| Size | Price | |
|---|---|---|
| 500mg | ||
| 1g | ||
| Other Sizes |
| ADME/Pharmacokinetics |
Absorption, Distribution and Excretion
Chloramphenicol succinate has a high degree of interpatient variability, with a Tmax of 18 minutes to 3 hours. A 1g oral chloramphenicol succinate dose every 6-8 hours reaches a mean Cmax of 11.2µg/mL with a Tmax of 1 hour. 6-80% of chloramphenicol succinate is eliminated unchanged in the urine, though this is highly variable between patients. On average, 30% of chloramphenicol succinate is eliminated unchanged in the urine and 10% is eliminated as the active chloramphenicol in the urine. Chloramphenicol succinate has a volume of distribution of 0.2-3.1L/kg. Chloramphenicol succinate's total clearance is 530-540mL/min in patients with normal renal and hepatic function, and 354mL/min in patients with renal or hepatic dysfunction. Chloramphenicol succinate's renal clearance is 222-260mL/min in patients with normal renal and hepatic function, and 66mL/min in patients with renal or hepatic dysfunction. Metabolism / Metabolites Chloramphenicol succinate is hydrolyzed to chloramphenicol. The propane-diol moiety of chloramphenicol can be metabolised through a number of pathways including glucuronidation, sulfate conjugation, phosphorylation, acetylation, and oxidation. The dichloroacetate moiety can be metabolised through hydrolysis of the amide group and dechlorination. The nitro functional group can also be metabolised to an aryl amine and aryl amide metabolite. Biological Half-Life The half life of chloramphenicol succinate in patients with normal renal and hepatic function is 0.6-2.7h. |
|---|---|
| Toxicity/Toxicokinetics |
Protein Binding
Chloramphenicol succinate is 57-92% protein bound in plasma. |
| References |
|
| Additional Infomation |
Chloramphenicol succinate is a member of amphetamines and a hemisuccinate.
Chloramphenicol succinate is an ester prodrug of [chloramphenicol]. Chloramphenicol is a bacteriostatic antibiotic. Use of chloramphenicol succinate and chloramphenicol has decreased due to the risk of potentially fatal blood dyscrasias. Chloramphenicol succinate was granted FDA approval on 20 February 1959. Drug Indication Chloramphenicol succinate is indicated to treat serious and susceptible bacterial infections where less dangerous drugs are ineffective or contraindicated. Mechanism of Action Chloramphenicol succinate is hydrolyzed into the active chloramphenicol. Chloramphenicol resembles uridine-5'-phosphate. It binds to the residues A2451 and A2452 in the 23S rRNA of the 50S ribosomal subunit of _E. coli_, which prevents translation. Pharmacodynamics Chloramphenicol succinate is a prodrug of chloramphenicol, which binds to bacterial ribosomes and prevents translation. It has a narrow therapeutic index and a moderate duration of action. Patients should be counselled regarding the risk of serious fatal blood dyscrasias. |
| Molecular Formula |
C15H16CL2N2O8
|
|---|---|
| Molecular Weight |
423.19
|
| Exact Mass |
422.028
|
| CAS # |
3544-94-3
|
| Related CAS # |
Chloramphenicol succinate sodium;982-57-0
|
| PubChem CID |
656580
|
| Appearance |
Typically exists as solid at room temperature
|
| Density |
1.536g/cm3
|
| Boiling Point |
716.3ºC at 760mmHg
|
| Flash Point |
387ºC
|
| Index of Refraction |
1.589
|
| LogP |
2.688
|
| Hydrogen Bond Donor Count |
3
|
| Hydrogen Bond Acceptor Count |
8
|
| Rotatable Bond Count |
10
|
| Heavy Atom Count |
27
|
| Complexity |
546
|
| Defined Atom Stereocenter Count |
2
|
| SMILES |
OC(CCC(OC[C@H]([C@@H](C1=CC=C([N+]([O-])=O)C=C1)O)NC(C(Cl)Cl)=O)=O)=O
|
| InChi Key |
LIRCDOVJWUGTMW-ZWNOBZJWSA-N
|
| InChi Code |
InChI=1S/C15H16Cl2N2O8/c16-14(17)15(24)18-10(7-27-12(22)6-5-11(20)21)13(23)8-1-3-9(4-2-8)19(25)26/h1-4,10,13-14,23H,5-7H2,(H,18,24)(H,20,21)/t10-,13-/m1/s1
|
| Chemical Name |
4-[(2R,3R)-2-[(2,2-dichloroacetyl)amino]-3-hydroxy-3-(4-nitrophenyl)propoxy]-4-oxobutanoic acid
|
| Synonyms |
Kemicetine succinate CPSA Chloramphenicol succinate
|
| HS Tariff Code |
2934.99.9001
|
| Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month |
| Shipping Condition |
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
|
| Solubility (In Vitro) |
May dissolve in DMSO (in most cases), if not, try other solvents such as H2O, Ethanol, or DMF with a minute amount of products to avoid loss of samples
|
|---|---|
| Solubility (In Vivo) |
Note: Listed below are some common formulations that may be used to formulate products with low water solubility (e.g. < 1 mg/mL), you may test these formulations using a minute amount of products to avoid loss of samples.
Injection Formulations
Injection Formulation 1: DMSO : Tween 80： Saline = 10 : 5 : 85 (i.e. 100 μL DMSO stock solution → 50 μL Tween 80 → 850 μL Saline)(e.g. IP/IV/IM/SC) *Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH ₂ O to obtain a clear solution. Injection Formulation 2: DMSO : PEG300 ：Tween 80 : Saline = 10 : 40 : 5 : 45 (i.e. 100 μL DMSO → 400 μLPEG300 → 50 μL Tween 80 → 450 μL Saline) Injection Formulation 3: DMSO : Corn oil = 10 : 90 (i.e. 100 μL DMSO → 900 μL Corn oil) Example: Take the Injection Formulation 3 (DMSO : Corn oil = 10 : 90) as an example, if 1 mL of 2.5 mg/mL working solution is to be prepared, you can take 100 μL 25 mg/mL DMSO stock solution and add to 900 μL corn oil, mix well to obtain a clear or suspension solution (2.5 mg/mL, ready for use in animals). View More
Injection Formulation 4: DMSO : 20% SBE-β-CD in saline = 10 : 90 [i.e. 100 μL DMSO → 900 μL (20% SBE-β-CD in saline)] Oral Formulations
Oral Formulation 1: Suspend in 0.5% CMC Na (carboxymethylcellulose sodium) Oral Formulation 2: Suspend in 0.5% Carboxymethyl cellulose Example: Take the Oral Formulation 1 (Suspend in 0.5% CMC Na) as an example, if 100 mL of 2.5 mg/mL working solution is to be prepared, you can first prepare 0.5% CMC Na solution by measuring 0.5 g CMC Na and dissolve it in 100 mL ddH2O to obtain a clear solution; then add 250 mg of the product to 100 mL 0.5% CMC Na solution, to make the suspension solution (2.5 mg/mL, ready for use in animals). View More
Oral Formulation 3: Dissolved in PEG400 (Please use freshly prepared in vivo formulations for optimal results.) |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 2.3630 mL | 11.8150 mL | 23.6300 mL | |
| 5 mM | 0.4726 mL | 2.3630 mL | 4.7260 mL | |
| 10 mM | 0.2363 mL | 1.1815 mL | 2.3630 mL |
*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.
Calculation results
Working concentration： mg/mL；
Method for preparing DMSO stock solution： mg drug pre-dissolved in μL DMSO (stock solution concentration mg/mL). Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug.
Method for preparing in vivo formulation:：Take μL DMSO stock solution, next add μL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O，mix and clarify.
(1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
(2) Be sure to add the solvent(s) in order.
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