| Size | Price | |
|---|---|---|
| 500mg | ||
| 1g | ||
| Other Sizes |
| ADME/Pharmacokinetics |
Absorption, Distribution and Excretion
The bioavailability in healthy subjects was 6%; the time to peak concentration (Tmax) was 10 minutes; and the time to steady state was 2 days. Following intravenous administration of radiolabeled aprazole bromide, it was extensively metabolized in healthy volunteers, with 1% excreted unchanged. Approximately 54% to 65% of the radioactive material was excreted in the urine, and 20% to 33% of the dose was excreted in the feces. These results suggest that almost all of aprazole bromide is eliminated through hydrolysis. Following inhalation of the dry powder, approximately 0.09% of the dose is excreted in the urine. The volume of distribution after intravenous administration was 300 liters. The total clearance after intravenous administration in young, healthy subjects was 170 liters/hour (inter-individual variability 36%). Metabolism / Metabolites The primary metabolic pathway of acrylidine bromide is hydrolysis, which includes both chemical hydrolysis and enzymatic hydrolysis by esterases in plasma. Acrylidine bromide is rapidly and extensively hydrolyzed into alcohols and dithienylglycolic acid derivatives. Neither of these derivatives binds to muscarinic receptors and therefore has no pharmacological activity. Biological Half-Life Plasma half-life = 2.4 minutes (indicating that aprazole is rapidly hydrolyzed in plasma into two inactive metabolites, reducing the likelihood of systemic side effects). Effective half-life = 5-8 hours. |
|---|---|
| Toxicity/Toxicokinetics |
Hepatotoxicity
As with other anticholinergic drugs, aprazole has not been found to be associated with elevated liver enzymes or clinically significant liver injury. Its high safety profile is likely primarily due to the low systemic absorption and exposure of inhaled anticholinergic drugs. References regarding the safety and potential hepatotoxicity of anticholinergic drugs are listed after the "Overview of Anticholinergic Drugs" section. Drug Category: Anticholinergic Drugs |
| References | |
| Additional Infomation |
Aclidinium is a carboxylic acid ester formed by the condensation of the carboxyl group of 2-hydroxy(di-2-thienyl)acetic acid and the hydroxyl group of N-(3-phenoxypropyl)-3-quininecyclool. Its bromide salt is used for long-term maintenance treatment of bronchospasm associated with chronic obstructive pulmonary disease (COPD). It has bronchodilation and muscarinic receptor antagonistic effects. It belongs to the thiophene class of compounds, carboxylic acid esters, quaternary ammonium ions, and aromatic ethers. Its function is similar to 3-quininecyclool. Aclidinium is an anticholinergic drug used for long-term treatment of COPD. It binds to muscarinic receptors much more readily than to nicotine receptors. It was approved by the FDA on July 24, 2012. Aclidinium is an anticholinergic drug. Its mechanism of action is as a cholinergic antagonist. Aprazole is a synthetic anticholinergic drug used as an inhaler to treat acute bronchospasm caused by chronic bronchitis or emphysema. Aprazole has not been shown to cause elevated liver enzymes or clinically significant acute liver injury. See also: Aprazole bromide (note moved to); Aprazole bromide; Formoterol fumarate (note moved to).
Drug Indication Acriflammium bromide inhalation powder is indicated for the long-term maintenance treatment of bronchospasm associated with chronic obstructive pulmonary disease (COPD), including chronic bronchitis and emphysema. FDA label Mechanism of Action Aclidinium is a long-acting, competitive, and reversible anticholinergic drug that specifically targets acetylcholine-muscarinic receptors. It has similar affinity to all five muscarinic receptor subtypes. Aclidinium exerts its effects on the airways by acting on M3 receptors on smooth muscle, causing bronchodilation. Its inhibitory effect on acetylcholine-induced bronchoconstriction is dose-dependent and lasts for more than 24 hours. Pharmacodynamics Aclairdoline does not prolong the QTc interval or significantly affect heart rhythm. |
| Molecular Formula |
C26H30NO4S2+
|
|---|---|
| Molecular Weight |
484.65
|
| Exact Mass |
484.162
|
| CAS # |
727649-81-2
|
| PubChem CID |
11434515
|
| Appearance |
Typically exists as solids at room temperature
|
| LogP |
4.626
|
| Hydrogen Bond Donor Count |
1
|
| Hydrogen Bond Acceptor Count |
6
|
| Rotatable Bond Count |
10
|
| Heavy Atom Count |
33
|
| Complexity |
647
|
| Defined Atom Stereocenter Count |
1
|
| SMILES |
S1C=CC=C1C(C1=CC=CS1)(C(=O)O[C@H]1C[N+]2(CCCOC3C=CC=CC=3)CCC1CC2)O
|
| InChi Key |
ASMXXROZKSBQIH-VITNCHFBSA-N
|
| InChi Code |
InChI=1S/C26H30NO4S2/c28-25(26(29,23-9-4-17-32-23)24-10-5-18-33-24)31-22-19-27(14-11-20(22)12-15-27)13-6-16-30-21-7-2-1-3-8-21/h1-5,7-10,17-18,20,22,29H,6,11-16,19H2/q+1/t20?,22-,27?/m0/s1
|
| Chemical Name |
[(3R)-1-(3-phenoxypropyl)-1-azoniabicyclo[2.2.2]octan-3-yl] 2-hydroxy-2,2-dithiophen-2-ylacetate
|
| 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 | 2.0633 mL | 10.3167 mL | 20.6334 mL | |
| 5 mM | 0.4127 mL | 2.0633 mL | 4.1267 mL | |
| 10 mM | 0.2063 mL | 1.0317 mL | 2.0633 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.
Link: https://clinicaltrials.gov/ct2/show/NCT02039050
Conditions:Pulmonary Disease, Chronic ObstructiveLink: https://clinicaltrials.gov/ct2/show/NCT02038829
Conditions:COPDProducts are for research use only; We do not sell to patients
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