泰地罗新单次口灌给药与连续饮水给药后在猪体内的药动学比较研究
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摘要
为了探究泰地罗新在猪体内瞬时和连续给药条件下药物动力学的差异,本试验通过给猪瞬时给药(单次口服)和连续给药(饮水添加给药)来探究药动学参数的差异;试验结果表明泰地罗新单次给药后在猪血浆中的消除较慢,给药240h后仍可在血浆中检测到,连续饮水添加给药刚开始符合有吸收一室模型,与单次给药一致。泰地罗新在猪体内吸收快,消除半衰期长,瞬时给药可长时间维持较高的血药浓度,而小剂量连续(饮水添加)给药,也可在短时间内达到稳态浓度;所以说泰地罗新在临床使用过程中瞬时给药和连续给药均能达到治疗疾病的目的。
The difference of Pharmacokinetics of Tidipirosin in pig after oral administration between instantaneous and continuous input would be discussed; The pharmacokinetic parameters of tildipirosin in pigs were studied comparatively in this experiment following by given instantaneous( single oral) and continuous( Drinking water added to medicine). These results revealed that the elimination of tidiloxine in pig plasma was slow after single administration,and it can still be detected in plasma after 240 h of administration.The continuous drinking water addition was initially consistent with the absorptive one-chamber model,which was consistent with single administration. Tidipirosin was absorbed quickly and eliminated slowly in pigs,so the instantaneous input can maintain a high blood concentration for a long time,However,a small dose of continuous( drinking water added) can also achieve steady state concentration in a short period of time. Therefore,Tidipirosin can achieve the aim of treating diseases with instantaneous and continuous administration in clinic use.
The difference of Pharmacokinetics of Tidipirosin in pig after oral administration between instantaneous and continuous input would be discussed; The pharmacokinetic parameters of tildipirosin in pigs were studied comparatively in this experiment following by given instantaneous( single oral) and continuous( Drinking water added to medicine). These results revealed that the elimination of tidiloxine in pig plasma was slow after single administration,and it can still be detected in plasma after 240 h of administration.The continuous drinking water addition was initially consistent with the absorptive one-chamber model,which was consistent with single administration. Tidipirosin was absorbed quickly and eliminated slowly in pigs,so the instantaneous input can maintain a high blood concentration for a long time,However,a small dose of continuous( drinking water added) can also achieve steady state concentration in a short period of time. Therefore,Tidipirosin can achieve the aim of treating diseases with instantaneous and continuous administration in clinic use.
引文
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[11]Wang,J.,Zhao,T.,Sun,X.,Liu,Y.,Zhu,J.,Zhang,S.,&Cao,X. Pharmacokinetics of tildipirosin inbeagle dogs[J]. Journal of veterinary pharmacology andtherapeutics,2018,41(1).
[12]Menge,M.,Rose,M.,Bohland,C.,Zschiesche,E.,Kilp,S.,Metz,W.,&Nürnberger,M. Pharmacokineticsof tildipirosin in bovine plasma,lung tissue,and bronchialfluid(from live,nonanesthetized cattle)[J]. Journal ofveterinary pharmacology and therapeutics,2012,35(6),550-559
[13]关红,李成应,刘明强,毛伟,&赵俊利.头孢噻呋酸晶体注射液对乳腺组织的刺激性及代谢规律的研究[J].内蒙古农业大学学报:自然科学版,2013,(2),21-25.
[2]Novotny,G. W.,Jakobsen,L.,Andersen,N. M.,Poe-hlsgaard,J.,&Douthwaite,S. Inhibition by Tildipirosin.Ketolide antimicrobial activity persists after disruption of in-teractions with domain II of 23S rRNA[J]. Antimicrob. A-gents Chemother,2004,48,3677-3683.
[3]Andersen,N. M.,Poehlsgaard,J.,Warrass,R.,&Douthwaite,S. Inhibition of protein synthesis on the ribo-some by tildipirosin compared with other veterinary macroli-des[J]. Antimicrobial agents and chemotherapy,2012,56(11),6033-6036.
[4]Poehlsgaard,J.,Andersen,N. M.,Warrass,R.,&Douthwaite,S. Visualizing the 16-membered ring macroli-des tildipirosin and tilmicosin bound to their ribosomal site.ACS chemical biology,2012,7(8),1351-1355.
[5]操继跃,刘雅红.兽医药理学与治疗学(第九版)[M].2012,中国农业出版社.
[6]Torres,F.,Santamaria,R.,Jimenez,M.,Menjon,R.,Ibanez,A.,Collell,M.,...&Fraile,L. Pharmacokinet-ics of tildipirosin in pig tonsils[J]. Journal of veterinarypharmacology and therapeutics,2016,39(2),199-201.
[7]Amrine,D. E.,White,B. J.,Larson,R. L.,&Mosier,D. A. Pulmonary lesions and clinical disease response tochallenge 10 days following administration of tildipirosin ortulathromycin[J]. Journal of animal science,2014,92(1),311-319.
[8]操继跃,卢笑丛.兽医药物动力学[M]. 2005,中国农业出版社.
[9]廖远军.(2015)泰地罗新注射液在猪体内的药代动力学研究[D].吉林大学.
[10]李伟岭,杨芳,于振梅,岳永波.泰地罗新研究进展[J].中国兽药杂志,2012,46(10),50-53.
[11]Wang,J.,Zhao,T.,Sun,X.,Liu,Y.,Zhu,J.,Zhang,S.,&Cao,X. Pharmacokinetics of tildipirosin inbeagle dogs[J]. Journal of veterinary pharmacology andtherapeutics,2018,41(1).
[12]Menge,M.,Rose,M.,Bohland,C.,Zschiesche,E.,Kilp,S.,Metz,W.,&Nürnberger,M. Pharmacokineticsof tildipirosin in bovine plasma,lung tissue,and bronchialfluid(from live,nonanesthetized cattle)[J]. Journal ofveterinary pharmacology and therapeutics,2012,35(6),550-559
[13]关红,李成应,刘明强,毛伟,&赵俊利.头孢噻呋酸晶体注射液对乳腺组织的刺激性及代谢规律的研究[J].内蒙古农业大学学报:自然科学版,2013,(2),21-25.