口服和静脉注射伊维菌素在Biłgorajska鹅体内的药动学。

IF 1.1 4区 农林科学 Q3 VETERINARY SCIENCES New Zealand veterinary journal Pub Date : 2022-11-01 Epub Date: 2022-08-16 DOI:10.1080/00480169.2022.2104398
I Sartini, B Łebkowska-Wieruszewska, M Krupa, A Lisowski, A Poapolathep, M Giorgi
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引用次数: 0

摘要

目的:评价伊维菌素在Biłgorajska鹅(国内鹅)单次给药或口服给药后的药动学特征,以比较这两种给药途径并评估口服生物利用度。方法:选取10只健康雄性鹅进行单剂量、两期研究,两期之间有3个月的洗脱期。在第一期试验中,所有鹅均给予0.2 mg/kg I/V的伊维菌素,在第二期试验中给予相同剂量的伊维菌素口服。在每次给药后480小时的选定时间点采集血样。用蛋白沉淀法纯化样品,用高效液相色谱法测定药物浓度。该方法在空白鹅血浆中得到验证,线性最佳,定量限为0.025 μg/mL。采用非区室方法进行药代动力学分析。结果:经I/V给药后240小时可定量,经口服给药后144小时可定量。伊维菌素的消除半衰期约为3.8 (95% CI = 1.98-7.92;p = 0.027)是口服I/V给药后的两倍。此外,从零到最后可检测时间点的曲线下面积为6.4 (95% CI = 4.65-8.74;结论:鹅口服伊维菌素的生物利用度约为20%。需要进一步研究伊维菌素在胃肠道中的作用,同时评估组织残留,以便计算停药时间,以确保消费者安全。AUC:浓度-时间曲线下面积;AUClast:从零到最后一个可检测时间点的曲线下面积;AUMC:第一弯矩曲线下面积;Cmax:最大浓度;Tmax:达到最大血浆浓度的时间。
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Pharmacokinetics of ivermectin after oral and intravenous administration in Biłgorajska geese (Anser anser domesticus).

Aims: To assess the pharmacokinetic profile of ivermectin in Biłgorajska geese (Anser anser domesticus) after single I/V or oral administration, in order to compare these routes of administration and assess oral bioavailability.

Methods: Ten healthy male geese were used in a single-dose, two-phase study with a 3-month washout period between phases. In the first phase, all geese were given 0.2 mg/kg I/V ivermectin, while in the second phase they were treated orally with the same dosage. Blood samples were collected at selected time points up to 480 hours after each administration. Samples were purified using protein precipitation and drug concentration was quantified using HPLC. The analytical method was validated on blank goose plasma and was characterised by an optimal linearity and a limit of quantification of 0.025 μg/mL. The pharmacokinetic analysis was carried out using a non-compartmental approach.

Results: The drug was quantifiable up to 240 hours after I/V administration, while after oral treatment it was quantifiable up to 144 hours in most of the geese. The elimination half-life of ivermectin was approximately 3.8 (95% CI = 1.98-7.92; p = 0.027) times higher after I/V administration compared to oral administration. Moreover, the area under the curve from zero to the last detectable timepoint was 6.4 (95% CI = 4.65-8.74; p < 0.001) hours greater after I/V than oral administration. This difference led to a bioavailability of 20.38 (SD 5.92) %.

Conclusions: Following oral administration in geese, ivermectin has a bioavailability of approximately 20%. Further research on the action of ivermectin in the gastrointestinal tract is required along with assessment of tissue residues to allow calculation of withdrawal time to ensure consumer safety.

Abbreviations: AUC: Area under the concentration-time curve; AUClast: Area under the curve from zero to the last detectable timepoint; AUMC: Area under the first moment curve; Cmax: Maximum concentration; Tmax: Time at maximum plasma concentration.

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来源期刊
New Zealand veterinary journal
New Zealand veterinary journal 农林科学-兽医学
CiteScore
3.00
自引率
0.00%
发文量
37
审稿时长
12-24 weeks
期刊介绍: The New Zealand Veterinary Journal (NZVJ) is an international journal publishing high quality peer-reviewed articles covering all aspects of veterinary science, including clinical practice, animal welfare and animal health. The NZVJ publishes original research findings, clinical communications (including novel case reports and case series), rapid communications, correspondence and review articles, originating from New Zealand and internationally. Topics should be relevant to, but not limited to, New Zealand veterinary and animal science communities, and include the disciplines of infectious disease, medicine, surgery and the health, management and welfare of production and companion animals, horses and New Zealand wildlife. All submissions are expected to meet the highest ethical and welfare standards, as detailed in the Journal’s instructions for authors.
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