CN103415292A - 用于治疗眼科病症的雄性激素组合物 - Google Patents
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Abstract
本公开提供用于治疗眼部病症的组合物。所述组合物包含生理有效量的雄性激素,其中所述组合物适于局部施用至眼睛。本公开还提供使用本发明所公开的所述组合物治疗眼部病症的方法。
Description
发明人:约翰·T·楚葛丹、阿德南·K·萨拉梅、切丹·P·普加若、安努拉达哈·V·戈尔和贾亚·吉亚纳尼
相关申请的交叉引用
本专利申请基于并且根据35U.S.C.§120要求提交于2011年1月26日的美国临时专利申请No.61/436,274的优先权,该专利申请以引用的方式并入本文。
发明背景
睑炎是睑板腺疾患,所述睑板腺产生泪膜的脂质组分。上眼睑和下眼睑均包括30-40个位于皮肤之下的腺体。腺孔在睑缘上眼睫毛的基部之后开口。患有睑炎,腺体会发炎,而且孔会阻塞。睑炎的症状包括眼睛过敏、疼痛、发红以及物质在眼睑上积聚。患者也可经历干眼。这些症状导致的结果是,睑炎通常误诊为结膜炎或干眼。
在某些情况下,局部雄性激素缺乏可导致睑炎。包含雄性激素的局部组合物对于睑炎的治疗可为期望的。
发明概述
本公开提供用于治疗一种或多种眼部病症的组合物和方法。
在一个实施例中,提供了包含生理有效量雄性激素的组合物,其中所述组合物适于局部施用至眼睛。
在另一个实施例中,公开了用于治疗雄性激素缺乏产生的眼部病症的方法。该方法包括施用有效量的包含生理有效量雄性激素的眼科组合物,其中所述组合物适于局部施用至眼睛,并且其中至少一种眼部病症的症状得以减轻。
发明详述
本公开提供包含生理有效量雄性激素的眼科组合物,其中所述组合物适于局部施用至眼睛。
本文还公开了治疗雄性激素缺乏相关的眼部病症的方法。该方法包括施用有效量的包含生理有效量雄性激素的眼科组合物,其中所述组合物适于局部施用至眼睛,并且其中至少一种眼部病症的症状得以减轻。
本文所公开的组合物包含雄性激素。如本文所用,除非另外指明,术语“雄性激素”包括所有内源性的和合成的睾酮和含睾酮部分,以及异构体、类似物、酯,以及它们的组合。雄性激素可以是内源产生的甾族雄性激素,其包括(但不限于):睾酮(即,(17β)-17-羟基雄甾-4-烯-3-酮)、二氢睾酮(DHT)、脱氢表雄甾酮、雄甾烯二酮、雄甾烯二醇和雄甾酮。还包括含睾酮部分,例如,睾酮的酯,如环戊丙酸酯、丙酸酯、苯基丙酸酯、环戊基丙酸酯、异己酸酯、庚酸酯、苯基乙酸酯、乙酸酯、丁环甲酸酯、庚酸酯、癸酸酯(caprate)、异癸酸酯和癸酸酯(decanoate ester),以及其他合成雄性激素,例如羟甲雄酮、17α-甲基去甲睾酮和7-甲基去甲睾酮及其乙酸酯。
眼部病症可以是局部或全身雄性激素缺乏导致的眼睛、眼睑、腺体或眼睛周围皮肤的任何病症。在某些实施例中,眼部病症是睑炎。雄性激素缺乏的发生可以有多种原因,例如,在绝经期间或自然衰老过程的结果。雄性激素缺乏可以是由于疾病或病症,例如舍格伦综合征。
待治疗的患者可以是任何年龄或性别的任何哺乳动物。哺乳动物可以是需要治疗的人、狗、猫、绵羊、奶牛等。在某些实施例中,待治疗的患者是男性或女性人类。
生理有效量是指足以实现指定用途或效果的物质的量。各种生物因素可影响效果发挥所需的量,例如年龄、性别、潜在病症的严重性以及患者的总体健康状态。如本文所用,如果剂量预防、减少或消除待治疗的眼部病症相关的症状,则其被视为有效的。
雄性激素可以约0.001重量%至约5重量%(w/w),或约0.09重量%至约2重量%,或约0.01重量%至约1.0重量%(w/w)的含量存在于本文所述的眼科组合物中。
本发明所公开的组合物可以是乳液、溶液、悬浮液、凝胶、膏剂、闭塞眼膜或缓释眼膜,并且可以是含防腐剂或无防腐剂制剂。组合物可配制为可施用至眼睛的滴眼剂、霜膏、膏剂和眼膜。制剂可施用至眼睛、上眼睑、下眼睑或它们的组合。组合物的局部施用在病症部位提供了最小全身药物水平的治疗。
表1中列出了制剂成分和示例性浓度的实例。
表1
本发明所公开的组合物的乳液可使用一种或多种选自交联聚丙烯酸酯家族的聚电解质,例如卡波姆和(Lubrizol)稳定。Pemulen是丙烯酸以及与季戊四醇的烯丙醚交联的长链甲基丙烯酸烷基酯的高分子量共聚物。它们包含不小于约52%并且不大于约62%的羧酸基团。中和的1.0%含水分散体的粘度在约9,500和约26,500厘泊之间。额外的乳化剂包括(但不限于):聚山梨醇酯-80、POE-40-硬脂酸酯、聚山梨醇酯-20、聚山梨醇酯40、聚山梨醇酯-60以及它们以组合物的约0重量%至约4重量%或约0.01重量%至约2.0重量%的含量的组合。
在一些实施例中,组合物包含亲脂性媒介物,例如蓖麻油、角鲨烷、二甘醇单乙醚、丙二、醇异硬脂酸异硬脂醇酯、肉豆蔻酸异丙酯、二丙二醇二甲醚、二甘醇、二丙二醇、矿物油、硅油、辛酸/癸酸甘油三酯、鲸蜡醇、硬脂醇以及它们的组合。亲脂性媒介物可以组合物的约0重量%至约85重量%、或约1重量%至约50重量%、或约2重量%至约15重量%的含量存在。
本发明所公开的组合物可包含中和剂,例如含量为组合物的约0至约2.5重量%的氢氧化钠和有机碱。
在某些实施例中,组合物可包括缓和剂,例如羧甲基纤维素钠、羟丙基甲基纤维素、羟乙基纤维素、甲基纤维素、聚乙烯醇、聚乙烯吡咯烷酮、甘油、丙二醇、PEG 300、PEG 400以及它们的组合。缓和剂可以组合物的约0至约10重量%、或约2重量%、5重量%、7重量%或9重量%的含量存在。
在一些实施例中,组合物包含含量为组合物的约0至约4重量%或约0.01重量%至约3重量%的等渗剂,例如氯化钠、甘油、甘露糖醇、氯化钾、赤藓醇以及它们的组合。
在一些实施例中,组合物可包括一种或多种缓冲剂。合适的缓冲剂包括(但不限于):磷酸盐、柠檬酸盐、乙酸盐、硼酸盐以及它们的组合。所用的缓冲组分的含量足以使组合的pH保持在约6至约8,或约6.5至约7.5的范围内。在某些实施例中,缓冲剂以组合物的约0至约2.0重量%的含量存在。
在某些实施例中,组合物包括增稠剂或粘度剂。粘度剂可选自卡波姆、羧甲基纤维素钠、甲基纤维素、羟丙基甲基纤维素、聚乙烯醇、黄原胶以及它们的组合。粘度剂可以组合物的约0重量%至约4重量%或约0.01重量%至约3.0重量%的含量存在。
在某些实施例中,组合物包括增溶剂或溶解度增强剂。增溶剂或溶解度增强剂可选自环糊精、α-环糊精、β-环糊精、γ-环糊精、羟丙基-β-环糊精、磺丁基醚-β-环糊精(Captisol)以及它们的组合。增溶剂或溶解度增强剂可以约0%至约10%的含量存在。在一些实施例中,增溶剂或溶解度增强剂可以约0.01%至约7.0%的含量存在。在一些实施例中,增溶剂或溶解度增强剂可以组合物的约0.1至约4重量%的含量存在。
组合物可以溶液(即,滴眼剂)、霜膏、膏剂、眼膜等等的形式局部施用。组合物可施用至左眼、右眼或双眼。当组合物以溶液施用时,溶液滴眼剂应在接触眼泪溶液时易于分散。
本公开的或用于本公开的组合物可包括有效地提供一种或多种有用性能和/或有益效果的含量的一种或多种其他组分。例如,虽然本发明的组合物可以基本上不含添加的防腐剂组分,但在其他实施例中,本发明的组合物包括有效量的防腐剂组分。此类防腐剂组分的实例包括(但不限于):(Allergan,Irvine,CA)、季铵防腐剂例如苯扎氯铵(”BAC”或”BAK”)和泊洛沙姆;双胍防腐剂例如聚六亚甲基双胍(PHMB);对羟基苯甲酸甲酯和乙酯;合克替啶;亚氯酸组分,例如稳定二氧化氯、金属氯酸盐等等;其他可眼用防腐剂以及它们的混合物。防腐剂组分,如果有的话,在本发明组合物中的浓度为可有效地保存组合物的浓度,并且(取决于所用的特定防腐剂的性质)是常见的,通常在组合物的约0体积%至约4.0体积%或约0.1体积%至约2.0体积%的范围内使用。
在某些实施例中,组合物可以是眼膜,例如闭塞眼膜或缓释眼膜的形式。还大胆地设想了干燥形成眼膜的液体。当使用眼膜时,眼膜在至少约0.5mm×0.5mm的范围内,通常约3-10mm×5-10mm、厚度约0.1-1.0mm,以易于处理。眼膜的尺寸和形式可用于控制释放速率。此类组合物可包含一种或多种成膜剂,例如丙烯酸酯/辛基丙烯酰胺共聚物、聚(丙烯酸乙酯-甲基丙烯酸甲酯)、脱乙酰壳多糖、聚乙烯醇、聚异丁烯、聚乙烯吡咯烷酮-乙酸乙烯酯共聚物、硅胶、聚乙烯吡咯烷酮、其他缓释聚合物膜以及它们的组合。成膜剂可以组合物的约0重量%至约10重量%的含量存在。
施用频次、持续时间和剂量由处方内科医师确定。剂量可根据剂型变化。当组合物为溶液时,例如,每眼每次可施用1、2、3或更多滴。施用频次可为每天(例如每天一次、两次、三次或四次或更多次)、每两周和/或每月一次或多次。施用的持续时间可继续直到待治疗的病症消退,即直到眼部病症的一个或多个症状减少或消除。因此,组合物可施用数小时、数天、数周、数月以及数年。
如果症状得以预防、减少或消除,则视为减轻。在通常经历特定症状的患有眼部病症的患者中(或如果类似处境的患者通常经历特定症状),症状得到预防,并且在施用本发明所公开的组合物后,患者不会经历症状的病发。如果患者眼部病症相关的一种或多种症状的严重性或持续时间减少5%、10%、20%、50%、75%、90%或更多,则视为实现症状的减少。当不再存在或基本上存在于患者中时,即实现眼部病症相关的一种或多种症状的消除。
本发明所公开的组合物的某些实施例掺入了局部麻醉剂,其可以选自氨布卡因、阿莫拉酮、阿米洛卡因、奥布卡因、苯佐卡因、贝托卡因、苯柳胺酯、布比卡因、布他卡因、氨苯丁酯、布坦卡因、丁胺卡因、丁托西卡因、卡铁卡因、氯普鲁卡因、可卡乙碱、可卡因、环美卡因、狄布卡因、二甲异喹啉、二甲卡因、地哌冬、双环维林、脱水芽子碱、芽子碱、氯乙烷、依替卡因、β-优卡因、尤普罗辛、非那可明、非莫卡因、已卡因、羟丁卡因、对氨基苯甲酸异丁酯、甲磺酸亮氨卡因、左沙屈尔、利多卡因、马比佛卡因、美普卡因、美布卡因、氯甲烷、麦替卡因、纳依卡因、奥他卡因、俄妥卡因、奥昔卡因、对乙氧卡因、非那卡因、苯酚、哌罗卡因、匹多卡因、聚多卡醇、普莫卡因、丙胺卡因、普鲁卡因、丙泮卡因、丙美卡因、丙哌卡因、丙氧卡因、伪可卡因、吡咯卡因、罗哌卡因、水杨醇、丁卡因、托利卡因、三甲卡因、佐拉敏以及它们的盐。本文所述的组合物中局部麻醉剂的浓度可为治疗有效的,意指浓度足以提供治疗有益效果,而不对患者造成伤害。
组合物还可包含眼用抗炎剂,例如有效地减少眼部炎症的含量的任何非甾族抗炎药(NSAID)。非限制性实例包括抑制环氧化酶(COX)-1和/或-2的试剂,包括(但不限于):丙酸例如萘普生、氟比洛芬、噁丙嗪、布洛芬、酮洛芬、非诺洛芬;酮咯酸氨基丁三醇;乙酸衍生物例如舒林酸、吲哚美辛和依托度酸;苯乙酸例如双氯芬酸、溴芬酸和舒洛芬;芳基乙酸前药例如奈帕芬胺和氨芬酸;水杨酸例如阿司匹林、双水杨酯、二氟苯水杨酸、三柳胆镁(CMT);对氨基苯酚衍生物例如对乙酰氨基酚;萘烷酮例如萘丁美酮;烯醇酸衍生物例如吡罗昔康和美洛昔康;芬那酸例如甲芬那酸、甲氯芬那酸和氟芬那酸;吡咯乙酸例如托美丁;和吡唑啉酮例如苯基保泰松;COX-2选择性抑制剂例如塞来昔布、伐地昔布、帕瑞昔布、依托昔布和罗美昔布;包括它们的所有酯和可药用盐。在某些实施例中,也可掺入甾族抗炎剂,包括(但不限于):氢化可的松、可的松、泼尼松龙和泼尼松。
适用于本发明所公开的组合物的抗微生物剂包括(但不限于):抗生素例如氨基糖苷类如庆大霉素、卡那霉素、新霉素和万古霉素;酰胺醇类例如氯霉素;头孢菌素类例如唑啉头孢菌素盐酸盐;青霉素类例如氨苄青霉素、青霉素、羧苄青霉素、氧西林、甲氧西林;林可胺类例如林肯霉素;多肽抗生素例如多粘菌素和杆菌肽;四环素类例如四环素;喹诺酮类例如环丙沙星等;磺酰胺类例如氯胺T;以及砜类例如对氨基苯磺酸作为亲水性实体;以及抗病毒药,如无环鸟苷、更昔洛韦、阿糖腺苷、叠氮胸苷、双脱氧肌苷和双脱氧胞嘧啶。本文还设想了抗真菌剂以及任何其他适于眼用的抗微生物剂。
表2、3和4分别提供了非限制性示例性滴眼剂、霜膏和眼膜的配方。
表2
表3
表4
表5和6示出了本发明实施中想到的额外的非限制性示例性配方。
表5
表6
实施例1
治疗实施例
50岁男性出现眼部两侧发红、炎症和过敏。他被诊断为睑炎,并且用表2中公开的组合物治疗。治疗3天后,症状减少,治疗1周后,症状消除。
实施例2
替代治疗实施例
55岁女性绝经后双眼出现持续过敏、发红以及物质积聚。她被诊断为睑炎,并且用表3中公开的组合物治疗。2天后,她经历了过敏和发红减少,在1周内经历了症状的完全终止。
实施例3
替代治疗实施例
47岁男性被诊断为睑炎。用表4中公开的组合物治疗2周,他经历了所有病症相关症状的消除。
除非另外指明,说明书和权利要求中用于表示成分数量、性质例如分子量、反应条件等等的所有数字在所有实例中应理解为被术语“约”修饰。因此,除非有相反的指示,说明书和所附权利要求中示出的数值参数是近似值,可根据本发明寻求获得的所需性质变化。在最低程度上,并且不试图将等同原则的应用限制到权利要求书的范围,每个数字参数应至少按照所报告的有效数位并通过应用惯常的四舍五入法加以解读。尽管示出了本发明广泛范围的数字范围和参数为近似值,但是在具体实例中所示的数值被尽可能精确地报告。然而,任何数值都固有地包含因存在于其相应测试测量中的标准偏差而必然导致的某些误差。
除非本文另外指明或上下文明显冲突,否则用在描述本发明的上下文中(尤其是以下权利要求书的上下文中)的术语“一个/一种(a)”、“一个/一种(an)”、“该/所述(the)”和相似指示物应被视为涵盖单数和复数形式。本文对值的范围的列举仅仅是为了用作单独提及落在该范围内的每个单独值的快捷方法。除非本文另外指明,否则每个单独的值均包括在本说明书中,就像在本文中单独列举一样。除非本文另外指明或上下文明显冲突,否则本文所述的所有方法可以按任何合适的顺序执行。使用本文提供的任何和所有实例或示例性语言(如,“例如”)仅仅是为了更好地阐明本发明,而不是对受权利要求书保护的本发明的范围进行限制。本说明书中的语言不应理解为指示任何未主张的要素对于实践本发明而言必不可少。
本文所公开发明的替代要素或实施例的分组不应解释为限制。每个小组成员可单独或与小组的其他成员或本文出现的其他要素的任何组合提及并且受权利要求书保护。据预计,出于便利和/或专利性的原因,小组的一个或多个成员可包括在一个小组内或从该小组内删除。当出现任何此类包括或删除时,将说明书视为包括如此修改的小组,从而满足所附权利要求书中所用的所有马库什组(Markush group)的书面说明。
本发明的某些实施例在本文中有所描述。当然,这些所描述的实施方案的变化形式在本领域普通技术人员阅读上述说明时将显而易见。发明人预计技术人员根据情况采用此类变化形式,并且发明人期望本发明的实施与本文中具体描述有所不同。因此,本发明包括适用法律允许的所附权利要求列举的主题的所有修改形式和等同形式。此外,本发明涵盖上述要素在其所有可能的变化形式中的任何组合,除非本文中另外指明,或换句话讲与语境明显矛盾。
本文所公开的具体实施方案还可限制于的使用由语言组成的或基本上由语言组成的权利要求内。当用于权利要求中时,无论根据修正提交还是添加,过渡术语“由……组成”排除了权利要求中未指明的所有要素、步骤或成分。过渡术语“基本上由……组成”将权利要求的范围限制于指定材料或步骤以及不会显著影响基本和新特性的那些材料或步骤。固有地或明确地描述并且在本文中实施了受权利要求书保护的本发明的实施方案。
最后,应当理解,本文所公开的本发明实施方案本发明原理的示例。可采用的其他修改形式在本发明的范围之内。因此,本发明可供选择的模型可根据本文的教导内容以举例的方式,但不限于其利用。因此,不会准确地如所示和所述限制本发明。
本文所公开的具体实施方案还可限制于的使用由语言组成的或基本上由语言组成的权利要求内。当用于权利要求中时,无论根据修正提交还是添加,过渡术语“由……组成”排除了权利要求中未指明的所有要素、步骤或成分。过渡术语“基本上由……组成”将权利要求的范围限制于指定材料或步骤以及不会显著影响基本和新特性的那些材料或步骤。固有地或明确地描述并且在本文中实施了受权利要求书保护的本发明的实施方。
Claims (22)
1.一种包含生理有效量雄性激素的眼科组合物,其中所述组合物适于局部施用至眼睛。
2.根据权利要求1所述的组合物,其中所述雄性激素选自睾酮、二氢睾酮、脱氢表雄甾酮、雄甾烯二酮、雄甾烯二醇、雄甾酮、羟甲雄酮和17α-甲基-去甲睾酮、甲基睾酮、7-甲基-去甲睾酮,以及酯、类似物,以及它们的组合。
3.根据权利要求1所述的组合物,其中所述雄性激素是睾酮。
4.根据权利要求1所述的组合物,其中睾酮以约0.01w/w%至约0.10w/w%存在于所述组合物中。
5.根据权利要求1所述的组合物,其中睾酮以约0.01w/w%至约0.05w/w%存在于所述组合物中。
6.根据权利要求1所述的组合物,其中睾酮以约0.01w/w%至约0.05w/w%存在于所述组合物中。
7.根据权利要求1所述的组合物,其中所述组合物选自溶液、乳液、悬浮液、凝胶、膏剂、闭塞眼膜和缓释眼膜。
8.根据权利要求1所述的组合物,其中所述组合物包含选自增稠剂、中和剂、乳化剂、亲脂性媒介物、缓冲剂、等渗剂、缓和剂、防腐剂、增塑剂、闭塞剂、成膜剂以及它们的组合的额外组分。
9.根据权利要求1所述的组合物,还包含选自抗炎剂、抗微生物剂、止痛剂、麻醉剂、润滑剂以及它们的组合的试剂。
10.根据权利要求1所述的组合物,还包含溶解度增强剂。
11.一种治疗雄性激素缺乏产生的眼部病症的方法,所述方法包括施用有效量包含生理有效量雄性激素的眼科组合物,其中所述组合物适于局部施用至眼睛,并且其中所述眼部病症的至少一个症状得以减轻。
12.根据权利要求11所述的方法,其中所述眼部病症是睑炎。
13.根据权利要求11所述的方法,其中所述雄性激素选自睾酮、二氢睾酮、脱氢表雄甾酮、雄甾烯二酮、雄甾烯二醇、雄甾酮、羟甲雄酮和17α-甲基-去甲睾酮、甲基睾酮、6-甲基-去甲睾酮,以及酯、类似物,以及它们的组合。
14.根据权利要求11所述的方法,其中所述组合物选自溶液、乳液、悬浮液、凝胶、膏剂、闭塞眼膜和缓释眼膜。
15.根据权利要求11所述的方法,其中所述载体包含选自增稠剂、中和剂、乳化剂、亲脂性媒介物、缓冲剂、等渗剂、缓和剂、防腐剂、增塑剂、闭塞剂、成膜剂以及它们的组合的额外组分。
16.根据权利要求11所述的方法,还包含选自抗炎剂、抗生素、止痛剂、麻醉剂、润滑剂、抚慰剂以及它们的组合的试剂。
17.根据权利要求11所述的方法,其中所述眼部病症相关的症状得以预防。
18.根据权利要求11所述的方法,其中所述眼部病症相关的症状得以减少。
19.根据权利要求11所述的方法,其中所述眼部病症相关的症状得以消除。
20.根据权利要求11所述的方法,其中所述施用重复进行直到所述眼部病症的一个或多个症状减少。
21.根据权利要求11所述的方法,其中所述施用重复进行直到所述眼部病症的一个或多个症状消除。
22.根据权利要求11所述的方法,其中所述组合物施用至所述眼睛、上眼睑、下眼睑以及它们的组合。
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CN115105512A (zh) * | 2022-08-29 | 2022-09-27 | 中山大学中山眼科中心 | 脱氢表雄酮在制备预防、治疗眼部近视的药物中的用途及其剂型和制备方法 |
WO2024045973A1 (zh) * | 2022-08-29 | 2024-03-07 | 中山大学中山眼科中心 | 脱氢表雄酮在制备预防、治疗眼部近视的药物中的用途及其剂型和制备方法 |
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