Molecular Formula | C22H29FO5 |
Molar Mass | 392.47 |
Density | 1.1283 (estimate) |
Melting Point | 235-237°C |
Boling Point | 568.2±50.0 °C(Predicted) |
Specific Rotation(α) | D +108° (acetone) |
Flash Point | 297.5°C |
Water Solubility | 58mg/L(25 ºC) |
Solubility | Practically insoluble in water, sparingly soluble in anhydrous ethanol, very slightly soluble in methylene chloride. |
Vapor Presure | 2.81E-15mmHg at 25°C |
Appearance | neat |
Color | White to Off-White |
Merck | 14,1180 |
pKa | 12.13±0.70(Predicted) |
Storage Condition | 0-6°C |
Refractive Index | 118 ° (C=1, Dioxane) |
Physical and Chemical Properties | Color crystalline powder. Melting point 231-234 °c (decomposition). Odorless. Betamethasone acetate ([987-24-6]) is also a white crystalline powder, melting point 205-208 ℃, slightly soluble in propanol, ethanol, extremely difficult to dissolve in chloroform or ether, insoluble in water, odorless. |
Use | Steroids. Mainly used for anti-inflammatory and anti-allergic. Suitable for rheumatoid arthritis and various skin diseases. The effect of betamethasone with dexamethasone, its anti-inflammatory effect than dexamethasone, dexamethasone, hydrocortisone strong, less side effects. |
In vitro study | Betamethasone has a specific affinity for type II glucocorticoid receptors and is present in most brain regions. |
In vivo study | In late gestation fetal sheep, Betamethasone has a direct vasoconstrictor effect on peripheral femoral artery resistant vessels. After 24 hours of infusion in sheep, Betamethasone decreased cerebral blood flow (CBF) in all brain regions measured except the hippocampus. In rats, Betamethasone reduces the activation of NF-κB and the elevation of tumor necrosis factors α and IL-1β, and induces the expression of IL-10 in the brain, all of which are associated with alterations in pain thresholds. Betamethasone reduced synaptophysin-LI in the frontal cortex, caudate putamen, and hippocampus by 46.9, 41.0, and 55.4 percent, respectively, without being accompanied by irreversible neuronal damage in the fetal sheep brain. Betamethasone modestly increased mRNA of cytidine acyltransferase (CT) but did not alter immunoreactive enzyme levels in adult rat lungs. Betamethasone reduces the activity of the hydrolase of sphingomyelin: acidic sphingomyelin by 33% and basic ceramide by 21%. Betamethasone injected at the time of nerve injury partially keeps the development of neuropathic hyperalgesia and reduces the subsequent elevated brain levels of pro-inflammatory cytokines, while stimulating the expression of anti-inflammatory cytokine IL-10. |
Risk Codes | R40 - Limited evidence of a carcinogenic effect R48/20/21 - R61 - May cause harm to the unborn child |
Safety Description | S22 - Do not breathe dust. S36 - Wear suitable protective clothing. S45 - In case of accident or if you feel unwell, seek medical advice immediately (show the label whenever possible.) S53 - Avoid exposure - obtain special instructions before use. |
WGK Germany | 2 |
RTECS | TU4000000 |
HS Code | 29379000 |
Toxicity | LD50 oral in mouse: > 4500mg/kg |
Raw Materials | betamethasone 21-acetate |
This product is 16b-methyl-11b, 17a,21-dihydroxy-9a-fluorogestatin -1, 4-dien-3, 20-dione. The content of C22H29F05 shall be 97.0% ~ 103.0% calculated as dry product.
take this product, precision weighing, plus dioxane dissolution and quantitative dilution of about 10 mg per lml solution, according to the law (General 0621), the specific rotation was 115 ° to 121 °.
take this product, precision weighing, plus ethanol dissolution and quantitative dilution to make a solution containing about 10ug per lml, according to UV-visible spectrophotometry (General 0401), the absorbance was measured at a wavelength of 239nm, and the absorption coefficient was 382 to 406.
take this product, add mobile phase to dissolve and dilute to make a solution containing about 0.4mg per 1ml as a test solution; Take 1ml for precision measurement and put it in a 100ml measuring flask, dilute to the scale with the mobile phase, shake, and serve as a control solution. According to the chromatographic conditions under the content determination item, 20ul of the test solution and the control solution are respectively injected into the liquid chromatograph, and the chromatogram is recorded to 2.5 times of the retention time of the main component peak. If there is any impurity peak in the chromatogram of the test solution, the impurity peak whose peak area is 0.5~1.0 times (0.5% ~ 1.0%) of the main peak area of the control solution shall not exceed 1, other single impurity peak area shall not be greater than 0.5 times (0.5%) of the main peak area in the control solution, and the sum of each impurity peak area shall not be greater than 2 times (2.0%) of the main peak area of the control solution. The chromatogram of the test solution is 0.01 times smaller than the main peak area of the control solution.
take this product, dry to constant weight at 105°C, weight loss shall not exceed 0.5% (General rule 0831).
not more than 0.1% (General rule 0841).
measured by high performance liquid chromatography (General 0512).
silica gel bonded with eighteen alkyl silane was used as the filler; Acetonitrile-water (25:75) was used as the mobile phase; The detection wavelength was 240nm. Take the dexamethasone control, add the test solution under the item of related substances to dissolve and dilute to make a solution containing 40ug of betamethasone and dexamethasone per 1 ml, and inject 20ul into the liquid chromatograph, the resolution of the betamethasone peak from the dexamethasone peak should be greater than 1.9.
take this product, precision weighing, adding mobile phase dissolution and quantitative dilution to make a solution containing about 40% per lml, as a test solution, the precision amount of 20ul injection liquid chromatography, the chromatogram was recorded; The betamethasone reference substance was taken and determined by the same method. According to the external standard method to calculate the peak area, that is.
adrenocortical hormone drugs.
light shielding, sealed storage.
This product contains betamethasone (C22H29F05) should be 90.0% ~ 110.0% of the label amount.
This product is white tablet.
In the chromatogram recorded under the content determination item, the retention time of the main peak of the test solution should be consistent with the retention time of the main peak of the control solution.
Take 20 tablets of this product, precision weighing, fine grinding, precision weighing appropriate amount (about 2mg equivalent to betamethasone), put it in 50ml measuring flask, add appropriate amount of mobile phase, ultrasonic dissolution of betamethasone, cool, dilute to the scale with mobile phase, shake well, centrifuge (4000 rpm) for 20 minutes, take the supernatant as the test solution, and determine it according to the method under betamethasone content determination, that's right.
same betamethasone.
0.5mg
light shielding, sealed storage.
This product contains betamethasone (C22H29F05) should be 90.0% ~ 110.0% of the label amount.
This product is white cream.
In the chromatogram recorded under the content determination item, the retention time of the main peak of the test solution should be consistent with the retention time of the main peak of the control solution.
should comply with the relevant provisions under Cream (General rule 0109).
take an appropriate amount of this product (about equivalent to betamethasone lmg), weigh it accurately, put it in a 50ml measuring flask, add an appropriate amount of methanol, heat it in a water bath at 80°C for 2 minutes, shake it, dissolve betamethasone, let it cool, dilute to scale with methanol, shake well, cool in an ice bath for 2 hours, quickly filter through an organic phase filter (0.45um), and discard 10ml of the initial filtrate, the continued filtrate was taken as the test solution; The betamethasone reference substance was precision weighed, dissolved with mobile phase and quantitatively diluted to prepare a solution containing about 20ug per 1 ml as the reference solution. According to the betamethasone content determination method under the item, that is obtained.
same betamethasone.
(l)4g:4mg (2)10g:lOmg (3)15g:15mg
sealed and stored in a cool place.