CN100382694C - 氟吗啉水分散片剂 - Google Patents
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- FPAFDBFIGPHWGO-UHFFFAOYSA-N dioxosilane;oxomagnesium;hydrate Chemical group O.[Mg]=O.[Mg]=O.[Mg]=O.O=[Si]=O.O=[Si]=O.O=[Si]=O.O=[Si]=O FPAFDBFIGPHWGO-UHFFFAOYSA-N 0.000 claims description 5
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- YDEXUEFDPVHGHE-GGMCWBHBSA-L disodium;(2r)-3-(2-hydroxy-3-methoxyphenyl)-2-[2-methoxy-4-(3-sulfonatopropyl)phenoxy]propane-1-sulfonate Chemical group [Na+].[Na+].COC1=CC=CC(C[C@H](CS([O-])(=O)=O)OC=2C(=CC(CCCS([O-])(=O)=O)=CC=2)OC)=C1O YDEXUEFDPVHGHE-GGMCWBHBSA-L 0.000 claims description 5
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- GUBGYTABKSRVRQ-QKKXKWKRSA-N lactose group Chemical group OC1[C@H](O)[C@@H](O)[C@H](O[C@H]2[C@H](O)[C@@H](O)[C@@H](O)[C@H](O2)CO)[C@H](O1)CO GUBGYTABKSRVRQ-QKKXKWKRSA-N 0.000 description 2
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- LWEAHXKXKDCSIE-UHFFFAOYSA-M 2,3-di(propan-2-yl)naphthalene-1-sulfonate Chemical compound C1=CC=C2C(S([O-])(=O)=O)=C(C(C)C)C(C(C)C)=CC2=C1 LWEAHXKXKDCSIE-UHFFFAOYSA-M 0.000 description 1
- 229920002134 Carboxymethyl cellulose Polymers 0.000 description 1
- LFQSCWFLJHTTHZ-UHFFFAOYSA-N Ethanol Chemical compound CCO LFQSCWFLJHTTHZ-UHFFFAOYSA-N 0.000 description 1
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- GQPLMRYTRLFLPF-UHFFFAOYSA-N Nitrous Oxide Chemical compound [O-][N+]#N GQPLMRYTRLFLPF-UHFFFAOYSA-N 0.000 description 1
- RCEAADKTGXTDOA-UHFFFAOYSA-N OS(O)(=O)=O.CCCCCCCCCCCC[Na] Chemical compound OS(O)(=O)=O.CCCCCCCCCCCC[Na] RCEAADKTGXTDOA-UHFFFAOYSA-N 0.000 description 1
- 241001223281 Peronospora Species 0.000 description 1
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- KWYUFKZDYYNOTN-UHFFFAOYSA-M Potassium hydroxide Chemical compound [OH-].[K+] KWYUFKZDYYNOTN-UHFFFAOYSA-M 0.000 description 1
- 241001281805 Pseudoperonospora cubensis Species 0.000 description 1
- 229920002472 Starch Polymers 0.000 description 1
- CZMRCDWAGMRECN-UGDNZRGBSA-N Sucrose Chemical compound O[C@H]1[C@H](O)[C@@H](CO)O[C@@]1(CO)O[C@@H]1[C@H](O)[C@@H](O)[C@H](O)[C@@H](CO)O1 CZMRCDWAGMRECN-UGDNZRGBSA-N 0.000 description 1
- 229930006000 Sucrose Natural products 0.000 description 1
- DPXJVFZANSGRMM-UHFFFAOYSA-N acetic acid;2,3,4,5,6-pentahydroxyhexanal;sodium Chemical compound [Na].CC(O)=O.OCC(O)C(O)C(O)C(O)C=O DPXJVFZANSGRMM-UHFFFAOYSA-N 0.000 description 1
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- 235000015320 potassium carbonate Nutrition 0.000 description 1
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Abstract
本发明提出了一种氟吗啉水分散片剂，含有氟吗啉原药及崩解剂、粘结剂、泡腾剂、润湿剂、分散剂、填充剂。各组分经混合、粉碎，采用全粉末直接压片法压片。与传统剂型相比较，该水分散片剂药效好，使用、运输安全、方便，利于贮存和容器配置，对环境污染小。
Description
技术领域
本发明属于农药加工领域，涉及农用杀菌剂氟吗啉(flumorph)的新剂型及其加工与应用。
背景技术
氟吗啉(flumorph)(化学名称：4-[3-(4-氟本基)-3-(3，4-二甲氧基苯基)丙烯酰]吗啉)作为农用杀菌剂广泛应用于多种作物病害的防治，尤其对霜霉属、疫霉属病菌有特效。中国专利CN1167568A中公开了该化合物及其制剂的杀菌活性与制备方法。随着氟吗啉推广应用的进一步扩大，发现目前所应用的剂型存在许多不足之处。例如：可湿粉使用时用量不好掌握，尤其在小剂量应用时使用者不易准确称量；乳油中含有大量有机溶剂例如二甲苯，对环境污染严重；同时两种剂型储存、运输均不方便。
发明内容
为了克服现有剂型存在的用量不好掌握，储存、运输不便且易造成环境污染的缺点，本发明提出了一种氟吗啉片剂新剂型。
本发明的氟吗啉片剂以氟吗啉原粉为活性组分。片剂中各组分的重量百分含量如下：氟吗啉0.1-50％，泡腾剂4-20％，粘结剂3-10％，崩解剂0.5-30％，润湿剂0.5-20％，分散剂0.5-30％，填充剂0.5-20％。
配方中所述的泡腾剂为两种，一种选自碳酸钠、碳酸氢钠或碳酸钾；另一种选自柠檬酸或枸橼酸；优选碳酸钠和柠檬酸。所述的粘结剂选自工业淀粉、羧甲基纤维素、甲基纤维素或聚乙烯吡咯烷酮，优选聚乙烯吡咯烷酮。所述的崩解剂选自微晶纤维素、交联羧甲基纤维素钠、羧甲基纤维素钠、交联聚乙烯比咯烷酮或羟丙基纤维素，优选微晶纤维素。所述的润湿剂选自月桂醇基硫酸钠、十二烷基苯磺酸钠或十二烷基硫酸钠，优选十二烷基苯磺酸钠。所述的分散剂选自木质素磺酸钠、NNO或二丁基萘磺酸钠，优选木质素磺酸钠或NNO。所述的填充剂选自乳糖、硫酸钙、蔗糖、滑石粉、硅胶、硬脂酸镁或轻质碳酸钙，优选滑石粉、硅胶、硬脂酸镁或轻质碳酸钙。
本发明所述的片剂剂型中较优选的为水分散片剂。上述配方中选用的崩解剂可以加快片剂在水中的崩解速度，其中尤以微晶纤维素效果最佳。加入两种以上分散剂可以改善该片剂在水中的分散效果，例如可以等比例加入木质素磺酸钠与NNO。
按照上述配方，将物料充分混合，经超微粉碎使之达到325目，采用全粉末干粉直接压片法加工工艺直接压片。按照此方法，可以制备本发明各种含量的氟吗啉水分散片剂。本发明所制备的水分散片剂重40毫克，直径5毫米，根据应用需要也可以制备其他不同规格的片剂。
与湿法压片工艺相比较，由于省略了制粒、烘干工序，本加工工艺可以缩短生产周期并节约能源，提高生产效率。该工艺亦适用于其他热敏感药物的剂型加工，可防止热敏感药物分解所至的含量下降，减少有效成分的损失。与湿法压片工艺相比，此工艺还可以进一步改善片剂崩解时间。
本发明的氟吗啉水分散片剂还具有使用计量准确方便、运输安全，利于贮存和容器配置，携带方便，对环境污染小等优点。施用效果与现有剂型相当。例如氟吗啉水分散片剂在相同的处理剂量下对黄瓜苗期霜霉病的防效接近或略优于氟吗啉可湿粉制剂对黄瓜霜霉病的防治效果。
最佳实施方式
以下实例用以进一步说明本发明，但并非限制本发明。
配方实例：
按照以下配方中所示的各种物料充分混合，经超微粉碎使之达到325目后直接压片，即得到片重40毫克、直径5毫米的氟吗啉水分散片剂。
实施例1 35％氟吗啉水分散片剂
氟吗啉原药 35克
微晶纤维素 14克
聚乙烯吡咯烷酮 4克
碳酸钠 6克
柠檬酸 6克
NNO 5克
木质素磺酸钠 5克
十二烷基苯磺酸钠 1克
硬脂酸镁 2克
滑石粉 2克
轻质碳酸钙 补足至100克
实施例2 30％氟吗啉水分散片剂
氟吗啉原药 30克
微晶纤维素 11克
聚乙烯吡咯烷酮 2克
碳酸钠 6克
柠檬酸 6克
NNO 5克
十二烷基苯磺酸钠 1克
硬脂酸镁 1克
硅胶 2克
轻质碳酸钙 补足至100克
实施例3 20％氟吗啉水分散片剂
氟吗啉原药 20克
微晶纤维素 16克
聚乙烯吡咯烷酮 4克
碳酸钠 6克
柠檬酸 6克
NNO 5克
十二烷基苯磺酸钠 1克
硬脂酸镁 1克
硅胶 2克
滑石粉 1克
轻质碳酸钙 补足至100克
水分散性试验
实施例4
水分散片剂的分散性试验采用以下方法：室温下，向顶端可以密封的容器中加入大约800毫升自来水。加入本发明的水分散片剂2片并密封容器顶端，可以观察到水分散片剂分散。对于实施例1、2、3的氟吗啉水分散片剂，落至容器底部并开始分散，可以观察到其完全分散不超过3分钟。
药效试验
实施例5 黄瓜霜霉病防治效果
采用温室幼苗盆栽法测定氟吗啉水分散片剂对黄瓜霜霉病的防治效果，并与氟吗啉可湿粉剂进行对比。黄瓜品种：山东密刺，病原菌：黄瓜苗期霜霉病病菌(Pseudoperonospora cubensis)。温室盆栽黄瓜幼苗长至三叶期时，按设计剂量在作物喷雾机上进行叶面喷雾处理，24小时后接种病原菌。接种后保湿培养7天后进行结果调查。本发明各种含量的氟吗啉水分散片剂均具有良好的防效并且未发现对黄瓜生长有任何不良影响。
30％氟吗啉水分散片剂的防治效果见下表：
Claims (2)
1.氟吗啉水分散片剂，各组分的重量百分含量如下：
氟吗啉0.1-50％，泡腾剂4-20％，粘结剂3-10％，崩解剂0.5-30％，润湿剂0.5-20％，分散剂0.5-30％，填充剂0.5-20％；
所述的泡腾剂选自碳酸钠和柠檬酸；粘结剂选自聚乙烯吡咯烷酮；填充剂选自滑石粉、硅胶、硬脂酸镁或轻质碳酸钙；崩解剂选自微晶纤维素；润湿剂选自十二烷基苯磺酸钠；分散剂选自木质素磺酸钠或NNO。
2.权利要求1所述氟吗啉水分散片剂的制备方法：各组分经混合、粉碎后，采用全粉末直接压片法压片。
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| CN101999348B (zh) * | 2010-10-26 | 2013-01-02 | 江苏七洲绿色化工股份有限公司 | 一种农药泡腾片剂的制备方法 |
| CN103385249B (zh) * | 2012-05-09 | 2014-07-23 | 中国中化股份有限公司 | 氟吗啉与咪鲜胺的杀真菌组合物 |
| CN103540161A (zh) * | 2012-07-09 | 2014-01-29 | 沈阳新纪化学有限公司 | 荧光增白剂351水溶性片剂及其制备和应用 |
| CN106942247A (zh) * | 2017-04-21 | 2017-07-14 | 扬州大学 | 甲氨基阿维菌素苯甲酸盐泡腾片剂及其制备方法 |
| CN113545344B (zh) * | 2021-07-23 | 2022-08-09 | 安徽省通源环境节能股份有限公司 | 一种沉水植物促生缓释片及其制备方法 |
Citations (1)
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| CN1226134A (zh) * | 1996-06-21 | 1999-08-18 | 泽尼卡有限公司 | 农药片剂 |
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2004
- 2004-07-16 CN CNB2004100209761A patent/CN100382694C/zh not_active Expired - Lifetime
Patent Citations (1)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN1226134A (zh) * | 1996-06-21 | 1999-08-18 | 泽尼卡有限公司 | 农药片剂 |
Non-Patent Citations (1)
| Title |
|---|
| 农药新剂型-水分散片剂. 王勇，孔宪滨，张文革，张宗俭.农药，第43卷第6期. 2004 * |
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| CN1720798A (zh) | 2006-01-18 |
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