Name | Domperidone |
Synonyms | kw-5338 Motilium Domperidone DoMperidone-d6 DOMPERIDONE BASE Domperidone,Motilium midazol-1-yl)propyl)-4-piperidinyl)- DoMperidone Sustained Release Pellets alpha-[2-(diisopropylamino) ethyl]-alpha-phenyl-2-pyridineacetamide 5-Chloro-1-[1-[3-(2-oxo-1-benzimidazolyl)propyl]-4-piperidyl]benzimidazol-2-one 5-chloro-1-{1-[3-(2-oxo-2,3-dihydro-1H-1,3-benzodiazol-1-yl)propyl]piperidin-4-yl}-2,3-dihydro-1H-1,3-benzodiazol-2-one |
CAS | 57808-66-9 |
EINECS | 260-968-7 |
InChI | InChI=1/C22H24ClN5O2/c23-15-6-7-20-18(14-15)25-22(30)28(20)16-8-12-26(13-9-16)10-3-11-27-19-5-2-1-4-17(19)24-21(27)29/h1-2,4-7,14,16H,3,8-13H2,(H,24,29)(H,25,30) |
InChIKey | FGXWKSZFVQUSTL-UHFFFAOYSA-N |
Molecular Formula | C22H24ClN5O2 |
Molar Mass | 425.91 |
Density | 1.2904 (rough estimate) |
Melting Point | 240-244°C |
Water Solubility | Slightly soluble in water. |
Solubility | DMSO 48 mg/mL Water <1 mg/mL Ethanol 1 mg/mL |
Appearance | solid |
Color | white |
Merck | 14,3418 |
pKa | pKa 7.90 (Uncertain) |
Storage Condition | Store at RT |
Stability | Stable. Incompatible with strong oxidizing agents. |
Refractive Index | 1.5400 (estimate) |
MDL | MFCD00069256 |
Physical and Chemical Properties | White crystalline powder from dimethylformamide-water, melting point 242.5 °c |
Use | Anticholinergic antispasmodic |
Hazard Symbols | Xn - Harmful |
Risk Codes | R62 - Possible risk of impaired fertility R63 - Possible risk of harm to the unborn child |
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 | DE2275900 |
HS Code | 29333990 |
Reference Show more | 1. Qiao Yujun, Jia Chen, Cao Aijia, Zhang Rui, Hua Xi, Jiao Haisheng. Effect of sodium valproate on pharmacokinetics of Tanshinone ⅱa in epileptic rats [J]. Modern Chinese medicine research and practice, 2020,34(06):31-35. 2. Mengqiu Lu, Haizhen Liang, Pengfei Tu, Yong Jiang. Pharmacodynamic comparison of two different source plants of Murrayae Folium et Cacumen[J]. Journal of Chinese Pharmaceutical Sciences, 2021, 30(1): 49-57.doi: 10.5246/jcps.2021.1.0005 |
white or off-white powder. Slightly soluble in ethanol, very slightly soluble in acetone. Practically insoluble in water. Generally stable. Melting point 242.5 °c.
2-nitro-1, 4-= chlorobenzene and 4-amino cyclohexyl carboxylic acid ethyl ester reaction, re-hydrogenation reduction, and urea cyclization, hydrolysis, 5 monochloro 1-(piperidin-4-yl) -1.3-dihydro -2H-benzoxazol-2-one was obtained. In addition, the nucleophilic substitution of hydroxypropylamine with 2-nitrochlorobenzene was performed, followed by hydrogenation and reduction, cyclization with potassium cyanide followed by chlorination to obtain 1-(3-chloropropyl)-2,3-= hydrogen -1H-benzobilazol -2 ketone. The above two compounds were stirred with sodium carbonate, potassium iodide and 4-methyl -2-pentanone, and domperidone was obtained.
This product is 5-chloro-l-[l-[3-(2, 3-dihydro-2-oxo-1h-benzimidazol-1-yl) propyl]-4-pyridinyl]-1, 3-dihydro-2h-benzimidazol-2-one. Calculated as dried product, the content of C22H24C1N502 shall not be less than 99.0%.
developed by pharmaceutical company Janssen, Belgium. Dopamine receptor antagonist with strong effect, with peripheral blocking effect, directly acting on the gastrointestinal wall, can increase the tension of lower esophageal sphincter, prevent gastroesophageal reflux, enhance gastric peristalsis, promote gastric emptying, coordination of gastric and duodenal movement, inhibit Nausea, Vomit, and can effectively prevent bile reflux, does not affect the secretion of gastric juice. It is suitable for dyspepsia caused by delayed gastric emptying, gastroesophageal reflux, esophagitis, such as upper abdominal distension, upper abdominal pain, belching, flatulence, Nausea, Vomit, burning sensation of the stomach in the mouth with or without reflux of the contents of the stomach. Because it has almost no inhibitory effect on dopamine receptors in the brain, it has no mental and neurological side effects. And can be used for taking dopamine receptor agonist treatment of Parkinson's disease caused by Nausea.
weigh about 0.1kg of this product accurately, put it in a 10ml measuring flask, add N,N-dimethylformamide to dissolve and dilute to the scale, shake well, and use it as a test solution, A solution containing 25ug of domperidone per 1 ml was prepared as a control solution by dilution with N,N-dimethylformamide. Determined by high performance liquid chromatography (General 0512). Silica gel bonded with eighteen alkyl silane was used as filler; Methanol was used as mobile phase A, 0.5% ammonium acetate solution was used as mobile Phase B, and gradient elution was carried out according to the following table. The flow rate was 1.2ml per minute; The detection wavelength was 285nm. Take domperidone and Droperidol about 15mg each, put them in 100ml measuring flask, add N, N-dimethylformamide to dissolve and dilute to scale, shake well, take 10u1 and inject human liquid chromatograph, the degree of separation of domperidone from Droperidol and other adjacent impurity peaks should meet the requirements. 10 u1 of the test solution and the control solution were respectively injected into the liquid chromatograph, and the chromatograms were recorded. If there are impurity peaks in the chromatogram of the test solution, the area of a single impurity peak shall not be greater than the area of the main peak of the control solution (0.25% ), and the sum of each impurity peak area shall not be greater than 2 times the area of the main peak of the control solution (0.5%).
methanol, dichloromethane, Tetrahydrofuran, N, N-dimethylformate Amine, toluene and xylene take about 0.2g of this product, weigh it accurately, put it in a 20ml headspace bottle, and add 2ml of dimethyl sulfoxide precisely, ultrasonic dissolution, seal, as a test solution; Take methanol, dichloromethane, Tetrahydrofuran, N, N-dimethylformamide, toluene and xylene each appropriate amount, precision weighing, prepare a mixed solution containing about 150ug of methanol, 60ug of dichloromethane, 72ug of tetrahydrofuran, 176ug of N, N-dimethylformamide, 44.5ug of toluene and 217ug of xylene per 1 ml of dimethyl sulfoxide, and take 2ml of the solution with a precise amount, A 20ml headspace bottle was placed, sealed, and used as a control solution. Determined as residual solvent assay (General 0861). A capillary column with 100% dimethylpolysiloxane (or similar polar) as the stationary liquid is used as the chromatographic column; The starting temperature is 40°C, the temperature is maintained for 9 minutes, and the temperature is raised to 120°C at a rate of 8°C per minute for 2 minutes, then at a rate of 20°C per minute to 160°C; Injection port temperature of 200°C; Detector for flame ionization detector (FID ), detector temperature of 250°C; Column flow rate of 2.5 per minute, the split ratio was 1:1, the headspace bottle equilibration temperature was 100°C, and the equilibration time was 30 minutes. Take the reference solution into the headspace, and the separation degree between the peaks of each component shall meet the requirements. The test solution and the reference solution were injected by Headspace, and the chromatograms were recorded. According to the external standard method to calculate the peak area, the residue should be in accordance with the provisions.
take about 0.2g of this product, accurately weigh it, put it in a 5ml measuring flask, add dimethyl sulfoxide to dissolve and dilute to the scale, shake it well, and use it as a test solution, A solution containing about 2.4ug of chloroform per 1 ml was prepared using dimethyl sulfoxide as a control solution. Determined as residual solvent assay (General 0861). The capillary column with 6% cyanopropylphenyl-94% dimethylpolysiloxane (or similar polarity) as the stationary liquid was used as the chromatographic column; The initial temperature was 60 ° C. For 6 minutes, the temperature was raised to 200°C at a rate of 20°C per minute for 4 minutes; The inlet temperature was 200°C; The detector was an electron capture detector (ECD), and the detector temperature was 300°C; column flow rate of 4.5 per minute, split ratio of 15:1. The test solution and the reference solution were injected by Headspace, and the chromatograms were recorded. According to the external standard method to calculate the peak area, the residue should comply with the provisions.
take this product, dry to constant weight at 105°C, weight loss shall not exceed 0.5% (General rule 0831).
take this product l.Og, check according to law (General rule 0841), shall not pass 0.
The residue left under the item of taking the ignition residue shall not contain more than 20 parts per million of heavy metal when examined by law (General rule 0821, Law II).
take about 0.35g of this product, precision weighing, add 40ml of glacial acetic acid to dissolve, add 1 drop of crystal violet indicator solution, and use perchloric acid titration solution (0.1 mol/L) titration to the solution showed blue-green, and the titration results were corrected by blank test. Each 1 ml of perchloric acid titration solution (0.1 mol/L) corresponds to 42.59mg of C22H24C1N502.
gastrointestinal motility drugs.
light shielding, sealed storage.
This product contains domperidone (C22H24C1N502) should be labeled the amount of 90.0% ~ 110.0%.
This product is white tablet.
Same as domperidone.
(l)5mg (2)10mg
light shielding, sealed storage.