CN116196345B - 一种用于眼部功能改善的组合物及其应用 - Google Patents
一种用于眼部功能改善的组合物及其应用 Download PDFInfo
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- CN116196345B CN116196345B CN202310356329.0A CN202310356329A CN116196345B CN 116196345 B CN116196345 B CN 116196345B CN 202310356329 A CN202310356329 A CN 202310356329A CN 116196345 B CN116196345 B CN 116196345B
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- VYPSYNLAJGMNEJ-UHFFFAOYSA-N Silicium dioxide Chemical compound O=[Si]=O VYPSYNLAJGMNEJ-UHFFFAOYSA-N 0.000 claims abstract description 16
- AERBNCYCJBRYDG-UHFFFAOYSA-N D-ribo-phytosphingosine Natural products CCCCCCCCCCCCCCC(O)C(O)C(N)CO AERBNCYCJBRYDG-UHFFFAOYSA-N 0.000 claims abstract description 14
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Abstract
本发明公开了一种用于眼部功能改善的组合物及其应用，属于眼用药物技术领域。一种用于眼部功能改善的组合物，包括下列重量份的各组分：所述组合物总质量的0.05%‑0.2%的人参提取物；所述组合物总质量的0.01%‑0.1%的介孔硅石；所述组合物总质量的0.01%‑0.1%的聚季铵盐‑1；所述组合物总质量的0.01%‑0.5%的植物鞘氨醇；余量为水。本发明以介孔硅石作为载体，复合聚季铵盐‑1的杀菌消毒的功效，并利用人参提取物提高机体免疫力，以植物鞘氨醇增强用药部位的皮肤保湿渗透功效，几种组分组合作用，可以显著的改善眼睑板的功能。
Description
技术领域
本发明属于眼用药物技术领域，涉及一种用于眼部功能改善的组合物及其应用。
背景技术
眼睑板位于睫毛根部旁边有软骨的位置，由于不良用眼习惯、内分泌紊乱、系统性疾病等，容易诱发睑板腺功能障碍（Meibomian gland dysfunction，MGD），睑板腺功能障碍是一种常见的眼科疾病，患者多表现为眼部干涩刺激、红痒、疼痛等。近年来，随着环境变化以及视频终端的广泛使用，MGD 的发病率逐年升高导致眼睑板腺口阻塞分泌物淤积眼睑板堵塞，临床上可引起泪膜异常、眼部刺激症状、眼表炎症反应，是导致干眼的主要原因。分析造成眼睑板堵塞的原因，主要包括：（1）自身分泌的皮脂腺过于旺盛，没有及时进行面部清洗而造成堵塞；（2）经常使用化妆品造成睑缘睑板腺开口堵塞；（3）由于自身的免疫力低，导致睑缘的睑板腺堵塞。MGD 的发病机制尚不明确，其治疗方案有限，目前主要的治疗方法有睑缘清洁、热敷、睑板腺按摩、人工泪液以及手术治疗等，而现有的治疗方法都存在一定程度的缺陷，很难达到满意的效果。
为了解决现有技术存在的上述缺陷，本发明研发了一种可以用于眼部功能改善的组合物及其应用。
发明内容
本发明的目的是提供一种用于眼部功能改善的组合物及其应用。
本发明是通过以下技术方案实现的：
一种用于眼部功能改善的组合物，包括下列重量份的各组分：
所述组合物总质量的0.05%-0.2%的人参提取物；
所述组合物总质量的0.01%-0.1%的介孔硅石；
所述组合物总质量的0.01%-0.1%的聚季铵盐-1；
所述组合物总质量的0.01%-0.5%的植物鞘氨醇；
余量为水。
进一步地，所述的人参提取物包括原人参二醇和人参皂苷rh2。
所述的原人参二醇和皂苷rh2占人参提取物总质量的0.5-3%。
所述组合物总质量的0.1%-0.15%的人参提取物。
所述组合物总质量的0.03%-0.08%的介孔硅石。
所述组合物总质量的0.05%-0.08%的聚季铵盐-1。
所述组合物总质量的0.1%-0.3%的植物鞘氨醇。
更进一步地，本发明还公开了上述组合物在制备眼部清洗剂中的应用。
本发明还公开了上述组合物在制备眼用消毒湿巾中的应用。
本发明人参提取物对中枢神经系统、心血管系统、消化系统、免疫系统、内分泌系统有广泛的作用，从而可提高人体免疫能力，增强机体对有害刺激的非特异性抵抗力，其中主要的有效成分为原人参二醇和人参皂苷rh2，占人参提取物总质量的0.5-3%，原人参二醇可以通过增强机体免疫来清除影响眼部功效的有害细胞，且其分子量和极性都小，便于吸收而发挥其药理作用，人参皂苷rh2可以诱导细胞周期停滞和凋亡，并在体外和体内显示免疫调节和抗转移活性；聚季铵盐-1为阳离子型杀菌消毒剂，可有效地杀灭大肠杆菌、铜绿色假单胞菌、金黄色葡萄球菌、白色念珠菌和黑曲霉等，其抑菌性能高于PHMB，毒性低于BAC，过敏刺激副作用相对更弱，非常适用于在眼科溶液中使用，本发明将其浓度控制在0.01%-0.1%之间，相比传统杀菌剂的使用量，其浓度更低；植物鞘氨醇为细胞膜组成成分之一，存在于表皮层和皮肤表层，在组合物中添加植物鞘氨醇可以很快渗透进皮肤，和角质层中的水结合，形成一种网状结构，锁住水分；此外，本发明选择介孔硅石作为载体，用于药物的递送。
综上，本发明以介孔硅石作为载体，复合聚季铵盐-1的杀菌消毒的功效，并利用人参提取物提高机体免疫力，以植物鞘氨醇增强用药部位的皮肤保湿渗透功效，几种组分组合作用，可以显著的改善眼睑板的功能。
实施方式
以下结合实施例对本发明作进一步说明。
实施例
按照表1所示组分制备组合物，分别获得五组组合物。
表1
制备方法：
将各组分溶液混合，加热混合物使溶解完全，冷却混合物，然后加入聚季铵盐-1，然后加注射用水至全量，搅拌均匀，用滤器过滤除菌后盛装于容器中，即得。
实施例
健康新西兰大白兔30只，雌雄各半，体重2-2.5kg，随机分为空白组、模型组、组合物中含人参提取物不同浓度组，分别为（含原人参二醇和人参皂苷Rh2 0.01%、0.02%、0.05%、0.1%、0.2%、0.5%、1%、1.5%、2%、2.5%）共十二组，每组6只。除空白组外其余各组大白兔每天8点 11点14 点和18点皮下注射氢溴酸东莨菪碱注射液2.0mg/次，连续注射三天，造兔干眼症模型，空白组注射生理盐水。
第四天开始，用棉棒蘸取不同的溶剂1mL擦拭兔左眼睑板4次/天，右眼不做处理，连续擦拭7天。空白组及模型组擦拭生理盐水、人参提取物组擦拭含不同浓度的人参提取物的组合物。在第三天和第七天观察模型兔双眼泪液分泌量，泪膜破裂时间（BUT）的改变。
泪液分泌酚红棉线进行兔基础泪液的测量。每天用药前，眼局部不使用麻药，用镊子将棉线反折端轻轻置于下睑中外1/3交界处穹窿部，保持兔睁眼且不眨眼15秒后取出棉线，以毫米为单位测定棉线颜色由黄变红的长度。
滴1%荧光素钠一滴于兔下睑结膜囊内，使其瞬目几次使荧光素分布均匀，
记录从最后一次瞬目到泪膜出现第一个黑色干燥斑的时间。
泪液分泌实验
空白组双侧泪液分泌量均无明显变化；模型组双侧泪液分泌量均减少；人参提取物组（含原人参二醇和人参皂苷Rh2 0.01%、0.02%、0.05%）这三个组双侧泪液分泌量均减少，与模型组无异。随着含人参二醇和人参皂苷Rh2浓度的升高，其左眼泪液分泌量慢慢的高于右眼；当人参提取物含原人参二醇和人参皂苷Rh2 含量达到2.5%时，其左眼的泪液分泌量与含原人参二醇和人参皂苷Rh2 含量为2%几乎一致，故我们后期试验选择含原人参二醇和人参皂苷Rh2 0.1%-2%,作为我们的剂量范围。
实施例
健康新西兰大白兔30只，雌雄各半，体重2-2.5kg，随机分为空白组、模型组、空白组溶剂、人参提取物组、植物鞘氨醇组、完全组合物组共六组，每组6只。除空白组外其余各组大白兔每天8点 11点14 点和18点皮下注射氢溴酸东莨菪碱注射液2.0mg/次，连续注射三天，造兔干眼症模型，空白组注射生理盐水。
第四天开始，用棉棒蘸取不同的溶剂1mL擦拭兔左眼睑板4次/天，右眼不做处理，连续擦拭7天。空白组及模型组擦拭生理盐水、人参提取物组擦拭含人参提取物的组合物（含原人参二醇及人参皂苷Rh2含量1%，不含植物鞘氨醇）、植物鞘氨醇组擦拭含植物鞘氨醇的组合物（含植物鞘氨醇含量1%，不含人参提取物）、组合物组擦拭同时含人参提取物及植物鞘氨醇的组合物（含原人参二醇及人参皂苷Rh2含量1%、含植物鞘氨醇含量1%）。在第三天和第七天观察模型兔双眼泪液分泌量，泪膜破裂时间（BUT）的改变。
泪液分泌酚红棉线进行兔基础泪液的测量。每天用药前，眼局部不使用麻药，
用镊子将棉线反折端轻轻置于下睑中外1/3交界处穹窿部，保持兔睁眼且不眨眼
15秒后取出棉线，以毫米为单位测定棉线颜色由黄变红的长度。
滴1%荧光素钠一滴于兔下睑结膜囊内，使其瞬目几次使荧光素分布均匀，
记录从最后一次瞬目到泪膜出现第一个黑色干燥斑的时间。
泪液分泌实验
空白组双侧泪液分泌量均无明显变化，模型组双侧泪液分泌量均减少，空白溶剂组双侧泪液分泌量均减少且无明显差异，人参提取物组左眼泪液分泌量显著高于右眼，植物鞘氨醇组左眼泪液分泌量显著高于右眼，完全组合物组左眼泪液分泌量显著高于右眼；完全组合物组左眼眼泪分泌量显著高于人参提取物组及植物鞘氨醇组的左眼眼泪分泌量。
泪膜破裂时间
空白组双侧眼泪膜破裂时间均无明显变化(BUT>20s)，第三天模型组双侧眼泪膜破裂时间均明显下降(BUT<5s)，第七天平均BUT<3s，空白溶剂组双侧眼泪膜破裂时间与模型组相比无显著差异，人参提取物组左眼泪膜破裂时间相较于右眼显著增加，植物鞘氨醇组左眼泪膜破裂时间相较于右眼显著增加，完全组合物组左眼泪膜破裂时间显著长于右眼。完全组合物组左眼泪膜破裂时间（＞15s）显著长于人参提取物组（＞10s）及植物鞘氨醇组（＞10s）。
给药后各组第3天及第7天BUT变化
显然，本领域的技术人员可以对本发明进行各种改动和变型而不脱离本发明的精神和范围。这样，倘若对本发明的这些修改和变型属于本发明权利要求及其同等技术的范围之内，则本发明也意图包含这些改动和变型在内。上述实施例或实施方式只是对本发明的举例说明，本发明也可以以其它的特定方式或其它的特定形式实施，而不偏离本发明的要旨或本质特征。因此，描述的实施方式从任何方面来看均应视为说明性而非限定性的。本发明的范围应由附加的权利要求说明，任何与权利要求的意图和范围等效的变化也应包含在本发明的范围内。
Claims (7)
1.一种用于眼部功能改善的组合物，其特征在于，包括下列重量份的各组分：
所述组合物总质量的0.05%-0.2%的人参提取物，所述的人参提取物包括原人参二醇和人参皂苷rh2，其中所述的原人参二醇和皂苷rh2占人参提取物总质量的0.5-3%；
所述组合物总质量的0.01%-0.1%的介孔硅石；
所述组合物总质量的0.01%-0.1%的聚季铵盐-1；
所述组合物总质量的0.01%-0.5%的植物鞘氨醇；
余量为水。
2.根据权利要求1所述的用于眼部功能改善的组合物，其特征在于，所述组合物总质量的0.1%-0.15%的人参提取物。
3.根据权利要求1所述的用于眼部功能改善的组合物，其特征在于，所述组合物总质量的0.03%-0.08%的介孔硅石。
4.根据权利要求1所述的用于眼部功能改善的组合物，其特征在于，所述组合物总质量的0.05%-0.08%的聚季铵盐-1。
5.根据权利要求1所述的用于眼部功能改善的组合物，其特征在于，所述组合物总质量的0.1%-0.3%的植物鞘氨醇。
6.权利要求1-5任意一项所述的用于眼部功能改善的组合物在制备眼部清洗剂中的应用。
7.权利要求1-5任意一项所述的用于眼部功能改善的组合物在制备眼用消毒湿巾中的应用。
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| CN112584818A (zh) * | 2018-07-12 | 2021-03-30 | 美国奥科视光有限公司 | 抗过敏眼用组合物和眼睑清洁湿巾 |
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| CN112584818A (zh) * | 2018-07-12 | 2021-03-30 | 美国奥科视光有限公司 | 抗过敏眼用组合物和眼睑清洁湿巾 |
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