Name | benorilate |
Synonyms | benoral benortan benorilate Benorylate benorilato fenasparate aspirinacetaminophenester p-acetamidophenylacetylsalicylate 4-acetamidophenyl O-acetylsalicylate 4'-(acetamido)phenyl-2-acetoxybenzoate 2-acetoxy-4'-(acetamino)phenylbenzoate 4-(acetylamino)phenyl 2-(acetyloxy)benzoate |
CAS | 5003-48-5 |
EINECS | 225-674-5 |
InChI | InChI=1/C17H15NO5/c1-11(19)18-13-7-9-14(10-8-13)23-17(21)15-5-3-4-6-16(15)22-12(2)20/h3-10H,1-2H3,(H,18,19) |
Molecular Formula | C17H15NO5 |
Molar Mass | 313.3 |
Density | 1.2016 (rough estimate) |
Melting Point | 177-181℃ |
Boling Point | 453.11°C (rough estimate) |
Flash Point | 279°C |
Water Solubility | 20mg/L(21 ºC) |
Solubility | DMSO (Slightly), Methanol (Slightly) |
Vapor Presure | 1.23E-11mmHg at 25°C |
Appearance | Solid |
Color | White |
Merck | 14,1045 |
pKa | 14.17±0.70(Predicted) |
Storage Condition | Sealed in dry,Room Temperature |
Refractive Index | 1.4500 (estimate) |
Physical and Chemical Properties | White crystalline powder. Melting Point 175-176 °c. Soluble in hot alcohol, insoluble in water. |
Use | Esterification of acetaminophen and aspirin, suitable for rheumatoid arthritis, rheumatoid arthritis, Head Pain, neuralgia, fever, etc |
RTECS | VO0720000 |
Toxicity | LD50 in mice, rats (mg/ml): 2000, ~10000 orally; 1255, 1830 i.p. (Robertson) |
Raw Materials | Thionyl chloride |
This product is 4-acetylaminophenyl acetylsalicylate. The content of C17H15N05 shall be between 99.0% and 102.0% based on the dry product.
The melting point of this product (General 0612) is 177~181°C.
take this product, precision weighing, plus absolute ethanol dissolution and quantitative dilution to make a solution containing about 7.5ug per lml, according to UV-visible spectrophotometry (General 0401) determination, the absorbance was measured at a wavelength of 240nm, and the absorption coefficient was 730 to 760.
take 2.0g of this product, add 100ml of water, heat and boil, cool, add water to 100ml, shake, filter, take 25ml filtrate, check according to law (General rule 0801), not more concentrated (0.01%) than the control solution made of 5ml of standard sodium chloride solution.
take 25ml of the filtrate remaining under the chloride item and check it according to law (General 0802). Compared with the control solution made of 1 ml of standard potassium sulfate solution, it should not be more concentrated (0.02%).
take 1.0g of this product, add 20ml of methanol solution (1-2), stir well, add 1ml of basic sodium nitrosoferricyanide solution, shake well, place for 30 minutes, and do not show blue-green.
take 0.lg of this product, add 5ml ethanol, heat and dissolve, add an appropriate amount of water, shake, filter a 50ml Cuvette, add water to make 50ml, immediately add a new dilute ammonium ferric sulfate solution (take 1ml of lmol/L hydrochloric acid solution, add 2ml of ammonium ferric sulfate indicator solution, then add an appropriate amount of water to make 100ml), shake, within 30 seconds such as color, add 0.lg of salicylic acid into 1000ml measuring flask, add 1ml of glacial acetic acid, shake well, add appropriate amount of water to the scale, shake well, take 1ml, add 5ml of ethanol and 44ml of water, then add 1ml of the newly prepared dilute ammonium ferric sulfate solution, shake well), and no deeper (0.1%).
new system for clinical use. Take this product, add methanol to dissolve and dilute to make a solution containing 0.4mg per lml, shake well, as a test solution; Take lml accurately and put it in a 100ml measuring flask, dilute to the scale with methanol, shake, as a control solution; Another appropriate amount of acetaminophen control was taken, dissolved in methanol and diluted to prepare a solution containing about 10ug per 1 ml as a control solution. According to the chromatographic condition test under the content determination item, the sample solution, the reference solution and the control solution are respectively l0ul, and the human liquid chromatograph is injected respectively, record the chromatogram to 2.5 times of the retention time of the main component peak. If there are chromatographic peaks in the chromatogram of the test solution that are consistent with the retention time of the main component peak of the reference solution, the peak area shall not be greater than 0.1 times (0.1%) of the main peak area of the control solution, and the peak area of other individual impurities shall not be greater than 0.5 times (0.5%) of the main peak area of the control solution, the sum of each impurity peak area shall not be greater than the main peak area of the control solution (1.0%).
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).
antipyretic analgesic, non-steroidal anti-inflammatory drugs.
light shielding, sealed storage.
This product contains Benorilate (C17H15N05) should be 95.0% to 105.0% of the label.
This product is white tablet.
Take 10 tablets of this product, precision weighing, fine grinding, precision weighing fine powder (about 20mg equivalent to Benorilate), methanol was added to dissolve and diluted to prepare a solution containing about 0.4mg of Benorilate per 1 ml, filtered, and the filtrate was taken as a test solution. According to the method under the content determination of Benorilate, it is obtained.
with Benorilate.
(1)0.2g (2)0.4g (3)0.5g
light shielding, sealed storage.
Pharmacological action and mechanism of action | Benorilate is a neutral compound that binds aspirin and acetaminophen with ester bonds. It has antipyretic and analgesic effects, and has less adverse reactions than aspirin. Patients are easy to tolerate. After oral administration, it is not hydrolyzed in the gastrointestinal tract, absorbed in the intestine and quickly reaches an effective concentration in the blood. The characteristic is that it rarely causes gastrointestinal bleeding. |
adverse reactions | 1. mild gastrointestinal reactions such as vomiting, constipation, heartburn, etc. have also been reported to cause diarrhea. 2. It can cause rash. 3. still visible drowsiness, dizziness, disorientation and other neurological and mental symptoms. |
use | this product is the esterification product of aspirin and paracetamol, and is a new anti-inflammatory, antipyretic, analgesic and rheumatic drug. Adverse reactions are smaller than aspirin, and patients are easy to tolerate. After oral administration, it is not hydrolyzed in the gastrointestinal tract, is easily absorbed and quickly reaches an effective concentration in the blood. Mainly used for rheumatoid arthritis, acute and chronic rheumatoid arthritis, rheumatic pain, cold and fever, headache, postoperative pain, neuralgia, etc. Adverse reactions include vomiting, dyspepsia and constipation. Sleepiness, dizziness and disorientation can still be seen. When the dosage is too large, most people may have tinnitus and deafness. Use with caution in patients with liver and kidney function impairment. Aspirin allergy is contraindicated. The oral LD50 was 2000mg/kg for mice and -10000mg/kg for rats. The LD50 was 1255mg/kg for mice and 1830mg/kg for rats. The esterification of acetaminophen and aspirin, suitable for rheumatoid arthritis, rheumatoid arthritis, headache, neuralgia, fever, etc. |
Production method | Acetylsalicylic acid is acyl chlorinated to generate acetylsalicylchloride, which is then condensed with p-acetamido phenol to obtain benorilate. |