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公开(公告)号：US20080004329A1
公开(公告)日：2008-01-03
申请号：US11823028
申请日：2007-06-26
CPC分类号： A61K9/06 , A61K9/0014 , A61K31/00 , A61K47/10 , A61K47/38
摘要： The present invention comprises compositions for pharmaceutical drug delivery of an indolone (e.g., ropinirole), or a pharmaceutically acceptable salt thereof. The composition may, for example, be a gel suitable for transdermal application. The compositions of the present invention typically comprise a hydroalcoholic vehicle, one or more antioxidant, and one or more buffering agent, wherein the pH of the gel is usually between about pH 7 and about pH 9. The compositions may include further components, for example, the hydroalcoholic vehicle may further comprise additional solvent(s), antioxidant(s), cosolvent(s), penetration enhancer(s), buffering agent(s), and/or gelling agent(s). The compositions may be used for the treatment of a variety of neurological disorders.
摘要翻译： 本发明包括用于药物递送吲哚酮（例如罗哌尼罗）或其药学上可接受的盐的组合物。 组合物可以例如是适合经皮施用的凝胶。 本发明的组合物通常包含水醇载体，一种或多种抗氧化剂和一种或多种缓冲剂，其中凝胶的pH通常在约pH 7至约pH 9之间。组合物可包括其它组分，例如 ，所述水醇载体可以进一步包含另外的溶剂，抗氧化剂，助溶剂，渗透增强剂，缓冲剂和/或胶凝剂。 组合物可用于治疗各种神经障碍。
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公开(公告)号：US20050287194A1
公开(公告)日：2005-12-29
申请号：US11120306
申请日：2005-05-02
CPC分类号： A61K47/18 , A61K9/0014 , A61K9/06 , A61K9/7023 , A61K31/17 , A61K31/195 , A61K47/10 , Y10S514/818 , Y10S514/821 , A61K2300/00
摘要： A transdermal or topical composition including anticholinergic agents, such as oxybutynin, a urea-containing compound and a carrier system. A method is disclosed for treating a subject for urinary incontinence while reducing the incidences of peak concentrations of drug and undesirable side effects.
摘要翻译： 一种透皮或局部组合物，包括抗胆碱剂，例如奥昔布宁，含尿素化合物和载体系统。 公开了一种用于治疗受试者尿失禁同时减少药物峰值浓度和不良副作用的发生率的方法。
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3.发明申请公开(公告)号：US20070196494A1
公开(公告)日：2007-08-23
申请号：US11670293
申请日：2007-02-01
IPC分类号： A61K31/78
CPC分类号： A61K9/0056 , A61K9/2018 , A61K9/2027 , A61K9/2095 , A61K31/78
摘要： The present invention relates to a rapidly disintegrating orally administratable solid dosage formulation that includes at least one active ingredient, at least one first disintegration agent that is at least one type-C methacrylic acid copolymer according to the U.S. Pharmacopoeia National Formulary US/NF, a second disintegration agent of crospovidone or a cross-linked povidone polymer derivative thereof, and a non-cariogenic diluent that does not increase glucose blood levels. The at least one first disintegration agent does not function as an enteric coating, insulation coating intended to protect active ingredient(s), or coating intended to mask taste or smell. The solid dosage form has a mass of about 50 to about 1000 mg, and the at least one first disintegration agent is present in the dosage form in an amount not exceeding 15%, with respect to the total weight of the dosage form. The second disintegration agent is present in the dosage form in an amount not exceeding 15% with respect to the total weight of the dosage form. The first and the second disintegration agent are present in total amounts that provide a weight ratio of about 1:1 to about 1:3, wherein the dosage form provides at least one of the in vitro or in vivo disintegration time that is less than 30 seconds, and has a friability of 1% or less according to the U.S. Pharmacopoeia test.
摘要翻译： 本发明涉及快速崩解的可口服给药的固体剂型制剂，其包含至少一种活性成分，至少一种第一崩解剂，其是根据US Pharmacopoeia National Formulary US / NF至少一种C型甲基丙烯酸共聚物， 交联聚维酮的第二崩解剂或其交联聚维酮聚合物衍生物和不增加葡萄糖血液水平的非致龋剂稀释剂。 至少一种第一崩解剂不用作肠溶衣，旨在保护活性成分的绝缘涂层或旨在掩蔽味道或气味的涂层。 相对于剂型的总重量，固体剂型具有约50至约1000mg的质量，并且至少一种第一崩解剂以不超过15％的量存在于剂型中。 相对于剂型的总重量，第二崩解剂以不超过15％的量存在于剂型中。 第一和第二崩解剂以提供重量比为约1:1至约1:3的总量存在，其中该剂型提供至少一种体外或体内崩解时间小于30 秒，根据美国药典测试，其脆度为1％以下。
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4.发明申请公开(公告)号：US20070225379A1
公开(公告)日：2007-09-27
申请号：US11755923
申请日：2007-05-31
IPC分类号： A61K47/00 , A61K31/025
CPC分类号： A61K47/10 , A61K9/006 , A61K9/08 , A61K9/7015 , A61K31/025 , A61K31/135 , A61K31/27 , A61K31/404 , A61K31/427 , A61K31/428 , A61K31/439 , A61K31/4468 , A61K31/4745 , A61K47/08
摘要： The invention relates to a transdermal or transmucosal non-occlusive, semi-solid pharmaceutical formulation that includes at least one systemically active agent that acts on the Central Nervous System (CNS) of a mammal; and a permeation enhancing solvent system present in an amount sufficient to solubilize the at least one active ingredient. The permeation enhancing solvent system includes a pharmaceutically acceptable monoalkyl ether of diethylene glycol; a pharmaceutically acceptable glycol; preferably also a fatty alcohol and or a fatty acid; and a mixture of a C2 to C4 alcohol and water so that the permeation enhancing solvent system (a) inhibits crystallization of the at least one active ingredient on a skin or mucosal surface of a mammal, (b) reduces or prevents transfer of the formulation to clothing or to another being, (c) modulates biodistribution of the at least one active agent within different layers of skin, (d) facilitates absorption of the at least one active agent by a skin or a mucosal surface of a mammal, or (e) provides a combination of one or more of (a) through (d).
摘要翻译： 本发明涉及透皮或透粘膜非闭塞性半固体药物制剂，其包括作用于哺乳动物的中枢神经系统（CNS）的至少一种全身活性剂; 和渗透增强溶剂系统，其量足以溶解至少一种活性成分。 渗透增强溶剂系统包括药学上可接受的二甘醇单烷基醚; 药学上可接受的二醇; 优选还包括脂肪醇和/或脂肪酸; 和C 2〜C 4醇与水的混合物，使得渗透促进溶剂体系（a）抑制至少一种活性成分在皮肤上的结晶或 哺乳动物的粘膜表面，（b）减少或阻止制剂向衣服或另一种转移，（c）调节至少一种活性剂在不同皮肤层内的生物分布，（d）促进吸收至少 一种由哺乳动物的皮肤或粘膜表面活性剂，或（e）提供（a）至（d）中的一种或多种的组合。
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