Molecular Formula | C20H22N4O6S |
Molar Mass | 446.48 |
Density | 1.2962 (rough estimate) |
Melting Point | 129-130°C |
Boling Point | 215°C (rough estimate) |
Solubility | Chloroform (Sparingly) |
Appearance | neat |
Color | White to Off-White |
Merck | 14,3944 |
pKa | 7.60±0.46(Predicted) |
Storage Condition | Sealed in dry,2-8°C |
Refractive Index | 1.6000 (estimate) |
Use | Broad-spectrum anthelmintic, highly active against nematodes, adults and larvae of dogs, sheep, pigs, horses and other animals |
Hazard Symbols | Xn - Harmful |
Risk Codes | 22 - Harmful if swallowed |
WGK Germany | 3 |
RTECS | FB3955000 |
HS Code | 2930902000 |
Overview | The broad-spectrum anthelmintic drug Febantel, also known as thioguanguanidine, is mainly used for the treatment and control of cattle, sheep, pigs, horses and other animals, gastrointestinal roundworm, lung worms, tapeworms, with high efficiency, low toxicity, short residence time in the body, a wide range of security and other characteristics. As a prodrug, it is metabolized in the body (cyclization) to the antiparasitic drug fenbendazole, or further metabolized (oxidation of sulfur atoms) to ofendazole. It was first developed by Bayer pharmaceutical company of Germany, and its synthetic route is rarely reported in China. Listing commodity (Drontalplus), is a kind of compound broad-spectrum anti-worm drug, containing non-bantaier, praziquantel and dihydroxynaphthalate thiazine three active ingredients, an anthelmintic for dogs, manufactured by Bayer Healthcare Co., Ltd., has been registered and applied in more than 30 countries and can be used to repel a variety of digestive tract worms in dogs. |
synthetic route | its synthetic route is rarely reported in China. In this paper, the synthesis and process optimization were obtained by the following route: using 5-chloro-2-nitroaniline (2) as raw material, 2-nitro-5-phenylthioaniline (3) was obtained by nucleophilic substitution of thiophenol in the presence of K2CO3, 3 2-methoxy-n-(2-nitro-5-phenylthio) phenylacetamide (4) was obtained by the acylation of methoxyacetyl chloride, 4-methoxy-n-(2-amino-5-phenylthio) phenylacetamide (5),5 and S-methyl-N, the condensation of N'-dimethoxycarbonylisothiourea (6) resulted in the final production of non-banthiol (1). |
pharmacological action | praziquantel is a broad-spectrum anti-tapeworm drug. After contact with the worm, the worm muscle tonic contraction and produce spastic paralysis. Praziquantel has a rapid and obvious damage effect on the cortex of the worm body, causing swelling of the outer skin of the syncytial body, the appearance of vacuoles, the formation of bullae, the protrusion of the body surface, and eventually the erosion and ulceration of the epidermis, ring muscle and longitudinal muscle dissolved rapidly. After the destruction of the cortex, the absorption and excretion functions of the worm are affected, and more importantly, the body surface antigen is exposed, which is vulnerable to the host's immune Aggression, a large number of eosinophils attach to the skin lesions and invade, contributed to the death of the worm. In addition, praziquantel can also cause secondary changes, depolarization of the worm surface membrane, alkaline phosphatase activity decreased significantly, resulting in inhibition of glucose uptake and depletion of Endogenous glycogen; praziquantel can also inhibit the synthesis of nucleic acid and protein in the worm. |
determination of content | HPLC Method for Determination of chromatographic conditions and system suitability test, using eighteen alkyl silane bonded silica gel as filler, 0.05 mol/L potassium dihydrogen phosphate solution-acetonitrile (57:43) as mobile phase, the detection wavelength was 280 nm. The number of theoretical plates shall be not less than 2500 based on non-bantaier peak. The separation degree of non-bantaier peak from imidazolium urethane, methoxymethylimidazole and methoxycarbonyl guanidine peaks shall meet the requirements. Determination of this product is about 50 mg, precision weighing, 50 ml flask, plus acetonitrile dissolved and diluted to the scale, shake, precision take 20 μl, injected into the liquid chromatography, the chromatogram was recorded, and the non-bantaier reference substance was taken for determination by the same method. According to the external standard method to calculate the peak area, that is. |
function and use | anti-worm drug. For the elimination of gastrointestinal nematodes and lung nematodes. For the treatment of nematode and tapeworm infections in pet dogs. |
usage and dosage | a single oral dose of 5mg per 1kg body weight of sheep and pigs. In the control of canine roundworm, should be in the nursing mother postpartum 2 weeks to the drug, once every 2 weeks to 12 weeks of age, the drug was then administered once every 3 months. For dogs with severe nematode infection, the first dose should be repeated for 2 weeks. Adult dogs were treated with deworming, 1 times every 3 months. |
note | Drug holiday: sheep, pig 14 days, goat milk 2 days. Only for the treatment of more than 3 kg dogs; Do not use with piperazine drugs. |
store | hermetically sealed and stored in a dry place. |
preparation | Febantel Tablets (C20H22N4O6S) it shall be 90.0% to 110.0% of the labeled amount. White or off-white tablets. Non-Bantel Granules the content of non-Bantel Granules (C20H22N4O6S) should be 90.0% ~ 110.0% of the labeled amount. White granules. |
drug residues | in dairy products, residues must be detected in accordance with national standards. |
references | [1] Zhu Jianmin, Liu Xiangyi, Wu Jiancai. Synthesis of a broad-spectrum anthelmintic drug, non-bamyl [J]. Zhejiang Chemical Industry, 2009,08:6-7. [2] Wang Zhiqiang, Wang Qinghua, Li Hao, Qiu Mei, Zhang Chang Qing, Zhao Yi Hui. Experimental study on anthelmintic effect of baiweiqing on dogs naturally infected with helminths [J]. Chinese Journal of Veterinary Medicine, 2010,01:69-71. [3] Ministry of Agriculture issues new quality standards for imported veterinary drugs [J]. Chinese Journal of Veterinary Medicine, 2000,03:38-41. [4] Li Zhihong, Qi Yingying, Wang Jing. Introduction of commonly used anthelmintics in dogs [J]. Heilongjiang Journal of Animal Science and Veterinary Medicine, 2014,22:104-105. [5] Han Rongwei, Wang Jiaqi, Zheng Nan, Xu Xiaomin, Zhen Yunpeng, Qu Xueyin, Zhao Liansheng. Analysis of main risk factors of milk quality and safety Ⅲ. Veterinary drug residues [J]. Chinese Journal of Animal Science and Veterinary Medicine, 2012,04:1-10. [6] Wu ningpeng, ban fu guo, Zhou Hongxia, Guo Furong, Du Hong pigeon. Determination of benzimidazoles and their metabolites residues in milk by UPLC-MS/MS [J]. Chinese Journal of Veterinary Medicine, 2010,11:1-4. |
Use | broad-spectrum anthelmintics, for the nematodes of dogs, sheep, pigs, horses and other animals, both adults and larvae are highly active |
category | toxic substances |
toxicity grade | poisoning |
Acute toxicity | oral-rat LD50: 10605 mg/kg; Oral-rabbit LD50: 1250 mg/kg |
flammability hazard characteristics | flammable; Thermal decomposition of toxic nitrogen oxides, sulfur oxide smoke |
storage and transportation characteristics | warehouse ventilation and low temperature drying |
extinguishing agent | dry powder, foam, sand, carbon dioxide, water mist |