CN112494526A - 盐肤木提取物及其药物组合物制备方法和应用 - Google Patents
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Abstract
本发明涉及盐肤木提取物及其药物组合物制备方法和应用，属于中药、天然药物制药领域。以本发明提取物为活性成份的抗疟疾的药物，其制备方法，取盐肤木植物的干燥地上部分或枝叶，粉碎到30目，用有机溶剂石油醚或氯仿或乙酸乙酯或丙酮或甲醇或乙醇或水提取。本发明盐肤木提取物制备抗疟疾剂中的应用：以0.01‑30 g的量施用于基材或一种群上，任选地与载体和/或媒体相结合，具有较好的抗疟疾活性。本发明拓展了盐肤木的药用范围，提高了传统盐肤木药材的药用价值。
Description
技术领域：
本发明属于中药、天然药物制药领域，具体地，涉及盐肤木提取物的制备方法和以该提取物为活性成份的药物组合，及其在抗疟疾剂中的应用。
技术背景：
盐肤木（Rhus chinensis Mill.）为漆树科（Anacardiaceae）盐肤木属（Rhus）植物，落叶小乔木或灌木，高2-10米；我国除东北、内蒙古和新疆外，其余省区均有，生于海拔170-2700米的向阳山坡、沟谷、溪边的疏林或灌丛中。本植物为五倍子蚜虫寄主植物之一，在幼枝和叶上形成虫瘿，即传统中药五倍子，可供鞣革、医药、塑料和墨水等工业上用。幼枝和叶可作土农药，果泡水代醋用，生食酸咸止渴，种子可榨油，根、叶、花及果均可供药用。据《中华本草》记载，盐肤木皮具有清热解毒、活血止痢功效，主治血痢、痈肿、疮疥、蛇犬咬伤等；盐肤木根皮具有清热利湿、解毒散瘀功效，主治黄疸、水肿、风湿痹痛、小儿疳积、疮疡肿毒、跌打损伤、毒蛇咬伤等；盐肤木根具有祛风湿、利水消肿、活血散毒功效，主治风湿痹痛、水肿、咳嗽、跌打肿痛、乳痈、癣疮等。现代研究表明，盐肤木主要含有没食子酸及其衍生物、黄酮和三萜类成分；具有抗菌、抗病毒、抗氧化、抗癌、抗炎、抗糖尿病、止泻、保肝等活性（贵 阳中医学院学报, 2019, 41(1): 70-74; Phytotherapy Research, 2010, 24(12):1739-1747; European Journal of Integrative Medicine, 2018, 21: 43-49）。
目前，国内外未见盐肤木提取物的制备方法和以该提取物为活性成份的药物组合，及其在抗疟疾中应用的报道。
发明内容：
本发明旨在提供盐肤木提取物的制备方法和以其为活性成份的药物组合物，以及它们在制备抗疟疾剂中的应用。
本发明的上述目的是通过下面的技术方案得以实现的：
盐肤木提取物的制备方法，取盐肤木植物的干燥地上部分或枝叶，粉碎到30目，用有机溶剂石油醚或氯仿或乙酸乙酯或丙酮或甲醇或乙醇或水在室温条件下浸提2-5次，每次12-48 h，合并提取液，提取液浓缩得浸膏。或将盐肤木植物的地上部分或枝叶干燥，粉碎到30目，用有机溶剂石油醚或氯仿或乙酸乙酯或丙酮或甲醇或乙醇或水在80-120 oC条件下回流提取2-5次，每次2-8 h，合并提取液，提取液浓缩得浸膏。浸泡或热回流时，可辅以超声或微波提取，每次用溶剂量为浸泡药渣重量的5-25倍。
抗疟疾剂，含有盐肤木提取物和常规辅剂。
药物组合物，其中含有治疗有效量的盐肤木提取物和药学上可接受的载体。
盐肤木提取物在制备抗疟疾剂中的应用。
本发明用于抗疟疾的药物组合物，其中含有盐肤木提取物和药学上可接受的载体。
本发明药物组合物中所述药学上可接受的载体是指药学领域常规的药物载体。本发明盐肤木提取物可以组合物的形式通过口服、鼻吸入、直肠或肠胃外给药的方式施用于需要这种治疗的患者。用于口服时，可将其制成常规的固体制剂如片剂、粉剂、颗粒剂、胶囊等，制成液体制剂如油悬浮剂、糖浆、酏剂等；用于肠胃外给药时，可将其制成注射用的溶液等。优选的形式是片剂、胶囊和注射剂。
本发明药物组合物的各种剂型可以按照药学领域的常规生产方法制备。例如使活性成份与一种或多种载体混合，然后将其制成所需的剂型。
本发明的药物组合物优选含有重量比为0.1%-99.5%的活性成份，最优选含有重量比为0.5%-95%的活性成份。
本发明盐肤木提取物的施用量可根据用药途径、患者的年龄、体重、所治疗的疾病的类型和严重程度等变化，其日剂量可以是0.1-100 mg/kg体重，优选0.5-50 mg/kg体重。可以一次或多次施用。
本发明的盐肤木提取物显示出较好的抗疟疾活性。
本发明对盐肤木提取物进行了抗疟疾活性筛选，盐肤木提取物显示出较好的抗疟活性。在抗疟活性应用中，盐肤木提取物是以如下的量施用于基材或一种群上，所述量的范围0.01-30 g，优选在0.03-10 g，任选地与载体和/或媒体相结合。
具体实施方式：
下面用本发明的实施例来进一步说明本发明的实质性内容，可以使本专业人员更全面地理解本发明，但不以任何方式限制本发明。
实施例1：
本发明盐肤木提取物的制备：
取盐肤木植物干燥枝叶111 g，粉碎到30目，用75%乙醇在95 oC条件下回流提3次，每次2 h，提取液合并，减压浓缩提取液得浸膏20.8 g，提取率18.7%。
实施例2：
本发明提取物的抗疟疾活性检测：
采用国际通用的4天抑制实验法，每只小鼠腹腔接种1×107个疟原虫感染的红细胞，接种疟原虫3 h后灌胃给药，之后每隔24 h给药一次，连续给药4天（接种日为D0，次日为D1，依此类推），于第5天（D4）尾静脉取血，涂制薄血膜，甲醇固定，瑞氏-吉姆萨（Wright-Giemsa）混合染色法染色，10×100显微镜油镜下观察。若随机查看50个视野后均未发现疟原虫无性体，则判定为阴性，阳性薄血膜片则随机计数5个视野，且红细胞总数不少于1000个，然后按照如下公式计算疟原虫抑制率。
疟原虫感染率(%) ＝感染疟原虫的红细胞/红细胞总数 × 100%
疟原虫抑制率(%) ＝ [(对照组平均感染率‒样品组平均感染率)/对照组平均感染率] ×100%
活性数据见表1。
表1 盐肤木提取物的抗疟活性数据（n = 4）
Claims (7)
1.盐肤木提取物的制备方法，其特征在于，用有机溶剂石油醚或氯仿或乙酸乙酯或丙酮或甲醇或乙醇或水直接冷浸或者热回流提取盐肤木植物的地上部分或枝叶，得到提取液，将提取液浓缩、干燥得到盐肤木提取物。
2.权利要求1所述提取物的制备方法，其特征在于将盐肤木植物的地上部分或枝叶干燥，粉碎到30目，用有机溶剂石油醚或氯仿或乙酸乙酯或丙酮或甲醇或乙醇或水在室温条件下提取，提取液浓缩得浸膏。
3.权利要求1所述提取物的制备方法，其特征在于将盐肤木植物的地上部分或枝叶干燥，粉碎到30目，用有机溶剂石油醚或氯仿或乙酸乙酯或丙酮或甲醇或乙醇或水热回流提取，提取液浓缩得浸膏。
4.如权利要求2和3所述的制备方法，其特征在于，浸泡或热回流时，可辅以超声或微波提取，每次用溶剂量为浸泡药渣重量的5-25倍。
5.药物组合物，其中含有治疗有效量的权利要求1所述提取物和药学上可接受的载体。
6.抗疟疾剂，其中含有权利要求1所述提取物和常规辅剂。
7.权利要求1所述提取物在制备抗疟疾剂中的应用。
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| CN116077540A (zh) * | 2021-11-08 | 2023-05-09 | 中国医学科学院药物研究所 | 盐肤木提取物在制备治疗胃相关疾病药物中的应用 |
| CN116077540B (zh) * | 2021-11-08 | 2024-01-12 | 中国医学科学院药物研究所 | 盐肤木提取物在制备治疗胃相关疾病药物中的应用 |
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