CN1145224A青蒿素作为抗真菌剂的应用---外用治疗手足癣、头皮癣、体癣、头皮屑等浅表真菌感染|CN1145224A Application of artemisinin as an antifungal agent---Topically treating superficial fungal infections such as tinea pedis, tinea capitis, tinea corporis, and dandruff.
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CN1145224A青蒿素作为抗真菌剂的应用---外用治疗手足癣、头皮癣、体癣、头皮屑等浅表真菌感染
CN1145224A Application of artemisinin as an antifungal agent---Topically treating superficial fungal infections such as tinea pedis, tinea capitis, tinea corporis, and dandruff.
青蒿素作为抗真菌剂的应用
本发明涉及将一种现有的抗疟药青蒿素作为抗真菌药应用，为青蒿素提供了新的用途。通过对青蒿素抗菌作用研究表明，青蒿素具有良好的抗真菌作用，其抗菌谱及作用与目前常用的广谱抗真菌药酮康唑相似，对某些真菌的作用可强于酮康唑。青蒿素可以制成各种制剂，现作为外用剂治疗手足癣、体癣、头癣等浅部真菌感染，还可以用于头皮屑的防治。青蒿素对癣病的疗效优于酮康唑且不良反应较小。
青蒿素作为抗真菌剂的应用
本发明涉及将一种现有的抗疟药青蒿素作为抗真菌药的应用，为中药治疗真菌感染性疾病提供了一种新的药物。
青蒿素系我国从中药黄花蒿中提取的有效单体成分(倍半萜内酯过氧化物)，有优良的抗疟作用。已被世界卫生组织推荐为新抗疟药，目前临床用于治疗疟疾(竺心影主编：药理学第三版，北京：人民卫生出版社，1993：370)。真菌感染尤其是浅部真菌感染-癣病是一种常见病，目前的治疗药物常用的有克霉唑、咪康唑、酮康唑、氟康唑等，均系人工合成品，不良反应较大，主要毒性有贫血、皮疹及胃肠道反应等(江明性主编：药理学第三版，北京：人民卫生出版社，1989年：348)。现有文献报导是将青蒿油搽剂应用于癣病的治疗，用鲜青蒿加水蒸馏获得青蒿油，其主要成份是按油精、青蒿酮、左旋樟脑、侧柏酮、丁香烯以及其它倍半萜衍生物(陈德宇等：青蒿油搽剂抗真菌作用实验及疗效观察，中国皮肤病学杂志，1990；4(1)：18-19)。
本发明的目的在于利用我国中草药资源开发新药，研究“老药新用”，从现有抗疟药青蒿素寻找出新的作用和应用。
本发明通过对青蒿素的体外抗真菌作用研究，证实青蒿素的抗菌谱及作用与目前常用的广谱抗真菌药酮康唑相似，且对某些真菌的作用强于酮康唑。药效学试验结果表明，青蒿素具有良好的抗真菌作用，对真菌属菌株均呈现抑制或杀灭作用，其中对石膏样毛菌、石膏样小孢子菌作用最强；其次对紫色毛癣菌、许兰氏毛癣菌、紫状表皮癣菌、曲霉菌作用均比酮康唑强或近似；对白色念珠菌抑菌作用略低于酮康唑、杀菌作用接近酮康唑(见附件：青蒿素制剂的体外抗菌作用)。临床应用证明青蒿素可以作为抗真菌药用于治疗真菌感染性疾病。目前已作为外用制剂用于治疗手足癣、体癣、头癣等浅部癣菌病，还可用于防治头皮屑，效果均好。青蒿素治疗癣病疗效优于酮康唑，其不良反应小，未见特殊毒性反应。
本发明青蒿素与现有技术青蒿油虽都能用于治疗癣病，但两药有效成份不同，青蒿素是从青蒿中提取的有效单体成分倍半萜内酯过氧化物，而青蒿油中成份较多，其中次要成份倍半萜衍生物未特指哪一种衍生物；其次青蒿素还可用于治疗头皮屑。青蒿素配制方便，可以直接利用现有的药用青蒿素制备成各种制剂供使用，而青蒿油须用青蒿蒸馏提取后再配制成搽剂。本发明青蒿素作为抗真菌剂应用，目前尚未见国内外文献报导。
青蒿素可制备成各种剂型应用，目前作为外用剂如搽剂、喷雾剂、洗剂等应用。青蒿素外用制剂的组成：青蒿素2-5％、二甲基亚砜20-80％、丙二醇30-60％、乙醇30-70％、食用香精0.05-0.5％，其制备方法：将青蒿素以乙醇溶解，加透皮吸收促进剂二甲基亚砜和丙二醇混合、过滤，再加香精搅匀即得。
本发明从青蒿素寻找到新的作用，为青蒿素“老药新用”提供了新的用途，使青蒿素不仅作为抗疟药应用，还可作为抗真菌药应用，为青蒿素临床应用开拓了新的前景。
实施例：
1、外用剂配方及制备：
①搽剂：青蒿素4g、二甲基亚砜30g、丙二醇30g、乙醇(95％)40g、食用香精0.3％，将青蒿素溶于乙醇中，加二甲基亚砜、丙二醇混匀，再加食用香精搅匀，灌装即得。
②洗剂：青蒿素3g，用70％乙醇配成3％溶液。
2、应用：
①猫体癣：将青蒿素搽剂涂于患部，用药一次，两日后痊愈。
②孙××，手足癣：将青蒿素搽剂涂于患部每日一次，应用三天后均痊愈。
③吴××，头皮屑：青蒿素洗剂适量与洗发剂配合使用，3次后头屑消除。
1、一种抗疟药青蒿素作为抗真菌剂的应用，其特征在于青蒿素具有良好的抗真菌作用，可以作为抗真菌药用于真菌感染性疾病的治疗，还可用于头皮屑的防治。
2、据权利要求1所述的青蒿素的应用，其特征在于青蒿素尤其适用于浅部真菌感染性疾病-癣病的治疗。
3、据权利要求1所述的青蒿素的应用，其特征在于青蒿素可以制成各种剂型应用，如搽剂、喷雾剂、洗剂等外用剂用于癣病。
Application of arteannuin as antifungal agent
The artabsin used as antimalarial originally can be used as antifungal medicine, which is externally applied for treating superficial fungus infections such as hand and foot tinea, favus of scalp, body ringworm and dandruff with curative effect similar to or higher than ketoconazole.
Arteannuin is as the application of antifungal
The present invention relates to of the application of a kind of existing antimalarial arteannuin, for the treatment by Chinese herbs fungal infectious disease provides a kind of new medicine as antifungal agent.
The effective monomer component that Herba Artemisiae Annuae prime system China extracts from the Chinese medicine Herba Artemisiae annuae (sesquiterpene lactones peroxide) has good malaria effect.Be new antimalarial by world health organisation recommendations, at present clinical be used for the treatment of malaria (the Zhu Xinying chief editor: pharmacology's third edition, Beijing: the People's Health Publisher, 1993:370).Fungal infection especially mycotic infection of superficial part-tinea is a kind of commonly encountered diseases, present medicine is commonly used clotrimazole, miconazole, ketoconazole, fluconazol etc., all be the synthetic product, untoward reaction is bigger, main toxicity has (Jiang Mingxing chief editor: pharmacology's third edition such as anemia, erythra and gastrointestinal reaction, Beijing: People's Health Publisher, 1989: 348).Existing reported in literature is the treatment that the Herba Artemisiae Annuae oil liniment is applied to tinea, add the water distillation with bright Herba Artemisiae Annuae and obtain Herba Artemisiae Annuae oil, its Main Ingredients and Appearance is by olein, artemisia ketone, left-handed Camphora, absinthol, Flos Caryophylli alkene and other sesquiterpene derivative (Chen Deyu etc.: experiment of Herba Artemisiae Annuae oil liniment antifungic action and observation of curative effect, China's dermatological magazine, 1990; 4 (1): 18-19).
The objective of the invention is to utilize China's Chinese herbal medicine resource developing new drug, research " old medicine is newly used " is sought effect and the application that makes new advances from existing antimalarial arteannuin.
The present invention confirms that the antimicrobial spectrum of arteannuin and effect are similar to broad-spectrum antifungal medicine ketoconazole commonly used at present, and the effect of some fungus is better than ketoconazole by the external antifungic action research to arteannuin.Results of pharmacodynamic test shows that arteannuin has good antifungic action, the fungi bacterial strain is all presented suppress or killing action, and is wherein the strongest to achorion gypseum, microsporon gypseum effect; Secondly all strong or approximate to Trichophyton violaceum, trichophyton, purple shape epidermophyton, aspergillosis effect than ketoconazole; The Candida albicans bacteriostasis (is seen Appendix: the vitro antibacterial activity of arteannuin preparation) near ketoconazole a little less than ketoconazole, bactericidal action.Clinical practice proof arteannuin can be used as antifungal agent and is used for the treatment of fungal infectious disease.Be used for the treatment of superficial part ringworm such as tinea manus and pedis, tinea corporis, tinea capitis at present as external preparation, also can be used for preventing and treating the dandruff, effect is all good.Arteannuin treatment tinea curative effect is better than ketoconazole, and its untoward reaction is little, does not see the specific toxicity reaction.
Though arteannuin of the present invention and prior art Herba Artemisiae Annuae oil can both be used for the treatment of tinea, but two medicine active ingredient differences, arteannuin is the effective monomer component sesquiterpene lactones peroxide that extracts from Herba Artemisiae Annuae, and composition is more in the Herba Artemisiae Annuae oil, and wherein less important composition sesquiterpene derivative does not refer in particular to any derivant; Secondly arteannuin also can be used for treating the dandruff.The arteannuin preparation is convenient, can directly utilize existing medicinal arteannuin to be prepared into various preparations for use, and Herba Artemisiae Annuae oil must be with being mixed with liniment behind the Herba Artemisiae Annuae distillation extraction again.Arteannuin of the present invention is used as antifungal, has not yet to see the domestic and foreign literature report.
Arteannuin can be prepared into various dosage forms and use, at present as application such as external agent such as liniment, spray, lotions.The composition of arteannuin external preparation: arteannuin 2-5%, dimethyl sulfoxide 20-80%, propylene glycol 30-60%, ethanol 30-70%, edible essence 0.05-0.5%, its preparation method: with arteannuin with dissolve with ethanol, add Percutaneous absorption enhancer dimethyl sulfoxide and mixed with propylene glycol, filtration, add essence again and stir evenly promptly.
The present invention searches out new effect from arteannuin, for arteannuin " old medicine is newly used " provides new purposes, arteannuin is not only used as antimalarial, also can be used as antifungal agent and uses, for new prospect has been opened up in the arteannuin clinical practice.
Embodiment:
1, external agent prescription and preparation:
1. liniment: arteannuin 4g, dimethyl sulfoxide 30g, propylene glycol 30g, ethanol (95%) 40g, edible essence 0.3%, arteannuin is dissolved in the ethanol, add dimethyl sulfoxide, propylene glycol mixing, add edible essence again and stir evenly, fill is promptly.
2. lotion: arteannuin 3g is made into 3% solution with 70% ethanol.
2, use:
1. cat tinea corporis: the arteannuin liniment is applied to affected part, medication once, recovery from illness after two days.
2. grandson * *, tinea manus and pedis: the arteannuin liniment is applied to affected part once a day, uses after three days all recoveries from illness.
3. Wu * *, the dandruff: the arteannuin lotion is an amount of to be used with shampoo, the bits elimination of 3 postocciput.
1, a kind of antimalarial arteannuin is characterized in that as the application of antifungal arteannuin has good antifungic action, can be used as the treatment that antifungal agent is used for fungal infectious disease, also can be used for the control of the dandruff.
2,, it is characterized in that arteannuin is particularly useful for the treatment of mycotic infection of superficial part disease-tinea according to the application of the described arteannuin of claim 1.
3, according to the application of the described arteannuin of claim 1, it is characterized in that arteannuin can make various dosage forms and use, be used for tinea as external agent such as liniment, spray, lotions.
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