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Other Sizes |
ADME/Pharmacokinetics |
Absorption, Distribution and Excretion
A method to estimate the total and regional deposition of disodium disulfite after aerosol inhalation was developed. Original particle sizes between 0.1 and 10 um were used. The particle size changes with the humidity of the environment because of the hygroscopic properties of the disulfite. It shows high deposition values of about 1/1000 of the inhaled particle mass/sq cm in the nasal region, values of about 1/100,000/sq cm in the tracheobronchial airways and a mean surface deposition in the pulmonary region which is a factor of 10,000 smaller than in the nose. The findings correspond to pathological effects found in animal inhalation studies. Metabolism / Metabolites Sulfites are generated in the human body by processing of the sulfur-containing amino acids, cysteine and methionine. Endogenous sulfite is maintained at a low, steady-state concentration by a mitochondrial enzyme, sulfite oxidase, that promotes the oxidation of sulfite to sulfate that is excreted in the urine. Sulfites can also be metabolized to thiosulfates (enzymatic reaction of sulfite with 3-mercaptopyruvate) or S-sulfonate compounds (nonenzymatic reaction with disulfide bonds). Thiosulfate and S-sulfonate were detected at very low concentrations in the urine of normal humans or rats, but were excreted in large amounts by those deficient in sulfite oxidase. /Sulfites/ Sulfite that enters the body via ingestion, inhalation, or injection is metabolized by sulfite oxidase to sulfate. Oral dose studies using dogs and rats and intravenous (IV) dose studies using rabbits, rats, and rhesus monkeys, demonstrated rapid metabolic clearance. In all species = 10% of the administered dose was excreted unchanged in the urine. One difference in the metabolism kinetics of exogenous sulfite versus endogenous sulfite is that hepatic oxidation of exogenous sulfite (at least in rats) is diffusion limited. The liver metabolizes a constant fraction of sulfite it receives, but a finite amount will pass through the organ and enter the systemic circulation. /Sulfite/ |
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Toxicity/Toxicokinetics |
Interactions
Sodium metabisulfite (Na2S2O5) is used as an antioxidant and antimicrobial agent in a variety of drugs and functions as a preservative in many food preparations. In addition to their antioxidant activity, sulfites oxidize to sulfite radicals (SO3-) initiating lipid peroxidation. This study was performed to elucidate the effect of subchronic Na2S2O5 (520 mg/kg/day) ingestion on hepatic and renal antioxidant enzyme activities and lipid peroxidation in albino rats. The antioxidant effect of L-carnitine was also tested in rats treated with Na2S2O5. Plasma uric acid levels were monitored in all rats included in the study. Malondialdehyde (MDA) levels significantly increased in Na2S2O5 treated rats vs. controls, with kidney values of 2.21+/-0.21 vs. 1.22+/-0.35 and liver values of 79.85+/-19.5 vs. 31.36+/-5.0 nmol/mg protein, respectively. Selenium-glutathione peroxidase (GPx) activity was significantly increased in Na2S2O5 treated rats vs. controls, with kidney values of 38.22+/-2.21 vs. 8.09+/-0.76 and liver values of 31.11+/-6.37 vs. 11.70+/-1.02 U/g protein, respectively. Sodium metabisulfite treatment increased plasma uric acid levels in rats that were included in the study. No protective effect of L-carnitine was observed against lipid peroxidation in both liver and kidneys of rats treated with Na2S2O5. The presented data confirm the prooxidant activity of sulfites and suggest that increased GPx activity and plasma uric acid levels may partially reduce the observed renal and hepatocellular oxidative damage caused via the ingestion of sulfites. Sodium metabisulfite is incompatible with chloramphenicol owing to a more complex reaction. /Sodium metabisulfite/ also inactivates cisplatin in solution. Sodium metabisulfite reacts with sympathomimetics and other drugs that are ortho- or para-hydroxybenzyl alcohol derivatives to form sulfonic acid derivatives possessing little or no pharmacological activity. The most important drugs subject to this inactivation are epinephrine (adrenaline) and its derivatives. The aim of the present experiment was to test the effects of a wet preservation of triticale contaminated mainly with deoxynivalenol (DON) with sodium metabisulphite (Na2S2O5, SBS) on growth performance, liver function, clinical-chemical plasma parameters and organ histopathology of piglets. For this purpose both the uncontaminated control triticale and the DON contaminated triticale were included in the piglet diet either untreated (CON, FUS) or SBS-treated (CON-SBS, FUS-SBS) and fed for 28 d starting from weaning. The dietary concentrations of DON and DON sulfonate (DONS), the DON derivative resulting from the SBS treatment, amounted to 0.156, 0.084, 2.312 and 0.275 mg DON per kg CON, CON-SBS, FUS and FUS-SBS diet, and to <0.05, <0.05, <0.05 and 1.841 mg/kg diet, respectively. Feeding the FUS diet significantly reduced the feed intake compared to the other three groups as indicated by the significant interactions between triticale source and SBS treatment when the whole experimental period of 28 d was considered (p = 0.014) while live weight gain and feed to gain ratio remained unaffected. The total plasma protein concentration was significantly depressed due to feeding the contaminated diets whereas SBS treatment exerted an increasing effect at the same time (45.4, 49.5, 40.7 and 46.5 g/L for piglets fed the CON, CON-SBS, FUS and FUS-SBS diet, respectively). The liver function was tested by the (13)C-methacetin breath test (MBT) allowing evaluation of the cytochrome P4501A2 activity. MBT results, expressed as cumulative percentage dose recovery after 360 min (cPDR360) revealed a slight stimulation of liver function due to SBS treatment (p = 0.052) (37.5, 39.4, 37.4 and 55.1% for piglets fed the CON, CON-SBS, FUS and FUS-SBS diet, respectively). Liver weight and histopathological scoring were only weakly related to the MBT results. Further histopathological examinations of kidneys, pancreas and heart revealed no treatment effects. It was concluded that the SBS treatment of the contaminated triticale restored the performance of piglets to the level of the piglets fed the control diet while the effects on liver function, clinical-chemical plasma parameters - excepting the protein concentration - and organ histopathology were only marginal. Non-Human Toxicity Values LD50 Rat dermal > 2000 mg/kg LD50 Hamster iv 95 mg/kg bw LD50 Rabbit iv 65 mg/kg bw LD50 Mouse iv 130 mg/kg bw For more Non-Human Toxicity Values (Complete) data for SODIUM METABISULFITE (13 total), please visit the HSDB record page. |
References | |
Additional Infomation |
Therapeutic Uses
Exptl Use: Conversion of Cr (VI) to Cr (III) via sodium metabisulfite or sodium dithionite prevents Cr dermatitis in sensitive individuals. |
Molecular Formula |
NA2O5S2
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Molecular Weight |
190.11
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Exact Mass |
189.898
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CAS # |
7681-57-4
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Related CAS # |
18403-71-9 (unspecified hydrochloride salt)
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PubChem CID |
656671
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Appearance |
White to off-white solid powder
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Density |
1.48
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Melting Point |
150 °C
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LogP |
0.272
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Hydrogen Bond Donor Count |
0
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Hydrogen Bond Acceptor Count |
6
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Rotatable Bond Count |
0
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Heavy Atom Count |
9
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Complexity |
136
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Defined Atom Stereocenter Count |
0
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InChi Key |
HRZFUMHJMZEROT-UHFFFAOYSA-L
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InChi Code |
InChI=1S/2Na.H2O5S2/c;;1-6(2)7(3,4)5/h;;(H,1,2)(H,3,4,5)/q2*+1;/p-2
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HS Tariff Code |
2934.99.9001
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Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month Note: Please store this product in a sealed and protected environment, avoid exposure to moisture. |
Shipping Condition |
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
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Solubility (In Vitro) |
H2O: 100 mg/mL (526.01 mM)
DMSO: 4 mg/mL (21.04 mM) |
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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 | 5.2601 mL | 26.3006 mL | 52.6011 mL | |
5 mM | 1.0520 mL | 5.2601 mL | 10.5202 mL | |
10 mM | 0.5260 mL | 2.6301 mL | 5.2601 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.