Name | (+)-sotalol hydrochloride |
Synonyms | SOTALEX SOTACOR Sotalol HCl meadjohnson1999 Sotalol Hydrochloride (+)-sotalol hydrochloride isopropylaminohydroxyethylmethanesulfonanilidehydrochloride 4-(2-isopropylamino-1-hydroxyaethyl)methanesulfonailidhydrochlorid 4-(1-hydroxy-2-isopropylaminoethyl)methanesulphonanilide hydrochloride n-isopropyl-beta-(4-methanesulfonamidophenyl)ethanolaminehydrochloride 4'-(1-hydroxy-2-(isopropylamino)ethyl)-methanesulfonanilidmonohydrochlorid 4'-(1-hydroxy-2-(isopropylamino)ethyl)methanesulfonanilidemonohydrochloride |
CAS | 959-24-0 |
EINECS | 213-496-0 |
InChI | InChI=1/C12H20N2O3S.ClH/c1-9(2)13-8-12(15)10-4-6-11(7-5-10)14-18(3,16)17;/h4-7,9,12-15H,8H2,1-3H3;1H |
Molecular Formula | C12H21ClN2O3S |
Molar Mass | 308.82 |
Melting Point | 218-220°C |
Water Solubility | Soluble in phosphate buffered saline, DMSO, ethanol, water, and methanol. |
Solubility | H2O: 20mg/mL |
Appearance | powder |
Color | white to off-white |
Storage Condition | 2-8°C |
Use | Used as cardiovascular drugs, beta blockers |
In vitro study | Sotalol hydrochloride (MJ 1999) is an adrenergic β-antagonist that is used in the treatment of life-threatening arrhythmias. Sotalol hydrochloride is a competitive beta adrenoceptor antagonist devoid of membrane-stabilizing activity and intrinsic sympathomimetic activity that has no preferential actions on beta 1 or beta 2 responses. Sotalol hydrochloride causes concentration-dependent increases in the contractility of isolated ventricular tissue that is not blocked by previous beta or alpha blockade or catecholamine depletion. Sotalol hydrochloride consistently reduces the heart rate to a greater degree than propranolol and causes significantly less cardiac suppression than propranolol at a given heart rate. Sotalol hydrochloride is not only a beta blocker but a class III antiarrhythmic drug. Its possible antifibrillatory activity was therefore investigated in both the ventricles and atria of dog heart in situ, since vulnerability to fibrillation is not the same in both these parts of the myocardium. |
Hazard Symbols | Xi - Irritant |
Risk Codes | 36/37/38 - Irritating to eyes, respiratory system and skin. |
Safety Description | S26 - In case of contact with eyes, rinse immediately with plenty of water and seek medical advice. S36 - Wear suitable protective clothing. |
WGK Germany | 3 |
RTECS | PB0826000 |
HS Code | 2935904000 |
Toxicity | LD50 in male mice, rats (mg/kg): 2600, 3450 orally; 670, 680 i.p.; LD50 orally in rabbits: 1000 mg/kg; LD50 i.p. in dogs: 330 mg/kg (Lish) |
This product is 4 '-(l-hydroxy-2-isopropylaminoethyl) methanesulfonylaniline hydrochloride. The content of C12H20N203S • HC1 shall be between 98.5% and 101.5% calculated on the dry product.
take this product, precision weighing, add 0.1 mol/L sodium hydroxide solution is dissolved and quantitatively diluted to prepare a solution containing about 10ug per 1 ml, and the absorbance is measured at the wavelength of 249nm by ultraviolet-visible spectrophotometry (General rule 0401), the absorption coefficient is 456 to 504.
take 0.4g of this product, add 20ml of water to dissolve, and then measure it according to law (General rule 0631). The pH value should be 4.5~6.0.
take this product l. After adding 10ml of water to dissolve, the solution should be clear and colorless; If it is turbid, it should not be more concentrated compared with No. 1 turbidity standard solution (General rule 0902 first method); If it is colored, it shall not be deeper in comparison with the yellow No. 1 Standard Colorimetric solution (General rule 0901 first method).
take 2.0g of this product and check it according to law (General rule 0802). Compared with the control solution made of 0.01% of standard potassium sulfate solution, it should not be more concentrated ().
take this product, add the dilution solvent under the item of content determination to dissolve and dilute to make a solution containing about 2mg per 1 ml, as the test solution; Take the appropriate amount of precision, A solution containing 10ug per 1 ml was prepared as a control solution by quantitative dilution with a dilution solvent. According to the chromatographic conditions under the content determination item, 20 u1 of the test solution and the control solution are respectively injected into the liquid chromatograph, and the chromatogram is recorded to 3 times of the retention time of the main component peak. If there are impurity peaks in the chromatogram of the test solution, the area of a single impurity peak shall not be greater than 0.6 times (0.3%) of the area of the main peak of the control solution; the sum of each impurity peak area shall not be greater than the main peak area of the control solution (0.5%).
take this product, dry to constant weight at 105°C, weight loss shall not exceed 0.5% (General rule 0831).
take l.Og of this product and check it according to law (General rule 0841). The residue left shall not exceed 0.1%.
The residue left under the item of taking the ignition residue shall not contain more than 10 parts per million of heavy metal when examined by law (General Principles 0821, Law II).
take l.Og of this product, add 25ml of water to dissolve, and then check according to law (General rule 0807). Compared with the control solution made of 0.001% of standard iron solution, it shall not be deeper ().
measured by high performance liquid chromatography (General 0512).
silica gel bonded with octanoalkyl silane was used as a filler; 0.2% sodium octane sulfonate solution (adjusted to pH 3.0 with phosphoric acid)-acetonitrile (79:21) was used as a mobile phase; The detection wavelength was 228mn. The number of theoretical plates shall not be less than 2000 calculated by sotalol peak, and the separation degree between sotalol peak and adjacent impurity peaks shall meet the requirements.
take an appropriate amount of this product, weigh it accurately, add Diluted solvent [water (adjust pH to 3.0 with phosphoric acid)-acetonitrile (79:21)] dissolve and quantitatively dilute to make about 0.lmg solution was used as the test solution, and 20 u1 was accurately measured. Human liquid chromatograph was used to record the chromatogram. According to the external standard method to calculate the peak area, that is.
B adrenergic receptor antagonists.
light-shielded, sealed, and preserved in a dry place.
This product contains Sotalol Hydrochloride (C12H20N203S • HCI) should be 95.0% ~ 105.0% of the label amount.
This product is white or off-white.
Take 20 tablets of this product, precise weighing, fine grinding, precise weighing appropriate amount (about equivalent to Sotalol Hydrochloride 50mg ), put it in 50ml measuring flask, add dilute solvent [water (adjust pH to 3.0 with phosphoric acid)-acetonitrile (79:21)] to dissolve Sotalol Hydrochloride and dilute to the scale, shake, filter, precision take the appropriate amount of filtrate, diluted with a quantitative dilution of solvent made per lml containing about 0. The 1 mg solution was obtained as a test solution by measurement according to the method described in the item of Sotalol Hydrochloride content measurement.
Same as Sotalol Hydrochloride.
80mg
light shielding, sealed storage.