Cefozopran hydrochloride (SCE-2787 hydrochloride)
(Synonyms: 盐酸头孢唑兰; SCE-2787 hydrochloride) 目录号 : GC32139
Cefozopran Hydrochloride is the hydrochloride salt form of cefozopran, a semi-synthetic, broad-spectrum, fourth-generation cephalosporin with antibacterial activity.
Cas No.:113981-44-5
Sample solution is provided at 25 µL, 10mM.
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Quality Control & SDS
- View current batch:
- Purity: >98.50%
- COA (Certificate Of Analysis)
- SDS (Safety Data Sheet)
- Datasheet
Cefozopran Hydrochloride is the hydrochloride salt form of cefozopran, a semi-synthetic, broad-spectrum, fourth-generation cephalosporin with antibacterial activity.
[1] Tomonobu Sato, et al. Pediatr Blood Cancer . 2008 Dec;51(6):774-7.
| Cas No. | 113981-44-5 | SDF | |
| 别名 | 盐酸头孢唑兰; SCE-2787 hydrochloride | ||
| Canonical SMILES | [H]Cl.[O-]C(C(N1[C@@]2([H])[C@H](NC(/C(C3=NSC(N)=N3)=N\OC)=O)C1=O)=C(CS2)C[N+]4=C(C=CC=N5)N5C=C4)=O | ||
| 分子式 | C19H18ClN9O5S2 | 分子量 | 551.99 |
| 溶解度 | Water : ≥ 52 mg/mL (94.20 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 | 1.8116 mL | 9.0581 mL | 18.1163 mL |
| 5 mM | 0.3623 mL | 1.8116 mL | 3.6233 mL |
| 10 mM | 0.1812 mL | 0.9058 mL | 1.8116 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。
Stability of Cefozopran hydrochloride in aqueous solutions
Drug Dev Ind Pharm 2016;42(4):572-7.PMID:26079426DOI:10.3109/03639045.2015.1054834.
The influence of pH on the stability of Cefozopran hydrochloride (CZH) was investigated in the pH range of 0.44-13.00. Six degradation products were identified with a hybrid ESI-Q-TOF mass spectrometer. The degradation of CZH as a result of hydrolysis was a pseudo-first-order reaction. As general acid-base hydrolysis of CZH was not occurred in the solutions of hydrochloric acid, sodium hydroxide, acetate, borate and phosphate buffers, kobs = kpH because specific acid-base catalysis was observed. Specific acid-base catalysis of CZH consisted of the following reactions: hydrolysis of CZH catalyzed by hydrogen ions (kH+), hydrolysis of dications (k1H2O), monocations (k2H2O) and zwitter ions (k3H2O) and hydrolysis of zwitter ions (k1OH-) and monoanions (k2OH-) of CZH catalyzed by hydroxide ions. The total rate of the reaction was equal to the sum of partial reactions: [Formula: see text]. CZH similarly like other fourth generation cephalosporin was most stable at slightly acidic and neutral pH and less stable in alkaline pH. The cleavage of the β-lactam ring resulting from a nucleophilic attack on the carbonyl carbon in the β-lactam moiety is the preferred degradation pathway of β-lactam antibiotics in aqueous solutions.
DEVELOPMENT AND VALIDATION OF THE STABILITY-INDICATING LC-UV METHOD FOR DETERMINATION OF Cefozopran hydrochloride
Acta Pol Pharm 2015 May-Jun;72(3):423-7.PMID:26642650doi
The stability-indicating LC assay method was developed and validated for quantitative determination of Cefozopran hydrochloride (CZH) in the presence of degradation products formed during the forced degradation studies. An isocratic, RP-HPLC method was developed with C-18 (250 mm x 4.6 mm, 5 µm) column and 12 mM ammonium acetate-acetonitrile (92:8, v/v) as a mobile phase. The flow rate of the mobile phase was 1.0 mL/min. Detection wavelength was 260 not and temperature was 30°C. Cefozopran hydrochloride as other cephalosporins was subjected to stress conditions of degradation in aqueous solutions including hydrolysis, oxidation, photolysis and thermal degradation. The developed method was validated with regard to linearity, accuracy, precision, selectivity and robustness. The method was applied successfully for identification and determination of Cefozopran hydrochloride in pharmaceuticals and during kinetic studies.
Pharmacokinetics of cefozopran by single and multiple intravenous infusions in healthy Chinese volunteers
Drugs R D 2015 Mar;15(1):63-70.PMID:25644122DOI:10.1007/s40268-014-0075-3.
Background and objectives: Cefozopran is a parenteral cephalosporin with a broad spectrum of activity against Gram-positive and Gram-negative bacteria. The objective of this study was to evaluate the pharmacokinetics of cefozopran after single- and multiple-dose intravenous administration in healthy subjects, to provide clinical guidance in its application. Methods: This was a single-center, open-label, randomized, two-phase study conducted in 12 subjects. In the single-dose phase, subjects were randomly assigned to receive single doses of 0.5, 1.0 and 2.0 g of injected Cefozopran hydrochloride in a three-way crossover design with a 5-day washout period between administrations. In the multiple-dose phase, subjects received 2.0 g every 12 h for 4 days. Plasma and urine pharmacokinetic samples were assayed by a validated high-performance liquid chromatography-tandem mass spectrometry method. Pharmacokinetic parameters were calculated and analyzed statistically. Safety assessments were conducted throughout the study. Results: Twelve healthy volunteers (six males and six females) were enrolled and completed the study. Following a single 1-h intravenous infusion of 0.5, 1.0 or 2.0 g cefozopran, maximum plasma concentration (C max) and area under the plasma concentration-time curve from time zero to the time of the last measurable concentration (AUClast) increased in a dose-proportional manner. The mean half-life in plasma (t ½) was in the range of 1.20-2.80 h. Cefozopran was mainly excreted in its unchanged form, with no tendency for accumulation, via the kidney, and varied from 65.99 to 73.33 %. No appreciable accumulation of either drug occurred with multiple intravenous doses of cefozopran, and pharmacokinetic parameters for cefozopran were similar on days 1 and 4. No serious adverse events were reported. Adverse events were generally mild. Conclusion: Cefozopran was safe and well tolerated in the volunteers and displayed linear increases in the C max and AUClast values.
[Pharmacokinetics of injected Cefozopran hydrochloride in healthy volunteers]
Sichuan Da Xue Xue Bao Yi Xue Ban 2012 Sep;43(5):711-4.PMID:23230745doi
Objective: To study the pharmacokinetics of injected Cefozopran hydrochloride in healthy volunteers. Methods: 24 healthy volunteers were enrolled to receive low (0.5 g), middle (1.0 g), high (2.0 g) doses of single injection and multiple doses (1.0 g) injection of Cefozopran hydrochloride in an open randomized study. The plasma concentrations of cefozopran were determined by RP-HPLC. The DAS2.0 was used to fit the concentration-time data and to calculate the pharmacokinetic parameters. Results: The main pharmaeokinetic parameters for a single injection of low, middle and high doses of cefozopran were as follows: Cmax (48.27 +/- 9.84), (77.99 +/- 15.08) and (171.59 +/- 18.27) mg/L; Tmax (0.50 +/- 0.00), (0.51 +/- 0.02) and (0.51 + 0.02) h; AUCo-t (92.43 +/- 24.02), (152.45 +/- 16.26) and (341.03 +/- 44.16) mg x h/L; t1/2beta (1.97 +/- 0.19), (2.44 +/- 0.24) and (2.18 +/- 0.31) h, respectively. The main pharmacokinetic parameters for a multiple doses injection of cefozopran were as follows: Cmax (80.39 +/- 11.86) mg/L; Tmax (0.51 +/- 0.02) h; AUCo-t (159.74 +/- 15.06) mg x h/L; t1/2beta (2.55 +/- 0.55) h. The accumulative rate of cefozopran through urine pathway within 24 h was (89.4 +/- 15.5)%. The statistical analysis showed that Cmax, AUCo-t, and AUCo-infinity increased significantly with increased doses of injection (P < 0.05). Those parameters were linearly correlated with the doses of injection (r = 0.9950, 0.9960, 0.9963). However, dosage did not have an impact on other pharmacokinetic parameters (P > 0.05). No gender differences in the parameters were found (P > 0.05). Conclusion: Cefozopran hydrochloride performs a linear kinetics in healthy volunteers. The main pharmacokinetic parameters have no significant gender differences, and there is no drug accumulated with multiple doses of injection.
Influence of impurities on the specific optical rotation of cefozopran
Pharmazie 2012 Jul;67(7):590-4.PMID:22888513doi
The impurities of Cefozopran hydrochloride are analyzed using high-performance liquid chromatography (HPLC) with UV absorbance and optical rotation (OR) detection. The results show that the impurities can affect the specific optical rotation of the cefozopran product. Due to the different composition of impurities, the Chinese Cefozopran hydrochloride product has a specific optical rotation different from the Japanese product. The relationship between impurity limits and specific optical rotation of Cefozopran hydrochloride is revealed. The results provide a scientific rationale for setting the limit of specific optical rotation of Cefozopran hydrochloride.