Journal of veterinary pharmacology and therapeutics最新文献

{"title":"Development of Machine Learning and Chemical Language Model-Based QSAR Models for Predicting Drug Residue Depletion Half-Lives in Plasma and Tissues of Cattle Across Various Administration Routes","authors":"Zhicheng Zhang,&nbsp;Lisa A. Tell,&nbsp;Zhoumeng Lin","doi":"10.1111/jvp.70039","DOIUrl":"10.1111/jvp.70039","url":null,"abstract":"<div>\u0000 \u0000 <p>Accurate prediction of drug depletion half-lives plays a pivotal role in determining extralabel withdrawal intervals and ensuring the safety of food products derived from livestock. In this study, we employed machine learning (ML)-based quantitative structure–activity relationship (QSAR) models and an innovative chemical language model-based QSAR approach (ImprovedChemBERTa) to estimate plasma and tissue half-lives of drugs administered to cattle through different administration routes. Utilizing a dataset from the Food Animal Residue Avoidance Databank (FARAD) Comparative Pharmacokinetic Database, we developed one “descriptor-free” ImprovedChemBERTa model and 20 ML-QSAR models, integrating four different ML algorithms with five categories of molecular descriptors. Among ML-QSAR approaches, the deep neural network (DNN) method employing all descriptors achieved the highest predictive accuracy (test <i>R</i>²: 0.37). In contrast, the ImprovedChemBERTa model significantly outperformed traditional methods, reaching a test <i>R</i>² of 0.69, underscoring the superior capability and transfer learning potential of chemical language models. Our findings highlight the effectiveness of chemical language model-based QSAR strategies, which directly process raw chemical representations without requiring explicitly generated molecular descriptors. Overall, this work provides a robust foundation for advancing tissue-specific QSAR modeling in major food-animal species and supports global efforts toward enhanced food safety regulation.</p>\u0000 </div>","PeriodicalId":17596,"journal":{"name":"Journal of veterinary pharmacology and therapeutics","volume":"49 2","pages":"150-171"},"PeriodicalIF":1.7,"publicationDate":"2026-03-08","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"145819987","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":4,"RegionCategory":"农林科学","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}

{"title":"Editorial: Meloxicam in Cats","authors":"Paul C. Mills","doi":"10.1111/jvp.70059","DOIUrl":"10.1111/jvp.70059","url":null,"abstract":"<p>In this issue of the Journal, we have a Commentary titled: ‘Should injectable meloxicam be approved for use in cats?’ (Wun et al. <span>2026</span>). JVPT always welcomes Commentaries and Letters to the Editor since they represent the views and opinions of members of our JVPT readership. These articles are not normally peer reviewed, since, as noted, they represent opinions, although the majority of these articles are written to comment on articles published in JVPT. Our policy is then to show the Commentary or Letter to the Editor to the authors in question and invite them to submit a response if they wish to, with both Commentaries then published in the same issue as JVPT. However, the Commentary by Wun and colleagues refers to a paper published over 25 years ago and in a different journal; therefore, it was not possible to pursue a response. But it is the JVPT editorial policy to seek a balanced response and to perhaps comment on any changes in the scientific understanding of the topic. Therefore, I invited experts in pharmacology, critical care and anesthesiology, and knowledgeable of NSAID administration to cats, to provide a responding commentary (see Pelligand, Cole and Pang in this issue). On a personal note (so yes, I am providing commentary also, despite wishing JVPT to remain neutral), the Commentary by Wun and colleagues may be interpreted by some of our readers as a personal rebuke of the authors of the original Carroll et al. (<span>2005</span>) regarding the availability of the original data. What has changed over the last 25 years as we moved towards digital publishing is the increased ability to include significantly more information, particularly as supplementary files, with many journals, including JVPT, requiring that raw data sets be available. This was not possible 25 years ago due to space restrictions. Since this article was in a different journal, it is not possible to investigate this further, although the full data from the Carroll study were disclosed and freely available on the FDA FOI for Meloxicam in Cats. Ensuring that Commentaries are collegial is an important component of encouraging scientific discussion and advancing knowledge.</p><p>As always, we invite our readership to submit Commentaries and Letters to the Editor on topics of importance to the JVPT community.</p><p>The author takes full responsibility for this article.</p><p>The author declares no conflicts of interest.</p>","PeriodicalId":17596,"journal":{"name":"Journal of veterinary pharmacology and therapeutics","volume":"49 2","pages":""},"PeriodicalIF":1.7,"publicationDate":"2026-03-08","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"https://onlinelibrary.wiley.com/doi/epdf/10.1111/jvp.70059","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"147378016","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":4,"RegionCategory":"农林科学","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"OA","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}

{"title":"Optimizing the Dosage of Ceftiofur to Treat Porcine Respiratory Infection Based on a Population Pharmacokinetic Model and Monte Carlo Simulation","authors":"Chengyang Zhang,&nbsp;Haiyan Liu,&nbsp;Ziyan Kou,&nbsp;Kun Mi,&nbsp;Lingli Huang","doi":"10.1111/jvp.70032","DOIUrl":"10.1111/jvp.70032","url":null,"abstract":"<div>\u0000 \u0000 <p>Porcine respiratory diseases is a major cause of economic losses in livestock, and ceftiofur is one of the core therapeutic agents for its treatment, but the clinical efficacy can be inconsistent. Therefore, it is necessary to utilize a population pharmacokinetic model to reveal the distribution and metabolic patterns of ceftiofur in pig populations, while also combining Monte Carlo simulation techniques to predict the probability of treatment success under different dosing regimens. To investigate the probability of attaining the pharmacokinetic/pharmacodynamic targets of ceftiofur in pigs infected with different respiratory bacteria, a population pharmacokinetic model for the intramuscular administration of ceftiofur in pigs was developed, and Monte Carlo simulation was performed to analyze the target attainment rate of ceftiofur at different doses. The results showed that the target attainment rate of ceftiofur was 100% for <i>Pasteurella multocida</i> at the dose of 0.5 mg/kg b.w. intramuscularly, 99.9% for <i>Actinobacillus pleuropneumoniae</i> at 1 mg/kg b.w. intramuscularly, 93.4% for <i>Streptococcus suis</i> at 0.5 mg/kg b.w. intramuscularly, and 95.4% for <i>Haemophilus parasuis</i> at 10 mg/kg b.w. intramuscularly. The results indicate that it is crucial to optimize the dosage based on specific infected bacteria to improve the success rate of treatment and extend the clinical application period of ceftiofur.</p>\u0000 </div>","PeriodicalId":17596,"journal":{"name":"Journal of veterinary pharmacology and therapeutics","volume":"49 2","pages":"189-197"},"PeriodicalIF":1.7,"publicationDate":"2026-03-08","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"145513243","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":4,"RegionCategory":"农林科学","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}

{"title":"Reply to the Commentary: Should Injectable Meloxicam Be Approved for Use in Cats?","authors":"Ludovic Pelligand,&nbsp;Laura Cole,&nbsp;Daniel S. J. Pang","doi":"10.1111/jvp.70056","DOIUrl":"10.1111/jvp.70056","url":null,"abstract":"&lt;p&gt;We thank Wun et al. (&lt;span&gt;2026&lt;/span&gt;) for their comment on the occurrence of peri-operative Acute Kidney Injury in a clinical trial that was pivotal for the marketing of meloxicam 5 mg/mL solution for cats (U.S. Food and Drug Administration &lt;span&gt;2004&lt;/span&gt;) and subsequent studies (Krekis et al. &lt;span&gt;2024&lt;/span&gt;). We have we been asked to provide a different perspective and we have complemented this letter with PK/PD simulations from available feline NSAID data.&lt;/p&gt;&lt;p&gt;Acute kidney injury (AKI) after surgical procedures in cats has received little attention until recently, although scoping reviews on this topic are emerging in dogs (Quinn &lt;span&gt;2025&lt;/span&gt;). It may therefore be informative to review evidence available from the human literature. In people, the incidence of peri-operative acute kidney injury is emerging as more common than previously recognised (Meersch et al. &lt;span&gt;2024&lt;/span&gt;). AKI and acute kidney disease (AKD) are a continuum (Chawla et al. &lt;span&gt;2017&lt;/span&gt;) that are described in standardised terms, mainly following the publication of the KDIGO staging (Kidney Disease: Improving Global Outcomes (KDIGO) &lt;span&gt;2012&lt;/span&gt;). Post-operative AKI (increase in creatinine ≥ 0.3 mg/dL or ≥ 26.5 μmol/L) is an abrupt decrease in kidney function after the initiating anaesthetic/surgical event. It can be transient (recovery within 48 h) or persisting (lasting up to 7 days). After 7 days, the persisting decrease in glomerular filtration rate (GFR) is classified as acute kidney disease (AKD), which may progress to chronic kidney disease (CKD) if persisting beyond 90 days.&lt;/p&gt;&lt;p&gt;The pathophysiology of peri-operative AKI is complex and likely to involve several predisposing factors, including intra-operative hypotension, blood loss, peri-operative systemic inflammation (as a response of the organism to the trauma of surgery) and administration of potentially nephrotoxic drugs (Meersch et al. &lt;span&gt;2017&lt;/span&gt;). Recovery of renal function can be explained through several mechanisms. The first mechanism is an early physiological recovery of normal circulating volume and haemodynamic conditions in the early post-operative period through resumption of normal water and feed intake. Secondly, there is a possibility of regeneration of lost tubular cells by renal progenitor cells (immature tubular cells with capacity to regenerate entire segments) (Kellum et al. &lt;span&gt;2021&lt;/span&gt;) leading to functional recovery within a few days to weeks. Thirdly, when tubular cells are lost, recovery of renal function is still possible beyond the regeneration stage by compensatory hypertrophy of remaining nephrons, but this happens over several months. The remnant single nephron GFR increase is initially adaptive, but sustained hyperfiltration is ultimately potentially detrimental (maladaptive), increasing the risk of progression to CKD.&lt;/p&gt;&lt;p&gt;What is the prevalence of peri-operative AKI in cats? Does AKI lead to AKD and predispose cats to CKD? What is the poss","PeriodicalId":17596,"journal":{"name":"Journal of veterinary pharmacology and therapeutics","volume":"49 2","pages":"231-234"},"PeriodicalIF":1.7,"publicationDate":"2026-03-08","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"https://www.ncbi.nlm.nih.gov/pmc/articles/PMC12968477/pdf/","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"147378002","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":4,"RegionCategory":"农林科学","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"OA","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}

{"title":"Single-Dose Pharmacokinetics of Intranasal Levetiracetam in Healthy Dogs","authors":"Jessica L. Wagner,&nbsp;Kari D. Foss,&nbsp;Jennifer M. Reinhart,&nbsp;Lauren E. Forsythe","doi":"10.1111/jvp.70046","DOIUrl":"10.1111/jvp.70046","url":null,"abstract":"<p>Cluster seizures and status epilepticus in dogs are emergencies requiring rapid intervention. Intranasal (IN) benzodiazepines are effective for early seizure cessation, but the pharmacokinetics of longer-acting antiseizure medications administered IN have not been investigated in dogs. This study aimed to describe the single-dose pharmacokinetics of a compounded IN levetiracetam product (IN-LEV) in healthy dogs. We hypothesized that the administration of IN-LEV to healthy dogs will demonstrate similar pharmacokinetic parameters to IV administration. In a randomized crossover design, nine healthy dogs received a single 30 mg/kg IV dose (100 mg/mL) or a single 30 mg/kg IN dose (460 mg/mL) of levetiracetam. Serum levetiracetam concentrations were serially measured over 24 h. Pharmacokinetic analysis was performed using non-compartmental methods and comparisons between routes of administration were made using the Wilcoxon signed-rank test. <i>C</i>_max, <i>T</i>_max, and <i>t</i>_1/2 for IN-LEV were 14.6 ± 5.4 μg/mL, 2.3 ± 1.5 h, and 3.6 ± 0.4 h, respectively. IN-LEV achieved minimum target concentrations (5 μg/mL) within 0.34 ± 0.22 h and maintained these levels for 6.57 ± 3.17 h. Bioavailability for IN-LEV was 70% ± 27.4%. This study demonstrates that IN levetiracetam rapidly achieves the lowest reference interval concentration, but the high end of the interval was not achieved in any dog with a single 30 mg/kg dose. IN-LEV may be a viable alternative for emergent seizure management when IV access is unavailable, but multiple doses may be required to achieve seizure cessation in some patients.</p>","PeriodicalId":17596,"journal":{"name":"Journal of veterinary pharmacology and therapeutics","volume":"49 2","pages":"110-119"},"PeriodicalIF":1.7,"publicationDate":"2026-03-08","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"https://www.ncbi.nlm.nih.gov/pmc/articles/PMC12968516/pdf/","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"146010149","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":4,"RegionCategory":"农林科学","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"OA","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}

{"title":"Comparison of Human and Canine P-Glycoprotein Substrates at R, P, and H Binding Sites","authors":"Neal S. Burke,&nbsp;Katrina L. Mealey","doi":"10.1111/jvp.70034","DOIUrl":"10.1111/jvp.70034","url":null,"abstract":"<p>P-glycoprotein (P-gp) greatly impacts substrate drug disposition, so much so that regulatory agencies recommend ascertaining the P-gp status of active pharmaceutical ingredients (APIs) intended for human use. Arguably, the P-gp status of drugs intended for canine patients is equally, if not more, important. Our research objectives were to assess whether human P-gp substrate data can predict canine P-gp substrate status and to explore the three previously reported binding sites within the P-gp binding pocket, the H-, R-, and P-sites. Competitive efflux assays employing cell lines expressing canine or human P-gp were used to compare the degree of overlap or independence of the three binding sites in canine versus human P-gp using site-specific fluorescent P-gp substrates rhodamine 123, calcein AM and Hoechst 33342. Because calcein AM can also be transported by multidrug resistance protein 1 (MRP1), experiments were performed to assess its potential influence on calcein AM efflux studies. Results indicate that: (i) MRP1 is either a non-factor or negligible factor for cells expressing canine or human P-gp respectively; (ii) determining an API's P-gp binding site may provide clinically relevant information; and (iii) use of human P-gp substrate data as a proxy for canine P-gp substrate data will often prove inaccurate.</p>","PeriodicalId":17596,"journal":{"name":"Journal of veterinary pharmacology and therapeutics","volume":"49 2","pages":"120-130"},"PeriodicalIF":1.7,"publicationDate":"2026-03-08","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"https://www.ncbi.nlm.nih.gov/pmc/articles/PMC12968481/pdf/","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"145550123","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":4,"RegionCategory":"农林科学","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"OA","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}

{"title":"The Need for a Revision of Fluoroquinolone Breakpoints for Interpretation of Antimicrobial Susceptibility Testing of Feline Bacterial Isolates","authors":"Mark G. Papich,&nbsp;Lacie A. Gunnett,&nbsp;Marilyn N. Martinez","doi":"10.1111/jvp.70028","DOIUrl":"10.1111/jvp.70028","url":null,"abstract":"<p>The fluoroquinolone antimicrobial agents, enrofloxacin and marbofloxacin, were approved in the United States for cats in 1990 and 2001, respectively. In 2023, revised breakpoints for testing isolates from dogs were published. These canine breakpoints are discordant with the current feline breakpoints. This study was aimed at suggesting new feline breakpoints using a pharmacokinetic-pharmacodynamic (PK-PD) approach and new pharmacokinetic data. The PK-PD derived cutoff values (CO_PD) were compared to microbiologic data available for testing the susceptibility of targeted pathogens since the original approval. Compared to the current Clinical and Laboratory Standards Institute (CLSI) breakpoints for enrofloxacin and marbofloxacin in cats, these revised breakpoints are lower by two dilutions for the Enterobacterales, <i>Pseudomonas aeruginosa, Staphylococcus</i> spp., and <i>Pasteurella multocida</i>. Isolates that may have previously tested susceptible (S) may test resistant (R) using these suggested breakpoints. We also are suggesting a susceptible dose-dependent (SDD) category for testing marbofloxacin against these isolates from cats that allows for a higher dose. These suggested breakpoints may be considered by laboratories, standard-setting organizations, and industry sponsors of these antimicrobials for testing common bacteria isolated from cats.</p>","PeriodicalId":17596,"journal":{"name":"Journal of veterinary pharmacology and therapeutics","volume":"49 2","pages":"131-140"},"PeriodicalIF":1.7,"publicationDate":"2026-03-08","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"https://www.ncbi.nlm.nih.gov/pmc/articles/PMC12968511/pdf/","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"145186235","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":4,"RegionCategory":"农林科学","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"OA","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}

{"title":"Pharmacokinetics of Ceftazidime After a Single Intramuscular Dose in Whitespotted Bamboo Sharks (Chiloscyllium plagiosum)","authors":"Miceala Shocklee,&nbsp;Jennifer Russell,&nbsp;Kelsey Herrick,&nbsp;Todd L. Schmitt,&nbsp;Todd R. Robeck,&nbsp;Mark G. Papich","doi":"10.1111/jvp.70031","DOIUrl":"10.1111/jvp.70031","url":null,"abstract":"<div>\u0000 \u0000 <p>Whitespotted bamboo sharks (<i>Chiloscyllium plagiosum</i>) are a common species of elasmobranchs housed in zoos and aquaria. Medical concerns like conspecific trauma and bacterial infections commonly lead to the empirical use of antibiotic medications like ceftazidime, despite limited pharmacokinetic studies in elasmobranchs. In this study, 36 whitespotted bamboo sharks were divided into six groups using a population pharmacokinetic design. They were administered a single intramuscular injection of ceftazidime at 20 mg/kg. Blood samples were collected for plasma drug concentration at time points <i>T</i> = 0 and 30 min, and 1, 2, 4, 6, 12, 24, 48, 72, and 96 h post-injection. Samples were analyzed by the Clinical Pharmacology Laboratory in the College of Veterinary Medicine of North Carolina State University using high-pressure liquid chromatography (HPLC) analysis. For at least 96 h, all sharks in the study maintained plasma concentrations of ceftazidime above the MIC of 4 μg/mL, which is considered susceptible when testing isolates from other animals. The long elimination half-time of 84.15 h suggests that recommended dosing intervals may be extended beyond the commonly used 3 days to at least every 96 h.</p>\u0000 </div>","PeriodicalId":17596,"journal":{"name":"Journal of veterinary pharmacology and therapeutics","volume":"49 2","pages":"213-219"},"PeriodicalIF":1.7,"publicationDate":"2026-03-08","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"145301605","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":4,"RegionCategory":"农林科学","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}

{"title":"Time Kill Curve PD Modelling Experiments Are Affected by Trailing MIC Endpoints: Refinement of MIC Determination for S. pseudintermedius","authors":"Andrew Mead,&nbsp;Ludovic Pelligand","doi":"10.1111/jvp.70033","DOIUrl":"10.1111/jvp.70033","url":null,"abstract":"<p>Trailing endpoints are a recognised challenge in broth microdilution MIC testing, particularly for bacteriostatic agents such as trimethoprim (TMP) and sulphonamides. In this study, we applied a pharmacodynamically guided refinement to determine the MIC of the combination against <i>Staphylococcus pseudintermedius</i>; we did not aim at redefining clinical susceptibility, but at refining MIC determination to better guide pharmacodynamic study design. By providing more reliable thresholds for growth suppression, this approach supports optimisation of PD modelling and may ultimately inform translational applications, such as dose prediction and reducing misclassification in PD contexts. Visual MICs were compared to those derived from log₁₀ changes in CFU/mL over 24 h, using pharmacodynamic thresholds of +2.3 log₁₀ (growth from standard inoculum of 5 × 10⁵ to ~10⁸ CFU/mL, corresponding to visible growth MIC) and 0 log₁₀ change (stationary concentration). Across 10 clinical isolates, visual MICs often underestimated the concentration required to suppress growth by 2–4 fold (more than one dilution step), particularly for sulphonamides. TMP-sulphonamide combinations at a 1:19 ratio showed reduced trailing and closer agreement between visual and count-based MICs, reflecting enhanced bactericidal activity. Time-kill curve experiments anchored on the log₁₀ count-based MIC provided a well-distributed range of PD responses, capturing both suppression and killing more accurately than curves centred on visual MICs. This method supports more rational selection of concentrations for PD studies and may be especially valuable for slow-acting or ratio-sensitive combinations, and has translational value for sulphonamides, such as sulfamethoxazole, used in both human and veterinary medicine.</p>","PeriodicalId":17596,"journal":{"name":"Journal of veterinary pharmacology and therapeutics","volume":"49 2","pages":"220-227"},"PeriodicalIF":1.7,"publicationDate":"2026-03-08","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"https://www.ncbi.nlm.nih.gov/pmc/articles/PMC12968473/pdf/","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"145377820","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":4,"RegionCategory":"农林科学","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"OA","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}

{"title":"Pharmacokinetic Evaluation of Buserelin Acetate (Receptal) in Gilts","authors":"Preechaphon Taechamaeteekul,&nbsp;Tussapon Boonyarattanasoonthorn,&nbsp;Chutikan Srisang,&nbsp;Yosua Kristian Adi,&nbsp;Natchanon Dumniem,&nbsp;Jinda Singlor,&nbsp;Hongyao Lin,&nbsp;Romchat Chutoprapat,&nbsp;Robert V. Knox,&nbsp;Padet Tummaruk","doi":"10.1111/jvp.70036","DOIUrl":"10.1111/jvp.70036","url":null,"abstract":"<div>\u0000 \u0000 <p>Buserelin acetate, a synthetic analog of gonadotropin-releasing hormone (GnRH), is used to induce ovulation and enable fixed-time artificial insemination (FTAI) in swine. Evaluating the pharmacokinetics of buserelin acetate is crucial for optimizing its application in precisely controlling ovulation timing and enhancing the effectiveness of FTAI in pigs. This study investigates the pharmacokinetics of buserelin acetate following intramuscular administration in gilts. Ten healthy prepuberty gilts (Landrace × Yorkshire × Duroc) with an average body weight of 72.0 ± 3.4 kg were included in the study. Before treatment, all ten gilts underwent surgical implantation of an indwelling venous catheter to allow repeated blood samplings for pharmacokinetic assessment. On Day 3 after surgery, each gilt received an intramuscular injection of 100 μg buserelin acetate (25 mL of 4 μg/mL Receptal, MSD Animal Health, USA). Blood samples (5 mL each) were collected 14 times from each gilt via the jugular catheter at the following time points: 0, 2, 5, 10, 15, 20, 30, and 45 min, as well as 1, 1.5, 2, 3, 4, and 6 h post-injection. Blood samples were collected into heparinized tubes, centrifuged to separate the plasma, and stored at −20°C until analysis. Plasma buserelin concentrations were then determined using Liquid Chromatography–Tandem Mass Spectrometry (LC–MS/MS). The LC–MS/MS system operated in positive ion mode using electrospray ionization with multiple reaction monitoring. Buserelin was quantified based on precursor/product ion pairs identified in the chromatogram. The calibration curve for buserelin acetate in pig plasma showed high linearity (<i>R</i>² ≥ 0.99), with a lower limit of quantification of 0.30 μg/L. The findings showed that the average maximum plasma concentration (<i>C</i>_max) of buserelin acetate was 2.21 ± 0.72 μg/L, occurring at 0.30 ± 0.10 h (<i>T</i>_max) after administration. The elimination half-life (<i>T</i>_1/2) was 0.51 ± 0.03 h. The area under the concentration–time curve from 0 to the last measurement point (AUC_0-t) was 7.30 ± 0.87 μg·h/L. The clearance rate (CL) was 0.20 ± 0.03 L/h/kg, and the apparent volume of distribution (Vd) was 0.13 ± 0.05 L/kg. These results suggest that buserelin acetate from Receptal is rapidly metabolized and eliminated in gilts, emphasizing the need for precise timing of administration to maintain effective drug concentrations.</p>\u0000 </div>","PeriodicalId":17596,"journal":{"name":"Journal of veterinary pharmacology and therapeutics","volume":"49 2","pages":"180-188"},"PeriodicalIF":1.7,"publicationDate":"2026-03-08","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"145635011","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":4,"RegionCategory":"农林科学","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}