CN109010352B - 一种抗疲劳药物组合物及其制备方法和用途 - Google Patents
一种抗疲劳药物组合物及其制备方法和用途 Download PDFInfo
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- CN109010352B CN109010352B CN201811318159.2A CN201811318159A CN109010352B CN 109010352 B CN109010352 B CN 109010352B CN 201811318159 A CN201811318159 A CN 201811318159A CN 109010352 B CN109010352 B CN 109010352B
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Abstract
本发明涉及一种抗疲劳药物组合物及其制备方法和用途，所述药物组合物包含高车前苷及药学上可接受的载体，进一步的所述药物组合物包含其他抗疲劳活性成分，优选的所述其他抗疲劳活性成分选自：红景天苷、牛磺酸、人参皂苷或绞股蓝皂苷。本发明药物组合物可显著缓解身体的疲劳状态，可广泛应用于运动疲劳、亚健康导致的疲劳及慢性疲劳等的预防和治疗，安全，无任何毒副作用。
Description
技术领域
本发明属于药物领域，具体涉及一种抗疲劳药物组合物及其制备方法和用途。
背景技术
随着生活节奏的不断加快，人们的生活压力、工作压力、学习压力越来越大，使人们长期处于亚健康状态，其中疲劳为亚健康的重要症状之一。疲劳作为机体的一种不适感受，多伴随于大强度运动、长时间工作、失眠、心理压力长期过大等，可导致神经、内分泌、免疫、消化、循环、运动等系统功能的紊乱，表现出急躁、易怒、反应迟钝、注意力不集中、皮肤干涩、无光泽、四肢乏力、头痛、肌肉疼痛、关节疼痛、食欲减退、精神不振、多梦、记忆力减退、视力减退、听力下降等。长期的疲劳在休息后仍无法及时恢复，严重的影响了人们的生活、工作和学习，甚至还会带来严重的健康问题，如过劳死等。
针对于机体的疲劳状态，目前一般采用运动调节、饮食调节和药物治疗，由于运动调节和饮食调节起效慢、周期长，并且仅对早期疲劳状态有一定的缓解作用，因此，往往不能达到理想的治疗效果。药物治疗为缓解机体疲劳的有效手段之一，近年来发现了多种具有抗疲劳效果的药物，如镇静催眠类药物(安定、三唑仑、褪黑素等)、中枢兴奋药(苯丙胺、咖啡因)等，虽然取得了良好的治疗效果，但毒副作用明显，如成瘾性、嗜睡、心脑血管损伤等。
高车前苷，又称高车前甙，为一种黄酮类化合物，药理学研究表明高车前苷具有止咳、平喘、抗菌、祛痰、保肝、抗组胺、抗氧化、降血糖、降血脂、保护血管内皮细胞等多重药理活性，但尚未见到高车前苷应用于抗疲劳的报道。
本发明致力于提供一种基于高车前苷的安全、高效的抗疲劳药物组合物。
发明内容
本发明的目的是提供一种抗疲劳药物组合物及其制备方法和用途。
一方面，本发明提供一种抗疲劳药物组合物，包含高车前苷和药学上可接受的辅料。
优选的，所述药物组合物以高车前苷作为唯一活性成分；
优选的，所述药物组合物还包含其他抗疲劳活性物质；
优选的，所述其他抗疲劳活性物质选自：红景天苷、牛磺酸、人参皂苷或绞股蓝皂苷；优选的，所述其他抗疲劳活性物质选自：红景天苷；更优选的，所述高车前苷与红景天苷的用量比为3-5：1-3；最优选的，所述高车前苷与红景天苷的用量比为3：1。
本发明药物组合物可通过胃肠道给药，优选的，所述胃肠道给药的剂型选自：口服液、片剂、胶囊剂、颗粒剂、丸剂、散剂等；优选的所述片剂选自：包衣片、咀嚼片、口腔崩解片等。
所述药学上接受的辅料选自：溶剂、稀释剂、粘合剂、崩解剂、润滑剂或助流剂、矫味剂、包衣剂、明胶胶囊壳等。
更优选的，所述溶剂为小苏打溶液；所述稀释剂选自微晶纤维素、糖粉、乳糖、淀粉、糊精、磷酸氢钙、碳酸钙、赤藓糖醇等；所述粘合剂选自：淀粉浆、羟丙基甲基纤维素、羧甲基纤维素钠、聚维酮等；所述崩解剂选自羧甲基淀粉钠、低取代羟丙基纤维素、海藻酸钠、交联聚维酮、交联羧甲基纤维素钠等；所述润滑剂或助流剂选自：硬脂酸镁、滑石粉、微粉硅胶等；所述矫味剂选自：甜味剂、香精等,所述甜味剂选自：甘草甜素、阿斯巴甜、甜叶菊苷等。
本发明药物组合物中高车前苷的含量占药物组合物总重量的1-50％，优选的，药物组合物中高车前苷的含量占药物组合物总重量的3-40％，更优选的，药物组合物中高车前苷的含量占药物组合物总重量的5-20％，最优选的，药物组合物中高车前苷的含量占药物组合物总重量的10％。
本发明的再一个目的是提供高车前苷在制备抗疲劳药物组合物中的用途。
高车前苷与其他抗疲劳活性物质在制备抗疲劳药物组合物中的用途。
优选的，所述其他抗疲劳活性物质选自：红景天苷、牛磺酸、人参皂苷或绞股蓝皂苷；优选的，所述其他抗疲劳活性物质选自：红景天苷；更优选的，所述高车前苷与红景天苷的用量比为3-5：1-3；最优选的，所述高车前苷与红景天苷的用量比为3：1。
本发明的另一个目的是一种抗疲劳药物组合物的制备方法，包括以下步骤：
(1)备料：按照配方称取各原料；
(2)制剂：将高车前苷粉碎过40-100目筛，添加任选的其他抗疲劳活性物质和药学上可接受的辅料后按照本领域常规的工艺制备成相应的剂型，即得本发明抗疲劳药物组合物。
本发明有益效果
药理学实验显示了高车前苷具有明显的缓解疲劳的效果，可明显延长运动疲劳小鼠的游泳时间，高车前苷与红景天苷联用后抗疲劳效果更为显著，明显优于高车前苷、红景天苷单用的效果或高车前苷与其他抗疲劳活性物质的联用效果。高车前苷在抗疲劳的同时，还具有止咳、平喘、抗菌、祛痰、保肝、抗组胺、抗氧化、降血糖、降血脂、保护血管内皮细胞等多重药理活性，且不具有镇静催眠类药物、中枢兴奋药物等抗疲劳药物的心脑血管副作用，安全、有效，可广泛应用于各类型疲劳的预防和治疗。
具体实施方式
在下文中更详细地描述了本发明以有助于对本发明的理解。
实施例1：一种抗疲劳的片剂
高车前苷10份、微晶纤维素55份、赤藓糖醇23份、羟丙纤维素5份、交联羧甲基纤维素钠10份1、硬脂酸镁2份量，按照以下方法制备：
(1)备料：按照配方称取各原料；
(2)制剂：将高车前苷粉碎过60目筛，添加微晶纤维素、赤藓糖醇、羟丙纤维素和交联羧甲基纤维素钠后制软材，过14目筛制粒，干燥，过12目筛整粒，添加硬脂酸镁混合均匀后压片，即得本发明抗疲劳的片剂。
实施例2:一种抗疲劳口服液
高车前苷5份、小苏打溶液82份、甘草甜素2份、橘子香精1份，按照以下方法制备：
(1)备料：按照配方称取各原料；
(2)制剂：将高车前苷粉碎过40目筛，加入小苏打溶液后，搅拌至完全溶解，然后添加甘草甜素、橘子香精后搅拌均匀，滤过后，灌装、灭菌，即得本发明抗疲劳的口服液。
实施例3：一种抗疲劳的胶囊剂
高车前苷6份、红景天苷3份、微晶纤维素55份、赤藓糖醇34份、羟丙纤维素5份、硬脂酸镁2份量，按照以下方法制备：
(1)备料：按照配方称取各原料；
(2)制剂：将高车前苷、红景天苷粉碎过80目筛，添加微晶纤维素、赤藓糖醇、羟丙纤维素后制软材，过14目筛制粒，干燥，过12目筛整粒，添加硬脂酸镁混合均匀后填充于明胶胶囊壳，即得本发明抗疲劳的胶囊剂。
效果例1：高车前苷对疲劳小鼠的影响
1.1实验药物：
1组：高车前苷；
2组：高车前苷：红景天苷＝3：1的混合物；
3组：高车前苷：红景天苷＝1：1的混合物；
4组：高车前苷：红景天苷＝1：3的混合物；
5组：高车前苷：牛磺酸＝3：1的混合物；
6组：高车前苷：绞股蓝皂苷＝3：1的混合物；
7组：高车前苷：人参皂苷＝3：1的混合物；
8组：车前子总黄酮；
9组：红景天苷。
1.2实验方法
四周龄昆明种雄性小鼠55只，体重18-22g，随机分为空白组、模型组、1-9组，每组5只，适应性饲养一天后，小鼠灌胃给药，其中1-9组灌胃相应药物，给药量均为50mg/Kg,空白组与模型组灌胃生理盐水，灌胃体积均为0.4mL，每天灌胃1次，连续灌胃给药21天，灌胃第14天开始，除空白组小鼠外，其他小鼠均尾根部系上体重10％的铅块后置于水深30cm、水温25℃的游泳箱中负重游泳，至力竭后捞出，其中力竭指小鼠沉入水底5S不能浮出水面。末次给药后30min，所有小鼠称重后，尾部系上体重10％的铅块后负重游泳，记录游泳时间，其中游泳时间是指小鼠自游泳开始至沉入水底10S仍不能浮出水面的时间，超过30min仍未沉底者游泳时间记为30min，具体结果见表1。
1.3实验结果
应用统计软件SPSS的多因素方差分析模块进行数据分析，P<0.05表示差异有统计学意义。
表1实验结果显示，至给药结束，相对于空白组，模型组小鼠体重明显减轻，小鼠毛皮污浊、潮湿，精神萎靡，游泳时间明显缩短，表明疲劳小鼠模型造模成功；各给药组中，灌胃车前子总黄酮的第8组小鼠体重、游泳时间指标相对于模型组均未显示出明显的改善，表明了车前子总黄酮并不具有抗疲劳的效果；灌胃红景天苷的第9组小鼠体重、游泳时间指标相对于模型组均明显改善，证明了红景天苷具有显著的抗疲劳的效果；灌胃高车前苷的第1组小鼠的体重、游泳时间指标相对于模型组均明显改善，其中体重和游泳时间指标的改善幅度还明显优于红景天苷，证明了高车前苷具有优异的抗疲劳效果；剩余各组小鼠的体重和游泳时间相对于模型组小鼠也均显示了一定的改善，其中以灌胃高车前苷：红景天苷＝3：1的混合物的第2组的改善效果最为明显，相应指标的改善效果均明显优于高车前苷、红景天苷单独应用时的效果，显示了高车前苷与红景天苷联合使用时具有显著的协同增效的抗疲劳的效果。
表1本发明药物组合物的抗疲劳效果
| 样本量(只) | 体重(g) | 游泳时间(s) | |
| 空白组 | 5 | 37.00±1.58 | 194.6±42.8 |
| 模型组 | 5 | 26.80±1.48△△ | 117.0±13.7△△ |
| 1组 | 5 | 31.20±0.84** | 170.2±21.6** |
| 2组 | 5 | 33.80±1.48** | 188.2±12.0** |
| 3组 | 5 | 29.80±2.49* | 162.4±13.5* |
| 4组 | 5 | 30.20±1.64* | 172.6±14.2** |
| 5组 | 5 | 28.60±2.70 | 165.8±10.0* |
| 6组 | 5 | 28.20±2.39 | 156.8±8.0* |
| 7组 | 5 | 28.80±2.28 | 175.2±7.7** |
| 8组 | 5 | 27.60±1.14 | 122.8±10.6 |
| 9组 | 5 | 28.80±0.84 | 157.8±9.3* |
与空白组比较，△△P<0.01；与模型组比较，*P<0.05,**P<0.01.
以上描述了本发明优选实施方式，然其并非用以限定本发明。本领域技术人员对在此公开的实施方案可进行并不偏离本发明范畴和精神的改进和变化。
Claims (5)
1.一种抗疲劳药物组合物，其特征在于，由高车前苷、红景天苷和药学上可接受的辅料制成，所述高车前苷与红景天苷的用量比为3：1。
2.根据权利要求1所述的抗疲劳药物组合物，其特征在于，所述药物组合物的剂型选自：口服液、片剂、胶囊剂、颗粒剂、丸剂、散剂。
3.根据权利要求2所述的抗疲劳药物组合物，其特征在于，所述片剂选自：包衣片、咀嚼片或口腔崩解片。
4.根据权利要求1-3任一项所述的抗疲劳药物组合物的制备方法，其特征在于包括以下步骤：
(1)备料：按照配方称取各原料；
(2)制剂：将高车前苷粉碎过40-100目筛，添加红景天苷和药学上可接受的辅料后按照本领域常规的工艺制备成相应的剂型，即得。
5.高车前苷和红景天苷的组合在制备抗疲劳药物组合物中的用途，其特征在于，所述高车前苷与红景天苷的用量比为3：1。
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