Fosaprepitant dimeglumine / CAS：265121-04-8
Short Description:
Product name: Fosaprepitant dimeglumine
Type:ZA-N
CAS: 265121-04-8
MF:C30H39F7N5O11P
MW: 809.63
STRUCTURE:
specification
|
Test Item |
Acceptance Criteria |
Result |
| Appearance | White or off-white powder |
White powder |
| Solubility |
This product is easily soluble in water and methanol, but insoluble in ethanol or acetonitrile |
Conform |
| Specific rotation | +28.0° to ＋33.0°
|
+31.5°
|
| UV identification | There is maximum absorption at wavelengths of 210nm and 263nm | Conform
|
|
Infrared identification |
The infrared absorption spectrum should be consistent with the spectrum of the reference substance | Conform
|
| Chromatographic identification | The retention time of the main peak of the test solution should be consistent with that of the reference solution | Conform
|
| Alkalinity | 7.0~9.0 |
7.7 |
| Clarity of solution | Should be clear; Any opalescence produced is not more pronounced than that of reference suspension II | Conform
|
| Related substances | Impurity A ≤ 0.15%
Impurity B ≤ 0.1% Impurity I3-1 ≤ 0.15% Other single impurities ≤ 0.10% Total impurities ≤ 1.0% |
0.08%
Undetected 0.04% 0.03% 0.15% |
| Enantiomer | Not exceeding 0.15% |
Undetected |
| Residual solvents 1 | Methanol ≤3000ppm
Ethanol ≤5000ppm Acetonitrile ≤410ppm Ether ≤5000ppm Acetone ≤5000ppm Methyl tert butyl ether ≤5000ppm Toluene ≤890ppm
|
1667ppm
92ppm Undetected 54ppm 2636ppm 187ppm Undetected
|
| Residual solvent 2 | Triethylamine ≤5000ppm
|
58ppm
|
| Water content | ≤2.0% | 1.4% |
| Heavy metals | Must not exceed 10 ppm | Conform |
| Palladium | Not exceeding five ppm | Undetected |
| Chloride | It should not exceed 0.01% | Conform |
| Sulfate | It should not exceed 0.1% | Conform |
| Meglumine | According to anhydrous calculation, the content of C7H17NO5 should be 37.8% to 39.8% | 38.5% |
| Assay | According to anhydrous calculation, the content of C23H22F7N4O6P·2(C7H17NO5) should be 98.0%~102.0% | 100.4%
|
| Bacterial endotoxin | The amount of endotoxin per mg of Fosaprepitant Dimeglumine should be less than 0.16 EU | Conform
|
| Microbial Limit | The total aerobic microbial count is not more than 100 cfu,the total combined molds and yeasts count is not more than 50 cfu per g of test sample and Escherichia coli is absent | The total aerobic microbial: 3cfu/g
the total combined molds and yeasts count: ＜10cfu/g Escherichia coli: Undetected
|
| Conclusion | Product confirms enterprise standard | |
Usage
There are three subtypes of neurokinin receptors: NK1, NK2 and NK3. Among them, the NK1 receptor has the strongest binding ability to substance P and the highest content in the vomiting center of the brain. After the NK1 receptor binds to substance P in the central nervous system, it triggers a series of pathophysiological processes such as vomiting, anxiety and migraine. NK1RAs such as apirpitan and fosapirpitan effectively prevent and treat CINV by selectively binding to the NK1 receptor. Usually, acute CINV is related to the activity of the peripheral 5-HT3 energy pathway, while delayed CINV is related to the central P substance. Therefore, compared with 5-HT3RAs, apirpitan and fosapirpitan show obvious advantages for delayed vomiting.
Fosapirtan dimethylmeglumine is a neurokinin-1receptorantagonist (NK-1RA) developed by Merck. It was first launched in the United States in January 2008. Fosarpitan dimethylmegalamine is the precursor drug of aprepitant, the first NK-1RA drug. After entering the body, it can be rapidly converted into aprepitant and is clinically used to prevent and treat acute or delayed nausea and vomiting caused by the initial and repeated use of moderate to high emetogenic chemotherapy (including high-dose cisplatin).
Fosaprepitant dimeglumine salt (MK-0517) is a water-soluble phosphoacyl precursor drug of aprepitant and an NK1 antagonist.
Packaging and Shipping
5kg ，25kg as customer requirements.
Belongs to common goods and can deliver by ocean and air
Keep and storage
Shelf life:24 month from date of manufacture in original unopened packaging stored in a cool dry place out of direct sunlight, water.
Ventilated warehouse, Low temperature drying, Separated from oxidants, acids.
