CN108651488A - 一种阿维菌素乳油制剂 - Google Patents
一种阿维菌素乳油制剂 Download PDFInfo
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- CN108651488A CN108651488A CN201810520004.0A CN201810520004A CN108651488A CN 108651488 A CN108651488 A CN 108651488A CN 201810520004 A CN201810520004 A CN 201810520004A CN 108651488 A CN108651488 A CN 108651488A
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Classifications
-
- A—HUMAN NECESSITIES
- A01—AGRICULTURE; FORESTRY; ANIMAL HUSBANDRY; HUNTING; TRAPPING; FISHING
- A01N—PRESERVATION OF BODIES OF HUMANS OR ANIMALS OR PLANTS OR PARTS THEREOF; BIOCIDES, e.g. AS DISINFECTANTS, AS PESTICIDES OR AS HERBICIDES; PEST REPELLANTS OR ATTRACTANTS; PLANT GROWTH REGULATORS
- A01N43/00—Biocides, pest repellants or attractants, or plant growth regulators containing heterocyclic compounds
- A01N43/90—Biocides, pest repellants or attractants, or plant growth regulators containing heterocyclic compounds having two or more relevant hetero rings, condensed among themselves or with a common carbocyclic ring system
-
- A—HUMAN NECESSITIES
- A01—AGRICULTURE; FORESTRY; ANIMAL HUSBANDRY; HUNTING; TRAPPING; FISHING
- A01N—PRESERVATION OF BODIES OF HUMANS OR ANIMALS OR PLANTS OR PARTS THEREOF; BIOCIDES, e.g. AS DISINFECTANTS, AS PESTICIDES OR AS HERBICIDES; PEST REPELLANTS OR ATTRACTANTS; PLANT GROWTH REGULATORS
- A01N25/00—Biocides, pest repellants or attractants, or plant growth regulators, characterised by their forms, or by their non-active ingredients or by their methods of application, e.g. seed treatment or sequential application; Substances for reducing the noxious effect of the active ingredients to organisms other than pests
- A01N25/02—Biocides, pest repellants or attractants, or plant growth regulators, characterised by their forms, or by their non-active ingredients or by their methods of application, e.g. seed treatment or sequential application; Substances for reducing the noxious effect of the active ingredients to organisms other than pests containing liquids as carriers, diluents or solvents
- A01N25/04—Dispersions, emulsions, suspoemulsions, suspension concentrates or gels
Landscapes
- Life Sciences & Earth Sciences (AREA)
- General Health & Medical Sciences (AREA)
- Health & Medical Sciences (AREA)
- Pest Control & Pesticides (AREA)
- Agronomy & Crop Science (AREA)
- Plant Pathology (AREA)
- Engineering & Computer Science (AREA)
- Dentistry (AREA)
- Wood Science & Technology (AREA)
- Zoology (AREA)
- Environmental Sciences (AREA)
- Dispersion Chemistry (AREA)
- Chemical & Material Sciences (AREA)
- Toxicology (AREA)
- Agricultural Chemicals And Associated Chemicals (AREA)
Abstract
本发明涉及一种阿维菌素乳油制剂,该制剂按重量百分比计:阿维菌素原药含量为4~6%;乳化剂选用茶皂素水溶液、农乳601和农乳501,其比例1︰2︰7,含量8~12%;乳油稳定剂选用N‑甲基吡咯烷酮,含量为1~3%;阿维菌素抗光解剂选择茶多酚棕榈酸酯、可可多酚酯、松树皮原花青素、葡萄籽花青素、单宁酸,或它们的脂肪酸酯中的一种或多种,含量0.5~5%;助溶剂为异丁醇,含量为12~15%;大豆油和松根油比例5~7︰3~5,含量59~74.5%。采用本发明,制备方法简单,使用普通制备乳油设备,其中抗光解剂为天然成分,无毒无害且对人体有益,与普通乳油相比,减少了甲苯类有机溶剂使用,对环境友好,能有效降低阿维菌素光降解作用,提高药物的利用率。
Description
技术领域
本发明涉及一种阿维菌素乳油制剂,属于农药制剂及其加工技术的领域。
背景技术
阿维菌素(Avermectins)是一种高选择性和高安全性的新型抗生素类生物农药,以其新颖的化学结构、独特的作用机制、超高的药效、杀虫活性极强、杀虫谱广、防治效果好、持效期长、用量极少等一系列特点,广泛地应用于人类医学、畜牧业、农业等方面。
茶皂素(Tea Saponin)又名茶皂甙,是存在于山茶科植物中的一类齐墩果烷型三萜类皂苷混合物。茶皂素因其分子中含有亲水性的糖体部分和疏水性的皂甙配基部分而成为性能优良的天然非离子型表面活性剂。农业上,有研究表明油茶皂素有抗菌防虫的效果。
茶多酚(Tea Polyphenols)是茶叶中所含的一类多羟基类化合物,易溶于水,具有较强的抗氧化作用,且抗氧化性能随温度的升高而增强。除抗氧化作用外还具有抑菌作用,如对葡萄球菌、大肠杆菌、枯草杆菌等有抑制作用。茶多酚棕榈酸酯(Tea Polyphenol-palmitate)是茶多酚与棕榈酸酯化得到的油溶性产物,有较强的抗氧化性,且与其他抗氧化剂,如特丁基对苯二酚(TBHQ)、2,6-二叔丁基-4-甲基苯酚(BHT)等物质有协同作用。
可可多酚酯由可可多酚与脂肪酸酯化得到,具有良好的脂溶性和抗氧化特性。
松树皮原花青素(Oligomeric Proantho Cyanidins,OPC)由法国海岸松树皮 提取得到,是一种有着特殊分子结构的生物类黄酮,同时是一种有效的天然抗氧化剂,溶于水和大多数有机溶剂。
葡萄籽花青素(Anthocyanin),由葡萄籽提取得到,属于一种水溶性的生物类黄酮物质,研究证明花青素是一种有效的抗氧化剂,也是最强效的自由基清除剂。
单宁酸(Tannic acid)又称鞣酸,一种多酚化合物,存在于柿子、茶叶、咖啡、石榴等植物组织中,溶于水及乙醇,极不溶于乙醚、氯仿或苯。单宁酸的一种酯化产物,硬脂酰单宁酸酯,油溶性好,且具有一定的抗氧化作用。
松根油是从植物中提取的一种化合物,其中含有酚类、酸类、掂烯类、醇类,醛类以及树脂酸等多种化学物质,研究证明它具有抗细菌及抗真菌作用。
目前,市场上存在一种阿维菌素微囊剂,所需要的制备设备复杂,防光降解效果不佳,影响了药物的利用率,同时普通乳油的制备过程需要加入甲苯类有机溶剂,对环境起到一定的副作用。
发明内容
本发明的目的是针对上述之不足,提供可防光降解的一种阿维菌素乳油制剂及其制备方法。
本发明采取的技术方案是:一种阿维菌素乳油制剂,其特征在于各组分按照重量百分比计为:阿维菌素原药含量为4~6%;乳化剂选用15%的茶皂素水溶液,农乳601和农乳501,三者比例为1︰2︰7,含量为8~12%;乳油稳定剂选用N-甲基吡咯烷酮,含量为1~3%;阿维菌素抗光解剂选择95%茶多酚棕榈酸酯、95%可可多酚酯、95%松树皮原花青素、95%葡萄籽花青素、95%单宁酸,或它们的脂肪酸酯中的一种或多种,含量为0.5~5%;助溶剂为异丁醇,含量为12~15%;剩余组分为大豆油和松根油,大豆油和松根油的比例为5~7︰3~5,含量为59~74.5%。
所述的一种阿维菌素乳油制剂,其特征在于其制备方法如下:(1)称取适量茶皂素和蒸馏水,制备浓度为15%的茶皂素水溶液;(2)取15%的茶皂素水溶液按照1︰2︰7的比例混合农乳501和农乳601,作为乳化剂;(3)取占重量百分比为4~6%的阿维菌素原药加热溶解于异丁醇中溶解,异丁醇占重量百分比为12~15%,温度为75~85℃;(4)将大豆油和松根油按5~7︰3~5比例混合,在混合的占重量百分比为59~74.5%的油相中搅拌加入上述溶有阿维菌素的异丁醇和占重量百分比为0.5~5%的阿维菌素抗光解剂;(5)在转速为2500~3500r/min的机械剪切力作用下把占重量百分比为8~12%的乳化剂和1~3%的N-甲基吡咯烷酮加入上述含有阿维菌素和抗光解剂的油相中,滴毕继续搅拌10~20min,然后静置、过滤即可得到阿维菌素乳油制剂。
所述的一种阿维菌素乳油制剂,其特征在于其中的大豆油和松根油的比例优选7︰3。
采用本发明,与其它抗光解阿维菌素微囊剂相比,制备方法简单,使用普通制备乳油设备即可。本发明中使用的抗光解剂为天然成分,无毒无害且对人体有益。同时与普通乳油相比,减少了甲苯类有机溶剂的使用,对环境友好,并能有效降低阿维菌素光降解作用,提高药物的利用率。
附图说明
图1为实施例二至七变动部分组份及测试结果。
图2为实施例八至十中采用的部分组份。
图3为实施例八、九、十中的阿维菌素光降解率。
图4为实施例八和九对红蜘蛛的药效实验结果。
图5为实施例八的详细配方。
图6为实施例八的质量指标测试结果。
具体实施方式
下面结合具体的实施例对本发明作进一步说明,但以下内容不应在任何程度上被解释为对发明请求保护范围的限制。
一、实施例一。
、该阿维菌素乳油制剂按各组分按照重量百分比计为:阿维菌素原药含量为4~6%;乳化剂选用15%的茶皂素水溶液,农乳601和农乳501,三者比例为1︰2︰7,含量为8~12%;乳油稳定剂选用N-甲基吡咯烷酮,含量为1~3%;阿维菌素抗光解剂选择95%茶多酚棕榈酸酯、95%可可多酚酯、95%松树皮原花青素、95%葡萄籽花青素、95%单宁酸,或它们的脂肪酸酯中的一种或多种,含量为0.5~5%;助溶剂为异丁醇,含量为12~15%;剩余组分为大豆油和松根油,大豆油和松根油的比例为5~7︰3~5,含量为59~74.5%。
、制备方法:称取15克茶皂素,加蒸馏水85克,充分溶解,制成15%的茶皂素水溶液;在上述茶皂素溶液中取出8克,与16克农乳601和56克农乳501组成乳化剂备用;将50克纯度为95%的阿维菌素溶解于150克异丁醇中,溶解时施予适当加热搅拌,并将温度控制在75~85℃内;待药物全部溶解后将异丁醇倒入装有418.5克大豆油和136.5克松根油的2000ml烧杯中;在转速为3000r/min电动搅拌机下,缓缓加入5克95%茶多酚棕榈酸酯、10克N-甲基吡咯烷酮和乳化剂,待全部加入完毕后继续搅拌15min,静置,过滤。
二、实验例二至七及测试。
1、参照实施例一的组份及制备方法制取阿维菌素乳油制剂,按图1所示改变油相、乳化剂和抗光解剂,而其余组份不变进行制备,测定乳油稀释稳定性和抗光解性能。
2、图1中油相为大豆油和松根油,乳化剂组成为茶皂素︰农乳601︰农乳501 = 1︰2︰7;实施例二和五中抗光解剂为茶多酚棕榈酸酯,实施例三和六中抗光解剂为可可多酚酯,实施例四和七中抗光解剂为花青素脂肪酸酯。
3、试验结果:稀释后乳液外观以无颜色变化,无浮油无沉淀为合格。
三、实验例八至十及测试。
1、参照实施例一的组份及制备方法制取阿维菌素乳油制剂,按图2所示改变油相、乳化剂和抗光解剂组分,其中的乳化剂①按茶皂素︰农乳601︰农乳501 = 1︰2︰7配比,其中的乳化剂②按农乳601︰农乳501 = 3︰7配比,而其余组份不变进行制备,比较本发明中的配方与普通配方对阿维菌素光降解率和杀虫性能的影响。
2、实施例八、九、十中阿维菌素含量由HPLC法测定(色谱柱:Waters Symmetry®C18 3.9×150mm;检测波长:254nm;流速:1.0ml·min-1;流动相:甲醇:水 = 85:15)。在32h内、254nm紫外光照射下的光降解率如图3。
3、实施例八、九对红蜘蛛的药效实验结果如图4所示。
四、结论。
从实验结果可以看出,本发明的抗光解阿维菌素乳油制备简单,质量合格,较同类产品不仅能降低其光降解率,同时其组分还能与阿维菌素产生协同作用,提高杀虫效果。
以上所述,仅为本发明的较佳实施例,并非对本发明做任何形式上的限制,凡是依据本发明的技术实质对以上实施例所做的任何简单修改、等同变化,均落入本发明的保护范围之内。
Claims (3)
1.一种阿维菌素乳油制剂,其特征在于各组分按照重量百分比计为:阿维菌素原药含量为4~6%;乳化剂选用15%的茶皂素水溶液,农乳601和农乳501,三者比例为1︰2︰7,含量为8~12%;乳油稳定剂选用N-甲基吡咯烷酮,含量为1~3%;阿维菌素抗光解剂选择95%茶多酚棕榈酸酯、95%可可多酚酯、95%松树皮原花青素、95%葡萄籽花青素、95%单宁酸,或它们的脂肪酸酯中的一种或多种,含量为0.5~5%;助溶剂为异丁醇,含量为12~15%;剩余组分为大豆油和松根油,大豆油和松根油的比例为5~7︰3~5,含量为59~74.5%。
2.根据权利要求1所述的一种阿维菌素乳油制剂,其特征在于其制备方法如下:(1)称取适量茶皂素和蒸馏水,制备浓度为15%的茶皂素水溶液;(2)取15%的茶皂素水溶液按照1︰2︰7的比例混合农乳501和农乳601,作为乳化剂;(3)取占重量百分比为4~6%的阿维菌素原药加热溶解于异丁醇中溶解,异丁醇占重量百分比为12~15%,温度为75~85℃;(4)将大豆油和松根油按5~7︰3~5比例混合,在混合的占重量百分比为59~74.5%的油相中搅拌加入上述溶有阿维菌素的异丁醇和占重量百分比为0.5~5%的阿维菌素抗光解剂;(5)在转速为2500~3500r/min的机械剪切力作用下把占重量百分比为8~12%的乳化剂和1~3%的N-甲基吡咯烷酮加入上述含有阿维菌素和抗光解剂的油相中,滴毕继续搅拌10~20min,然后静置、过滤即可得到阿维菌素乳油制剂。
3.根据权利要求1或2所述的一种阿维菌素乳油制剂,其特征在于其中的大豆油和松根油的比例优选7︰3。
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Cited By (4)
Publication number | Priority date | Publication date | Assignee | Title |
---|---|---|---|---|
CN110432267A (zh) * | 2019-08-22 | 2019-11-12 | 西南大学 | 一种防治叶螨的助剂 |
CN111802399A (zh) * | 2020-08-13 | 2020-10-23 | 河南波尔森农业科技有限公司 | 一种阿维菌素组合物及其制备方法、应用 |
CN114652619A (zh) * | 2022-05-09 | 2022-06-24 | 中国科学院烟台海岸带研究所 | 一种活性油溶花青素及其制备方法和应用 |
CN114766476A (zh) * | 2022-04-18 | 2022-07-22 | 安徽农业大学 | 延长丙溴磷水溶液持效期的方法 |
Citations (4)
Publication number | Priority date | Publication date | Assignee | Title |
---|---|---|---|---|
JP2001302410A (ja) * | 2000-04-27 | 2001-10-31 | Dai Ichi Kogyo Seiyaku Co Ltd | 展着剤、及び該展着剤が配合された駆虫剤 |
CN102204548A (zh) * | 2011-04-26 | 2011-10-05 | 张福志 | 一种高效环保型阿维菌素乳油及制备方法 |
CN103234930A (zh) * | 2013-03-29 | 2013-08-07 | 江汉大学 | 一种测定茶多酚棕榈酸酯含量的方法 |
CN103621498A (zh) * | 2012-08-23 | 2014-03-12 | 上海农乐生物制品股份有限公司 | 一种植物源溶剂制备甲维盐乳油及其制备方法 |
-
2018
- 2018-05-28 CN CN201810520004.0A patent/CN108651488A/zh active Pending
Patent Citations (4)
Publication number | Priority date | Publication date | Assignee | Title |
---|---|---|---|---|
JP2001302410A (ja) * | 2000-04-27 | 2001-10-31 | Dai Ichi Kogyo Seiyaku Co Ltd | 展着剤、及び該展着剤が配合された駆虫剤 |
CN102204548A (zh) * | 2011-04-26 | 2011-10-05 | 张福志 | 一种高效环保型阿维菌素乳油及制备方法 |
CN103621498A (zh) * | 2012-08-23 | 2014-03-12 | 上海农乐生物制品股份有限公司 | 一种植物源溶剂制备甲维盐乳油及其制备方法 |
CN103234930A (zh) * | 2013-03-29 | 2013-08-07 | 江汉大学 | 一种测定茶多酚棕榈酸酯含量的方法 |
Cited By (5)
Publication number | Priority date | Publication date | Assignee | Title |
---|---|---|---|---|
CN110432267A (zh) * | 2019-08-22 | 2019-11-12 | 西南大学 | 一种防治叶螨的助剂 |
CN111802399A (zh) * | 2020-08-13 | 2020-10-23 | 河南波尔森农业科技有限公司 | 一种阿维菌素组合物及其制备方法、应用 |
CN114766476A (zh) * | 2022-04-18 | 2022-07-22 | 安徽农业大学 | 延长丙溴磷水溶液持效期的方法 |
CN114652619A (zh) * | 2022-05-09 | 2022-06-24 | 中国科学院烟台海岸带研究所 | 一种活性油溶花青素及其制备方法和应用 |
CN114652619B (zh) * | 2022-05-09 | 2023-12-12 | 中国科学院烟台海岸带研究所 | 一种活性油溶花青素及其制备方法和应用 |
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