Turtle Chinemys reevesiis with body weight(BW) of 0.745 kg(♀) and 0.361 kg(♂) were forced to take praziquantel by intragastric perfusion at a dose of 30 mg/kg BW(group Ⅰand groupⅡ), respectively, the male turtle was administrated by intragastric perfusion at a dose 15 mg/kg(group Ⅲ) and the female turtle was administrated three times, 0.05, 3.05, and 6.05 h after blood sampling, by intragastric perfusion at a dose of 10 mg/kg (group Ⅳ, a total of 30 mg/kg) to provide scientific guidance for the safe and effective use of praziquantel in the clinical deworming of turtles. The blood was sampled from the dorsal jugular sinus in the turtle in the groups Ⅰ,Ⅱ, Ⅲ and Ⅳ 0, 0.5, 1, 3, 6, 12, 24, 48, 72, and 96 h after administration, and then the concentration of praziquantel in the plasma of the turtle was determined by liquid chromatography-mass spectrometry(LC-MS) to investigate the pharmacokinetics of praziquantel in different gender turtles by various doses and times of intragastric administration by Kinetic 4.4 software. The results showed that the drug-time data of praziquantel in the turtle conformed to the one-compartment open model, with bimodal effect: the first peak at 0.5 h in groups Ⅰ, Ⅱ, and Ⅳ or 3 h in group Ⅲ; the second peak at 12 h in groups I and Ⅳ and 72 h in groups Ⅱ and Ⅲ. The main pharmacokinetic parameters in the four groups were described as follows: Tmax=15.949 h, Cmax=0.615 μg/mL, AUC=26.664 μg/(mL) in group Ⅰ(dose 30 mg/kg, single, female); Tmax=74.857 h, Cmax=0.592 μg/mL, AUC=123.427 μg/(mL·h) in group Ⅱ (dose 30 mg/kg, single, male) ; Tmax=75.523 h, Cmax=0.234 μg/mL, AUC=48.760 μg/(mL·h) in group Ⅲ (dose 15 mg/kg, single, male) ; and Tmax=14.161 h, Cmax=0.303 μg/mL, AUC=15.726 μg/(mL·h) in group Ⅳ (dose 10 mg/kg, 3 times, female). Intragastric administration revealed that the turtle had slower and less absorption of praziquantel, with relatively wide distribution. There were less absorption rate and elimination rate in the male than those in the females, with significantly different absorption and metabolism levels between male and female turtles(P<0.05). The strong adverse reactions were observed in the turtles in the single-dose group (dose 15 mg/kg and 30 mg/kg). The necropsy revealed that different lesions or necrosis were found in liver, kidney, muscle and other tissues and organs to some extent, with mild adverse reactions in only one(192 h) in the multiple-dose group(dose 10 mg/kg, 3 times). It is recommended that the single intragastric dose of praziquantel used for clinical deworming of turtles is 10 mg/kg or less. If it is necessary to increase the dose, it can be administered multiple times, within three times, and at intervals of more than 3 h.
Abstract: Turtle Chinemys reevesiis with body weight(BW) of 0.745 kg(♀) and 0.361 kg(♂) were forced to take praziquantel by intragastric perfusion at a dose of 30 mg/kg BW(group Ⅰand groupⅡ), respectively, the male turtle was administrated by intragastric perfusion at a dose 15 mg/kg(group Ⅲ) and the female turtle was administrated three times, 0.05, 3.05, and 6.05 h after blood sampling, by intragastric perfusion at a dose of 10 mg/kg (group Ⅳ, a total of 30 mg/kg) to provide scientific guidance for the safe and effective use of praziquantel in the clinical deworming of turtles. The blood was sampled from the dorsal jugular sinus in the turtle in the groups Ⅰ,Ⅱ, Ⅲ and Ⅳ 0, 0.5, 1, 3, 6, 12, 24, 48, 72, and 96 h after administration, and then the concentration of praziquantel in the plasma of the turtle was determined by liquid chromatography-mass spectrometry(LC-MS) to investigate the pharmacokinetics of praziquantel in different gender turtles by various doses and times of intragastric administration by Kinetic 4.4 software. The results showed that the drug-time data of praziquantel in the turtle conformed to the one-compartment open model, with bimodal effect: the first peak at 0.5 h in groups Ⅰ, Ⅱ, and Ⅳ or 3 h in group Ⅲ; the second peak at 12 h in groups I and Ⅳ and 72 h in groups Ⅱ and Ⅲ. The main pharmacokinetic parameters in the four groups were described as follows: Tmax=15.949 h, Cmax=0.615 μg/mL, AUC=26.664 μg/(mL) in group Ⅰ(dose 30 mg/kg, single, female); Tmax=74.857 h, Cmax=0.592 μg/mL, AUC=123.427 μg/(mL·h) in group Ⅱ (dose 30 mg/kg, single, male) ; Tmax=75.523 h, Cmax=0.234 μg/mL, AUC=48.760 μg/(mL·h) in group Ⅲ (dose 15 mg/kg, single, male) ; and Tmax=14.161 h, Cmax=0.303 μg/mL, AUC=15.726 μg/(mL·h) in group Ⅳ (dose 10 mg/kg, 3 times, female). Intragastric administration revealed that the turtle had slower and less absorption of praziquantel, with relatively wide distribution. There were less absorption rate and elimination rate in the male than those in the females, with significantly different absorption and metabolism levels between male and female turtles(P<0.05). The strong adverse reactions were observed in the turtles in the single-dose group (dose 15 mg/kg and 30 mg/kg). The necropsy revealed that different lesions or necrosis were found in liver, kidney, muscle and other tissues and organs to some extent, with mild adverse reactions in only one(192 h) in the multiple-dose group(dose 10 mg/kg, 3 times). It is recommended that the single intragastric dose of praziquantel used for clinical deworming of turtles is 10 mg/kg or less. If it is necessary to increase the dose, it can be administered multiple times, within three times, and at intervals of more than 3 h.
2020, Vol. 35 
