Tilmicosin (phosphate)
(Synonyms: 磷酸替米考星; LY-177370 phosphate; EL-870 phosphate) 目录号 : GC45056
A macrolide antibiotic
Cas No.:137330-13-3
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
Tilmicosin phosphate is a antibiotic, is used in veterinary medicine for the treatment of bovine respiratory disease and ovine respiratory disease associated with Mannheimia (Pasteurella) haemolytica.
References:
[1]. Galyean ML, et al. Effects of arrival medication with tilmicosin phosphate on health and performance of newly received beef cattle. J Anim Sci. 1995 May;73(5):1219-26.
[2]. Fittipaldi N, et al. Assessment of the efficacy of tilmicosin phosphate to eliminate Actinobacillus pleuropneumoniae from carrier pigs. Can J Vet Res. 2005 Apr;69(2):146-50.
| Cas No. | 137330-13-3 | SDF | |
| 别名 | 磷酸替米考星; LY-177370 phosphate; EL-870 phosphate | ||
| Canonical SMILES | CC[C@@H](OC(C[C@@H](O)[C@H](C)[C@@H](O[C@@]1([H])[C@H](O)[C@@H](N(C)C)[C@H](O)[C@@H](C)O1)[C@@H](CCN2C[C@@H](C)C[C@@H](C)C2)C[C@H]3C)=O)[C@@H](CO[C@@H]4O[C@H](C)[C@@H](O)[C@@H](OC)[C@H]4OC)/C=C(C)/C=C/C3=O.O=P(O)(O)O | ||
| 分子式 | C46H80N2O13•H3PO4 | 分子量 | 967.1 |
| 溶解度 | DMF: 25 mg/ml,DMSO: 30 mg/ml,Ethanol: 25 mg/ml,PBS (pH 7.2): 10 mg/ml | 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 | |||
 |
1 mg | 5 mg | 10 mg |
| 1 mM | 1.034 mL | 5.1701 mL | 10.3402 mL |
| 5 mM | 0.2068 mL | 1.034 mL | 2.068 mL |
| 10 mM | 0.1034 mL | 0.517 mL | 1.034 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。
Preparation of tilmicosin-resin complex microsphere and its Pharmacokinetics study in rat
Pak J Pharm Sci 2020 Sep;33(5):2143-2151.PMID:33824123doi
The objective of this study is to mask the extremely bitter taste of Tilmicosin, and the tilmicosin-resin complex (DRC) microsphere were prepared by entrapping Tilmicosin into resins (Tulsion® 339 and Eudragit® RS/ RL 100) for further pharmacokinetics study in rat. The DRC was characterized by FTIR and X-ray diffraction, and the microsphere containing DRC and Eudragit® RS/RL 100 were characterized by scanning electron microscopy (SEM). The rats were orally administrated with Tilmicosin phosphate (10 mg/kg) and the microsphere containing the same dose of Tilmicosin, respectively. These microspheres do not taste bitter and the kinetics study suggests that the drug released from microsphere meet the first order kinetics (r = 0.9911). The experimental results showed that T½ and Tmax of microsphere were much longer than Tilmicosin phosphate, which indicates that the oral microsphere can be a promising long-active formulation for taste masking of Tilmicosin.
Effects of Tilmicosin phosphate, administered prior to transport or at time of arrival, and feeding of chlortetracycline, after arrival in a feedlot, on Mannheimia haemolytica in nasal secretions of transported steers
Am J Vet Res 2000 Dec;61(12):1479-83.PMID:11131584DOI:10.2460/ajvr.2000.61.1479.
Objective: To determine effects of time of administration of Tilmicosin and feeding of chlortetracycline on colonization of the nasopharynx of transported cattle by Mannheimia haemolytica (MH). Animals: 454 steers (body weight, 200 kg). Procedure: 3 studies included 4 truckloads of steers assembled and processed in the southeastern United States. For each truckload of steers, a third received Tilmicosin before transportation (PRIOR), then all were transported to a feedlot in New Mexico (23 hours). At arrival (day 0), another third received Tilmicosin (ARR). The remaining third did not receive Tilmicosin (control steers [CTR]). Steers in studies 1 and 2 were housed in a feedlot, and steers in study 3 were housed on wheat pasture. One half of the steers from each group in studies 2 and 3 were fed chlortetracycline on days 5 to 9. Steer with signs of respiratory tract disease were treated. Nasal swab specimens were examined for MH to determine colonization. Results: PRIOR and ARR steers had a lower incidence of respiratory tract disease and MH colonization than CTR steers, but PRIOR and ARR steers did not differ. Feeding chlortetracycline did not have an effect. Conclusions and clinical relevance: Tilmicosin can inhibit MH from colonizing the nasopharynx of cattle. Because Tilmicosin inhibits the growth of MH in the respiratory tract, medication with Tilmicosin prior to transport should reduce the incidence of acute respiratory tract disease during the first week at the feedlot when calves are most susceptible to infectious organisms.
Efficacy of Tilmicosin phosphate (Pulmotil premix) in feed for the treatment of a clinical outbreak of Actinobacillus pleuropneumoniae infection in growing-finishing pigs
J Vet Med B Infect Dis Vet Public Health 2001 Nov;48(9):655-64.PMID:11765801DOI:10.1046/j.1439-0450.2001.00492.x.
A double-blind randomized clinical trial was carried out to investigate the efficacy of Tilmicosin (Pulmotil premix) for the treatment of a clinical outbreak of Actinobacillus pleuropneumoniae infection in growing-finishing pigs. The effects of Tilmicosin administration in the feed at 400 mg/kg and an injection therapy of clinically diseased pigs with long-acting oxytetracycline (Terramycine LA) at 20 mg/kg bodyweight were compared. Both groups, totalling 147 pigs, were compared during a medication period of 15 days and a post-medication period of 11 days by means of different clinical and performance parameters. During the medication period, the Tilmicosin group showed a significant advantage with respect to the number of new disease cases (P < 0.01), and a non-significant advantage regarding the number of removed pigs (P = 0.16), the number of sick pigs that recovered (P = 0.27) and the time to recovery (P = 0.42). During the post-medication period, the pigs of the Tilmicosin group showed numerical non-significant benefits (P > 0.05) with respect to the clinical parameters. During the overall study period (26 days), the average daily gain and the feed conversion ratio were both significantly (P < 0.01) better in pigs from the Tilmicosin group compared with pigs from the oxytetracycline group. This study demonstrated that in-feed medication of Tilmicosin at a dosage of 400 mg/kg is efficacious for the treatment of a clinical respiratory disease outbreak of A. pleuropneumoniae infection in growing-finishing pigs. Compared with oxytetracycline injection of clinically diseased pigs, the Tilmicosin treatment is particularly beneficial in the prevention of new disease cases while increasing or maintaining the performance of the pigs.
Assessment of the efficacy of Tilmicosin phosphate to eliminate Actinobacillus pleuropneumoniae from carrier pigs
Can J Vet Res 2005 Apr;69(2):146-50.PMID:15971680doi
The aim of this study was to evaluate the efficacy of in-feed medication with Tilmicosin phosphate in order to eliminate or reduce the carriage of Actinobacillus pleuropneumoniae in the tonsils of carrier pigs. Two groups of 6 carrier animals received either a non-medicated feed (control group) or feed medicated with 400 ppm of Tilmicosin phosphate (treated group) for 30 d. Three sentinel pigs were then introduced in each group and left for 29 d. The presence of A. pleuropneumoniae in tonsils was monitored using several techniques, including polymerase chain reaction (PCR). At the end of the treatment all of the control animals, but only 1 treated pig, were positive by PCR from tonsillar surface material. However, at necropsy, all control and most treated animals, as well as 1 sentinel animal, in both groups were positive by PCR from whole tonsils. In conclusion, under the experimental conditions, in-feed treatment with 400 ppm of Tilmicosin phosphate significantly reduced the presence of A. pleuropneumoniae on the surface of tonsils but was unable to completely eliminate the organism from deeper tonsillar tissues and to prevent bacterial shedding by carrier animals.
Evaluation of the antibacterial activity of tilmicosin-SLN against Streptococcus agalactiae: in vitro and in vivo studies
Int J Nanomedicine 2018 Aug 17;13:4747-4755.PMID:30147316DOI:10.2147/IJN.S168179.
Background: Streptococcus and Staphylococcus are the major contagious organisms causing dairy cow mastitis. Our previous studies have demonstrated that solid lipid nanoparticles (SLNs) can effectively enhance the antimicrobial activity of Tilmicosin against Staphylococcus. This study aimed to evaluate the antibacterial efficacy of tilmicosin-loaded SLN (Til-SLN) against Streptococcus agalactiae. Methods: Til-SLN was prepared using a hot homogenization and ultrasonication method as described previously. Til-SLN was labeled with rhodamine B for nanoparticle tracking. In vitro antibacterial experiments were carried out by broth dilution technique. Pharmacokinetics of the drug and distribution of the nanoparticles in mammary gland were studied after subcutaneous injection in Kunming mice. The therapeutic study was conducted in a mouse mastitis model infected with S. agalactiae. Results: The results showed that the diameter, polydispersity index, zeta potential, encapsulation efficiency, and loading capacity of the nanoparticles were not significantly affected by fluorescence labeling. Til-SLN showed a sustained and enhanced antibacterial activity in vitro. Til-SLN maintained a sustained drug concentration above 17 µg/g for at least 6 days in the mammary gland, as compared with only 3 days for the same amount of Tilmicosin phosphate solution. The mean residence time and elimination half-life (T1/2) of Til-SLN were much longer than those of Tilmicosin phosphate solution. Most of the nanoparticles remained at the injection site and a few were transferred to the mammary glands, indicating that the drug was slowly released at the injection site and then distributed to the mammary glands. SLN significantly enhanced the therapeutic efficacy of Tilmicosin as determined by lower colony forming unit counts. Conclusion: These results demonstrate that SLN could effectively enhance the antibacterial activity of Tilmicosin against Streptococcus.