Chloramphenicol succinate sodium
(Synonyms: 氯霉素琥珀酸钠) 目录号 : GC39661
A prodrug form of chloramphenicol
Cas No.:982-57-0
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
Chloramphenicol succinate is a water-soluble prodrug form of the antibiotic chloramphenicol.1 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.2 Chloramphenicol succinate reduces human leukocyte migration in vitro.3 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.4 Chloramphenicol succinate (20 mg/kg) reduces infarct size in a porcine model of myocardial ischemia-reperfusion injury.5 Formulations containing chloramphenicol succinate have been used in the treatment of severe bacterial infections.
1.Ceriotti, G., Defranceschi, A., De Carneri, I., et al.Chloramphenicol succinate, a water-soluble derivative of chloramphenicolFarmaco Sci.9(1)21-38(1954) 2.Ambekar, C.S., Lee, J.S., Cheung, B.M., et al.Chloramphenicol succinate, a competitive substrate and inhibitor of succinate dehydrogenase: Possible reason for its toxicityToxicol. In Vitro18(4)441-447(2004) 3.Forsgren, A., and Schmeling, D.Effect of antibiotics of chemotaxis of human leukocytesAntimicrob. Agents Chemother.11(4)590-584(1977) 4.Prat, V., Konickova, L., Ritzerfeld, W., et al.Effect of chloramphenicol against different E. coli strains in vitro and in experimental pyelonephritisArzneimittelforschung18(9)1123-1127(1968) 5.Sala-Mercado, J.A., Wider, J., Undyala, V.V., et al.Profound cardioprotection with chloramphenicol succinate in the swine model of myocardial ischemia-reperfusion injuryCirculation122(11 Suppl)S179-S184(2010)
| Cas No. | 982-57-0 | SDF | |
| 别名 | 氯霉素琥珀酸钠 | ||
| Canonical SMILES | O=C(OC[C@@H](NC(C(Cl)Cl)=O)[C@H](O)C1=CC=C([N+]([O-])=O)C=C1)CCC([O-])=O.[Na+] | ||
| 分子式 | C15H15Cl2N2NaO8 | 分子量 | 445.18 |
| 溶解度 | DMSO: 250 mg/mL (561.57 mM) | 储存条件 | -20°C, protect from light, stored under argon |
| 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 | 2.2463 mL | 11.2314 mL | 22.4628 mL |
| 5 mM | 0.4493 mL | 2.2463 mL | 4.4926 mL |
| 10 mM | 0.2246 mL | 1.1231 mL | 2.2463 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。
Absorption of Chloramphenicol sodium succinate after intramuscular administration in children
N Engl J Med 1985 Aug 15;313(7):410-4.PMID:4022068DOI:10.1056/NEJM198508153130703.
Because it is thought that chloramphenicol is poorly absorbed after intramuscular administration, we compared blood levels of chloramphenicol after intramuscular administration with those after intravenous administration in children with a variety of diagnoses. Fifty-seven children were studied on 62 occasions while they were receiving Chloramphenicol sodium succinate (25 mg of chloramphenicol per kilogram of body weight) intramuscularly every six hours. The peak level of chloramphenicol was 19.5 +/- 5.99 micrograms per milliliter (mean +/- S.D.) in 11 children after the first dose and 31.4 +/- 12.99 micrograms per milliliter in 51 children after two or more doses. The lowest peak level after intramuscular administration was 13 micrograms per milliliter, which is in the therapeutic range of 10 to 30 micrograms per milliliter. Thirteen children were studied on 17 occasions while they were receiving Chloramphenicol sodium succinate (25 mg of chloramphenicol per kilogram) intravenously every six hours. The peak level of chloramphenicol was 19.4 +/- 6.37 micrograms per milliliter in eight children after the first dose and 28.2 +/- 11.09 micrograms per milliliter in nine children after two or more doses. The area under the serum level curve was not significantly different after intramuscular and intravenous administration. We conclude that Chloramphenicol sodium succinate is well absorbed after intramuscular administration. This route is cheaper, it demands less staff time, and it does not carry the risks of sepsis and overhydration associated with intravenous therapy.
Pharmacokinetics of intravenous Chloramphenicol sodium succinate in adult patients with normal renal and hepatic function
J Pharmacokinet Biopharm 1982 Dec;10(6):601-14.PMID:7182457DOI:10.1007/BF01062543.
The pharmacokinetics of chloramphenicol (CAP) and total chloramphenicol succinate (CAPS) were studied in eight hospitalized adult patients with normal renal and hepatic function receiving intravenous Chloramphenicol sodium succinate therapy. The steady-state peak concentrations of CAP (8.4-26.0 micrograms/ml) occurred at an average of 18.0 min (range 5.4-40.2) after cessation of the Chloramphenicol sodium succinate infusion. Unhydrolyzed CAPS prodrug, representing 26.0 +/- 7.0% of the dose, was recovered unchanged in the urine indicating that the bioavailability of CAP from a dose of intravenous chloramphenicol succinate is not complete. A pharmacokinetic model was developed for simultaneous fitting of CAP and CAPS plasma concentration data. Pharmacokinetic parameters determined by simultaneous fitting were: V, 0.81 +/- 0.18 liters/kg; t1/2, 3.20 +/- 1.02 hr; CLB, 3.21 +/- 1.27 ml/min/kg for chloramphenicol; and V, 0.38 +/- 0.13 liters/kg; t1/2, 0.57 +/- 0.12 hr; CLB, 7.72 +/- 1.87 ml/min/kg for total chloramphenicol succinate.
Chloramphenicol sodium succinate kinetics in critically ill patients
Clin Pharmacol Ther 1980 Jul;28(1):69-77.PMID:7389257DOI:10.1038/clpt.1980.133.
Chloramphenicol sodium succinate (SCAP) kinetics were studied in 10 critically ill patients. High-performance liquid chromatography was used to assay SCAP and chloramphenicol (CAP) in serum and urine. Total body (ClTB), metabolic (ClM), and renal (ClR) clearances of SCAP were variable. Correlations were found between creatinine clearance (Clcr) and ClTB, ClM, and ClR of SCAP (r = 0.92, p less than 0.001; r = 0.84, p less than 0.005; and r = 0.84, p less than 0.005). Recovery of SCAP in the urine also demonstrated large interpatient variability. Between 6.5% and 43.5% of the SCAP dose was recovered in the urine of 6 patients. This variability could not be explained by incomplete urine collection or by differences in renal function. Renal excretion of SCAP was shown to influence CAP serum levels. CAP ClTB was diminished, but no relationship was found between routine liver function studies and CAP ClTB. Therefore we caution the use of such relationships in using CAP in critically ill patients.
Pharmacokinetic, residue and irritation aspects of Chloramphenicol sodium succinate and a chloramphenicol base formulation following intramuscular administration to ruminants
Vet Q 1986 Jul;8(3):224-32.PMID:3750804DOI:10.1080/01652176.1986.9694046.
The disposition of chloramphenicol (CAP) and of its glucuronide metabolite in plasma and milk was studied following a single intramuscular injection of a chloramphenicol base formulation (Amicol Forte; product A) and of Chloramphenicol sodium succinate (product B) to dairy cows. The dose applied of both formulations was equivalent to 50 mg CAP base/kg body weight. The HPLC determined CAP concentrations were microbiologically active. Product A revealed 30% higher plasma CAP peak concentrations (13.0 vs 9.0 micrograms/ml) and 36% larger areas under the plasma concentration-time curves than product B, whereas their absorption and elimination half-lives were of the same order of magnitude. In the onset phase (during 4 h p.i.) unhydrolysed CAP sodium succinate could be detected in plasma and the glucuronide fraction was 26% of the parent drug. After 25 h p.i. the glucuronide fraction equalled that of the parent drug. The maximum CAP concentration in milk was for product B equal to, and for product A 80% of, the CAP plasma concentration. In milk no chloramphenicol glucuronide metabolites could be detected. HPLC methods for detecting ultra-trace CAP concentrations in edible tissues were developed by the employment of extraction with or without a clean-up procedure. Seven days after i.m. administration of product A and B to calves, the CAP residue concentrations in the kidney, liver, and muscle were less than 2 nanogram/g tissue. Traces of CAP residues could be still found at the injection site and in the urine. Chloramphenicol sodium succinate (product B) caused extensive tissue irritation at the injection site, while in the case of product A the irritation was limited.(ABSTRACT TRUNCATED AT 250 WORDS)
Pharmacokinetics of chloramphenicol following administration of intravenous and subcutaneous Chloramphenicol sodium succinate, and subcutaneous chloramphenicol, to koalas (Phascolarctos cinereus)
J Vet Pharmacol Ther 2013 Oct;36(5):478-85.PMID:23157306DOI:10.1111/jvp.12024.
Clinically normal koalas (n = 19) received a single dose of intravenous (i.v.) Chloramphenicol sodium succinate (SS) (25 mg/kg; n = 6), subcutaneous (s.c.) chloramphenicol SS (60 mg/kg; n = 7) or s.c. chloramphenicol base (60 mg/kg; n = 6). Serial plasma samples were collected over 24-48 h, and chloramphenicol concentrations were determined using a validated high-performance liquid chromatography assay. The median (range) apparent clearance (CL/F) and elimination half-life (t(1/2)) of chloramphenicol after i.v. chloramphenicol SS administration were 0.52 (0.35-0.99) L/h/kg and 1.13 (0.76-1.40) h, respectively. Although the area under the concentration-time curve was comparable for the two s.c. formulations, the absorption rate-limited disposition of chloramphenicol base resulted in a lower median C(max) (2.52; range 0.75-6.80 μg/mL) and longer median tmax (8.00; range 4.00-12.00 h) than chloramphenicol SS (C(max) 20.37, range 13.88-25.15 μg/mL; t(max) 1.25, range 1.00-2.00 h). When these results were compared with susceptibility data for human Chlamydia isolates, the expected efficacy of the current chloramphenicol dosing regimen used in koalas to treat chlamydiosis remains uncertain and at odds with clinical observations.