Molecular Formula | C29H34Cl2N2O2 |
Molar Mass | 513.5 |
Density | 1.1905 (rough estimate) |
Melting Point | 223-225°C |
Boling Point | 647.2°C at 760 mmHg |
Flash Point | 345.2°C |
Solubility | Soluble in water (160 mg/ml), methanol (286 mg/ml), ethanol (53.7 mg/ml), DMSO (205 mg/ |
Vapor Presure | 1.23E-17mmHg at 25°C |
Appearance | neat |
Color | White to Almost white |
Merck | 14,5571 |
pKa | 8.66(at 25℃) |
Storage Condition | 2-8°C |
Refractive Index | 1.6100 (estimate) |
MDL | MFCD00058581 |
Use | Used as antidiarrheal |
Hazard Symbols | T - Toxic |
Risk Codes | 25 - Toxic if swallowed |
Safety Description | 45 - In case of accident or if you feel unwell, seek medical advice immediately (show the label whenever possible.) |
UN IDs | UN 2811 6.1/PG 3 |
WGK Germany | 3 |
RTECS | TM4960000 |
HS Code | 29333990 |
Hazard Class | 6.1(b) |
Packing Group | III |
Toxicity | LD50 in mice (mg/kg): 75 s.c.; 28 i.p.; 105 orally; in rats (mg/kg): 185 orally (Niemegeers) |
Reference Show more | 1. Li Mengwei, Yang Haiyang, Sun Wenyan, et al. Effects of Moringa oleifera leaves and its compound on defecation and gastrointestinal hormone levels in rats with constipation [J]. Chinese scientific and technological data catalogue-Chinese herbal medicine, 2019, 042(007):1291-1296. 2. [IF = 3.412] Yuefeng Zhang et al."Study on the Effective Material Basis and Mechanism of Traditional Chinese Medicine Prescription (QJC) Against Stress Diarrhea in Mice."Front Vet Sci. 2021; 8: 724491 3. [IF=4.932] Jing Xu et al."Atractyloside-A ameliorates spleen deficiency diarrhea by interfering with TLR4/MyD88/NF-κB signaling activation and regulating intestinal flora homeostasis."Int Immunopharmacol. 2022 Jun;107:108679 |
crystallized from isopropanol, melting point 222-223 °c.
after the action of diphenylacetonitrile and sodium amino acid, ethylene oxide was introduced into the reaction. To the resulting product of the reaction, 36% hydrogen bromide in glacial acetic acid was added to give 4 Bromo -2,2-= phenyl butyric acid. Next, the reaction is carried out by oxidizing sulfoxide chloride, and then adding dimethylamine to toluene and water for acylation, and finally reacting with 4-monohydroxy-4-p-chlorophenylpiperidine to obtain loperamide.
This product is N ,N-dimethyl-a,a-diphenyl -4-(p-chlorophenyl)-4-hydroyl-1-piperidinylbutanamide hydrochloride. The content of C29H33ClN202 • HC1 shall be between 98.0% and 102.0% calculated as dry.
long-acting anti-diarrhea drugs. Similar to morphine, can significantly inhibit intestinal peristalsis and diarrhea, but no morphine-like central inhibitory effect, also does not affect the intestinal cavity solute and water transport. Can be effective and safe control of acute and chronic diarrhea, can reduce ileostomy outflow and increase its hardness. It is suitable for acute Diarrhea and chronic Diarrhea caused by various causes, such as ulcerative colitis, nonspecific colitis, irritable bowel syndrome and the treatment of chronic Diarrhea caused by partial gastrectomy and hyperthyroidism.
loperamide hydrochloride: Mouse LDso(mg/kg): 75 subcutaneous injection, 105 by mouth. Rat oral LDso (mg/kg):185.
take about 15mg of this product, precision weighing, according to the oxygen flask combustion method (General 0703) for organic destruction, with lmol/L sodium hydroxide solution 20ml as the absorption liquid, once the combustion is completed, shake strongly for 15 minutes, rinse the bottle stopper and platinum wire with a small amount of water, add 1 drop of bromophenol blue indicator solution to the liquid, adjust with dilute nitric acid until the solution turns yellow, then add lml of dilute nitric acid, 20ml of ethanol and 5-10 drops of 1% diphenylhydrazine ethanol solution, titrate with mercury nitrate titration solution (0.005mol/L), with strong shaking near the end point, the solution was given a light rose-red color and the results of the titration were corrected with a blank test. Each 1 ml of mercury nitrate titration solution (0.005mol/L) is equivalent to 0.3545mg of C1. Chlorine content should be 13.52% ~ 14.20%.
take this product O.lg, put in 100ml measuring flask, add methanol to dissolve and dilute to the scale, shake well, as a test solution; Take 1ml, put in 200ml measuring flask, dilute to the scale with methanol, as a control solution. Determined by high performance liquid chromatography (General 0512). Silica gel bonded with eighteen alkyl silane was used as the filler, and O.Olmol/L tetrabutylammonium hydrogen sulfate solution-acetonitrile-methanol (63:26:11) was used as the mobile phase. The detection wavelength was 220nm. The number of theoretical plates shall not be less than 3000 calculated by loperamide hydrochloride peak, and the separation degree between the main peak and the adjacent impurity peak shall meet the requirements. 20ul of control solution and 20ul of test solution were respectively injected into human liquid chromatograph, and the chromatogram was recorded to 2 times of the retention time of principal 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 0.4 times (0.2%) 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).
This product l.Og, inspection according to law (General rule 0841), residual flooding shall not exceed 0.2%.
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 0.4g of this product, weigh it accurately, add 50ml of ethanol and 5.0ml of O.Olmol/L hydrochloric acid solution, shake to dissolve. Potentiometric titration (General 0701), with sodium hydroxide titration solution (0.lmol/L) titration, record the volume difference of two breakthrough point consumption titration solution, each lml sodium hydroxide titration solution (0.1 mol/L) corresponds to 51.35mg of C29H33C1N202. HCl.
antidiarrheal drugs.
light shielding, sealed storage.
This product contains loperamide hydrochloride (C29H33C1N202 • HCl) should be 90.0% ~ 110.0% of label amount.
The content of this product is white or white powder.
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.
with loperamide hydrochloride.
2mg
sealed and stored in a dry place.