Thiethylperazine Maleate is the maleate salt of thiethylperazine, a phenothiazine derivative with antiemetic and dopamine-antagonist properties. It is used as a pharmaceutical active ingredient in formulations intended to control nausea and vomiting.
Thiethylperazine Maleate has the molecular formula C₂₂H₂₉N₃S₂·2C₄H₄O₄ and a molecular weight of 631.76 g/mol. Its CAS number is 1179-69-7. The free base thiethylperazine has CAS number 1420-55-9 and molecular weight 399.6 g/mol.
Thiethylperazine belongs to the phenothiazine class and contains an ethylthio substituent and a methylpiperazine side chain. The pharmaceutical API is commonly encountered as the maleate salt, also known as thiethylperazine dimaleate.
USP recognizes Thiethylperazine Maleate as an official pharmaceutical substance and specifies its identity, assay, pH, loss on drying, residue on ignition, selenium content and chromatographic purity requirements.
Thiethylperazine Maleate is a phenothiazine derivative containing a sulfur-containing phenothiazine ring system and a substituted piperazine side chain. Conversion to the maleate salt provides the pharmaceutical salt form used in recognized drug products.
The USP monograph identifies the substance as 2-(ethylthio)-10-[3-(4-methyl-1-piperazinyl)propyl]phenothiazine maleate (1:2).
Thiethylperazine primarily acts as a dopamine receptor antagonist. Its antiemetic activity is associated with inhibition of dopaminergic signaling involved in the vomiting reflex.
Thiethylperazine also exhibits activity at several other receptor systems, but its principal pharmacological classification is as a dopamine-antagonist phenothiazine antiemetic. NCBI identifies thiethylperazine as an antiemetic and dopamine antagonist.
Thiethylperazine Maleate is used as an active pharmaceutical ingredient in antiemetic formulations.
Its therapeutic applications include the management of nausea and vomiting associated with conditions such as anesthesia, certain chemotherapy treatments, radiation and other emetic stimuli. NCBI specifically describes thiethylperazine as useful for nausea and vomiting associated with anesthesia, mildly emetic cancer chemotherapy agents, radiation therapy and toxins.
The API has been incorporated into pharmaceutical dosage forms including tablets and injectable formulations. Historical US prescribing information identifies thiethylperazine maleate as the active ingredient in Torecan tablets and injection.
Thiethylperazine Maleate quality is evaluated using pharmacopoeial and validated analytical methods.
Important quality-control parameters include:
The USP monograph specifies an assay of 98.0–101.5% on the dried basis. The pH of a 1 mg/mL aqueous solution is specified as 2.8–3.8, loss on drying is NMT 0.5%, residue on ignition is NMT 0.1%, and selenium is limited to 0.003%. Chromatographic purity requires any individual secondary spot to be NMT 0.5% and the sum of all secondary spots to be NMT 2.0%.
Swapnroop Drugs and Pharmaceuticals is a WHO-GMP certified pharmaceutical company engaged in pharmaceutical APIs and pharmaceutical raw materials for domestic and international markets.
Thiethylperazine Maleate API can be evaluated according to USP requirements, customer-specific specifications and applicable regulatory requirements. Product documentation and analytical information can be provided according to the intended pharmaceutical application and destination market.
Thiethylperazine Maleate should be protected from light and stored in appropriately closed pharmaceutical containers.
The USP monograph specifies preservation in tight, light-resistant containers. Analytical procedures also emphasize minimizing exposure to daylight during testing because of the light sensitivity of the analytical material.
Technical documentation for Thiethylperazine Maleate API may include:
Swapnroop Drugs and Pharmaceuticals operates as a WHO-GMP certified pharmaceutical company with a portfolio of pharmaceutical APIs and pharmaceutical raw materials.
For Thiethylperazine Maleate API requirements, customers can request product specifications, analytical documentation, packaging information and commercial details according to their pharmaceutical development, manufacturing and regulatory requirements.
| Parameter | Specification |
|---|---|
| Appearance | white to off-white crystalline powder |
| Identification | IR & HPLC compliant |
| Assay (HPLC) | 98.0–101.5%, |
| Loss on Drying | NMT 0.5% |
| Residue on Ignition | NMT 0.1% |
| Heavy Metals | NMT 30 ppm |
| pH (1% Solution) | 2.8–3.8 |
| Individual Impurity | NMT 0.5% |
| Total Impurities | NMT 2.0% |