驱杀牛皮蝇蛆的新药剂—倍硫磷点涂剂的研究
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摘要
为根除我国牛皮蝇蛆病，试验了一种经皮肤给药透皮吸收的新药剂—点涂剂。本实验选择倍硫磷作为杀虫药物，应用了丙二醇、氮酮、乙酸乙酯和乙酰乙酸乙酯等几种高效安全的透皮促进剂与其合理配比，将5种配方在牛体上进行了透皮吸收实验。对10头牛在背部皮肤涂药后，通过4、8、12、16、24小时采血，用气相色谱仪测定血中药物浓度。依据药物的血药浓度的峰值及维持时间的长短，确立了10％倍硫磷点涂剂为较优配方。用2头牛对该配方进行了药物代谢情况研究，表明该组药物血药浓度在16小时达到峰值，约为10.813ng／ml，血药浓度维持在5ng／ml以上的时间超过24小时。用10％倍硫磷点涂剂对30头牛进行临床防治试验，表明该浓度的倍硫磷点涂剂对牛皮蝇第一、二期幼虫杀灭率为100％，可使牛皮蝇蛆的感染率由30％降至0，防治中无1例牛发生中毒。以3倍剂量对3头牛作毒性试验，未见中毒反应。在牛皮蝇防治中，该药剂与倍硫磷注射剂相比，杀虫率提高10％，使用中具有操作简便、安全范围大的优点，与倍硫磷浇泼剂相比，降低了成本、使用更简便。
To eradicate bovine hypodermosis disease Fenthion spot-on as a new medicine absorbed percutaneously was tested and exploited. Fenthion as primary medicine and high efficient cutaneous penetration enhancers which include 1,2-propylene glycol, Azone, Ethyl acetate and Ethyl acetoacetate C.P. were rationally compounded to get 5 Fenthion spot-on. After Fenthion spot-on was daubed on the back of 10 cattle, blood samples were collected and handled on different time. Fenthion density of the blood samples were measured with Gas chromatograph and compared each other. The medicine density and continuous time of 10% Fenthion spot-on in the blood samples were higher other groups, so it was selected as the best medicine group. By the research of medicine metabolism to 10% Fenthion spot-on with 2 cattle it was indicated that the highest medicine density in the blood is 10.813ng/ml on 16 hour and continuous time in which its density in the blood exceed 5ng/ml is more than 24 hours. The clinical test achieved 100% efficacy
to kill bovine hypodermosis larvae with 10%.fenthion spot-on. The infection ratio of bovine hypodermosis declined from 30% to 0. Moreover, there was no one poisoned cattle. There was no one poisoned cattle when 10% Fenthion spot-on was tested with 3 times dosage. The efficacy of 10% Fenthion spot-on exceed 10% than the of Fenthion injection. Compared with Fenthion pour-on 10% Fenthion spot-on have advantages of lower cost and more convenient use.
To eradicate bovine hypodermosis disease Fenthion spot-on as a new medicine absorbed percutaneously was tested and exploited. Fenthion as primary medicine and high efficient cutaneous penetration enhancers which include 1,2-propylene glycol, Azone, Ethyl acetate and Ethyl acetoacetate C.P. were rationally compounded to get 5 Fenthion spot-on. After Fenthion spot-on was daubed on the back of 10 cattle, blood samples were collected and handled on different time. Fenthion density of the blood samples were measured with Gas chromatograph and compared each other. The medicine density and continuous time of 10% Fenthion spot-on in the blood samples were higher other groups, so it was selected as the best medicine group. By the research of medicine metabolism to 10% Fenthion spot-on with 2 cattle it was indicated that the highest medicine density in the blood is 10.813ng/ml on 16 hour and continuous time in which its density in the blood exceed 5ng/ml is more than 24 hours. The clinical test achieved 100% efficacy
to kill bovine hypodermosis larvae with 10%.fenthion spot-on. The infection ratio of bovine hypodermosis declined from 30% to 0. Moreover, there was no one poisoned cattle. There was no one poisoned cattle when 10% Fenthion spot-on was tested with 3 times dosage. The efficacy of 10% Fenthion spot-on exceed 10% than the of Fenthion injection. Compared with Fenthion pour-on 10% Fenthion spot-on have advantages of lower cost and more convenient use.
引文
1． 申允中．三蝇防治专题文献资料汇编(三)．锡盟科学技术情报研究所．内蒙古自治区兽医工作站，1982．39-55
2． 李晋．三蝇防治专题文献资料汇编(四)．锡盟科学技术情报研究所，内蒙古自治区兽医工作站，1990．1-28
3. B.A.Khan. Warble control in Alberta. Alberta Agriculture, 1991(12):420-423
4. N.Araujo Chaveron,J.L.Charbon. Improvements in the Control methods for warble-fly in Cattle and Goats. Belgium: European Commission, 1994.121-125
5. Tarry. D.W. Improvements in the Control methods for warble-fly in Catde and Goats. Belgium: European Commission, 1998.14-26
6. Tarry. D.W. Improvements in the Control methods for warble-fly in Cattle and Goats. Belgium: European Commission, 1994.3-5
7. D.J.Brien. Improvements in the Control methods for warble-fly in Cattle and Goats.. Belgium: European Commission, 1994.11-15
8. A.Liebisch,G.liebisch. Improvements in the Control methods for warble-fly in Catde and Goats. Belgium: European Commission, 1994.17-19
9. G.Argente. Improvements in the Control methods for warble-fly in Cattle and Goats. Belgium: European Commission, 1994.29-31
10. J.Sol,O.Csarnpimon. Improvements in the Control methods for warble-fly in Carrie and Goats. Belgium: European Commission, 1994.45-46
11. J.Minar. Improvements in the Control methods for warble-fly in Cattle and Goats. Belgium: European Commission, 1994.47-49
12． 周家驷．三蝇防治专题文献资料汇编(四)．锡盟科学技术情报研究所．内蒙古自治区兽医工作站，1990．98-100
13. K.A.Webster. Improvements in the Control methods for warble-fly in Cattle and Goats. Belgium: European Commission, 1994.105-106
14. N.Moire. Improvements in the Control methods for warble-fly in Cattle and Goats. Belgium: European Commission, 1994.109-110
15． 羽贺正．三蝇防治专题文献资料汇编(四)．锡盟科学技术情报研究所．内蒙古自治区兽医工作站，1990．114-115
16． 孔繁瑶．家畜寄生虫学．北京：农业出版社，1981，341-344
17． 呼和巴特尔．倍硫磷浇泼剂治疗牛皮蝇蛆病的疗效．中国兽药杂志，1995，29(4)：45-46
18. Losson. B. Improvements in the Control methods for warble-fly in Cattle and Goats. Belgium: European Commission, 1998.62-66
19. C.Bauer. Improvements in the Control methods for warble-fly in Cattle and Goats. Belgium: European Commission, 1994.145-147
20. Waltess.R.A. Pharmaceutical Skin Penetration Enhancement.New York: Marcel Dekker. Inc, 1993.20-25
21．梁文权．药物分子体积和油水分配系数与经皮吸收的关系．药学学报，1992，27(9)：684-689
22．陈国神．透皮控释系统研究进展．国外药学—合成药、生化药、制剂分册，1988，9(2)：99-100
23．周金泰．兽医透皮治疗体系的中西结合研究．中兽医学杂志，1993，(1)：34-36
24. Pfister. W.R. Penetration Enhances in Pescutaneaus Absorption. Pharm Tech.Japan, 1990,14(9): 132
25．Chien．Y．W．透皮控释药剂的进展．王大林．国外药学—合成药、生化药、制剂分册，1985，6(1)：40-45
26．周瑞仪．透皮促进剂Azone的合成和应用研究．国外药学—合成药、生化药、制剂分册，1988，9(6)：353-354
27．陈国神．月桂氮卓酮对雌二醇皮肤渗透的促进作用及机理．中国药学杂志，1994，29(8)：467-469
28．矢田．登．透皮吸收促进剂的最新研究动向．伊协和．国外药学—合成药、生化药、制剂分册， 1991，12(3)：165-167
29．齐瑗晶．布洛芬软膏渗透促进剂的选择及体外透皮释放率的测定．中国药学杂志，1992，27(6)：346-347
30．曹瑞敏．丙硫咪唑透皮剂对小鼠蛲虫的驱虫效果．中国兽药科技，1995，25(10)：11-12
31．梁文权．美国透皮吸收研究进展．国外药学—合成药、生化药、制剂分册，1990，11(2)： 98-103
32．温玉麟．药物与化学物质毒性数据．天津：科学技术出版社，1989．195，366
33. Khan. M.A. Control of Cattle Grubs with Fention pour-on and Trichlorphon spot-on in Germany. Veterrinary Parasitology, 1977,3(3):245-249
34．张世铨．三蝇防治专题文献资料汇编(四)．锡盟科学技术情报研究所．内蒙古自治区兽医工作站，1990．60-63
35．C．O．Knowles，B．W．Arthur．同位素标记倍硫磷在奶牛体内的代谢以及外用和肌注后的残留． 朱鑫元．美国经济昆虫学杂志，1966，59(6)：50-54
2． 李晋．三蝇防治专题文献资料汇编(四)．锡盟科学技术情报研究所，内蒙古自治区兽医工作站，1990．1-28
3. B.A.Khan. Warble control in Alberta. Alberta Agriculture, 1991(12):420-423
4. N.Araujo Chaveron,J.L.Charbon. Improvements in the Control methods for warble-fly in Cattle and Goats. Belgium: European Commission, 1994.121-125
5. Tarry. D.W. Improvements in the Control methods for warble-fly in Catde and Goats. Belgium: European Commission, 1998.14-26
6. Tarry. D.W. Improvements in the Control methods for warble-fly in Cattle and Goats. Belgium: European Commission, 1994.3-5
7. D.J.Brien. Improvements in the Control methods for warble-fly in Cattle and Goats.. Belgium: European Commission, 1994.11-15
8. A.Liebisch,G.liebisch. Improvements in the Control methods for warble-fly in Catde and Goats. Belgium: European Commission, 1994.17-19
9. G.Argente. Improvements in the Control methods for warble-fly in Cattle and Goats. Belgium: European Commission, 1994.29-31
10. J.Sol,O.Csarnpimon. Improvements in the Control methods for warble-fly in Carrie and Goats. Belgium: European Commission, 1994.45-46
11. J.Minar. Improvements in the Control methods for warble-fly in Cattle and Goats. Belgium: European Commission, 1994.47-49
12． 周家驷．三蝇防治专题文献资料汇编(四)．锡盟科学技术情报研究所．内蒙古自治区兽医工作站，1990．98-100
13. K.A.Webster. Improvements in the Control methods for warble-fly in Cattle and Goats. Belgium: European Commission, 1994.105-106
14. N.Moire. Improvements in the Control methods for warble-fly in Cattle and Goats. Belgium: European Commission, 1994.109-110
15． 羽贺正．三蝇防治专题文献资料汇编(四)．锡盟科学技术情报研究所．内蒙古自治区兽医工作站，1990．114-115
16． 孔繁瑶．家畜寄生虫学．北京：农业出版社，1981，341-344
17． 呼和巴特尔．倍硫磷浇泼剂治疗牛皮蝇蛆病的疗效．中国兽药杂志，1995，29(4)：45-46
18. Losson. B. Improvements in the Control methods for warble-fly in Cattle and Goats. Belgium: European Commission, 1998.62-66
19. C.Bauer. Improvements in the Control methods for warble-fly in Cattle and Goats. Belgium: European Commission, 1994.145-147
20. Waltess.R.A. Pharmaceutical Skin Penetration Enhancement.New York: Marcel Dekker. Inc, 1993.20-25
21．梁文权．药物分子体积和油水分配系数与经皮吸收的关系．药学学报，1992，27(9)：684-689
22．陈国神．透皮控释系统研究进展．国外药学—合成药、生化药、制剂分册，1988，9(2)：99-100
23．周金泰．兽医透皮治疗体系的中西结合研究．中兽医学杂志，1993，(1)：34-36
24. Pfister. W.R. Penetration Enhances in Pescutaneaus Absorption. Pharm Tech.Japan, 1990,14(9): 132
25．Chien．Y．W．透皮控释药剂的进展．王大林．国外药学—合成药、生化药、制剂分册，1985，6(1)：40-45
26．周瑞仪．透皮促进剂Azone的合成和应用研究．国外药学—合成药、生化药、制剂分册，1988，9(6)：353-354
27．陈国神．月桂氮卓酮对雌二醇皮肤渗透的促进作用及机理．中国药学杂志，1994，29(8)：467-469
28．矢田．登．透皮吸收促进剂的最新研究动向．伊协和．国外药学—合成药、生化药、制剂分册， 1991，12(3)：165-167
29．齐瑗晶．布洛芬软膏渗透促进剂的选择及体外透皮释放率的测定．中国药学杂志，1992，27(6)：346-347
30．曹瑞敏．丙硫咪唑透皮剂对小鼠蛲虫的驱虫效果．中国兽药科技，1995，25(10)：11-12
31．梁文权．美国透皮吸收研究进展．国外药学—合成药、生化药、制剂分册，1990，11(2)： 98-103
32．温玉麟．药物与化学物质毒性数据．天津：科学技术出版社，1989．195，366
33. Khan. M.A. Control of Cattle Grubs with Fention pour-on and Trichlorphon spot-on in Germany. Veterrinary Parasitology, 1977,3(3):245-249
34．张世铨．三蝇防治专题文献资料汇编(四)．锡盟科学技术情报研究所．内蒙古自治区兽医工作站，1990．60-63
35．C．O．Knowles，B．W．Arthur．同位素标记倍硫磷在奶牛体内的代谢以及外用和肌注后的残留． 朱鑫元．美国经济昆虫学杂志，1966，59(6)：50-54