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磷酸替米考星在猪体内的药代动力学研究 被引量:7

Pharmacokinetics of tilmicosin phosphate in swine
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摘要 为了探讨磷酸替米考星在猪体内的药物代谢动力学(药代动力学)特征,本试验给受试猪口服以及静脉注射不同剂量的10%磷酸替米考星可溶性粉,利用HPLC方法分析不同时间点受试猪血浆中替米考星的药物浓度。试验结果显示,10%磷酸替米考星可溶性粉经静脉注射和口服后,药物在猪体内吸收、分布很快,消除较慢,消除半衰期远远大于分布半衰期,符合二室开放模型,这种药代动力学特征与替米考星在猪体内经静脉注射和口服后相似,并且磷酸替米考星与替米考星一样,其在猪体内组织穿透力强,组织分布广泛。磷酸替米考星可溶性粉(9.6 mg·kg-1)口服后血药浓度-时间曲线下面积(AUC)为(5.249 8±1.177 8)μg·h·mL-1,磷酸替米考星可溶性粉(5.0 mg·kg-1)静脉注射后的AUC为(3.065 6±1.3426)μg·h·mL-1,磷酸替米考星绝对生物利用度(F)为89.19%,说明磷酸替米考星可溶性粉口服后的生物利用度较高。 To investigate the pharmacokinetic characteristics of tilmicosin phosphate in swine, HPLC method is used to detect tilmicosin concentrations in the tested swine plasma after giving tilmicosin phosphate by oral administration and intravenous injection. The results show that after the swines take 10% tilmicosin phosphate soluble powder orally or by intravenous injection, drug is absorbed and distributed quickly, but it is eliminated slowly. The elimination half-life is far greater than the distribution half-life. The drug conforms to the two-compartment model. The pharmacokinetic characteristics of tilmicosin phosphate in swines are similar to those of tilmicosin. The same with tilmicosin, tilmicosin phosphate has strong penetrating power and is distributed widely in swines. After taking phosphate tilmicosin soluble powder orally ( 9.6 mg· kg^-1 ), the area under the concentration-time curve ( A UC) is ( 5. 259 8 ±1. 177 8 ) μg·h·mL^-1. After the injection of phosphate tilmicosin soluble powder(5.0mg. kg-1 ) , the AUC is ( 3. 065 6± 1. 342 6 ) μg·h·mL^-1. The absolute bioavailability degree(F) of tilmicosin phosphate is 89.19%. After the oral administration of tilmicosin phosphate soluble powder, the bioavailability is higher.
出处 《南京农业大学学报》 CAS CSCD 北大核心 2013年第5期120-124,共5页 Journal of Nanjing Agricultural University
基金 江苏高校优势学科建设工程资助项目(PAPD) 2012年大学生实践创新计划 江苏省高校自然科学基金项目(11KJD230001)
关键词 磷酸替米考星 药代动力学 tilmicosin phosphate pharmaeokinetics swine
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