Febantel
(Synonyms: 苯硫胍) 目录号 : GC32270
Febantel (Rintal, Combotel, Oratel, Bay Vh 5757, Negabot Plus) is a prodrug that is metabolized to fenbendazole and oxfendazole, which are undoubtedly the active parasiticides.
Cas No.:58306-30-2
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
Febantel (Rintal, Combotel, Oratel, Bay Vh 5757, Negabot Plus) is a prodrug that is metabolized to fenbendazole and oxfendazole, which are undoubtedly the active parasiticides.
| Cas No. | 58306-30-2 | SDF | |
| 别名 | 苯硫胍 | ||
| Canonical SMILES | COCC(NC1=CC(SC2=CC=CC=C2)=CC=C1/N=C(NC(OC)=O)\NC(OC)=O)=O | ||
| 分子式 | C20H22N4O6S | 分子量 | 446.48 |
| 溶解度 | DMSO : 89mg/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 | |||
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1 mg | 5 mg | 10 mg |
| 1 mM | 2.2397 mL | 11.1987 mL | 22.3974 mL |
| 5 mM | 0.4479 mL | 2.2397 mL | 4.4795 mL |
| 10 mM | 0.224 mL | 1.1199 mL | 2.2397 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。
The bioavailability of Febantel in dehydrated camels
J Vet Pharmacol Ther 1996 Aug;19(4):288-94.PMID:8866457DOI:10.1111/j.1365-2885.1996.tb00051.x.
In the present study the bioavailability of Febantel paste and Febantel suspension was investigated in the fully hydrated and the dehydrated camel. The serum concentrations of Febantel and its metabolites, fenbendazole, oxfendazole and fenbendazole sulfone were determined by high performance liquid chromatography following extraction with ether. The exposure to Febantel and its metabolites in fully hydrated camels was significantly higher in camels dosed with Febantel paste compared to Febantel suspension, as measured by AUC and Cmax. The AUC and Cmax of fenbendazole and oxfendazole were significantly lower in dehydrated camels as compared to control camels dosed with Febantel paste. The systemic availability of Febantel suspension in control and dehydrated camels was very low and differences between dehydration and control phases were insignificant. The low systemic availability of Febantel in camels dosed with Febantel suspension may cause nematodes to become resistant to this anthelmintic. It is, thus, suggested to increase the dose of Febantel paste in dehydrated camels in order to increase the exposure to Febantel and its metabolites. The binding of Febantel, fenbendazole, oxfendazole and fenbendazole sulfone to camels' serum proteins was over 85%. Oxfendazole was only about 70% bound. Dehydration of 10 days did not affect the binding of these benzimidazole derivatives to serum proteins.
Fate of Febantel in the aquatic environment-the role of abiotic elimination processes
Environ Sci Pollut Res Int 2018 Oct;25(29):28917-28927.PMID:30105676DOI:10.1007/s11356-018-2935-9.
Febantel is widely used anthelmintic drug active against a range of gastrointestinal parasites in animals. Despite the fact that it has been detected in the aquatic environment, there is no information on its environmental fate. Therefore, abiotic elimination processes of Febantel in the aquatic environment have been studied. The results of direct and indirect photodegradation experiments showed that Febantel was persistent against solar radiation. Kinetics of hydrolytic elimination was pH and temperature dependent with half-lives in the range from 210 min to 99 days. Febantel metabolites, fenbendazole and fenbendazole sulfone, were found as major degradation products using high-resolution mass spectrometry. The proposed hydrolytic degradation pathway consisted of the base catalyzed hydrolysis followed by consecutive oxidative cyclization to the five-membered ring of the benzo-imidazole derivative. Aquatic toxicity of Febantel and its hydrolytic mixture were evaluated toward the luminescence bacteria Vibrio fischeri. Investigation of Febantel sorption onto river sediments showed that the best agreement was obtained with the linear model (R2 > 0.99), while the rate of sorption is the best described with the kinetic model of pseudo-second order. The organic carbon-normalized sorption coefficient, KOC, ranged from 1490 to 3894 L kg-1 for five sediment samples. The results of this research demonstrate that Febantel persist in the natural waters and potentially could travel far from the source.
Synergistic effect of Febantel and pyrantel embonate in elimination of Giardia in a gerbil model
Parasitol Res 2009 Aug;105 Suppl 1:S135-40.PMID:19575234DOI:10.1007/s00436-009-1504-z.
The objectives of the study were to determine the optimal dose of Febantel, pyrantel embonate and a combination of Febantel/pyrantel embonate required to effectively treat Giardia in a gerbil model and to determine if there is a synergistic effect with the two drugs. SPF gerbils were infected by oral inoculation with 105 Giardia duodenalis trophozoites (day 0). On days 5 to 7, animals (n = 6) were treated once daily via oral gavage with Febantel, pyrantel embonate, Febantel and pyrantel embonate, metronidazole or placebo. Gerbils were euthanised 24 hours after last treatment and duodenal trophozoites were enumerated on a haemocytometer to obtain a concentration of trophozoites/ cm of gut. Febantel alone, effectively eliminated Giardia trophozoites at 160 and 80 mg/kg. Pyrantel embonate did not eliminate Giardia from the animals but significantly reduced parasite counts at all dosages. Febantel combined with pyrantel embonate effectively eliminated Giardia trophozoites at 160, 80 and 40 mg/kg. Metronidazole did not eliminate Giardia trophozoites from the gut. All placebo-treated animals were heavily infected with Giardia trophozoites. It can be concluded that Febantel is more effective in elimination of Giardia infections when combined with pyrantel embonate compared to the agents used alone.
Comparison of Febantel tablets and Vercom paste against gastrointestinal nematodes of dogs
Vet Parasitol 1992 Feb;41(1-2):151-6.PMID:1561756DOI:10.1016/0304-4017(92)90018-5.
Thirty adult dogs with naturally acquired gastrointestinal nematode infections were assigned at random to ten replicates and treated daily for 3 days with either a combination Febantel/praziquantel (Vercom) paste, Febantel tablets or placebo tablets. Numbers of hookworm and whipworm eggs after treatment were reduced similarly for both drug formulations when compared with pretreatment egg counts, whereas these counts increased in the controls. Vercom paste reduced the hookworm egg count by 99.9% and the whipworm egg count by 99.6%. The Febantel tablet decreased the hookworm egg count by 99.9% and the whipworm egg count by 100%. As determined at necropsy, the controlled test efficacy against adult hookworms and whipworms was similar for the Vercom paste and the Febantel tablets. The controlled test efficacies of Vercom paste against Ancylostoma caninum, Ancylostoma braziliense, and Trichuris vulpis were, respectively, 99.7%, 100% and 95.8% and those of Febantel tablets were 98.2%, 100% and 99.7%. These results indicate that the nematocidal efficacy of Febantel against these nematodes remains unchanged in these two formulations. No adverse reactions to either Febantel tablets or to Vercom paste were observed.
Formulation of poorly water-soluble drugs via coacervation--a pilot study using Febantel
Eur J Pharm Biopharm 2013 Nov;85(3 Pt B):930-5.PMID:23872178DOI:10.1016/j.ejpb.2013.07.006.
In this study, Febantel was dissolved under increased temperature in a nonionic surfactant Lutrol L44庐 and subsequently mixed into an aqueous maltodextrin solution. After 8h under static conditions, coacervation or phase separation took place. (1)H NMR spectra and HPLC analysis showed that the upper phase contained mainly all Febantel, while no Febantel was detected in the lower phase. Fluorescent microscopy showed that maltodextrin is distributed in the lower phase. Coacervation proved to be a promising formulation technology for certain poorly water-soluble drugs, such as Febantel. The coacervate phase showed an increase in in vitro dissolution kinetics, compared to Rintal庐 granules. These results were confirmed in an in vivo study performed on dogs. Febantel and fenbendazole showed a significant increase in plasma concentration compared to Rintal庐 granules. Further studies have to be performed to transform coacervates into a solid dosage form and to prove broad applicability to other poorly soluble drugs.