Albuterol Sulfate Powder CAS 51022-70-9

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Albuterol sulfate powder, CAS 51022-70-9, Molecular formula C13H23NO7S, white or almost white odorless powder. Very slightly dissolved in ethanol; Almost insoluble in ether. Good thermal stability, half-life of 4-6 hours. Salbutamol was discovered and developed by British scholars in 1962, first marketed in 1968, registered in China in 1988, and produced domestically in 1975. In 2012, it became the only nebulized inhalation bronchodilator to enter the National Essential Medicines List. Store in a sealed container in a cool and dry place, and ensure good ventilation or exhaust in the workspace. It is generally used to treat bronchospasm in patients with bronchial asthma, asthmatic bronchitis, and emphysema. This product is for laboratory use only.

1. Starting from p-hydroxyacetophenone, it is synthesized in 8 steps of bromination, hydrolysis, amination, hydrolysis, neutralization, catalytic hydrogenation, Hydrogenolysis and salt formation, with a total yield of 11% ~ 13%. Moreover, the reaction conditions of this method are harsh, the "three wastes" pollution is serious, and the cost is high.

2. 4-bromoacetyl salicylaldehyde and 4-chloroacetyl salicylaldehyde were obtained from salicylaldehyde and acyl chloride by Friedel crafts acylation. After condensation, hydrolysis and salt formation in the same bath, they were converted into 5-11-dimethylethyl) amino] acetyl-2-hydroxybenzaldehyde hydrochloride. Then, salbutamol sulfate was prepared by cooperative reduction of potassium borohydride and zinc chloride at room temperature and salt formation with sulfuric acid.

3. Taking salicylaldehyde and tert butylamine as starting materials, 2-chloro-1 - {[(1,1-dimethylethyl) iminomethyl-4-hydroxyphenyl} - ethyl ketone is prepared through condensation, esterification and fries rearrangement in three steps and one pot reaction, and then converted into 5 - {[(1,1-dimethylethyl) aminoacetyl} - 2-antelin benzaldehyde hydrochloride through condensation, hydrolysis and salt formation in three steps and one pot reaction, and then neutralized with sodium methoxide, catalytically transferred to hydrogenated and reduced, and salt formed.

Albuterol sulfate powder, as a representative drug of selective β - adrenergic receptor agonists, has become a core drug for the treatment of respiratory diseases, obstetrics and gynecology, cardiovascular diseases, and special populations since its emergence in the 1960s due to its rapid onset, potent bronchodilator effect, and multi system regulatory function.

Pharmacological mechanism: molecular key for precise regulation of β ₂ receptors

 

By selectively activating β ₂ receptors on bronchial smooth muscle, uterine smooth muscle, and vascular smooth muscle, adenylate cyclase (AC) activation is triggered, promoting intracellular cyclic adenosine monophosphate (cAMP) synthesis and subsequently activating protein kinase A (PKA). This signaling pathway leads to:
Bronchial smooth muscle relaxation: PKA phosphorylates myosin light chain kinase (MLCK), reduces its activity, decreases myosin actin binding, and directly relaxes airway smooth muscle; Simultaneously inhibiting the influx of calcium ions and reducing intracellular calcium concentration to alleviate bronchospasm through a dual mechanism.

 

Inhibiting the release of inflammatory mediators: Inhibiting mast cell degranulation through the cAMP/PKA pathway, reducing the release of inflammatory mediators such as histamine and leukotrienes, and alleviating airway mucosal edema and mucus secretion.
Enhanced ciliary movement: promotes the frequency of bronchial ciliary oscillation, accelerates the function of mucus ciliary clearance system, and improves sputum discharge.
Uterine smooth muscle inhibition: activates β ₂ receptors in uterine smooth muscle cells, reduces intracellular calcium concentration, inhibits uterine contractions frequency and intensity, and prolongs pregnancy cycle.
Vasodilatory effect: Activated by β ₂ receptors, it leads to relaxation of vascular smooth muscle, reduces peripheral vascular resistance, and improves tissue perfusion.

Core indication: Full cycle management of respiratory system diseases

 

1. Acute exacerbation and prevention of bronchial asthma
Acute attack treatment: It is the preferred medication for acute attacks recommended by the Global Initiative for Asthma (GINA). It takes effect 5-15 minutes after inhalation and lasts for 4-6 hours. It can quickly relieve symptoms such as wheezing, chest tightness, and difficulty breathing. For patients with moderate to severe seizures, the combination of inhaled corticosteroids (ICS) can significantly reduce hospitalization rates.
Prevention of Exercise Induced Asthma (EIA): Inhaling salbutamol sulfate 15-20 minutes before exercise can inhibit exercise induced airway hyperresponsiveness and prevent EIA attacks. Research has shown that its preventive effect is superior to sodium succinate and oral beta agonists.
Chronic duration control: Although not a long-term control medication, regular use can reduce airway hyperresponsiveness. For patients with mild persistent asthma, the use of salbutamol sulfate combined with low-dose ICS as needed can reduce the frequency of acute attacks.

2. Acute exacerbation of chronic obstructive pulmonary disease (COPD)
Bronchial spasm relief:

 

In the acute exacerbation stage of COPD, nebulized inhalation of salbutamol sulfate combined with ipratropium bromide (anticholinergic drug) can significantly improve lung function (FEV ₁ increased by 15% -20%) and shorten hospitalization time.
Management of mucus hypersecretion: By enhancing ciliary movement and inhibiting mucus secretion, respiratory distress caused by sputum obstruction can be alleviated. For patients with high mucus secretion COPD, the combination of expectorant drugs (such as ambroxol) can improve the efficacy.

3. Asthmatic bronchitis and emphysema
Asthmatic bronchitis: can quickly relieve wheezing and coughing symptoms, especially suitable for pediatric patients. Research shows that its efficacy is superior to theophylline drugs, and the incidence of adverse reactions is lower.
Acute exacerbation of emphysema: For patients with emphysema accompanied by bronchospasm, ventilation function can be improved, arterial partial pressure of carbon dioxide (PaCO ₂) can be reduced, and respiratory failure can be prevented.

Application for special populations: precise intervention from obstetrics to pediatrics

 

1. Obstetrics field: prevention and treatment of premature birth and fetal protection
Premature birth suppression: It is the only FDA approved beta agonist for premature birth suppression. By inhibiting uterine smooth muscle contraction, the pregnancy cycle is extended by 24-48 hours, buying time for glucocorticoids to promote fetal lung maturation. The recommended dosage is 2.4-4.8 mg orally every 4-6 hours, or 10-20 μ g/min intravenously.
Treatment for intrauterine growth retardation (IUGR): By dilating the uterine placental blood vessels, increasing fetal blood supply, and improving the growth rate of IUGR fetuses. Combining low-dose aspirin can further enhance the therapeutic effect.

Threatened miscarriage management: For threatened miscarriage caused by cervical dysfunction, uterine contractions can be suppressed, and combined with cervical cerclage surgery, the success rate of fetal preservation can be significantly improved.

 

2. Pediatric field: Asthma and respiratory distress syndrome
Acute exacerbation of childhood asthma: Inhalation agents are the preferred medication for acute exacerbation of childhood asthma. For children under 5 years old, it is recommended to use nebulized inhalation (dose 0.15 mg/kg, maximum 2.5 mg); Children aged ≥ 5 can use a quantitative aerosol (MDI) with a mist storage canister (dosage 100-200 μ g/time).
Neonatal respiratory distress syndrome (NRDS): For premature infants with NRDS, albuterol sulfate powder can stimulate the secretion of pulmonary surfactant (PS) and improve lung compliance. The combination of exogenous PS replacement therapy can reduce the need for mechanical ventilation.
Premature infant apnea: By activating the beta ₂ receptors in the brainstem respiratory center, the frequency of apnea episodes is reduced. The recommended dosage is 0.2 mg/kg orally every 6-8 hours.

Combination therapy strategy: synergistic enhancement and offsetting of adverse reactions

 

1. Combined use with inhaled corticosteroids (ICS)
Long term control of asthma: Combining ICS (such as budesonide) can achieve the dual goal of "rapid relief+long-term control". Research shows that the combination therapy group reduces the frequency of acute attacks by 50% and improves lung function more significantly.
COPD maintenance therapy: For COPD patients with frequent acute exacerbations, the combination of ICS and long-acting anticholinergic drugs (LAMA) can reduce the risk of acute exacerbations by 30%.
2. Combined use with anticholinergic drugs
Nebulized inhalation plan: Salbutamol sulfate (2.5 mg) combined with ipratropium bromide (0.5 mg) nebulized inhalation can simultaneously activate β ₂ receptors and block M receptors, producing a synergistic bronchodilator effect. Suitable for patients with moderate to severe asthma and acute exacerbation of COPD.

 

Pharmacokinetic advantages: anticholinergic drugs can reduce mucosal edema induced by salbutamol sulfate and prolong its duration of action; β ₂ agonists can counteract adverse reactions such as dry mouth caused by anticholinergic drugs.
3. Combined use with theophylline drugs
Acute exacerbation of severe asthma: Combined with intravenous infusion of aminophylline, it can quickly relieve bronchospasm. But it is necessary to closely monitor the blood theophylline concentration (target range 10-20 μ g/mL) to avoid adverse reactions such as arrhythmia.
Nighttime asthma control: Salbutamol sulfate sustained-release tablets combined with theophylline controlled-release tablets can cover the period of decreased sensitivity of β ₂ receptors at night and reduce the frequency of nighttime awakenings.

Salbutamol sulfate, as a core drug for the treatment of respiratory diseases and special populations, has been widely validated for its clinical value. By precisely regulating β ₂ receptors, it not only achieves rapid and effective bronchiectasis, but also demonstrates unique advantages in premature birth prevention and fetal protection.

1. Method name: salbutamol sulfate determination of salbutamol sulfate nonaqueous solution titration

Application: this method uses non-aqueous solution titration to determine the content of salbutamol sulfate ((c13h21no3) 2 · H2SO4).

This method is suitable for the determination of salbutamol sulfate.

Method principle: after the test article is slightly dissolved with glacial acetic acid, cool it, add 15ml of acetic anhydride and 1 drop of crystal violet indicator solution, and titrate it with perchloric acid titrant (0.1 mol / L) until the solution turns blue-green. And the titration results were corrected with blank test. Every 1ml of perchloric acid titrant (0.1 mol / L) is equivalent to 57.67mg of (c13h21no3) 2 · H2SO4.

Reagent: water (fresh boiling to room temperature), glacial acetic acid, acetic anhydride, crystal violet indicator solution, perchloric acid titrant (0.1mol/l), reference potassium hydrogen phthalate

Instruments and equipment:

Sample preparation: 1. Crystal violet indicator solution: take 0.5g crystal violet and add 100ml glacial acetic acid to dissolve albuterol sulfate powder.

2. Perchloric acid titrant (0.1mol/l):

Preparation: take 750ml of water-free glacial acetic acid (5.22ml acetic anhydride per 1g of water, add 8.5ml perchloric acid (70 ~ 72%), shake well, cool down, add an appropriate amount of anhydrous glacial acetic acid to 1000ml, shake well, and leave for 24h. If the tested sample is easy to acetylate, the water content of the solution must be determined by the moisture determination method, and then adjusted to 0.01% ~ 0.2% with water and acetic anhydride.

Calibration: take about 0.16g of benchmark potassium hydrogen phthalate dried to constant weight at 105 ℃, weigh precisely, add 20ml of anhydrous glacial acetic acid to dissolve, add 1 drop of crystal violet indicator solution, titrate slowly to blue with this solution, and correct the titration result with blank test. Every 1ml of perchloric acid titrant (0.1mol/l) is equivalent to 20.42mg of potassium hydrogen phthalate. Calculate the concentration of the liquid according to the consumption of the liquid and the amount of potassium hydrogen phthalate.

3. Reference potassium hydrogen phthalate

Storage: put it in a brown glass bottle and keep it tightly.

Operating steps: take about 0.4g of this product, weigh accurately, add 10ml of glacial acetic acid, dissolve it at mild temperature, cool it, add 15ml of acetic anhydride and 1 drop of crystal violet indicator solution, titrate it with perchloric acid titrant (0.1 mol / L) until the solution turns blue-green, and correct the titration result with blank test. Every 1ml of perchloric acid titrant (0.1 mol / L) is equivalent to 57.67mg of (c13h21no3) 2 · H2SO4.

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