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公开(公告)号：US07294347B2
公开(公告)日：2007-11-13
申请号：US10871534
申请日：2004-06-21
CPC分类号： A61K9/2866 , A61K9/284
摘要： The present invention discloses coating compositions with taste masking property, comprising a blend of pH sensitive polymers and optionally a pH independent polymer or a blend of the pH sensitive polymer and pH independent polymer used for taste masking of highly bitter drugs. The pH sensitive polymers used comprise the acid soluble polymers and the enteric polymers. The process for the preparation of taste masked pharmaceutical compositions of the bitter drugs comprising the said coating compositions is disclosed. The concomitant use of the polymers inhibits the release of the bitter drug at the pH of saliva. The said coating compositions deliver substantial amount of the bitter drug immediately with improved palatability.
摘要翻译： 本发明公开了具有掩味性质的涂料组合物，其包含pH敏感聚合物和任选的与pH无关的聚合物的混合物或用于高度苦味药物的味道掩蔽的pH敏感聚合物和与pH无关的聚合物的共混物。 所用的pH敏感聚合物包括酸溶性聚合物和肠溶聚合物。 公开了制备包含所述涂料组合物的苦味药物的掩味药物组合物的方法。 伴随使用聚合物抑制苦涩药物在唾液pH下的释放。 所述涂料组合物立即提供大量的苦味，具有改善的适口性。
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公开(公告)号：US07531612B2
公开(公告)日：2009-05-12
申请号：US10738949
申请日：2003-12-19
IPC分类号： C08F118/02
CPC分类号： C08F246/00 , A61K9/2846 , A61K9/5026 , C08F220/12
摘要： The present invention relates a novel pH sensitive polymer which exhibits pH dependant swelling/dissolution behavior. The composition is useful for taste masking of bitter drugs and also for the gastric delivery of the drugs. The said polymer comprises a hydrophobic monomer polymerized along with a basic monomer or a hydrophobic monomer polymerized along with a basic monomer and a hydrophilic monomer.
摘要翻译： 本发明涉及一种具有pH依赖性溶胀/溶解行为的新型pH敏感性聚合物。 该组合物可用于苦味药物的掩味和用于胃输送药物。 所述聚合物包含与碱性单体一起聚合的疏水性单体或与碱性单体和亲水性单体一起聚合的疏水性单体。
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公开(公告)号：US09211358B2
公开(公告)日：2015-12-15
申请号：US12450995
申请日：2008-04-23
申请人： Patrick J. Sinko , Stanley Stein , Anupa R. Menjoge , Simi Gunaseelan , Siva Naga Sree Priay Anumolu , Raghavandra Navath
发明人： Patrick J. Sinko , Stanley Stein , Anupa R. Menjoge , Simi Gunaseelan , Siva Naga Sree Priay Anumolu , Raghavandra Navath
IPC分类号： A61K47/30 , A61P17/02 , A61K38/18 , A61K38/06 , A61L15/22 , A61L26/00 , A61L15/26 , A61L15/44
CPC分类号： A61L26/0052 , A61L15/26 , A61L15/44 , A61L26/0066 , A61L26/0076 , A61L26/008 , A61L2300/204 , A61L2300/21 , A61L2300/25 , A61L2300/402 , A61L2300/404 , A61L2300/41 , A61L2300/414 , A61L2300/602 , C08L71/02
摘要： Described is a spray-on hydrogel comprising water-soluble PEG polymers that cross-link in situ to form a hydrogel such that the cross-links are reversible. The hydrogel can be useful as a drug delivery composition, wound dressing or surgery adjuvant. Polyethylene glycol polymer and cross-linker solutions are sprayed simultaneously through a common orifice. Cross-linking via formation of thioether or disulfide bonds is initiated upon mixing, providing rapid gelation. The hydrogel components can be derivatized with RGD peptides or analogs thereof to promote retention in/on a body compartment such as the skin, surface of the eye, or a mucosa such as the vaginal mucosa. The cross-links are reversed using a reducing solution enabling easy removal of the hydrogel by dissolution. Processes for preparation of the cross-linker, RGD derivatized PEG and RGD-linked agents are also disclosed.
摘要翻译： 描述了包含水溶性PEG聚合物的喷雾型水凝胶，其在原位交联以形成水凝胶，使得交联是可逆的。 水凝胶可用作药物递送组合物，伤口敷料或手术辅助剂。 聚乙二醇聚合物和交联剂溶液通过共同的孔口同时喷雾。 通过形成硫醚或二硫键的交联在混合时开始，提供快速凝胶化。 水凝胶组分可以用RGD肽或其类似物衍生，以促进保留在身体隔室中，例如皮肤，眼表或粘膜如阴道粘膜。 使用还原溶液使交联反转，从而易于通过溶解除去水凝胶。 还公开了制备交联剂，RGD衍生的PEG和RGD连接剂的方法。
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4.发明申请公开(公告)号：US20120003155A1
公开(公告)日：2012-01-05
申请号：US12797657
申请日：2010-06-10
申请人： Rangaramanujam M. Kannan , Sujatha Kannan , Roberto Romero , Raghavendra S. Navath , Hui Dai , Anupa R. Menjoge
发明人： Rangaramanujam M. Kannan , Sujatha Kannan , Roberto Romero , Raghavendra S. Navath , Hui Dai , Anupa R. Menjoge
CPC分类号： A61K47/48215 , A61K31/198 , A61K31/405 , A61K31/43 , A61K31/57 , A61K31/573 , A61K31/65 , A61K38/10 , A61K47/595 , A61K47/60 , A61K47/64 , C08G83/004
摘要： A nanodevice composition including N-acetyl cysteine linked to a dendrimer, such as a PAMAM dendrimer or a multiarm PEG polymer, is provided. Also provided is a nanodevice for targeted delivery of a compound to a location in need of treatment. The nanodevice includes a PAMAM dendrimer or multiarm PEG polymer, linked to the compound via a disulfide bond. There is provided a nanodevice composition for localizing and delivering therapeutically active agents, the nanodevice includes a PAMAM dendrimer or multiarm PEG polymer and at least one therapeutically active agent attached to the PAMAM dendrimer or multiarm PEG polymer. A method of site-specific delivery of a therapeutically active agent, by attaching a therapeutically active agent to a PAMAM dendrimer or multiarm PEG polymer using a disulfide bond, administering the PAMAM dendrimer or multiarm PEG polymer to a patient in need of treatment, localizing the dendrimer or multiarm PEG polymer to a site in need of treatment, and releasing the therapeutically active agent at the site in need of treatment.
摘要翻译： 提供包含与树枝状大分子连接的N-乙酰半胱氨酸的纳米设备组合物，例如PAMAM树枝状聚合物或多臂PEG聚合物。 还提供了用于将化合物靶向递送至需要治疗的位置的纳米设备。 纳米器件包括通过二硫键与化合物连接的PAMAM树枝状聚合物或多臂PEG聚合物。 提供了用于定位和递送治疗活性剂的纳米设备组合物，纳米设备包括PAMAM树枝状聚合物或多臂PEG聚合物和连接到PAMAM树枝状聚合物或多臂PEG聚合物的至少一种治疗活性剂。 通过使用二硫键将治疗活性剂附着到PAMAM树枝状聚合物或多臂PEG聚合物上来施用治疗活性剂的位点特异性递送方法，将PAMAM树枝状聚合物或多臂PEG聚合物施用于需要治疗的患者，将 树枝状大分子或多臂PEG聚合物连接到需要处理的部位，并在需要治疗的部位释放治疗活性剂。
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公开(公告)号：US20110033503A1
公开(公告)日：2011-02-10
申请号：US12450995
申请日：2008-04-23
申请人： Patrick J. Sinko , Stanley Stein , Anupa R. Menjoge , Simi Gunaseelan , Siva Naga Sree priay Anumolu , Raghavandra Navath
发明人： Patrick J. Sinko , Stanley Stein , Anupa R. Menjoge , Simi Gunaseelan , Siva Naga Sree priay Anumolu , Raghavandra Navath
IPC分类号： A61K38/06 , A61K31/65 , A61K31/405 , A61K31/165 , A61K9/00 , A61K38/18 , A61K38/19 , A61K38/39 , A61P17/02 , A61K47/30
CPC分类号： A61L26/0052 , A61L15/26 , A61L15/44 , A61L26/0066 , A61L26/0076 , A61L26/008 , A61L2300/204 , A61L2300/21 , A61L2300/25 , A61L2300/402 , A61L2300/404 , A61L2300/41 , A61L2300/414 , A61L2300/602 , C08L71/02
摘要： Described is a spray-on hydrogel comprising water-soluble PEG polymers that cross-link in situ to form a hydrogel such that the cross-links are reversible. The hydrogel can be useful as a drug delivery composition, wound dressing or surgery adjuvant. Polyethylene glycol polymer and cross-linker solutions are sprayed simultaneously through a common orifice. Cross-linking via formation of thioether or disulfide bonds is initiated upon mixing, providing rapid gelation. The hydrogel components can be derivatized with RGD peptides or analogs thereof to promote retention in/on a body compartment such as the skin, surface of the eye, or a mucosa such as the vaginal mucosa. The cross-links are reversed using a reducing solution enabling easy removal of the hydrogel by dissolution. Processes for preparation of the cross-linker, RGD derivatized PEG and RGD-linked agents are also disclosed.
摘要翻译： 描述了包含水溶性PEG聚合物的喷雾型水凝胶，其在原位交联以形成水凝胶，使得交联是可逆的。 水凝胶可用作药物递送组合物，伤口敷料或手术辅助剂。 聚乙二醇聚合物和交联剂溶液通过共同的孔口同时喷雾。 通过形成硫醚或二硫键的交联在混合时开始，提供快速的凝胶化。 水凝胶组分可以用RGD肽或其类似物衍生，以促进保留在身体隔室中，例如皮肤，眼表或粘膜如阴道粘膜。 使用还原溶液使交联反转，从而易于通过溶解除去水凝胶。 还公开了制备交联剂，RGD衍生的PEG和RGD连接剂的方法。
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6.发明授权Pharmaceutical composition for improving palatability of drugs and process for preparation thereof 有权用于改善药物适口性的药物组合物及其制备方法公开(公告)号：US07378109B2
公开(公告)日：2008-05-27
申请号：US11019648
申请日：2004-12-23
IPC分类号： A61K9/14
CPC分类号： A61K9/1617 , A61K9/1635
摘要： The present invention discloses compositions, comprising a lipid-polymer matrix to mask the bitter or unpleasant taste of the medicament. The lipid or a blend of lipids, are used in combination with the pH dependent polymer where the said polymer is acid soluble or swellable The process for the preparation of taste masked pharmaceutical compositions of the bitter drugs comprising the said lipid-polymer compositions are disclosed. The concomitant use of the acid soluble polymer, which remains collapsed at the pH of saliva, inhibits the release of drug at that pH and hence they further help in bitterness inhibition. The said compositions deliver substantial amount of the bitter drug immediately at the gastric pH with improved palatability.
摘要翻译： 本发明公开了包含脂质 - 聚合物基质以掩盖药物的苦味或不愉快味道的组合物。 脂质或脂质的混合物与pH依赖性聚合物组合使用，其中所述聚合物是酸溶性或可溶胀的。公开了制备包含所述脂质 - 聚合物组合物的苦味药物的掩味药物组合物的方法。 伴随使用酸溶性聚合物，其在唾液的pH下保持崩解，抑制药物在该pH下的释放，因此它们进一步有助于苦味抑制。 所述组合物立即在胃pH下提供大量的苦味药物，具有改善的适口性。
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