Pharmaceutical Bulk Levosulpiride Powder

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Levosulpiride Powder Usage and Synthesis.

Levosulpiride different dosage forms, different specifications of the dosage may vary, please read the specific drug instructions for use, or follow doctor's advice.

1、Schizophrenia: Adults take 100mg orally once, 2 times/day; Intramuscular injection once 100mg, 2 times/day.

2、Gastrointestinal disorders: 25mg orally once, 3 times/day.

3、Vomiting due to chemotherapy: Intravenous injection 1mg/kg once, 3 times/day.

4、Prevention of postoperative vomiting: single dose of 50-100mg intravenously before general anaesthesia.

Uses and functions of Levosulpiride.

Levosulpiride is the levorotatory form of sulpiride, and both have similar effects and uses, but the dosage of levosulpiride is only half or less, which results in fewer toxic side effects.

Levosulpiride is mainly used for the treatment of schizophrenia, somatoform disorders, depression, as well as for the treatment of irritable bowel syndrome, dyspepsia, diabetic paraparesis, reflux oesophagitis and chemotherapy-induced vomiting.

Pharmacological Effects of Levosulpiride Raw.

Levosulpiride is a benzamide derivative, the left enantiomer of sulpiride, which is biologically active, blocking dopamine receptors and producing antipsychotic, antidepressant, antinausea and digestive effects. It is excitatory at low doses and inhibitory only at very high doses, with a lower D2/D3 affinity ratio. It is used at lower doses and has fewer adverse effects than the eliminators.

Levosulpiride primarily blocks dopamine D2 receptors, especially at low doses, and its own receptors located on the presynaptic membrane of the CNS and gastrointestinal dopamine transduction pathway.

Production method of Bulk Levosulpiride Powder.

The preparation is the same as that of sulpiride, except that 2-aminomethyl-1-ethylpyrrolidine is chemically split to give the S-type before reacting with methyl 2-methoxy-5-sulfamoylbenzoate.

The racemic 2-aminomethyl-1-ethylpyrrolidine was added dropwise to an aqueous solution of D-(-)-tartaric acid at room temperature with stirring. Anhydrous ethanol was then added and left in the refrigerator overnight. The solid was collected by filtration, refluxed with methanol, filtered hot and dried to give the tartaric acid salt in 36.8% yield.

The salt and aqueous sodium hydroxide solution were stirred at room temperature and extracted with chloroform. The extract was dried and concentrated, distilled under reduced pressure, and the fraction was collected at 65 °C/2.0 kPa to give (S)-(-)-2aminomethyl-1-ethylpyrrolidine in 43.5% yield. The obtained pyrrolidine of type S, and methyl 2-methoxy-5-sulfamoylbenzoate in ethylene glycol were stirred at 120 °C. Cooled to 5°C and filtered, the crude obtained was recrystallised with 95% ethanol to give levosulpiride in 72.6% yield, melting point 184-186°C, [α]D23-66.4° (C=0.5, dimethylformamide).

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