Chloramphenicol Succinate
(Synonyms: 琥珀酸氯霉素) 目录号 : GC43242A prodrug form of chloramphenicol
Cas No.:3544-94-3
Sample solution is provided at 25 µL, 10mM.
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Quality Control & SDS
- View current batch:
- Purity: >99.00%
- COA (Certificate Of Analysis)
- SDS (Safety Data Sheet)
- Datasheet
Chloramphenicol succinate is a water-soluble prodrug form of the antibiotic chloramphenicol. It is a substrate for succinate dehydrogenase (SDH) and is oxidized by human liver and rat liver and kidney mitochondria to release chloramphenicol in vitro. Chloramphenicol succinate reduces human leukocyte migration in vitro. In vivo, chloramphenicol succinate reduces E. coli growth in rabbit and rat models of pyelonephritis when administered at doses of 150 and 200 mg/kg, respectively. Chloramphenicol succinate (20 mg/kg) reduces infarct size in a porcine model of myocardial ischemia-reperfusion injury. Formulations containing chloramphenicol succinate have been used in the treatment of severe bacterial infections.
| Cas No. | 3544-94-3 | SDF | |
| 别名 | 琥珀酸氯霉素 | ||
| Canonical SMILES | O=C(CCC(O)=O)OC[C@@H](NC(C(Cl)Cl)=O)[C@H](O)C1=CC=C([N+]([O-])=O)C=C1 | ||
| 分子式 | C15H16Cl2N2O8 | 分子量 | 423.2 |
| 溶解度 | DMF: soluble,DMSO: soluble,Ethanol: soluble,Methanol: soluble | 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 | 2.3629 mL | 11.8147 mL | 23.6295 mL |
| 5 mM | 0.4726 mL | 2.3629 mL | 4.7259 mL |
| 10 mM | 0.2363 mL | 1.1815 mL | 2.3629 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。
Clinical pharmacokinetics of chloramphenicol and Chloramphenicol Succinate
Clin Pharmacokinet 1984 May-Jun;9(3):222-38.PMID:6375931DOI:10.2165/00003088-198409030-00004.
In recent years there has been a renewal of interest in chloramphenicol, predominantly because of the emergence of ampicillin-resistant Haemophilus influenzae, the leading cause of bacterial meningitis in infants and children. Three preparations of chloramphenicol are most commonly used in clinical practice: a crystalline powder for oral administration, a palmitate ester for oral administration as a suspension, and a succinate ester for parenteral administration. Both esters are inactive, requiring hydrolysis to chloramphenicol for anti-bacterial activity. The palmitate ester is hydrolysed in the small intestine to active chloramphenicol prior to absorption. Chloramphenicol Succinate acts as a prodrug, being converted to active chloramphenicol while it is circulating in the body. Various assays have been developed to determine the concentration of chloramphenicol in biological fluids. Of these, high-performance liquid chromatographic and radioenzymatic assays are accurate, precise, specific, and have excellent sensitivities for chloramphenicol. They are rapid and have made therapeutic drug monitoring practical for chloramphenicol. The bioavailability of oral crystalline chloramphenicol and chloramphenicol palmitate is approximately 80%. The time for peak plasma concentrations is dependent on particle size and correlates with in vitro dissolution and deaggregation rates. The bioavailability of chloramphenicol after intravenous administration of the succinate ester averages approximately 70%, but the range is quite variable. Incomplete bioavailability is the result of renal excretion of unchanged Chloramphenicol Succinate prior to it being hydrolysed to active chloramphenicol. Plasma protein binding of chloramphenicol is approximately 60% in healthy adults. The drug is extensively distributed to many tissues and body fluids, including cerebrospinal fluid and breast milk, and it crosses the placenta. Reported mean values for the apparent volume of distribution range from 0.6 to 1.0 L/kg. Most of a chloramphenicol dose is metabolised by the liver to inactive products, the chief metabolite being a glucuronide conjugate; only 5 to 15% of chloramphenicol is excreted unchanged in the urine. The elimination half-life is approximately 4 hours. Inaccurate determinations of the pharmacokinetic parameters may result by incorrectly assuming rapid and complete hydrolysis of Chloramphenicol Succinate. The pharmacokinetics of Chloramphenicol Succinate have been described by a 2-compartment model. The reported values for the apparent volume of distribution range from 0.2 to 3.1 L/kg.(ABSTRACT TRUNCATED AT 400 WORDS)
Chloramphenicol serum concentration falls during Chloramphenicol Succinate dosing
Clin Pharmacol Ther 1983 Mar;33(3):308-13.PMID:6825386DOI:10.1038/clpt.1983.38.
Chloramphenicol Succinate and chloramphenicol kinetics were examined on two occasions at steady state, separated by 2 to 17 days, in 10 pediatric patients on the same intravenous dose of Chloramphenicol Succinate. The steady-state peak serum concentration of Chloramphenicol Succinate fell from an average of 77.1 micrograms/ml during the first study to 42.2 micrograms/ml during the second. The steady-state peak serum concentration of chloramphenicol also decreased from an average of 27.8 micrograms/ml to 24.9 micrograms/ml. There was a marked decrease in the steady-state trough serum concentration of chloramphenicol, which averaged 8.4 micrograms/ml during the first and 5.3 micrograms/ml at the time of the second study. Mean area under the serum concentration-time curve (AUC) of Chloramphenicol Succinate decreased from 59.7 micrograms . hr/ml to 24.0 micrograms . hr/ml. The AUC of chloramphenicol averaged 105.7 micrograms . hr/ml at the time of the first and decreased to 79.5 micrograms . hr/ml during the second study. Mean percent decrease in the AUC of chloramphenicol was about 28% and occurred most substantially in patients with high AUCs during the first study. Mean elimination chloramphenicol half-life was 3.0 hr during the first study and fell to 2.3 hr at the time of the second study. Our data indicate that chloramphenicol serum concentration should be monitored frequently, especially in patients not responsive to a set dose.
Bioavailability and clearance of chloramphenicol after intravenous Chloramphenicol Succinate
Clin Pharmacol Ther 1981 Sep;30(3):368-72.PMID:7273601DOI:10.1038/clpt.1981.174.
Bioavailability of chloramphenicol and kinetics of Chloramphenicol Succinate and chloramphenicol were studied in 12 patients. Chloramphenicol Succinate, 25 mg/kg, was injected intravenously every 6 hr over 0.5 to 1 hr. Both the drug and the prodrug were analyzed by high-pressure liquid chromatography. Bioabailability of chlorampenicol ranged from 0.55 to 0.92 and total, renal, and nonrenal clearance from 6.81 to 98.22, 2.54 to 26.90, and 3.73 to 87.38 ml/m2/min, while clearances of Chloramphenicol Succinate ranged from 84.75 to 916.00 28.40 to 312.00, and 26.06 to 760.93 ml/m2/min. Urinary recovery of chloramphenicol was 3% to 25% and that of Chloramphenicol Succinate was 7% to 45%. Mean apparent volumes of distribution were 0.71 l/kg for chloramphenicol and 2.10 l/kg for Chloramphenicol Succinate and elimination half-lifes were 4.03 and 2.65 hr, respecitively. There were relationships between patient age and clearance of both drugs. Incomplete bioavailability of chloramphenicol and the more than 10-fold variability in clearance of both chloramphenicol and Chloramphenicol Succinate explain the need for individualizing doses to achieve thrapeutic effect and minimize the risk to toxicity.
Chloramphenicol Succinate pharmacokinetics in Macaca nemestrina: dose dependency study
J Pharmacol Exp Ther 1981 Nov;219(2):316-20.PMID:7288623doi
Chloramphenicol Succinate ester in doses equivalent to 25, 100 and 250 mg/kg of chloramphenicol were administered by rapid i.v. infusion in a randomized crossover fashion to five adolescent ((18-36 month) male Macaca nemestrina monkeys. Thirteen serum samples and all voided urine were collected over a 5- to 6-hr period. Urinary excretion of unhydrolyzed ester was independent of dose and averaged 26.3 +/- 6.2% of the administered dose. Dose dependency was observed for the elimination rate constant, total body clearance and metabolic clearance of Chloramphenicol Succinate. Dose dependency was also observed for the apparent volume of distribution, total body clearance, metabolic clearance and time to peak concentration of chloramphenicol. Although significant dose dependency of various pharmacokinetic parameters ws demonstrated, the peak chloramphenicol concentration and the elimination rate constant of chloramphenicol after administration of Chloramphenicol Succinate showed no significant dose-dependent changes. Therefore, peak chloramphenicol concentrations would be expected to reflect changes in dose in a linear or proportional manner.
Relative bioavailability of intravenous Chloramphenicol Succinate and oral chloramphenicol palmitate in infants and children
J Pediatr 1981 Dec;99(6):963-7.PMID:7310593DOI:10.1016/s0022-3476(81)80034-0.
The relative bioavailability of intravenously administered Chloramphenicol Succinate and orally administered chloramphenicol palmitate was compared in 18 children, age 2 months to 14 years. The area under the serum concentration vs time curve of chloramphenicol and urinary excretion of Chloramphenicol Succinate were determined in each child under steady-state conditions while receiving Chloramphenicol Succinate and again while receiving chloramphenicol palmitate. The mean AUC was significantly greater during oral therapy compared to intravenous therapy (110 vs 78 mg hr/L, P less than 0.001). The relative bioavailability of Chloramphenicol Succinate was 70% compared to chloramphenicol palmitate. This could be explained by the mean loss of 36% of the intravenous dose in the urine as unhydrolyzed Chloramphenicol Succinate. The intravenous dose of Chloramphenicol Succinate did not correlate with AUC (r = 0.193). However, there was a significant correlation between the oral dose of chloramphenicol palmitate and AUC (r = 0.429, P = 0.025). The bioavailability of orally administered chloramphenicol palmitate is superior to that of Chloramphenicol Succinate given intravenously. Furthermore, there is a greater correlation between dose and amount of active drug in the body when the oral preparation is used. Oral administration of chloramphenicol palmitate appears to offer significant therapeutic advantages in patients who can tolerate medication given orally.