Diloxanide
(Synonyms: 二氯尼特) 目录号 : GC60778
Diloxanide是一种抗原虫制剂(anti-protozoalagent)，可用于组织学内阿米巴原虫或者其他原虫感染引起的无症状肠道阿米巴病的研究。Diloxanide是一种活性的鲁米那抗阿米巴试剂，在胃肠道中，由其前药二氯尼特糠酸酯水解得来。
Cas No.:579-38-4
Sample solution is provided at 25 µL, 10mM.
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Quality Control & SDS
- View current batch:
- Purity: >95.00%
- COA (Certificate Of Analysis)
- SDS (Safety Data Sheet)
- Datasheet
Diloxanide is an anti-protozoal agent and can be used for the research of asymptomatic-intestinal amebiasis caused by Entamoeba histolytica or some other protozoal infections. Diloxanide is an active luminal amebicide and hydrolyzed in the gastrointestinal tract from its prodrug Diloxanide furoate [1].
Diloxanide is hydrolyzed in the gastrointestinal tract from its prodrug Diloxanide furoate[1].Diloxanide furoate (oral administraion; 75-200 mg/kg; 3 days; once daily) is effective at different dose of dayin weanling rats. At 200 mg/kg, 100% of the treated rats are cured and no amoebic lesions are observed in the caecum. Besides, 85%,77%, and 44.4% of the treated rats are cured at the dose 150 mg/kg, 100 mg/kg, and 75 mg/kg, respectively. The ED50 value is 77.9 mg/kg for this agent in rats[2].
[1]. DB08792 [2]. D K Chatterjee, et al. Antiamoebic activity of chonemorphine, a steroidal alkaloid, in experimental models. Parasitol Res. 1987;74(1):30-3.
| Cas No. | 579-38-4 | SDF | |
| 别名 | 二氯尼特 | ||
| Canonical SMILES | O=C(C(Cl)Cl)N(C)C1=CC=C(C=C1)O | ||
| 分子式 | C9H9Cl2NO2 | 分子量 | 234.08 |
| 溶解度 | 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 | 4.272 mL | 21.3602 mL | 42.7204 mL |
| 5 mM | 0.8544 mL | 4.272 mL | 8.5441 mL |
| 10 mM | 0.4272 mL | 2.136 mL | 4.272 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。
Cost-Effectiveness Analysis of Metronidazole versus Metronidazole with Diloxanide Furoate in the Treatment of Amoebiasis in Ethiopia
Clinicoecon Outcomes Res 2021 Jul 1;13:611-617.PMID:34234483DOI:10.2147/CEOR.S312821.
Introduction: Amoebiasis is one of the world's most prevalent and fatal infectious diseases. Several surveys revealed that amoebiasis is one of the most widely distributed diseases in Ethiopia. The combination of metronidazole with Diloxanide furoate represents a new approach for the treatment of the infection. Objective: This study aimed to analyze the cost-effectiveness of Diloxanide plus metronidazole compared with metronidazole alone in the treatment of amoebiasis in Ethiopia. Methods: An analytical decision model was used to analyze costs and effectiveness from a societal perspective by taking adult amoebic patients as the study population with a time horizon of two months. The potential impacts of uncertainty in single parameters were explored in one-way sensitivity analyses. Results: Metronidazole with Diloxanide had a higher cost and effect compared to metronidazole alone with an incremental cost-effectiveness ratio (ICER) of 8 US$ per amoebic case cured. The result was sensitive to the decrease in the effectiveness of metronidazole with Diloxanide. Conclusion: This study revealed the addition of Diloxanide to standard treatment to be a more effective and more costly treatment strategy. Therefore, a decision for choosing the medication should be based on the ability of patients to pay for the treatment.
Diloxanide furoate binary complexes with β-, methyl-β-, and hydroxypropyl-β-cyclodextrins: inclusion mode, characterization in solution and in solid state and in vitro dissolution studies
Pharm Dev Technol 2018 Sep;23(7):723-731.PMID:28758845DOI:10.1080/10837450.2017.1362435.
The purpose of this study was to investigate the effect on solubility and dissolution rate of binary complexes of β-(βCD), methyl-(MβCD) and hydroxypropyl-β-cyclodextrin (HPβCD) with Diloxanide furoate (DF). The complexation in solution was evaluated by phase solubility studies and 1H nuclear magnetic resonance (NMR). Enhanced water solubility of DF was obtained with the DF:MβCD system (61-fold). The mode of inclusion was supported by NMR experiments, which indicated that real inclusion complexes were formed between DF and MβCD or HPβCD. Solid state analysis was performed using infrared and thermal methods, which suggested the formation of true inclusion complexes of DF with two derivatized cyclodextrins, MβCD and HPβCD, and an exclusion complex with βCD when the systems were prepared by freeze-dried technique. Dissolution studies conducted in simulated gastric fluid (2 h) and subsequent simulated intestinal fluid (next 4 h) showed increased dissolution rate of DF from the freeze-dried systems with βCD, MβCD, and HPβCD (85; 77 and 75% of dissolved drug at 5 min, respectively) and 100% of the drug dissolved at 150 min for the three systems. The enhancement of the solubility and the dissolution of DF observed make these complexes promising candidates for the preparation of oral pharmaceutical formulations.
RPLC Determination of Tinidazole and Diloxanide Furoate in Tablets
Indian J Pharm Sci 2008 Sep;70(5):670-2.PMID:21394273DOI:10.4103/0250-474X.45415.
A simple reverse phase liquid chromatographic method has been developed and subsequently validated for simultaneous determination of tinidazole and Diloxanide furoate. The separation was carried out using a mobile phase consisting of acetonitrile, methanol and 0.2 M potassium dihydrogen phosphate (pH 5) in the ratio 2:3:2.The column used was SS Wakosil-II C-18 with a flow rate of 1 ml/min and UV detection at 282 nm. The described method was linear over a concentration range of 10-70 μg/ml and 10-90 μg/ml for the assay of Diloxanide furoate and tinidazole, respectively. The mean recovery was found to be 100-101% for tinidazole and 97-103% for Diloxanide furoate when determined at three different levels.
Diloxanide furoate for treating asymptomatic Entamoeba histolytica cyst passers: 14 years' experience in the United States
Clin Infect Dis 1992 Sep;15(3):464-8.PMID:1520794DOI:10.1093/clind/15.3.464.
Diloxanide furoate is used for treating asymptomatic or mildly symptomatic persons who are passing cysts of Entamoeba histolytica. The Centers for Disease Control (Atlanta) released this drug for 4,371 treatment courses from 1977 through 1990. Of the 2,815 report forms (64%) returned, 656 adverse effects were reported for 390 treatment courses (14%); they included flatulence (260), diarrhea or cramping (100), nausea (93), headache (17), disorientation or dizziness (9), and diplopia (4). During 1984-1990 uniform collection of data allowed more detailed analysis of toxicity and efficacy; fewer adverse effects were reported for persons aged 20 months to 10 years than for persons aged greater than 10 years (6 of 206 [3%] vs. 89 of 763 [12%], relative risk = 0.27, 95% confidence interval = 0.12 less than relative risk less than 0.61). Parasitological cures were achieved during 497 (86%) of the 575 treatment courses (52%) administered to asymptomatic persons who were passing cysts, who had received a full 10-day treatment course, and for whom results of a follow-up stool examination (greater than or equal to 14 days post-treatment) were available. Diloxanide furoate is safe and effective for treating asymptomatic persons who are passing E. histolytica cysts and may be particularly well tolerated in children.
Enhancement of site specific delivery of Diloxanide furoate as an antiamoebic drug
Eur J Pharm Sci 2016 Apr 30;86:50-7.PMID:26952868DOI:10.1016/j.ejps.2016.03.001.
The basic aim of the present research work is to deliver the Diloxanide furoate (DF) at specific area using pectin microspheres. The microspheres were prepared by spray drying method and cross-linked by zinc acetate. Different concentrations of polymer (pectin 0.5-3%) and cross-linking agent (0-3% w/v in a mixture of ethanol:water) are taken to optimize the entrapment efficiency, swelling behavior, size and first 6h in-vitro release in simulated gastric fluids. Optimized formulation was characterized in the terms of in-vitro release, in-vivo drug disposition in various organs and in the blood of Sprague-Dawley albino rats and in-vivo gastrointestinal tract transit behavior using X-ray imaging method on albino rabbits. Findings suggested that microspheres containing a concentration of polymer (2% w/v) have average size of 100-500 μm, entrapment efficiency 85.82 ± 0.5 with swelling index 18.77 ± 5.21. In-vitro results and in-vivo gastric transit behavior (using X-ray imaging) have shown no release in first 3-6h that proved the colon specific delivery of DF. The results also suggested that the above approach have not only site specific delivery, but it improves the conversion of active drug by increasing the enzyme mediated hydrolytic degradation of DF due to the presence of polysaccharide polymer:water gel complex.