Metronidazole Benzoate
(Synonyms: 苯酰甲硝唑; Benzoyl metronidazole) 目录号 : GC39660
An antibiotic and antiprotozoal agent
Cas No.:13182-89-3
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
Metronidazole benzoate is an antibiotic and antiprotozoal agent and ester form of metronidazole .1 It is active against P. asaccharolyticus, C. perfringens, C. septicum, B. fragilis, and B. thetaiotaomicron (MICs = 3.6, 7.3, 1.8, 7.3, and 7.3 ?M, respectively). Metronidazole reduces parasitemia in rats when cultured with T. congolense or T. b. gambiense prior to infection.2
1.Bowden, K., and Izadi, J.Prodrugs - Part 2. Acylbenzoate esters of metronidazoleEur. J. Med. Chem.32(12)995-1000(1998) 2.Ogunbanwo, J.A., Agbonlahor, D.E., Adamu, A., et al.Effects of anti-protozoal drugs and histopathological studies on trypanosome speciesFEMS Immunol. Med. Microbiol.30(1)73-83(2001)
| Cas No. | 13182-89-3 | SDF | |
| 别名 | 苯酰甲硝唑; Benzoyl metronidazole | ||
| Canonical SMILES | O=[N+](C1=CN=C(C)N1CCOC(C2=CC=CC=C2)=O)[O-] | ||
| 分子式 | C13H13N3O4 | 分子量 | 275.26 |
| 溶解度 | DMSO: 250 mg/mL (908.23 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 | 3.6329 mL | 18.1646 mL | 36.3293 mL |
| 5 mM | 0.7266 mL | 3.6329 mL | 7.2659 mL |
| 10 mM | 0.3633 mL | 1.8165 mL | 3.6329 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。
Effects of commercial metronidazole and Metronidazole Benzoate suspensions on food intake in chinchillas
J Small Anim Pract 2021 Mar;62(3):174-177.PMID:33260253DOI:10.1111/jsap.13276.
Objectives: To evaluate if commercially available metronidazole and Metronidazole Benzoate suspensions cause a reduction in food intake in healthy chinchillas and if the reduction in food intake is dose-dependent. Materials and methods: Twelve chinchillas were used in a randomised, controlled, blinded, complete-crossover study. All treatments were administered orally every 12 hours for 3 days. Metronidazole (125 mg/mL) was administered at 20 mg/kg and Metronidazole Benzoate (25 mg/mL) was administered at 20 and 10 mg/kg. Food intake was recorded daily. The washout period between treatments was at least 14 days. Results: At 20 mg/kg PO q12h administration of both commercial suspensions resulted in a significant reduction of food intake. The greatest mean reduction in food intake occurred after 2 to 3 days of drug administration (metronidazole: -54 ± 25%; Metronidazole Benzoate: -44 ± 36%). After administration of Metronidazole Benzoate at 10 mg/kg PO q12h, the reduction in food intake was significantly less pronounced (-24 ± 36%), suggesting that negative effect of metronidazole on food intake in chinchillas is dose-dependent. Variation in metronidazole-induced food intake reduction differed widely between individual chinchillas. Clinical significance: The oral administration of commercial metronidazole and Metronidazole Benzoate suspensions results in a dose-dependent clinically relevant reduction in food intake in chinchillas. Metronidazole should be used cautiously in this species and food intake should be monitored during treatment. Future studies are needed in order to determine if metronidazole at 10 mg/kg q12h is an effective therapeutic dosage in chinchillas.
Novel copper complexes of metronidazole and Metronidazole Benzoate: synthesis, characterization, biological and computational studies
J Biomol Struct Dyn 2022 Aug;40(12):5446-5461.PMID:33427586DOI:10.1080/07391102.2020.1871072.
Synthesis and characterization of novel copper complexes of Metronidazole Benzoate (MTZ Benz), metronidazole (MTZ) in the presence of another ligand; dichloroacetic acid (DCA) were compared and reported in the present work. Different bacterial and fungus strains were ascertained to evaluate the biological potency of the synthesized complexes, that is, Escherichia coli, Bordetella bronceptica, Staphylococcus epidermidis, Baccilus pumilus, Staphylococcus aureus and yeast strain Saccharomyces cerevisiae. Agar diffusion method was employed to investigate in vitro antibacterial activities of the synthesized metal complexes and the tested parent ligands. α-Amylase and α-glucosidase inhibition studies of the synthesized complexes were also carried out. The antibacterial potential and α-amylase and α-glucosidase inhibition studies of complexes were further investigated by molecular docking studies, which supported the experimental results. Significant α-amylase and α-glucosidase inhibition activities were shown by the synthesized complexes. S-1 and S-5 were found to be most inhibitors of α-amylase and α-glucosidase having IC50 42.50, 44.80 and 4.52 µg/mL, 4.80 µg/mL, respectively. The newly synthesized copper complexes showed overall better biological activities compared to each parent ligands used.Communicated by Ramaswamy H. Sarma.
New Miniaturized Disposable Screen-Printed Microchip Integrated with Molecularly Imprinted Polymer for Metronidazole Benzoate Drug Detection
Micromachines (Basel) 2022 Nov 29;13(12):2107.PMID:36557405DOI:10.3390/mi13122107.
A novel potentiometric microelectrode incorporating a molecularly imprinted polymer (MIP) was fabricated, characterized, and successfully applied to the recognition and quantification of the drug, Metronidazole Benzoate. The elaborated MIP-based sensor was realized by thermal polarization, using Metronidazole Benzoate as the template material, 1-vinyl-2-pyrrolidine (VP) as a functional monomer, and ethylene glycol dimethacrylate (EGDMA) as the cross-linking agent in the presence of benzoyl peroxide as the initiator. The MIP-based sensor exhibited a super-Nernstian response (61.5 ± 0.5, mV/decade) covering the linear concentration range of 1 × 10-8-1 × 10-3 mole L-1 of Metronidazole Benzoate with a fast response time (≤10, s.) and detection limit of 7 × 10-9 mole L-1. The microchip showed high selectivity toward the template drug molecule in the presence of many investigated interfering species. The chip electrode was successfully used in the quantification of Metronidazole Benzoate in some real biological samples with high accuracy (recovery, 95.4%) and precision (RSD, 1.5). Moreover, the merits offered by the elaborated MIP-based MB microchip assembly include small size, miniaturization, integration, and consequently, automation feasibility.
The design of novel Metronidazole Benzoate structures: exploring stoichiometric diversity
Acta Crystallogr C Struct Chem 2019 May 1;75(Pt 5):483-495.PMID:31062703DOI:10.1107/S2053229619003838.
The use of supramolecular synthons as a strategy to control crystalline structure is a crucial factor in developing new solid forms with physicochemical properties optimized by design. However, to achieve this objective, it is necessary to understand the intermolecular interactions in the context of crystal packing. The feasibility of a given synthon depends on its flexibility to combine the drug with a variety of coformers. In the present work, the imidazole-hydroxy synthon is investigated using as the target molecule benzoylmetronidazole [BZMD; systematic name 2-(2-methyl-5-nitro-1H-imidazol-1-yl)ethyl benzoate], whose imidazole group seems to be a suitable acceptor for hydrogen bonds. Thus, coformers with carboxylic acid and phenol groups were chosen. According to the availability of binding sites presented in the coformer, and considering the proposed synthon and hydrogen-bond complementarity as major factors, different drug-coformer stoichiometric ratios were explored (1:1, 2:1 and 3:1). Thirteen new solid forms (two salts and eleven cocrystals) were produced, namely BZMD-benzoic acid (1/1), C13H13N3O4·C7H6O2, BZMD-β-naphthol (1/1), C13H13N3O4·C10H8O, BZMD-4-methoxybenzoic acid (1/1), C13H13N3O4·C8H8O3, BZMD-3,5-dinitrobenzoic acid (1/1), C13H13N3O4·C7H4N2O6, BZMD-3-aminobenzoic acid (1/1), C13H13N3O4·C7H7NO2, BZMD-salicylic acid (1/1), C13H13N3O4·C7H6O3, BZMD-maleic acid (1/1) {as the salt 1-[2-(benzoyloxy)ethyl]-2-methyl-5-nitro-1H-imidazol-3-ium 3-carboxyprop-2-enoate}, C13H14N3O4+·C4H3O4-, BZMD-isophthalic acid (1/1), C13H13N3O4·C8H6O4, BZMD-resorcinol (2/1), 2C13H13N3O4·C6H6O2, BZMD-fumaric acid (2/1), C13H13N3O4·0.5C4H4O4, BZMD-malonic acid (2/1), 2C13H13N3O4·C3H2O4, BZMD-2,6-dihydroxybenzoic acid (1/1) {as the salt 1-[2-(benzoyloxy)ethyl]-2-methyl-5-nitro-1H-imidazol-3-ium 2,6-dihydroxybenzoate}, C13H14N3O4+·C7H5O4-, and BZMD-3,5-dihydroxybenzoic acid (3/1), 3C13H13N3O4·C7H6O4, and their crystalline structures elucidated, confirming the robustness of the selected synthon.
Stability of Metronidazole Benzoate in SyrSpend SF One-Step Suspension System
Int J Pharm Compd 2008 Nov-Dec;12(6):558-64.PMID:23969934doi
The objective of this study was to determine the stability of Metronidazole Benzoate suspension in SyrSpend SF One-Step Suspension system. The studied samples were packaged in 60-mL amber plastic prescription bottles, which were stored protected from light under controlled environmental conditions for a period of 360 days. Stability of Metronidazole Benzoate suspension in SyrSpend SF was assessed based on retention of initial color or appearance, pH of suspension, and recovery of Metronidazole Benzoate from the packaged product. Duplicate samples were evaluated at each predefined time interval. An assay method by high performance liquid chromatography was validated for its specificity and stability-indicating characteristscs through a forced-degradation study, and was used in Metronidazole Benzoate assay. Metronidazole Benzoate in SyrSpend SF retained its normal appearance of an opaque suspension, with acceptable pH values ranging from 4.43 to 4.53 (range 4.45 +/- 0.5). Recovery of Metronidazole Benzoate at subsequent time points was within 90% to 110% of inital concentration for samples stored at refrigerated temperature (2 deg C to 8 deg C), and ambient condition (25 deg C/60% relative humidity), with no detectable changes in chromatographic profile for most tested samples. The rates of change in potency for Metronidazole Benzoate were determined under the assumptions of first-order kinetics, and the time to reach 90% to 110% initial concentration was determined to be 366 days for samples in ambient storage, or 716 days for samples stored at refrigerated temperature. Metronidazole Benzoate in SyrSpend SF, which was packaged in amber plastic prescription bottles, is stable for at least 1 year when stored protected from light at ambient condition (25 deg C/60% relative humidity). The shelf life for this product may be extended to 2 years when stored at refrigerated temperature.