| Size | Price | Stock | Qty |
|---|---|---|---|
| 5g |
|
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| Other Sizes |
| ADME/Pharmacokinetics |
Absorption, Distribution and Excretion
Following ingestion of colloidal bismuth citrate (214 mg bismuth), the mean peak concentration of bismuth in whole blood exceeded 50 mg/L, reaching its peak at 30 minutes. However, after ingestion of bismuth nitrate (205 mg bismuth), no evidence of bismuth absorption into the blood was observed, although baseline blood bismuth levels remained elevated in three volunteers who took bismuth nitrate one week after taking colloidal bismuth citrate. The mean plasma concentration in all five volunteers was assessed 45 minutes after administration of colloidal bismuth subcitrate, yielding a concentration of 79.76 μg/L, compared to a blood concentration of 47.6 μg/L. Bismuth is primarily excreted via urine and bile. Renal excretion appeared to reach steady state after 2 weeks of discontinuation, with similar rates observed after 6 weeks. In the first two weeks after discontinuation, the mean urinary excretion rate of bismuth was 2.6% per day (urinary drug concentration ranging from 24 to 250 μg/mL), indicating accumulation in tissues and slow excretion. Biological Half-Life The elimination half-life of bismuth is approximately 5 days. |
|---|---|
| Toxicity/Toxicokinetics |
Protein Binding
90% |
| Additional Infomation |
Bismuth compounds used to treat peptic ulcers and gastroesophageal reflux disease (GORD). Bismuth subcitrate is a mineral compound used to treat duodenal and gastric ulcers caused by Helicobacter pylori. Bismuth subcitrate potassium is a soluble complex bismuth salt used in combination with metronidazole and tetracycline to treat gastric ulcers caused by Helicobacter pylori infection.
Drug Indications For the treatment of peptic ulcers and gastroesophageal reflux disease (GORD). For the treatment of inflammatory and erosive ulcerative diseases of the gastric and duodenal mucosa: gastritis, gastric and duodenal ulcers, functional non-ulcer dyspepsia, erosive duodenitis, postoperative inflammation and erosive changes—anastomotic stomatitis, anastomotic peptic ulcers. Mechanism of Action Colloidal bismuth subcitrate is very effective in treating gastroduodenal diseases, and its mechanism of action appears to be multifaceted. It has little to no acid-neutralizing effect and does not affect gastric acid secretion. It is currently uncertain whether it affects pepsin secretion, but it does inhibit pepsin activity. It increases the secretion of mucoglycoproteins and may bind to the gastric mucus layer, thus preventing hydrochloric acid diffusion. It accelerates ulcer healing and leads to the accumulation of epidermal growth factor around ulcers. Furthermore, it has cytoprotective effects and increases the secretion of mucosal prostaglandins and bicarbonate. It has bactericidal activity against Helicobacter pylori (associated with gastritis and peptic ulcers). It also prevents Helicobacter pylori from adhering to epithelial cells and inhibits enzymes secreted by Helicobacter pylori, such as proteases, lipases, glycosidases, and phospholipases. Pharmacodynamics Bismuth citrate is very effective in treating gastroduodenal diseases, and its mechanism of action appears to be multifaceted. It has little to no acid-neutralizing effect and does not affect gastric acid secretion. |
| Molecular Formula |
C12H10BIK3O14
|
|---|---|
| Molecular Weight |
704.4747
|
| Exact Mass |
703.878
|
| CAS # |
57644-54-9
|
| PubChem CID |
10101269
|
| Appearance |
White to off-white solid powder
|
| Boiling Point |
309.6ºC at 760 mmHg
|
| Flash Point |
155.2ºC
|
| Hydrogen Bond Donor Count |
2
|
| Hydrogen Bond Acceptor Count |
14
|
| Rotatable Bond Count |
4
|
| Heavy Atom Count |
30
|
| Complexity |
211
|
| Defined Atom Stereocenter Count |
0
|
| InChi Key |
ZQUAVILLCXTKTF-UHFFFAOYSA-H
|
| InChi Code |
InChI=1S/2C6H8O7.Bi.3K/c2*7-3(8)1-6(13,5(11)12)2-4(9)10;;;;/h2*13H,1-2H2,(H,7,8)(H,9,10)(H,11,12);;;;/q;;+3;3*+1/p-6
|
| Chemical Name |
bismuth;tripotassium;2-hydroxypropane-1,2,3-tricarboxylate
|
| 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 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)
|
| Solubility (In Vitro) |
H2O : ~100 mg/mL (~141.95 mM)
|
|---|---|
| Solubility (In Vivo) |
Solubility in Formulation 1: 100 mg/mL (141.95 mM) in PBS (add these co-solvents sequentially from left to right, and one by one), clear solution; with sonication.
 (Please use freshly prepared in vivo formulations for optimal results.) |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 1.4195 mL | 7.0975 mL | 14.1951 mL | |
| 5 mM | 0.2839 mL | 1.4195 mL | 2.8390 mL | |
| 10 mM | 0.1420 mL | 0.7098 mL | 1.4195 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.