/or enteric coating. In a preferred embodiment, the composition is administered orally. This may also be packaged to provide for an escalating or tapering dosage.

摘要翻译： 已经开发了用于改善皮质类固醇（例如丙酸氟替卡松）在旨在实现药物在小肠和/或结肠中的局部释放的组合物中的溶解度的制剂。 在一个实施方案中，制备氟替卡松的固体分散体，其中将药物与高水溶性底物如非乳糖（糖珠）混合或涂覆在其上，然后用可溶于小肠液的聚合物层涂覆，然后用肠溶衣 。 内部聚合物层控制药物的释放，并且肠溶衣（在回肠和结肠中分解的pH敏感聚合物）控制药物在胃肠道内各处的局部释放。 该多层药物组合物可以是丸粒形式，从颗粒或丸剂包装的胶囊中压制的片剂。 可通过（1）改变惰性底物的尺寸或形状（即表面积）和溶解度来操纵药物的释放曲线; （2）药物与聚合物的比例，聚合物组成和溶解度，聚合物的孔隙率; （3）药物形式（即游离碱或盐，或其盐）; 以及药物/聚合物和/或肠溶衣的厚度和/或表面积。 在优选的实施方案中，组合物经口施用。 这也可以被包装以提供逐渐升高或渐细的剂量。

公开(公告)号：US20070141147A1

公开(公告)日：2007-06-21

申请号：US11461238

申请日：2006-07-31

申请人： Matthew F. Heil ,  Glynn Wilson

发明人： Matthew F. Heil ,  Glynn Wilson

IPC分类号： A61K31/55 ,  A61K31/485 ,  A61K9/22 ,  A61K31/137 ,  A01N31/08

CPC分类号： A61K9/5084 ,  A61K9/0056 ,  A61K9/1652 ,  A61K9/2054 ,  A61K9/2077 ,  A61K9/2081 ,  A61K9/209 ,  A61K9/4808 ,  A61K9/5026 ,  A61K9/5047 ,  A61K9/5078 ,  A61K31/137 ,  A61K31/485 ,  A61K31/55 ,  A61K45/06 ,  A61K2300/00

摘要： A mixed-release tablet or capsule formulation including vehicles for the delivery of a plurality of drugs in various combinations of immediate release, extended release, and/or delayed release modes over a predetermined time period have been developed, which provide for controlled release not just of the drugs, but controlled release that is designed to create more effective coordination between the drugs being delivered. The drugs can be any medically and/or physiologically appropriate combination of drugs and active ingredients, preferably decongestant drugs, antihistamines, expectorants, antitussives, cough suppressants, and drying agents.

摘要翻译： 已经开发了一种混合释放片剂或胶囊制剂，其包括用于在预定时间段内以各种组合即时释放，延长释放和/或延迟释放模式递送多种药物的载体，其不仅提供控制释放 的药物，但控制释放旨在创造更有效的协调药物正在交付。 药物可以是药物和活性成分，优选减充血药物，抗组胺剂，祛痰剂，止咳药，止咳剂和干燥剂的任何医学上和/或生理上适当的组合。

公开(公告)号：US20100041759A1

公开(公告)日：2010-02-18

申请号：US12582872

申请日：2009-10-21

申请人： Glynn Wilson ,  Matthew F. Heil

发明人： Glynn Wilson ,  Matthew F. Heil

IPC分类号： A61K31/185 ,  C07C309/29 ,  A61P25/00

CPC分类号： A61K31/075 ,  A61K9/209 ,  Y02A50/401

摘要： Formulations have been developed administering a guaiacolsulfonate salt, preferably potassium salt, in multi-phases. In a preferred embodiment, the formulation contains potassium guaiacolsulfonate in an immediate release (“IR”) form and a sustained or delayed release (“DR”) form and/or pulsed release (“PR”) form. In another embodiment, the potassium guaiacolsulfonate is released in a gradient, decreasing the side effects associated with rapidly elevated blood levels. In another embodiment, the drug is bound to an ion-exchange resin, which can be suspended in a liquid or incorporated into a matrix for delayed, sustained and/or pulsed release. Dosage unit forms may be tablets, gels, liquids, capsules, beads, microparticles, films or lozenges. Multi-phase delivery can also be achieved through the use of a kit that provides for dosage escalation. The formulations are useful in the treatment of one or more symptoms of coughs, colds, sinusitis and other respiratory illnesses. The formulations are also useful in the treatment or relief of fibromyalgia, pain, and Irritable Bowel Syndrome.

摘要翻译： 已经开发出多次施用愈创木酚磺酸盐，优选钾盐的制剂。 在优选的实施方案中，制剂含有立即释放（“IR”）形式的愈创木酚磺酸钾和持续或延迟释放（“DR”）形式和/或脉冲释放（“PR”）形式。 在另一个实施方案中，愈创木酚磺酸钾以梯度释放，减少与快速升高的血液水平相关的副作用。 在另一个实施方案中，药物与离子交换树脂结合，离子交换树脂可以悬浮在液体中或并入基质中用于延迟，持续和/或脉冲释放。 剂量单位形式可以是片剂，凝胶，液体，胶囊，珠粒，微粒，薄膜或锭剂。 多相递送也可以通过使用提供剂量递增的试剂盒来实现。 该制剂可用于治疗一种或多种咳嗽，感冒，鼻窦炎和其它呼吸系统疾病的症状。 制剂也可用于治疗或缓解纤维肌痛，疼痛和肠易激综合征。

公开(公告)号：US20080064694A1

公开(公告)日：2008-03-13

申请号：US11680290

申请日：2007-02-28

申请人： Matthew F. Heil ,  Glynn Wilson

发明人： Matthew F. Heil ,  Glynn Wilson

IPC分类号： A61K31/537 ,  C07D265/36

CPC分类号： A61K31/537 ,  A61K9/5084 ,  C07D451/10 ,  Y02A50/478

摘要： Formulations have been developed administering methscopolamine in multi-phases. In a preferred embodiment, the formulation contains methscopolamine in an immediate release. (“IR”) form and a sustained or delayed release (“DR”) form and/or poised release (“PR”) form. In another embodiment, the methscopolamine is released in a gradient, decreasing the side effects associated with rapidly elevated blood levels. In another embodiment the drug is bound to an ion-exchange resin, which can be suspended in a liquid or incorporated into a matrix for delayed, sustained and/or pulsed release. Dosage unit forms may be tablets, gels, liquids, capsules, beads, microparticles, films or lozenges. Multi-phase delivery can also be achieved through the use of a kit that provides for dosage escalation. This kit can be a blister pack or equivalent, wherein the drug is packaged so that a first dosage is taken, then sequentially larger dosages. The dosages can be the same in each unit, and instructions provided so that the correct dosage is obtained through the number of units and the time of administration or the dosages may be different, and the units ordered so dial the desired dosage administration profile is obtained when the patient takes the units in order as instructed.

摘要翻译： 已经开发了多阶段施用甲泊泊胺的制剂。 在优选的实施方案中，制剂在立即释放中含有甲基东莨菪碱。 （“IR”）形式和持续或延迟释放（“DR”）形式和/或准备释放（“PR”）形式。 在另一个实施方案中，甲基东莨菪碱以梯度释放，减少与快速升高的血液水平相关的副作用。 在另一个实施方案中，药物结合于离子交换树脂，其可以悬浮在液体中或并入基质中用于延迟，持续和/或脉冲释放。 剂量单位形式可以是片剂，凝胶，液体，胶囊，珠粒，微粒，薄膜或锭剂。 多相递送也可以通过使用提供剂量递增的试剂盒来实现。 该试剂盒可以是泡罩包装或等同物，其中药物被包装以便服用第一剂量，然后顺序地更大剂量。 每个单位的剂量可以相同，并且提供说明书，以便通过单位数量和给药时间获得正确的剂量或剂量可能不同，并且获得所选择的单位，从而拨出所需的剂量给药谱 当患者按照指示按顺序接受单位时。