Tildipirosin
(Synonyms: 泰地罗新) 目录号 : GC37793
A macrolide antibiotic
Cas No.:328898-40-4
Sample solution is provided at 25 µL, 10mM.
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Quality Control & SDS
- View current batch:
- Purity: >98.00%
- COA (Certificate Of Analysis)
- SDS (Safety Data Sheet)
- Datasheet
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Animal experiment: |
On day 0, each pen of 4 calves is randomly assigned by means of drawing numbers from a hat to receive 1 of 3 treatments; thus, each treatment group consists of 8 calves. Calves in group 1 receive tildipirosinb (4 mg/kg, SC), calves in group 2 receive tulathromycinc (2.5 mg/kg, SC), and calves in group 3 receive saline (0.9% NaCl) solution (1 mL/45 kg, SC; control). The volume of saline solution administered to the calves in group 3 approximates the volume of the assigned antimicrobial administered to the calves of groups 1 and 2.On day 5, all calves are experimentally inoculated (challenged) with 10 mL of PBS solution supplemented with 5% bovine fetal serum containing 1.6×109 CFUs of H somni/mL instilled via a flexible bronchoalveolar lavage tube (length, 3 m; external diameter, 11 mm; internal diameter, 3 mm) that is passed through the nasal passage and nasopharynx to the level of the tracheal bifurcation. Proper placement of the tube at the tracheal bifurcation is verified on the basis of qualitative observations that includ an elicited cough, absence of evidence of esophageal or ruminal placement as determined by smell and lack of tension and failure to observe the tube within the esophagus during placement, the presence of resistance at the carina, and the passage of the tube to a predetermined mark that approximates the distance from the nares to the carina. Following experimental inoculation, the tube is flushed with 60 mL of saline solution and 120 mL of air before it is removed from the calf.On day 8, all calves are weighed, sedated with xylazined (0.25 mg/kg), and transported in a trailer in groups of 4 to 6 calves. Immediately after euthanasia, a necropsy is performed on each calf. |
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References: [1]. Rose M, et al. A microbiological assay to estimate the antimicrobial activity of parenteral tildipirosin against foodborne pathogens and commensals in the colon of beef cattle and pigs. J Vet Pharmacol Ther. 2016 Jun;39(3):277-86. |
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Tildipirosin is a 16-membered macrolide used as an antibiotic in veterinary medicine. Like other macrolides, it inhibits protein synthesis in bacteria and blocks the production of biofilms.1,2 Tildipirosin is particularly effective against Gram-
1.Andersen, N.M., Poehlsgaard, J., Warrass, R., et al.Inhibition of protein synthesis on the ribosome by tildipirosin compared with other veterinary macrolidesAntimicrob. Agents Chemother.56(11)6033-6036(2012) 2.Rademacher, J., and Welte, T.Bronchiectasis-diagnosis and treatmentDtsch. Arztebl. Int.108(48)809-815(2011) 3.Michael, G.B., Eidam, C., Kadlec, K., et al.Increased MICs of gamithromycin and tildipirosin in the presence of the genes erm(42) and msr(E)-mph(E) for bovine Pasteurella multocida and Mannheimia haemolyticaJ. Antimicrob. Chemother.67(6)1555-1557(2012)
| Cas No. | 328898-40-4 | SDF | |
| 别名 | 泰地罗新 | ||
| Canonical SMILES | O=C(/C=C/C(C)=C/[C@H](CN1CCCCC1)[C@@H](CC)O2)[C@H](C)C[C@H](CCN3CCCCC3)[C@H](OC4[C@@H](O)[C@@H](N(C)C)[C@H](O)[C@H](C)O4)[C@@H](C)[C@H](O)CC2=O | ||
| 分子式 | C41H71N3O8 | 分子量 | 734.02 |
| 溶解度 | DMSO: ≥ 100 mg/mL (136.24 mM) | 储存条件 | Store at -20°C |
| General tips | 请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液；一旦配成溶液，请分装保存，避免反复冻融造成的产品失效。 储备液的保存方式和期限：-80°C 储存时，请在 6 个月内使用，-20°C 储存时，请在 1 个月内使用。 为了提高溶解度，请将管子加热至37℃，然后在超声波浴中震荡一段时间。 |
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| Shipping Condition | 评估样品解决方案：配备蓝冰进行发货。所有其他可用尺寸：配备RT，或根据请求配备蓝冰。 | ||
| 制备储备液 | |||
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1 mg | 5 mg | 10 mg |
| 1 mM | 1.3624 mL | 6.8118 mL | 13.6236 mL |
| 5 mM | 0.2725 mL | 1.3624 mL | 2.7247 mL |
| 10 mM | 0.1362 mL | 0.6812 mL | 1.3624 mL |
| 第一步：请输入基本实验信息（考虑到实验过程中的损耗，建议多配一只动物的药量） | ||||||||||
| 给药剂量 | mg/kg |  |
动物平均体重 | g | |
每只动物给药体积 | ul | |
动物数量 | 只 |
| 第二步：请输入动物体内配方组成（配方适用于不溶于水的药物；不同批次药物配方比例不同，请联系GLPBIO为您提供正确的澄清溶液配方） | ||||||||||
| % DMSO % % Tween 80 % saline | ||||||||||
| 计算重置 | ||||||||||
计算结果:
工作液浓度： mg/ml；
DMSO母液配制方法： mg 药物溶于 μL DMSO溶液（母液浓度 mg/mL，
体内配方配制方法：取 μL DMSO母液，加入 μL PEG300，混匀澄清后加入μL Tween 80，混匀澄清后加入 μL saline，混匀澄清。
1. 首先保证母液是澄清的；
2.
一定要按照顺序依次将溶剂加入，进行下一步操作之前必须保证上一步操作得到的是澄清的溶液，可采用涡旋、超声或水浴加热等物理方法助溶。
3. 以上所有助溶剂都可在 GlpBio 网站选购。
Pharmacokinetics of Tildipirosin in horses after intravenous and intramuscular administration and its potential muscle damage
Res Vet Sci 2022 Dec 20;152:20-25.PMID:35908422DOI:10.1016/j.rvsc.2022.06.033.
Tildipirosin is a novel semisynthetic macrolide antibiotic exclusively used in veterinary practice to treat respiratory infections. There are no pharmacokinetic or safety information available regarding the use of Tildipirosin after intramuscular administration in horses. Thus, the objective of this work was to determine the disposition kinetics of Tildipirosin after intravenous (IV) and intramuscular (IM) administration in horses and its potential muscle damage and cardiotoxicity. Six mature, Spanish-breed horses were used in a crossover study with a washout period of 30 days. Tildipirosin (18%) was administered at single doses by IV (2 mg/kg) and IM (4 mg/kg) routes. Tildipirosin plasma concentrations were determined by HPLC assay with ultraviolet detection. Muscle damage and inflammation were assessed by creatine kinase (CK) and haptoglobin (Hp), respectively. Creatine kinase myocardial band (CK-MB) and troponin (Tn) were used to evaluate cardiotoxicity. Tildipirosin in horses reached peak concentrations (Cmax = 1.13 μg/mL) at 0.60 h (tmax) after IM administration with an absolute bioavailability of 109.2%. Steady-state volume of distribution and clearance were 3.31 ± 0.57 L/kg and 0.22 ± 0.02 L/h/kg, respectively. Tildipirosin did not cause cardiotoxicity since CK-MB and Tn basal levels were not significantly different from those obtained after several days post-administration. Mild local reactions were observed after IM administration. This local inflammation was associated with mild myolysis (CK 239-837 UI/L), which was detectable for 48 h. In brief, Tildipirosin could help to treat respiratory infections in horses because it showed extensive distribution, high bioavailability and did not provoke general adverse reactions.
Tildipirosin: An effective antibiotic against Glaesserella parasuis from an in vitro analysis
Vet Anim Sci 2020 Jul 21;10:100136.PMID:32964167DOI:10.1016/j.vas.2020.100136.
Tildipirosin is a latest generation macrolide that is used to battle infection diseases caused by Gram-negative bacteria. Recent studies have shown the effectiveness of this antimicrobial agent against Actinobacillus pleuropneumoniae; however, little information is available about Glaesserella parasuis, the etiological agent of Glässer's disease. In this study, the Tildipirosin activity to 100 Brazilian clinical isolates of G. parasuis was assessed using a broth microdilution assay. A total of 90% of G. parasuis isolates were sensitive at concentrations ≤ 4 µg/mL Tildipirosin, thus showing to be efficiently controlled by the therapeutic concentration recommended for pigs. On the other hand, a total of ten isolates have shown resistance to this antibiotic, with a minimal inhibitory concentration (MIC) ≥ 8 and ≤ 16 µg/ml. Notably, our findings highly support the use of Tildipirosin for treating Glässer's disease outbreaks, and it also advises the using of MIC approach to monitor the evolution of sensitivity or resistance exhibited by G. parasuis to this molecule, as well as to adjust therapeutic doses when necessary.
Pharmacokinetics and bioavailability of Tildipirosin following intravenous and subcutaneous administration in horses
J Vet Pharmacol Ther 2021 Jul;44(4):544-551.PMID:33609061DOI:10.1111/jvp.12958.
This study was designed to investigate the safety and pharmacokinetic (PK) profile of Tildipirosin in horses after intravenous (i.v.) and subcutaneous (s.c.) injection of a single dose at 4 mg/kg of body weight (b.w.). A total of 12 healthy mixed breed horses were used in the study. Horses were monitored for systemic and local adverse effects, and whole blood samples were collected for hematology and plasma biochemistry analysis at time (0) and at 6, 24, and 72 h after drug administration. For PK analysis, blood samples were collected at pre-determined times before and after Tildipirosin administration. Plasma concentrations of Tildipirosin were determined using ultra-high-performance liquid chromatography-ultraviolet detection method (UHPLC-UV). All horses tolerated the i.v. injection of Tildipirosin without showing any systemic adverse effects. However, a non-painful, soft swelling appeared at the s.c. injection site in 5 horses (41.7%). On average, Tildipirosin reached a maximum plasma concentration (Cmax ) of 1257 ng/ml (geometric mean) between 0.5 and 1.5 h after s.c. administration (Tmax ). The geometric mean values for total body clearance (Cl), the apparent volume of distribution based on the terminal phase (Vz ), and the apparent volume of distribution at steady-state (Vss ) were 0.52 L/kg·h, 22 L/kg, and 10.0 L/kg, respectively. Data collected in this study suggests that Tildipirosin can be used safely in horses with caution.
Pharmacokinetics of Tildipirosin in Plasma, Milk, and Somatic Cells Following Intravenous, Intramuscular, and Subcutaneous Administration in Dairy Goats
Pharmaceutics 2022 Apr 13;14(4):860.PMID:35456694DOI:10.3390/pharmaceutics14040860.
Tildipirosin is a macrolide currently authorized for treating respiratory diseases in cattle and swine. The disposition kinetics of Tildipirosin in plasma, milk, and somatic cells were investigated in dairy goats. Tildipirosin was administered at a single dose of 2 mg/kg by intravenous (IV) and 4 mg/kg by intramuscular (IM) and subcutaneous (SC) routes. Concentrations of Tildipirosin were determined by an HPLC method with UV detection. Pharmacokinetic parameters were estimated by non-compartmental analysis. Muscle damage, cardiotoxicity, and inflammation were evaluated. After IV administration, the apparent volume of distribution in the steady state was 7.2 L/kg and clearance 0.64 L/h/kg. Plasma and milk half-lives were 6.2 and 58.3 h, respectively, indicating nine times longer persistence of Tildipirosin in milk than in plasma. Moreover, if somatic cells are considered, persistence and exposure measured by the area under concentration-time curve (AUC) significantly exceeded those obtained in plasma. Similarly, longer half-lives in whole milk and somatic cells compared to plasma were observed after IM and SC administration. No adverse effects were observed. In brief, Tildipirosin should be reserved for cases where other suitable antibiotics have been unsuccessful, discarding milk production of treated animals for at least 45 days or treating goats at the dry-off period.
Pharmacokinetics and bioavailability of Tildipirosin following intravenous and subcutaneous administration in sheep
J Vet Pharmacol Ther 2021 Jan;44(1):79-85.PMID:32748450DOI:10.1111/jvp.12901.
Tildipirosin is a semi-synthetic macrolide antibiotic commonly used in cattle and swine to treat bacterial pneumonia. The objective of this study was to investigate the pharmacokinetic profile of Tildipirosin after a single intravenous (i.v.) and subcutaneous (s.c.) administration in healthy lambs. Eighteen lambs were randomly divided into three groups (n = 6 each). Lambs received a single s.c. dose of Tildipirosin at 4 and 6 mg/kg b.w. in group 1 and 2, respectively. Lambs in group 3 received a single i.v. dose of Tildipirosin at 4 mg/kg b.w. Blood samples were collected at 0, 0.5, 0.75, 1.5, 2, 3, 4, 6, 8, 10, 24, 36, 48 hr, and every 24 hr to day 21, and thereafter at day 28 posttildipirosin administration. The plasma concentrations of Tildipirosin were determined using high-performance liquid chromatography with tandem mass spectrometry detection (LC⁄MS⁄MS). All lambs appeared to tolerate both the intravenous and subcutaneous injection of Tildipirosin. Following i.v. administration, the elimination half-life (T1/2 ), mean residence time (MRT), volume of distribution (Vd/F), and total body clearance (Cl/F) were 119.6 ± 9.0 hr, 281.9 ± 25.7 hr, 521.1 ± 107.2 L, and 2.9 ± 0.5 L/hr, respectively. No significant differences in Cmax (657.0 ± 142.8 and 754.6 ± 227.1 ng/ml), Tmax (1.21 ± 0.38 and 1.35 ± 0.44 hr), T1/2 (144 ± 17.5, 156.5 ± 33.4 hr), and MRT (262.0 ± 30.2 and 250.6 ± 54.5 hr) were found in Tildipirosin after s.c. dosing at 4 and 6 mg/kg b.w., respectively. The absolute bioavailability (F) of Tildipirosin was 71.5% and 75.3% after s.c. administration of 4 and 6 mg/kg b.w., respectively. In conclusion, Tildipirosin was rapidly absorbed and slowly eliminated after a single s.c. administration in healthy lambs. Tildipirosin could be used for the treatment and prevention of respiratory bacterial infections in sheep. However, further in vitro and in vivo studies to determine the efficacy and safety are warranted. To our knowledge, this is the first study to determine the Tildipirosin pharmacokinetic parameters in sheep plasma.