CN112402479A - 红花杜鹃提取物及其药物组合物制备方法和抗疟用途 - Google Patents

红花杜鹃提取物及其药物组合物制备方法和抗疟用途 Download PDF

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CN112402479A
CN112402479A CN202011557332.1A CN202011557332A CN112402479A CN 112402479 A CN112402479 A CN 112402479A CN 202011557332 A CN202011557332 A CN 202011557332A CN 112402479 A CN112402479 A CN 112402479A
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姜北
肖朝江
刁红梅
李靖
张伟
沈磊
董相
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Abstract

本发明涉及红花杜鹃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，取红花杜鹃植物的干燥地上部分或全株，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。本发明红花杜鹃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。本发明开发了红花杜鹃的药用价值。

Description

红花杜鹃提取物及其药物组合物制备方法和抗疟用途
技术领域：
本发明属于中药、天然药物制药领域，具体地，涉及红花杜鹃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：
红花杜鹃（Rhododendron spanotrichum Balf. f. et W. W. Smith）为杜鹃花科（Ericaceae）杜鹃花属（Rhododendron）植物，小乔木，高约6-7米，生于海拔1500-2300米的常绿阔叶林中，为中国特有植物，产云南东南部。《中华本草》记载，许多红花杜鹃同属植物具有一定的药用价值。如，大白花杜鹃（R. decorum Franch.）的根和叶具有清利湿热、活血止痛功效，用于白浊、带下、风湿疼痛、跌打损伤等；岭南杜鹃（R. mariae Hance）的花、叶、嫩枝和根具有祛痰止咳、消肿止痛功效，用于咳嗽多痰、气喘、跌打损伤等；头花杜鹃（R. capitatum Maxim.）的叶和花具有祛痰止咳、暖胃止痛功效，用于咳喘多痰、胃寒腹痛等。此外，杜鹃花（R. simsii Planch.）的叶、花、果实和根也都具有药用价值。然而，国内外未见红花杜鹃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：
本发明旨在提供红花杜鹃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：
红花杜鹃提取物的制备方法，取红花杜鹃植物的干燥地上部分或全株，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。或将红花杜鹃植物的地上部分或全株干燥，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，含有红花杜鹃提取物和常规辅剂。
药物组合物，其中含有治疗有效量的红花杜鹃提取物和药学上可接受的载体。
红花杜鹃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，其中含有红花杜鹃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。本发明红花杜鹃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。
本发明红花杜鹃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。
本发明的红花杜鹃提取物显示出较好的抗疟疾活性。
本发明对红花杜鹃提取物进行了抗疟疾活性筛选，红花杜鹃提取物显示出较好的抗疟活性。在抗疟活性应用中，红花杜鹃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：
本发明红花杜鹃提取物的制备：
取红花杜鹃植物干燥地上部分117 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22.1 g，提取率18.9%。
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 红花杜鹃提取物的抗疟活性数据（n = 4）
Figure DEST_PATH_IMAGE002

Claims (7)

1.红花杜鹃提取物的制备方法，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红花杜鹃植物的地上部分或全株，得到提取液，将提取液浓缩、干燥得到红花杜鹃提取物。
2.权利要求1所述提取物的制备方法，其特征在于将红花杜鹃植物的地上部分或全株干燥，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，其特征在于将红花杜鹃植物的地上部分或全株干燥，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。
CN202011557332.1A 2020-12-25 2020-12-25 红花杜鹃提取物及其药物组合物制备方法和抗疟用途 Pending CN112402479A (zh)

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