Atracurium Besylate is a neuromuscular blocking agent API and reference standard for quality control. The recommended initial dose for most patients is 0.4 to 0.5 mg/kg given as an intravenous bolus injection. With this dose, good or excellent conditions for nonemergency intubation can be expected in 2 to 2.5 minutes, with maximum neuromuscular block achieved approximately 3 to 5 minutes after injection . Atracurium Besylate Injection should be administered over a period of at least 60 seconds to patients who may be unusually sensitive to falls in arterial blood pressure .
|
Parameter |
Specification |
|
Product Name |
Atracurium Besylate |
|
CAS Number |
64228-81-5 |
|
Storage |
Refrigerate at 2–8°C (per label) |
Atracurium besilate has the characteristics of metabolism via non-hepatic and non-renal pathways and cardiovascular protective effects, giving it advantages among similar drugs. Its muscle relaxant effect is 3 times stronger than that of atracurium besilate commonly used in clinical practice.
Purpose: Non-depolarizing muscle relaxant, with a potency 2.5 times that of tubocurarine, but a shorter duration of action. It is used for various surgical procedures, especially for tracheal intubation and caesarean section.
0.1 mol of 1,5-pentanediol, 0.2 mol of triethylamine and 0.1 g of 1,2,3-benzenetriol are dissolved in 100 ml of anhydrous benzene. Under vigorous stirring, a solution of 0.2 mol of acryloyl chloride dissolved in 60 ml of anhydrous benzene is added within 0.5 h. Then about 100 ml of anhydrous benzene and 10 ml of triethylamine are added, followed by stirring at 50 °C for 0.5 h. Triethylamine hydrochloride is removed by filtration, and the solvent is removed under reduced pressure. The remaining yellow oil is distilled in the dark in the presence of a trace amount of p-methoxyphenol, and the fraction at 90~95 °C/1.33 Pa is collected to obtain 1,5-pentamethylene diacrylate with a yield of 61%. 4.43 g of tetrahydropapaverine and 1.30 g of the 1,5-pentamethylene diacrylate obtained above are dissolved in 15 ml of anhydrous benzene, and the mixture is stirred and refluxed in the dark for 48 h. The solvent is removed under reduced pressure, and the remaining dark red oil is dissolved in 10 ml of chloroform. About 400 ml of diethyl ether is added, followed by about 500 ml of a saturated ether solution of oxalic acid, to obtain a flocculent white precipitate. The precipitate is filtered, washed with diethyl ether and dried. Recrystallization from ethanol twice yields 3.5 g of white powdery compound (I) with a yield of 51% and a melting point of 117~121 °C.
Compound (I) is dissolved in aqueous sodium bicarbonate solution and extracted with toluene. The extract is concentrated to obtain a colorless viscous liquid, which is Compound (II). 0.5 g of dried Compound (II) is dissolved in 8 ml of spectroscopic-grade acetonitrile, methyl benzenesulfonate is added, and the mixture is reacted at room temperature for 22 h. Under vigorous stirring, the solution is added dropwise to approximately 450 ml of dry diethyl ether. The formed flocculent white precipitate is collected by filtration, washed with dry diethyl ether, and dried under vacuum at 50 °C in the presence of phosphorus pentoxide. An off-white atracurium besilate powder is obtained, with a melting point of 85~90 °C.
Contact Cosperpharm for Atracurium Besylate reference standard and API inquiries.
Address
No. 2 Yangguang 3rd Road, Duodao Chemical Cycle Industrial Park, Jingmen City, Hubei Province, China
Tel
