CN101052404B - 杀虫剂组合物 - Google Patents
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Abstract
本发明涉及用于治疗头虱和跳蚤等体表寄生虫的局部组合物。该组合物包括分散在液态载体中的杀虫有效量的水杨酸(典型的为1-10重量%)。该载体可以是包括石蜡油等矿物油、橄榄油或蓖麻油等植物油或者不含硫酸盐的酒精洗发液基料的油性载体。
Description
技术领域
本发明涉及用于治疗头虱和跳蚤寄生的制剂。
背景技术
这类寄生最常见于学龄儿童中。在教室和玩耍区等近距离区域内,这些寄生虫会在每个人之间相互转移。成虱在头发内和耳朵后产卵并孵化,所以,如果不加以治疗,它们会不断繁衍,使其寄生一直延续。头发是寄生虫的理想栖息所。一旦头皮皮脂扩散到头发内,虱卵就特别难以去除。
头虱制剂通常含有杀虫剂。去除头虱卵或者使卵松脱的组合物可能含有与虱卵排出的使其黏附在产卵位置的胶黏剂发生作用的酶。由于患者怀疑这些水性酶组合物会损坏发质,所以它们并不受欢迎。美国专利5,557,665中公开了这些酶。
美国专利3,023,144描述了在人和动物皮肤上施用以控制真菌和细菌感染的组合物。这些组合物的主要成分是柑橘油,其活性成分是a-柠檬油精和p-异丙基甲苯。它们含橄榄油和0.25%-10%(重量百分比)的水杨酸,文中记载加入水杨酸起杀菌作用,柑橘油可以减弱水杨酸产生的蜕皮反应。
美国专利6,524,604描述了一种通过施用由黄原胶、硅调理剂和少量醋酸或柠檬酸等有机酸构成的凝胶来去除人头发中虱卵的组合物。该专利中记载,使用3%水杨酸作pH调节剂。主要成分为异山梨醇二甲醚(DMI)。施用这些组合物可减小使用细齿梳去除人头发中虱卵所需的力度。
发明内容
本发明的组合物方面通常提供一种用于治疗体表寄生虫寄生、包括分散在液态载体中的杀卵有效量的水杨酸的局部组合物。
水杨酸的量可以为1-10%,优选为5-8%。组合物中含重量百分比为5、6、7或8%的水杨酸对杀灭虫卵有效。该组合物可以是任何适于施用在头皮和头发上的物理剂型。洗液、凝胶和乳膏均可。另外该组合物还可以包括乳化剂、防腐剂/稳定剂、表面活性剂、香料和着色剂。载体可以是包括石蜡油等矿物油或者橄榄油或蓖麻油等植物油的油性载体。油能润湿虫卵并能一直与卵保持接触直到清洗时洗脱。
油性组合物和水性组合物在浓度低于4%或5%时效果较弱且杀灭作用较低。组合物中水杨酸浓度高于8%时有杀灭效果,但可能会出现蜕皮。由于虱子治疗对象大多都是儿童,所以最好能避免这种皮肤反应。
洗发基料(shampoo base)可以是酒精皂液。用作该目的的溶液可以包含几乎等量的乙醇或甲醇和软皂。基料是可流动凝胶。
由于软皂洗发液会使皮肤发干,所以可加入少量的植物油(3-8%)。这有助于人头发洗完后的梳理。给动物用的洗液中是否加入油则不太重要。
施用方法如下。将该凝胶头发上,并用手指揉搓。让凝胶在毛发上保留1-2小时。刚开始可以看到虱子在爬动,但10-15分钟后虱子爬动逐渐缓慢,20分钟后所有虱子都不动弹了。
施用2小时后,用水清洗头发将虱卵和死虱洗掉。用毛巾擦干头发,然后完全晾干。7天后重复治疗,以免第一次治疗后可能残留有活的虱卵。
皂液中酒精成分的作用尚不确定。虱子浸没在液体中会产生防御反射,所以在液体中虱子仍能存活,据猜测,当该浸没反射(immersion reflex)期间虱子悬浮呼吸时,水杨酸将其杀死。因此浸没后虱子的吸血被阻止。幼虱在浸没后特别需要尽早进食,据认为它们对洗发液与水杨酸的组合特别敏感。
具体实施方式
洗发液
水杨酸 6g
95%乙醇(alc) 50ml
基料(不含SO4″) 50ml
实施例:不含硫酸盐的洗发液
水杨酸 6g
95%乙醇 50ml
不含硫酸盐的Melrose“每日”的洗发基料 加至100ml
100ml
实施步骤:
将水杨酸溶解到乙醇中,然后加到洗发基料中混合。十二烷基硫酸钠本来是合适的基料,但由于加入水杨酸酒精溶液后会产生沉淀,所以避免使用。
实施例:酒精皂液
水杨酸 6g
蓖麻油(5g) 5ml
乙醇95%(309) 30ml
酒精皂液 加至100ml
100ml
实施步骤:
将95%乙醇与溶解有水杨酸的大部分酒精皂液搅拌混合。溶解时,加入蓖麻油及剩余的皂液。该制剂用作洗狗液。将动物关在洗狗机内。操作人员一边与狗说话,让狗保持安静,一边在狗毛上揉搓该溶液几分钟。然后用喷头喷出的水将溶液冲洗掉。用毛巾将狗擦干,但在周围温度下(21℃)继续维持湿度40分钟。
实施例:蓖麻油/橄榄油制剂
本实施例是一种蓖麻/橄榄油中含水杨酸的油性制剂。
水杨酸 12g
丁基羟基甲苯(0.1%) 0.2g
0.1%的维生素E油 0.2ml
相当于50IU D-1-a-生育酚醋酸酯
橄榄油(3.0%) 60ml
蓖麻油(约70%) 200ml
实施步骤:
将按70∶30混合的蓖麻/橄榄油加热到50℃。把水杨酸、BHT(丁基羟基甲苯)和维生素E油搅拌溶解到蓖麻/橄榄油混合物中。
按以下试验检测治疗液的疗效。
从体虱的成虱、蛹和卵群中,试验人员随机挑选雌性和雄性虱子。将100只健壮的成虱插入注射器内,注射器针头口用纱布塞住。虱子会与纱布保持接触。加入一定量治疗液样品将虱子全部润湿,然后在环境温度下(32℃)放置10分钟。与治疗液接触后,从注射器内把虱子释放出来,保留在纱布上,用水清洗60秒以洗去治疗液。用绵纸轻轻地把水吸干,然后把虱子再次置于浅盘内的一块布的表面上(1个盘内大约50只虱子)。将盘子置于保温箱内,1小时后检查虱子的活力。然后再放回保温箱内,17小时后再次观察,并把它们分成濒临死亡1级或濒临死亡2级。
虱子分类
存活:能爬动,翻身背朝下时,能自己翻回来。
濒临死亡(1级):翻身背朝下时,自己不能翻回来。
濒临死亡(2级):翻身背朝下时,自己不能翻回来。被刺后,只有腿和触须能动弹。
死亡:不能动弹。
% | 0 | 0 | |
濒临死亡_2级 | 5 | 1 | |
% | 10 | 2 | |
死亡 | 40 | 45 | |
% | 80 | 90 | |
复制份3 | 存活 | 9 | 7 |
50只虱子 | % | 18 | 14 |
濒临死亡_1级 | 0 | 0 |
% | 0 | 0 | |
濒临死亡_2级 | 4 | 0 | |
% | 8 | 0 | |
死亡 | 37 | 43 | |
% | 74 | 86 | |
复制份4 | 存活 | 8 | 7 |
50只虱子 | % | 16 | 14 |
濒临死亡_1级 | 0 | 0 | |
% | 0 | 0 | |
濒临死亡_2级 | 4 | 0 | |
% | 8 | 0 | |
死亡 | 38 | 43 | |
% | 76 | 86 | |
总数 | 存活 | 29 | 24 |
200个虱子 | % | 14.5 | 12 |
濒临死亡_1级 | 0 | 1 | |
% | 0 | 0.5 | |
濒临死亡_2级 | 17 | 2 | |
% | 8.5 | 1 | |
死亡 | 154 | 173 |
% | 77 | 86.5 | |
%(死亡+濒临死亡) | 85.5 | 88.5 |
治疗液的杀卵特性检测如下:
将雌性体虱置于舒适环境中产卵24-48小时。然后把雌虱从虱卵和受测虱卵分离出来。仅挑选健康的虱卵进行试验。将那些没有受损伤和挤压的虱卵挑出来放在纱布上。将虱子转移到微盘试验容器内,在环境温度下让治疗液没过虱卵。10分钟后第一批用水清洗60秒,然后用绵纸轻轻吸干。20分钟后第二批进行同样处理。将这两批转到盘中,在32℃烘箱内放置9天。没有孵化的虱卵视为死亡。
这些试验只针对体虱进行,但预计其结果与针对头虱进行的试验结果并无不同。
对人施用
把洗液倒在2岁儿童的被头虱和虱卵中度寄生的干头发上。要用足量的洗液完全盖住头皮和头发。使用量视头发长度而定。油性基料向头发内扩散时,将洗液刷开,头发变得光亮顺滑,按摩头皮5分钟。这个时期可以看到虱子正在尽力逃离治疗区。
让洗液在头皮和头发上停留2-8小时,随后用细齿梳将虱卵梳掉。油性基料将虱卵染黑后,则更容易看到和去除虱卵。用洗发液清洗洗液。每天都检查一下,7-10天后重复处理一次,以杀死第一次处理时未杀死的残留虱卵所孵化出的活虱。每隔7天检查一次头发直到寄生被根除。必要的话,该儿童的所有家庭成员都同时进行检查并治疗。
用酒精皂液重复以上试验。酒精皂液接触10分钟后,虱卵致死率为67%。一般认为该致死率并不理想,但当接触时间达到2-8小时时,致死率则大得多。
另外用不含硫酸盐的洗发液重复以上试验。获得理想的杀虫结果,第11天的记录显示没有虱卵孵化。
能理解,本说明书和权利要求书所用的“包括”一词应按其包容形式解释,即,使用“包括”一词并不排除加入其他成分。
能理解,可以对本发明做出各种变更和/补充而不脱离本发明的基本特性。所以这些变更和/或补充应属于本发明的范围。
Claims (6)
1.一种局部组合物在制备治疗体表寄生虫寄生的药物中的应用,其中该组合物包括分散在油状载体中的、占组合物总重5-8%的水杨酸。
2.根据权利要求1所述的应用,其中的油状载体是植物油。
3.根据权利要求2所述的应用,其中的植物油是蓖麻油。
4.根据权利要求2所述的应用,其中的植物油是橄榄油。
5.根据权利要求1所述的应用,其中的油状载体是矿物油。
6.根据权利要求5所述的应用,其中的矿物油是石蜡油。
Applications Claiming Priority (5)
Application Number | Priority Date | Filing Date | Title |
---|---|---|---|
AU2004905230A AU2004905230A0 (en) | 2004-09-10 | Insecticidal composition | |
AU2004905230 | 2004-09-10 | ||
AU2005901290 | 2005-03-16 | ||
AU2005901290A AU2005901290A0 (en) | 2005-03-16 | Insecticidal compositions | |
PCT/AU2005/001303 WO2006026806A1 (en) | 2004-09-10 | 2005-09-09 | Insecticidal compositions |
Publications (2)
Publication Number | Publication Date |
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CN101052404A CN101052404A (zh) | 2007-10-10 |
CN101052404B true CN101052404B (zh) | 2011-01-05 |
Family
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Application Number | Title | Priority Date | Filing Date |
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CN2005800305507A Expired - Fee Related CN101052404B (zh) | 2004-09-10 | 2005-09-09 | 杀虫剂组合物 |
Country Status (7)
Country | Link |
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US (2) | US20080058291A1 (zh) |
EP (1) | EP1786434A4 (zh) |
JP (1) | JP2008512393A (zh) |
KR (1) | KR20070051321A (zh) |
CN (1) | CN101052404B (zh) |
NZ (1) | NZ553715A (zh) |
WO (1) | WO2006026806A1 (zh) |
Families Citing this family (4)
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ITMC20060039A1 (it) * | 2006-04-11 | 2007-10-12 | Mario Antonello Principato | Formulazione insettcida e acaricida. |
ES2350075B1 (es) * | 2009-05-11 | 2011-11-10 | Maria Pilar Mateo Herrero | Composicion microencapsulada a base de olea europaea saponificada, suuso y su procedimiento de obtencion. |
CN103536611B (zh) * | 2013-10-15 | 2015-08-12 | 黄学松 | 一种寄生虫用杀虫剂 |
US10328112B2 (en) | 2017-11-29 | 2019-06-25 | Michael S. Hatten | Abrasive pediculicide compositions comprising materials, kits, and methods of use |
Citations (2)
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GB2341091A (en) * | 1998-11-11 | 2000-03-08 | Ore An Ltd | Essential oil composition for treatment of head-lice |
US6524604B1 (en) * | 2000-07-21 | 2003-02-25 | Del Laboratories, Inc. | Method, composition and kit to remove lice ova from the hair |
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US3023144A (en) | 1959-08-17 | 1962-02-27 | Mar Tay Inc | Biocidal compositions for topical application |
US4551480A (en) * | 1983-06-21 | 1985-11-05 | Stiefel Laboratories, Inc. | Compositions for the treatment of psoriasis |
JP2634858B2 (ja) | 1988-06-03 | 1997-07-30 | 東洋エアゾール工業株式会社 | 速破性発泡エアゾール組成物 |
JPH0715523A (ja) | 1993-06-23 | 1995-01-17 | Toshiba Corp | 電話装置 |
FR2761912B1 (fr) * | 1997-04-14 | 1999-07-02 | Capsulis | Procede destine a faire adherer un produit sur une surface |
US20010005721A1 (en) * | 1998-04-23 | 2001-06-28 | Fereidoon Pourbastani | Heel crack healing composition and method therefor |
US6455058B1 (en) * | 2000-09-13 | 2002-09-24 | Amitee Cosmetics, Inc. | Composition and method for hair and scalp treatment |
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2005
- 2005-09-09 US US11/575,053 patent/US20080058291A1/en not_active Abandoned
- 2005-09-09 CN CN2005800305507A patent/CN101052404B/zh not_active Expired - Fee Related
- 2005-09-09 WO PCT/AU2005/001303 patent/WO2006026806A1/en active Application Filing
- 2005-09-09 NZ NZ553715A patent/NZ553715A/en not_active IP Right Cessation
- 2005-09-09 EP EP05776052A patent/EP1786434A4/en not_active Withdrawn
- 2005-09-09 KR KR1020077005622A patent/KR20070051321A/ko not_active Application Discontinuation
- 2005-09-09 JP JP2007530538A patent/JP2008512393A/ja active Pending
-
2010
- 2010-07-19 US US12/839,299 patent/US20100286097A1/en not_active Abandoned
Patent Citations (2)
Publication number | Priority date | Publication date | Assignee | Title |
---|---|---|---|---|
GB2341091A (en) * | 1998-11-11 | 2000-03-08 | Ore An Ltd | Essential oil composition for treatment of head-lice |
US6524604B1 (en) * | 2000-07-21 | 2003-02-25 | Del Laboratories, Inc. | Method, composition and kit to remove lice ova from the hair |
Also Published As
Publication number | Publication date |
---|---|
CN101052404A (zh) | 2007-10-10 |
NZ553715A (en) | 2009-10-30 |
EP1786434A4 (en) | 2008-11-19 |
WO2006026806A1 (en) | 2006-03-16 |
KR20070051321A (ko) | 2007-05-17 |
EP1786434A1 (en) | 2007-05-23 |
JP2008512393A (ja) | 2008-04-24 |
US20100286097A1 (en) | 2010-11-11 |
US20080058291A1 (en) | 2008-03-06 |
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