| Size | Price | |
|---|---|---|
| 500mg | ||
| 1g | ||
| Other Sizes |
| ADME/Pharmacokinetics |
Absorption, Distribution and Excretion
Despite high ocular surface concentrations, the mean systemic concentration after three daily doses is less than 0.5 ng/mL. This indicates that besifloxacin is almost not absorbed systemically, and the risk of systemic side effects is extremely low. Not Applicable Not Absorbed Systemically Not Applicable Metabolism/Metabolites No significant metabolism Biological Half-Life After multiple doses, the mean elimination half-life of besifloxacin in plasma is estimated to be 7 hours. |
|---|---|
| Toxicity/Toxicokinetics |
Effects During Pregnancy and Lactation
◉ Overview of Medication Use During Lactation The risk to a breastfeeding infant from a mother using becifloxacin eye drops is negligible. To significantly reduce the amount of medication that enters breast milk after instillation, press your finger against the tear duct at the corner of the eye for at least 1 minute, then blot away any excess medication with absorbent paper. ◉ Effects on Breastfed Infants No published information found as of the revision date. ◉ Effects on Lactation and Breast Milk No published information found as of the revision date. Protein Binding None |
| References | |
| Additional Infomation |
Besifloxacin belongs to the quinolone class of drugs. Besifloxacin is a fourth-generation fluoroquinolone ophthalmic antibiotic used to treat bacterial conjunctivitis. It was approved by the FDA on May 28, 2009. Besifloxacin is a quinolone antibacterial drug. Besifloxacin is a synthetic fourth-generation fluoroquinolone antibiotic with broad-spectrum antibacterial activity. After administration, besifloxacin targets and binds to bacterial DNA gyrase (an enzyme essential for bacterial DNA replication, transcription, and repair) and bacterial topoisomerase IV (an enzyme required for chromosomal DNA allocation during bacterial cell division), thereby inhibiting DNA replication, transcription, and repair, as well as cell division. See also: Besifloxacin hydrochloride (in salt form).
Indications Treatment of bacterial conjunctivitis. Bacterial isolates sensitive to besifloxacin include: CDC Group G Corynebacterium; Corynebacterium pseudodiphtheriae; Corynebacterium styloides; Haemophilus influenzae; Moraxella catarrhalis; Staphylococcus aureus; Staphylococcus epidermidis; Staphylococcus hominis; Staphylococcus ludens; Streptococcus pyogenes; Streptococcus salivarius; Streptococcus oralis; Streptococcus pneumoniae; Streptococcus salivarius FDA label Mechanism of Action Besifloxacin is a bactericidal fluoroquinolone antibiotic that inhibits bacterial enzymes, DNA gyrase, and topoisomerase IV. By inhibiting DNA gyrase, DNA replication, transcription, and repair are impaired. By inhibiting topoisomerase IV, chain dissociation during cell division is inhibited. Inhibition of these two targets also slows the development of resistance. Pharmacodynamics Besifloxacin tear concentrations are higher than the MIC90 (minimum inhibitory concentration) for common pathogens and can persist for 24 hours or longer. The average residence time in the conjunctiva is 4.7 hours. |
| Molecular Formula |
C19H21N3O3FCL
|
|---|---|
| Molecular Weight |
393.83974
|
| Exact Mass |
393.125
|
| CAS # |
141388-76-3
|
| Related CAS # |
Besifloxacin Hydrochloride;405165-61-9
|
| PubChem CID |
10178705
|
| Appearance |
Typically exists as solid at room temperature
|
| Density |
1.5±0.1 g/cm3
|
| Boiling Point |
607.0±55.0 °C at 760 mmHg
|
| Flash Point |
320.9±31.5 °C
|
| Vapour Pressure |
0.0±1.8 mmHg at 25°C
|
| Index of Refraction |
1.649
|
| LogP |
1.91
|
| Hydrogen Bond Donor Count |
2
|
| Hydrogen Bond Acceptor Count |
7
|
| Rotatable Bond Count |
3
|
| Heavy Atom Count |
27
|
| Complexity |
656
|
| Defined Atom Stereocenter Count |
1
|
| SMILES |
C1CCN(C[C@@H](C1)N)C2=C(C=C3C(=C2Cl)N(C=C(C3=O)C(=O)O)C4CC4)F
|
| InChi Key |
QFFGVLORLPOAEC-SNVBAGLBSA-N
|
| InChi Code |
InChI=1S/C19H21ClFN3O3/c20-15-16-12(18(25)13(19(26)27)9-24(16)11-4-5-11)7-14(21)17(15)23-6-2-1-3-10(22)8-23/h7,9-11H,1-6,8,22H2,(H,26,27)/t10-/m1/s1
|
| Chemical Name |
7-[(3R)-3-aminoazepan-1-yl]-8-chloro-1-cyclopropyl-6-fluoro-4-oxoquinoline-3-carboxylic acid
|
| 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 | 2.5391 mL | 12.6955 mL | 25.3910 mL | |
| 5 mM | 0.5078 mL | 2.5391 mL | 5.0782 mL | |
| 10 mM | 0.2539 mL | 1.2696 mL | 2.5391 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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