| Size | Price | |
|---|---|---|
| 500mg | ||
| 1g | ||
| Other Sizes |
| ADME/Pharmacokinetics |
Absorption, Distribution and Excretion
The inter-individual variability of chloramphenicol succinate is significant, with a time to peak concentration (Tmax) ranging from 18 minutes to 3 hours. Oral administration of 1 gram of chloramphenicol succinate every 6-8 hours results in a mean peak plasma concentration (Cmax) of 11.2 µg/mL, with a time to peak concentration of 1 hour. 6-80% of chloramphenicol succinate is excreted unchanged in the urine, but this varies considerably between individuals.On average, 30% of chloramphenicol succinate is excreted unchanged in the urine, and 10% is excreted as active chloramphenicol. The volume of distribution of chloramphenicol succinate is 0.2-3.1 L/kg. In patients with normal renal and hepatic function, the total clearance of chloramphenicol succinate is 530-540 mL/min; in patients with renal or hepatic impairment, the total clearance is 354 mL/min. In patients with normal renal and hepatic function, the renal clearance of chloramphenicol succinate is 222-260 mL/min; in patients with renal or hepatic impairment, the renal clearance is 66 mL/min. Metabolism/Metabolites Chloramphenicol succinate is hydrolyzed to chloramphenicol. The propylene glycol moiety of chloramphenicol can be metabolized through multiple pathways, including glucuronidation, sulfate conjugation, phosphorylation, acetylation, and oxidation. The dichloroacetic acid moiety can be metabolized through amide hydrolysis and dechlorination. The nitro functional group can also be metabolized to aromatic amines and aromatic amide metabolites. Biological Half-Life The half-life of chloramphenicol succinate in patients with normal renal and hepatic function is 0.6-2.7 hours. |
|---|---|
| Toxicity/Toxicokinetics |
Protein Binding
Chloramphenicol succinate has a protein binding rate of 57-92% in plasma. |
| References |
|
| Additional Infomation |
Chloramphenicol succinate belongs to the amphetamine class of drugs and is a hemisuccinate. Chloramphenicol succinate is an ester prodrug of chloramphenicol. Chloramphenicol is a bacteriostatic antibiotic. Due to the risk of potentially fatal blood disorders, the use of chloramphenicol succinate and chloramphenicol has been reduced. Chloramphenicol succinate was approved by the U.S. Food and Drug Administration (FDA) on February 20, 1959. Indications: Chloramphenicol succinate is indicated for the treatment of severe infections caused by susceptible bacteria that are unresponsive to or contraindicated with other low-risk medications. Mechanism of Action: Chloramphenicol succinate is hydrolyzed to the active ingredient, chloramphenicol. The structure of chloramphenicol is similar to uridine-5'-phosphate. It binds to residues A2451 and A2452 of the 23S rRNA of the 50S ribosomal subunit of E. coli, thereby preventing translation. Pharmacodynamics: Chloramphenicol succinate is a prodrug of chloramphenicol that binds to bacterial ribosomes and prevents translation. It has a narrow therapeutic index and a moderate duration of action. Patients should be informed of the risk of developing serious and fatal blood disorders.
|
| 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.
Products are for research use only; We do not sell to patients
Copyright 2020 InvivoChem LLC | All Rights Reserved
