Morinidazole
(Synonyms: 吗啉硝唑) 目录号 : GC32157
Morinidazole是一种新型的5-硝基咪唑抗菌药,用于治疗细菌感染,包括厌氧菌引起的阑尾炎盆腔炎(PID)。
Cas No.:92478-27-8
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
Morinidazole is a novel 5-nitroimidazole antimicrobial drug that undergoes extensive metabolism in humans via N+-glucuronidation and sulfation, for the treatment of bacterial infections including appendicitis and pelvic inflammatory disease (PID) caused by anaerobic bacteria.
[1]. Zhong K, et al. Effects of renal impairment on the pharmacokinetics of morinidazole: uptake transporter-mediated renal clearanceof the conjugated metabolites. Antimicrob Agents Chemother. 2014 Jul;58(7):4153-61.
| Cas No. | 92478-27-8 | SDF | |
| 别名 | 吗啉硝唑 | ||
| Canonical SMILES | OC(CN1C([N+]([O-])=O)=CN=C1C)CN2CCOCC2 | ||
| 分子式 | C11H18N4O4 | 分子量 | 270.29 |
| 溶解度 | DMSO : ≥ 100 mg/mL (369.97 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 | 3.6997 mL | 18.4986 mL | 36.9973 mL |
| 5 mM | 0.7399 mL | 3.6997 mL | 7.3995 mL |
| 10 mM | 0.37 mL | 1.8499 mL | 3.6997 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。
Effectiveness and safety of Morinidazole in the treatment of pelvic inflammatory disease: A multicenter, prospective, open-label phase IV trial
Front Med (Lausanne) 2022 Aug 3;9:888186.PMID:35991648DOI:10.3389/fmed.2022.888186.
Background: Antimicrobial resistance to metronidazole has emerged after several decades of worldwide use of the drug. The purpose of this study was to evaluate the effectiveness, safety and population pharmacokinetics of Morinidazole plus levofloxacin in adult women with pelvic inflammatory disease (PID). Methods: Patients in 30 hospitals received a 14-day course of 500 mg intravenous Morinidazole twice daily plus 500 mg of levofloxacin daily. A total of 474 patients were included in the safety analysis set (SS); 398 patients were included in the full analysis set (FAS); 377 patients were included in the per protocol set (PPS); 16 patients were included in the microbiologically valid (MBV) population. Results: The clinical resolution rates in the FAS and PPS populations at the test of cure (TOC, primary effectiveness end point, 7-30 days post-therapy) visit were 81.91 and 82.49% (311/377), respectively. There were 332 patients who did not receive antibiotics before treatment, and the clinical cure rate was 82.83%. Among 66 patients who received antibiotics before treatment, 51 patients were clinically cured 7-30 days after treatment, with a clinical cure rate of 77.27%. The bacteriological success rate in the MBV population at the TOC visit was 87.5%. The minimum inhibitory concentration (MIC) values of Morinidazole for use against these anaerobes ranged from 1 to 8 μg/mL. The rate of drug-related adverse events (AEs) was 27.43%, and no serious AEs or deaths occurred during the study. Conclusions: The study showed that treatment with a 14-day course of intravenous Morinidazole, 500 mg twice daily, plus levofloxacin 500 mg daily, was effective and safe. The results of this study were consistent with the results of a phase III clinical trial, which verified the effectiveness and safety of Morinidazole.
Efficacy and safety of Morinidazole in pelvic inflammatory disease: results of a multicenter, double-blind, randomized trial
Eur J Clin Microbiol Infect Dis 2017 Jul;36(7):1225-1230.PMID:28265816DOI:10.1007/s10096-017-2913-z.
This multicenter, double-blind, randomized, parallel-group, non-inferiority study compared the efficacy and safety of Morinidazole with those of ornidazole in women with pelvic inflammatory disease. Women from 18 hospitals in China received a 14-day course of either intravenous Morinidazole, 500 mg twice daily (n = 168), or intravenous ornidazole, 500 mg twice daily (n = 170). A total of 312 of 338 patients in the full analysis set (FAS) (92.3%) were included in the per protocol set (PPS) analyses, 61 (19.6%) of whom were included in the microbiologically valid (MBV) population. The clinical resolution rates in the PPS population at the test of cure (TOC, primary efficacy end point, 7-30 days post-therapy) visit were 96.86% (154/159) for Morinidazole and 96.73% (148/153) for ornidazole (95% CI: -3.79% to 4.03%). The bacteriological success rates in the MBV population at the TOC visit were 100% (32/32) for Morinidazole and 89.66% (26/29) for ornidazole (95% CI: -16.15% to 11.21%). Drug-related adverse events occurred less frequently with Morinidazole (32.74%, 55/168) than with ornidazole (47.06%, 80/170) (p < 0.01). For women with pelvic inflammatory disease, twice-daily Morinidazole for 14 days was clinically and bacteriologically as efficacious as twice-daily ornidazole for 14 days, while the former was associated with fewer drug-related adverse events than the latter.
Pharmacokinetics of single-dose Morinidazole in patients with severe renal impairment
Int J Clin Pharmacol Ther 2014 Feb;52(2):159-65.PMID:24290410DOI:10.5414/CP202000.
Objective: To evaluate the pharmacokinetics of Morinidazole in individuals with severe renal impairment (RI). Methods: This open-label Phase I study enrolled healthy volunteers and patients with severe RI aged 18 - 65 years. All subjects received a single infusion of sodium chloride injection with 500 mg Morinidazole. Plasma and urine concentration of Morinidazole and one of its metabolites (M4-1) were evaluated by using HPLC-UV and HPLC-MS/MS respectively. Pharmacokinetic parameters were calculated by Phoenix WinNonlin 6.0 software. Results: 22 individuals (healthy: n = 11, severe RI: n = 11) received Morinidazole. In both groups, maximum plasma concentration of Morinidazole was reached within 1 hour, while the tmax of M4-1 differed greatly. Both AUC0-t and AUC0-∿of Morinidazole were 1.4 times higher in patients with severe RI, while M4-1 were over 7 times higher than healthy groups. Renal excretion of unchanged Morinidazole was decreased by 65% in patients with RI, and M4-1 was decreased by 72%. Apparent correlation between CLcr and CL, AUC, t1/2 and CLr were seen in two groups. Conclusions: A single dose of 500 mg Morinidazole is well tolerated. Changes in pharmacokinetic parameters of Morinidazole and M4-1 are seen in patients with RI and may be clinically important.
Effects of rifampin and ketoconazole on pharmacokinetics of Morinidazole in healthy chinese subjects
Antimicrob Agents Chemother 2014 Oct;58(10):5987-93.PMID:25070100DOI:10.1128/AAC.03382-14.
Morinidazole, a 5-nitroimidazole antimicrobial drug, has been approved for the treatment of amoebiasis, trichomoniasis, and anaerobic bacterial infections in China. It was reported that drug-drug interaction happened after the coadministration of ornidazole, an analog of Morinidazole, and rifampin or ketoconazole. Therefore, we measured the plasma pharmacokinetics (PK) of Morinidazole and its metabolites in the healthy Chinese volunteers prior to and following the administration of rifampin or ketoconazole using liquid chromatography-tandem mass spectrometry (LC-MS/MS). The area under the concentration-time curve from time 0 to time t (AUC0-t) and maximum concentration in serum (Cmax) of Morinidazole were decreased by 28% and 23%, respectively, after 6 days of exposure to 600 mg of rifampin once daily; the Cmaxs of N(+)-glucuronides were increased by 14%, while their AUC0-ts were hardly changed. After 7 days of exposure to 200 mg of ketoconazole once daily, the AUC0-t and Cmax of the parent drug were not affected significantly. Cmaxs of N(+)-glucuronides were decreased by 23%; AUC0-ts were decreased by 14%. The exposure of sulfate conjugate was hardly changed after the coadministration of rifampin or ketoconazole. Using recombinant enzyme of UGT1A9 and human hepatocytes, the mechanism of the altered PK behaviors of Morinidazole and its metabolites was investigated. In human hepatocytes, ketoconazole dose dependently inhibited the formation of N(+)-glucuronides (50% inhibitory concentration [IC50], 1.5 μM), while rifampin induced the mRNA level of UGT1A9 by 28% and the activity of UGT1A9 by 53%. In conclusion, the effects of rifampin and ketoconazole on the plasma exposures of Morinidazole and N(+)-glucuronide are less than 50%; therefore, rifampin and ketoconazole have little clinical significance in the pharmacokinetics of Morinidazole.
Simultaneous determination of Morinidazole, its N-oxide, sulfate, and diastereoisomeric N(+)-glucuronides in human plasma by liquid chromatography-tandem mass spectrometry
J Chromatogr B Analyt Technol Biomed Life Sci 2012 Nov 1;908:52-8.PMID:23122401DOI:10.1016/j.jchromb.2012.09.017.
Morinidazole is a new third-generation 5-nitroimidazole antimicrobial drug. To investigate the pharmacokinetic profiles of Morinidazole and its major metabolites in humans, a liquid chromatography-tandem mass spectrometry method was developed and validated for simultaneous determination of Morinidazole, its N-oxide metabolite (M4-1), a sulfate conjugate (M7), and two diastereoisomeric N(+)-glucuronides (M8-1 and M8-2) in human plasma. A simple acetonitrile-induced protein precipitation was employed to extract five analytes and internal standard metronidazole from 50μL human plasma. To avoid the interference from the in-source dissociation of the sulfate and achieve the baseline-separation of diastereoisomeric N(+)-glucuronides, all the analytes were separated from each other with the mobile phase consisting of 10mM ammonium formate and acetonitrile using gradient elution on a Hydro-RP C(18) column (50mm×2mm, 4μm) with a total run time of 5min. The API 4000 triple quadrupole mass spectrometer was operated under the multiple reaction-monitoring mode using the electrospray ionization technique. The developed method was linear in the concentration ranges of 10.0-12,000ng/mL for Morinidazole, 1.00-200ng/mL for M4-1, 2.50-500ng/mL for M7, 3.00-600ng/mL for M8-1, and 10.0-3000ng/mL for M8-2. The intra- and inter-day precisions for each analyte met the accepted value. Results of the stability of Morinidazole and its metabolites in human plasma were also presented. The method was successfully applied to the clinical pharmacokinetic studies of Morinidazole injection in healthy subjects, patients with moderate hepatic insufficiency, and patients with severe renal insufficiency, respectively.