Rivastigmine Tartrate is the hydrogen tartrate salt of Rivastigmine, a reversible cholinesterase inhibitor used in pharmaceutical products for the management of cognitive symptoms associated with Alzheimer's disease and Parkinson's disease dementia.
Rivastigmine Tartrate has the molecular formula C₁₈H₂₈N₂O₈ and a molecular weight of 400.42 g/mol. Its CAS Registry Number is 129101-54-8. The USP-NF monograph identifies the substance as Rivastigmine Tartrate and specifies its content on an anhydrous basis.
The current USP-NF definition requires Rivastigmine Tartrate to contain 98.0–102.0% of the labeled amount of the tartrate salt, calculated on the anhydrous basis.
Rivastigmine Tartrate consists of the S-enantiomer of Rivastigmine combined with one equivalent of (2R,3R)-tartaric acid. The salt form is used in pharmaceutical development because it provides the active Rivastigmine moiety in a defined pharmaceutical salt form.
The API is chemically related to the phenylcarbamate class of cholinesterase inhibitors. Because Rivastigmine contains a stereogenic center, control of the R-enantiomer is an important quality attribute. The current USP monograph specifically establishes a limit for the R-enantiomer.
| Property | Details |
|---|---|
| API Name | Rivastigmine Tartrate |
| Chemical Form | Rivastigmine Hydrogen Tartrate |
| CAS Number | 129101-54-8 |
| Molecular Formula | C₁₈H₂₈N₂O₈ |
| Molecular Weight | 400.42 g/mol |
| Rivastigmine Moiety MW | 250.34 g/mol |
| FDA UNII | 9IY2357JPE |
| ChEBI ID | CHEBI:64358 |
| API Type | Synthetic small-molecule salt |
| Pharmacological Class | Cholinesterase inhibitor |
| Therapeutic Area | Neurology |
| Active Enantiomer | S-Rivastigmine |
| Physical Form | Pharmaceutical active ingredient in tartrate salt form |
PubChem identifies Rivastigmine Tartrate as a tartrate salt obtained by reaction of Rivastigmine with one equivalent of (R,R)-tartaric acid.
Rivastigmine Tartrate is used as an active pharmaceutical ingredient in medicines containing Rivastigmine.
Rivastigmine is a cholinesterase inhibitor that inhibits both acetylcholinesterase and butyrylcholinesterase.
Pharmaceutical applications include treatment of cognitive symptoms associated with:
Rivastigmine Tartrate can be incorporated into oral pharmaceutical dosage forms and other formulations containing Rivastigmine as the active moiety.
Rivastigmine is a reversible inhibitor of acetylcholinesterase and butyrylcholinesterase. By inhibiting these enzymes, it reduces the breakdown of acetylcholine in the brain.
The resulting increase in cholinergic activity can support neurotransmission in areas of the brain involved in cognition and memory. The pharmacological activity is associated with the Rivastigmine active moiety rather than the tartrate counter-ion.
Rivastigmine Tartrate has a current USP-NF drug-substance monograph with defined analytical requirements. The monograph specifies an assay range of 98.0–102.0% on the anhydrous basis.
The USP analytical framework includes:
The USP assay uses liquid chromatography with UV detection at 215 nm. The system suitability requirements include resolution of at least 1.5, column efficiency of at least 5000 theoretical plates, tailing factor of NMT 3.0, and standard-solution RSD of NMT 2.0%.
The USP monograph also controls the R-enantiomer at NMT 0.3%, demonstrating the importance of stereochemical purity for this API.
Rivastigmine Tartrate manufacturing involves controlled synthesis of the Rivastigmine active moiety followed by formation and purification of the tartrate salt.
Manufacturing controls are important for maintaining the required stereochemical configuration and controlling related substances, residual process materials and inorganic residues.
The final API should undergo appropriate purification, crystallization and drying processes followed by validated analytical testing against the applicable drug-substance specification.
Rivastigmine Tartrate has a molecular weight of 400.42 g/mol, compared with 250.34 g/mol for the Rivastigmine active moiety.
The salt consists of Rivastigmine and L-tartaric acid components in a defined 1:1 relationship.
Because the API is a defined salt containing a stereochemically active pharmaceutical moiety, salt identity and enantiomeric purity are important characteristics during API quality assessment.
The USP-NF monograph specifies that Rivastigmine Tartrate should be preserved in tight containers and stored at room temperature.
Pharmaceutical-grade material should be packaged in suitable containers that protect the API from contamination and inappropriate environmental exposure. Packaging should maintain product identity, batch traceability and integrity throughout storage and transportation.
Pharmaceutical-grade Rivastigmine Tartrate API can be supported by appropriate technical and quality documentation, including:
Rivastigmine Tartrate is a stereochemically defined pharmaceutical salt requiring control of assay, organic impurities, water, inorganic residue and enantiomeric purity.
A quality-focused Rivastigmine Tartrate API manufacturer in India should maintain controlled synthesis and salt-formation processes, validated chromatographic methods and appropriate batch-release testing.
The USP-NF monograph provides clear quality benchmarks, including 98.0–102.0% assay on the anhydrous basis, NMT 0.1% residue on ignition, NMT 0.5% water and NMT 0.3% R-enantiomer.
| Parameter | Specification |
|---|---|
| Appearance | white to off-white crystalline powder |
| Identification | IR & HPLC compliant |
| Assay (HPLC) | 98.0% – 102.0% |
| Loss on Drying | NMT 0.5% |
| Individual Impurity | NMT 0.15% |
| Water Content | NMT 0.5% |