盐酸林可霉素-硫酸大观霉素混悬注射液在猪体内的药动学研究

摘要

8头健康猪按体质量单次深部肌内注射盐酸林可霉素-硫酸大观霉素(5 mg·kg-1林可霉素,10 mg·kg-1大观霉素)混悬注射液后,用高效液相色谱法分别测定林可霉素和大观霉素的血药浓度,使用非房室统计矩分析方法处理得到血药浓度-时间数据.林可霉素主要药动学参数分别为:κe=(0.21 ±0.01)h-1；t1/2β=(3.38 ±0.09)h;tmax=(0.29 ±0.02)h;Cmax=(5.15 ±0.18)μg·mL-1;AUCo-LOQ=(10.27±0.38)μg·mL-1·h;MRT=(3.52±0.11)h;ClB/F=(0.46 ±0.01)L·h-1·kg-1；Vz/F=(2.26 ±0.12)L·kg-1.大观霉素主要药动学参数分别为:κe=(0.43 ±0.01)h-1；t1/2β=(1.64±0.06)h;tmax=(0.44 ±0.03)h;Cmax=(20.05±0.70)μg· mL-1;AUCo-LOQ=(51.82±0.98)μg· mL-1· h;MRT=(2.39 +0.04)h;Cl8/F=(0.19 ±0.01)L·h-1· kg-1;Vz/F=(0.46±0.02)L·kg-1.结果表明,肌内注射盐酸林可霉素-硫酸大观霉素混悬注射液后,两药均迅速吸收并快速消除,但后者吸收稍慢,消除较快.%The lincomycin hydrochloride and spectinomycin sulfate suspension was injected into the neck muscle in 8 healthy pigs(5 mg · Kg-1 lincomycin, 10 mg · Kg-1spectinomycin). The concentrations of lincomycin and spectinomycin in plasma were determined by HPLC with UV detection, respectively. The plasma concentration-time data were fit to a non-compartmental analysis based on statistical moment theory. The main pharmacokinetic parameters of lincomycin were as follows: ke = (0. 21 ±0.01) h -1 ;t1/2β = (3. 38 ± 0-09) h;tmax= (0.29 ±0.02) h; Cmax = (5.15 ± 0. 18)+- μg · Ml-1; AUCo.~LOQ = (10. 27 ± 0. 38) μg · Ml-1 · H;MRT = (3.52±0. 11) h;ClB/F =(0.46 ±0.01) L · H-1 · Kg-1 ;VZ/F =(2.26±0. 12) L · Kg-1, whereas, those of spectinomycin were; ke = (0.43 ±0.01) h-1 ;t1/2β = (1.64 ±0.06) h;tmax = (0.44 ±0.03) h:Cmax = (20.05 ±0.70) μg · Ml-1 AUCo~LOQ, = (51. 82 ±0. 98) μg · Ml-1 · H;MRT = (2. 39 ±0.04) h;ClB/F =(0. 19 ±0.01) L · H-1 · Kg-1;Vz/F =(0.46±0.02) L · Kg-1. It was noted that both lincomycin hydrochloride and spectinomycin sulfate were rapidly absorbed and eliminated, however, the latter was more slowly absorbed but more rapidly eliminated after the intramuscular administration of lincomycin hydrochloride and spectinomycin sulfate suspension in pigs.