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CN1625395A - 叶黄素/玉米黄质用于眩光保护 - Google Patents

叶黄素/玉米黄质用于眩光保护 Download PDF

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CN1625395A
CN1625395A CNA038029944A CN03802994A CN1625395A CN 1625395 A CN1625395 A CN 1625395A CN A038029944 A CNA038029944 A CN A038029944A CN 03802994 A CN03802994 A CN 03802994A CN 1625395 A CN1625395 A CN 1625395A
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cryptoxanthin
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费利克斯·巴克
里贾纳·戈拉尔齐克
沃尔夫冈·沙尔赫
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Abstract

本发明涉及通过给药能够被引入眼组织和/或造成眼组织黄化的色料,特别是类胡萝卜素,如叶黄素和玉米黄质,使视觉功效提高,特别是黑暗中的视觉功效。

Description

叶黄素/玉米黄质用于眩光保护
技术领域
本发明涉及提高视觉功效(visual performance)。本发明更具体涉及黑暗中使视觉功效提高,例如在弱光线或暗光线条件(如在夜晚或黎明)下驾驶机动车(vehicle)或飞机,或在隧道驾驶机动车时。
发明内容
本发明发现,用能够被引入眼组织和/或造成眼组织黄化的色料(colorant)给药会使视觉功效提高。这些色料的一个共同特征是,当它们在眼组织,特别是视网膜沉积时,提供吸收蓝光的黄色滤器(filter)。蓝光被认为对所述视网膜有潜在损伤。根据本发明可用的色料实例为类胡萝卜素(carotenoid),如叶黄素(lutein),玉米黄质(zeaxanthin),中玉米黄质(mesozeaxanthin),虾青素(astaxanthin),或其酯,或角黄素(canthaxanthin),或它们的混合物,及具有维生素A活性的化合物或其前体。已发现给药叶黄素和玉米黄质会降低与年龄相关的斑点(macular)疾病(AMD)的发作风险。然而,这些化合物也可在无AMD时用于提高视觉功效。相应地,本发明一方面涉及能够被引入眼组织和/或造成眼组织黄化的色料在生产用于在黑暗中使视觉功效提高的组合物中的用途,所述色料具体为类胡萝卜素,如选自如下的化合物:叶黄素,玉米黄质,中玉米黄质,虾青素,或其酯,或角黄素,或它们的混合物,和/或具有维生素A活性的化合物或其前体。本发明的另一方面涉及通过给药有效量的一或多种上述色料,在黑暗中提高视觉功效的方法。
本发明的另一实施方案涉及上述色料结合选自如下的抗氧化剂在生产用于使视觉功效提高的组合物中的用途:维生素E,维生素C,锌或无机硒盐如硒代磷酸盐(selenophosphate)或亚硒酸钠或硒酸钠或硒基(seleno)氨基酸如L-硒基甲硫氨酸,或含有或富含硒的含硒(selenized)酵母如啤酒酵母(brewer’s yeast)或面包酵母(baker’s yeast)(酿酒酵母(Saccharomycescerevisiae)),及含约20-30花色素苷(anthocyanosides)的覆盆子(bilberry)提取物,或其混合物。
叶黄素,玉米黄质,中玉米黄质或虾青素的酯优选为下述酸的酯:饱和链烷酸如乙酸,丙酸,棕榈酸,硬脂酸和琥珀酸,单不饱和脂肪酸如油酸,和多不饱和脂肪酸如亚油酸(linolic),亚油酸(linoleic),二十二碳六烯酸和花生四烯酸。
具有维生素A活性的化合物或其前体的实例为视黄醇(retinol)及其酯,如棕榈酸视黄酯;α-和β-胡萝卜素,β-隐黄质(cryptoxanthin)和番茄红素(lycopene)。锌盐的实例为无机酸的锌盐如硫酸锌,或有机酸的锌盐如乳清酸锌。有机硒盐的实例为硒代磷酸盐或亚硒酸钠或硒酸钠。
术语“维生素E”指天然的或外消旋的α-维生素E(tocopherol)及其酯如乙酸酯。术语“维生素C”包括抗坏血酸及其酯和盐,如棕榈酸抗坏血酸酯(ascorbyl palmitate)和抗坏血酸磷酸钠(sodium ascorbyl phosphate)。
本文所用术语“视觉功效”指视觉功能如敏度(acuity),对比(contrast)敏感性,暗适应,眩光恢复,光应激(photo stress)恢复,视网膜(retinal)敏感性,蓝椎体(blue cone)敏感性,色觉(color vision)及视野(visual field)。特别关注的是从眩光恢复以及眩光生理效应的减弱,特别是由蓝光造成的眩光,例如当在黑暗中(即在夜晚或黎明)驾驶时,或在隧道里时。根据本发明,另一可提高的视觉功能是目标锁定(target shooting)的准确性。
术语“眼组织”包含视网膜,晶状体,玻璃体,视网膜色素上皮,虹膜和睫状体。
本文所用术语“组合物”指任何适合给药人体的组合物,如药物制剂,食物或饮料。
根据本发明用来使视觉功效提高的药物制剂可用任何常用口服给药的形式,例如固体形式如片剂包括泡腾片或软壳或硬壳胶囊,或液体形式如溶液或悬液,优选油性(oily)悬液。所述药物制剂除了所述活性成分还可含有常用药物载体物质,添加剂和助剂,其包括水,明胶,植物胶(gum),糖,植物油,聚亚烷基二醇,调味剂,保存剂,稳定剂,乳化剂,缓冲剂等等。该药剂可以是可控(延迟)释放制剂的形式。为本发明目的,可将所述色料以及上述可选组分掺入食物或饮料中,如焙烤物品(items),例如蛋糕和饼干(cookies),柠檬水和水果汁。
本发明优选方面涉及上述色料在生产用于在夜晚驾驶时降低眩光或促进眩光恢复的药剂,食物或饮料中的用途。优选使用叶黄素和玉米黄质的组合物(combination)。在此组合中这些化合物优选按0.1-1.0∶1.0-0.1的重量份比例来应用。
在固体药物制剂中,选自叶黄素,玉米黄质,中玉米黄质,虾青素,β-隐黄质或其酯,或角黄素的化合物适合以每个剂量单位约0.1mg到约500mg的量,优选从约1mg到约100mg的量存在。在液体制剂中,上述组分适合占所述组合物总重的约0.1%到约5%。在有维生素E的情况下,其量适合为每个剂量单位的固体制剂中约10到约1000mg以及液体制剂中约0.1到约500mg。在液体制剂中维生素E可作为本发明配制剂中其它亲脂组分的载体并可占所述组合物总重的99,9-50%。在有维生素C的情况下,其量适合为每个剂量单位约10到约1000mg。具有维生素A活性的化合物或其前体可以以每个剂量单位提供约100到约10000个国际单位的维生素A活性的量存在。锌可以以每剂量单位1到100mg(基于元素(elementary)锌)的量存在。硒可以以每剂量单位10到200μgmg(基于元素硒)的量存在。覆盆子提取物可以以每剂量单位50到150mg(通常含有20%到30%花色素苷)的量应用。
优选每剂量单位的固体药物制剂包含约6mg到约12mg的叶黄素,玉米黄质,中玉米黄质,虾青素,β-隐黄质或其酯,或角黄素,或它们的混合物;约200mg的维生素E;及1mg到约10mg的锌,并可选约1000国际单位的维生素A,还可选约1mg到约10mg的β-胡萝卜素。因此,本发明另一方面还涉及此类优选的固体药物制剂。
在根据本发明制备的药物制剂中或包含在任何食物或饮料中的成分叶黄素,玉米黄质,中玉米黄质,虾青素,β-隐黄质或其酯,或角黄素,其合适的每日剂量为,例如在每公斤体重0.001mg到约20mg的范围。基于非酯化形式的这些组分的总重,每日剂量更优选为每公斤体重约0.01到约10mg,并更优选为每日每公斤体重约0.1到1.0mg。
实施例
实施例1
制备软明胶胶囊,包含如下成分:
成分                          每个胶囊的量
叶黄素                        10mg
卵磷脂                        50mg
大豆油                        200mg
实施例2
制备软明胶胶囊,包含如下成分:
成分                          每个胶囊的量
叶黄素                        10mg
玉米黄质                      10mg
卵磷脂                        50mg
大豆油                        200mg
实施例3
制备软明胶胶囊,包含如下成分:
成分                          每个胶囊的量
叶黄素                        6mg
玉米黄质                      6mg
维生素E(α-d,l-维生素E)      200mg
维生素C                       500mg
卵磷脂                        50mg
大豆油                        200mg
实施例4
制备软明胶胶囊,包含如下成分:
成分                          每个胶囊的量
叶黄素                        12mg
维生素E(α-d,l-维生素E)      200mg
维生素C                       500mg
卵磷脂                        50mg
大豆油                        200mg
实施例5
制备软明胶胶囊,包含如下成分:
成分                          每个胶囊的量
玉米黄质                      12mg
维生素E(α-d,l-维生素E)      200mg
维生素C                       500mg
卵磷脂                        50mg
大豆油                        200mg
实施例6
制备软明胶胶囊,包含如下成分:
成分                          每个胶囊的量
叶黄素                        6mg
玉米黄质                      6mg
β-胡萝卜素                   6mg
维生素E(α-d,l-维生素E)      200mg
维生素C                       500mg
锌(为乳清酸盐)                7.5mg
卵磷脂                        50mg
大豆油                        200mg
实施例7
制备软明胶胶囊,包含如下成分:
成分                         每个胶囊的量
叶黄素                       6mg
玉米黄质                     6mg
维生素E(α-d,l-维生素E)     200mg
维生素C                      500mg
维生素A                      1000国际单位
锌(为乳清酸盐)               7.5mg
卵磷脂                        50mg
大豆油                        200mg
实施例8
制备软明胶胶囊,包含如下成分:
成分                          每个胶囊的量
叶黄素                        6mg
玉米黄质                      6mg
β-胡萝卜素                   6mg
维生素E(α-d,l-维生素E)      200mg
维生素C                       500mg
维生素A                       1000国际单位
锌(为乳清酸盐)                7.5mg
卵磷脂                        50mg
大豆油                        200mg

Claims (27)

1.能够被引入眼组织和/或造成眼组织黄化的色料在生产用于在黑暗中使视觉功效提高的组合物中的用途。
2.根据权利要求1的用途,其中所述提高在于降低眩光或促进从眩光恢复,特别是当在弱光线或暗光线条件下驾驶机动车或飞机时。
3.根据权利要求1或2的用途,其中所述色料是类胡萝卜素。
4.根据权利要求1-3中任一项的用途,其中所述色料选自叶黄素,玉米黄质,中玉米黄质,虾青素,或其酯,或角黄素,或具有维生素A活性的化合物或其前体,或它们的混合物。
5.根据权利要求4的用途,其中所述选自具有维生素A活性的化合物或其前体的色料为视黄醇或其酯,如棕榈酸视黄酯;α-和β-胡萝卜素,β-隐黄质,或番茄红素,或它们的混合物。
6.根据权利要求1-5中任一项的用途,其另外包含选自如下的抗氧化剂:维生素E,维生素C,锌或硒盐或硒基氨基酸,含硒酵母和覆盆子提取物,或其混合物。
7.根据权利要求1-6中任一项的用途,其中所述化合物为叶黄素或玉米黄质,或叶黄素或玉米黄质的酯,或其任何组合物。
8.根据权利要求7用途,是叶黄素与玉米黄质的组合的用途。
9.根据权利要求1-8中任一项的用途,其中所述组合物为药物组合物。
10.根据权利要求9的用途,其中所述药物组合物是为了口服应用并且包含每剂量单位量为约0.1mg到约500mg的叶黄素,玉米黄质,中玉米黄质,虾青素,或其酯,或角黄素,或它们的混合物。
11.根据权利要求9或10的用途,其中所述组合物包含具有维生素A活性的化合物或其前体,特别是视黄醇及其酯,如棕榈酸视黄酯;α-和β-胡萝卜素,β-隐黄质,和番茄红素或它们的混合物,其量为每剂量单位提供约100到约10000国际单位的维生素A的活性。
12.根据权利要求9-11中任一项的用途,其中在所述组合物另外包含每剂量单位约10mg到约1000mg的维生素E。
13.根据权利要求9-12中任一项的用途,其中所述组合物另外包含每剂量单位约1mg到约100mg的锌。
14.根据权利要求1-8中任一项的用途,其中所述组合物是食物或饮料。
15.固体药物组合物,其每剂量单位包含各约6mg到约12mg的叶黄素和玉米黄质;约200mg的维生素E;和1mg到约10mg的锌。
16.根据权利要求15的组合物,其另外包含每剂量单位约1000国际单位的维生素A。
17.根据权利要求15或16的组合物,其另外包含每剂量单位约1mg到约10mg的β-胡萝卜素。
18.在黑暗中提高视觉功效的方法,其包括对需要此治疗的人给药有效量的色料,所述色料能被引入眼组织和/或造成眼组织黄化。
19.根据权利要求18的方法,其中所述提高在于降低眩光或促进从眩光恢复,特别是当在弱光线或暗光线条件下驾驶机动车或飞机时。
20.根据权利要求18或19的方法,其中所述色料为类胡萝卜素。
21.根据权利要求18-20中任一项的方法,其中所述色料选自叶黄素,玉米黄质,中玉米黄质,虾青素,或其酯,或角黄素,或具有维生素A活性的化合物或其前体,或它们的混合物。
22.根据权利要求18-20中任一项的方法,其中所述选自具有维生素A活性的化合物或其前体的色料是视黄醇或其酯,如棕榈酸视黄酯;α-和β-胡萝卜素,β-隐黄质,或番茄红素,或它们的混合物。
23.根据权利要求18-22中任一项的方法,其另外包含给药选自如下的抗氧化剂:维生素E,维生素C,锌或硒盐,或硒基氨基酸,含硒酵母和覆盆子提取物,或其混合物。
24.根据权利要求18-23中任一项的方法,其中所述色料为叶黄素或玉米黄质,或叶黄素或玉米黄质的酯,或其任何组合物。
25.根据权利要求24的方法,其中所述色料是叶黄素和玉米黄质的组合。
26.根据权利要求18-25中任一项的方法,其中基于非酯化形式的色料的总重,所述色料的每日剂量在每公斤体重0.001mg到每公斤体重约20mg,优选每公斤体重约0.01到约10mg,最优选每日每公斤体重约0.1到1.0mg的范围内。
27.基本如本文所述的本发明,特别参考所述实施例。
CNA038029944A 2002-01-30 2003-01-23 叶黄素/玉米黄质用于眩光保护 Pending CN1625395A (zh)

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