Rivastigmine Tartrate

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Cat Number

API0232076

CAS Number

129101-54-8

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Product Detail Description Scientific Support Customer Q&A

CAS Number

129101-54-8

EINECS

603-318-3

Storage

Store at room temperature

Synonyms

Rivastigmine Hydrogen Tartrate; Rivastigmine bitartrate; Rivastigmine hydrogentartrate; Rivastigmine actavis

Molecular Formula

C18H28N2O8

Molecular Weight

400.4

Smiles

CCN(C)C(=O)OC1=CC=CC(=C1)[C@H](C)N(C)C.[C@@H]([C@H](C(=O)O)O)(C(=O)O)O

Appearance

White to off-white crystalline powder

Melting Point

123-125°C

Boiling Point

316.2°C at 760 mmHg

General Description

Rivastigmine tartrate is a synthetic carbamate derivative, a cholinesterase inhibitor, with a phenyl and an ethyl group. Its chemical structure is (S)-3-[1-(dimethylamino)ethyl]phenyl ethyl(methyl)carbamate tartrate. It is a white to off-white crystalline powder that is soluble in water.

Mechanism of Action

Rivastigmine acts by reversibly inhibiting both acetylcholinesterase (AChE) and butyrylcholinesterase (BuChE) in the brain, increasing the levels of acetylcholine in the synaptic cleft. This enhances cholinergic neurotransmission, which is deficient in Alzheimer's disease and Parkinson's disease dementia.

Application

Rivastigmine is indicated for the treatment of mild to moderate dementia associated with Alzheimer's disease and Parkinson's disease. It is effective in improving cognitive function, global function, and activities of daily living.

Rivastigmine in situ‑forming microparticles (RV‑ISM) were optimized using a central composite design to minimize burst release (Q₁ 15.5%) and sustain release over 30 days (T₅₀% 13.09 days). The optimal formulation (MF/D ratio 11.7:1, SAIB/PLGA 1.64:1) showed pseudoplastic flow, uniform particles, good injectability, low cytotoxicity, and tolerance to γ‑sterilization. In vivo PK showed controlled absorption following IM/SC injection. RV‑ISM is a promising long‑acting delivery system for rivastigmine.

Fig. 1 <i>In vitro</i> cytotoxicity results using EBTr cells treated for 48 h with different concentrations of the optimal drug-free-ISM system. (Haider M, <i>et al</i>., 2021) Fig. 1 In vitro cytotoxicity results using EBTr cells treated for 48 h with different concentrations of the optimal drug-free-ISM system. (Haider M, et al., 2021)

References

Haider M, et al. In Situ-Forming Microparticles for Controlled Release of Rivastigmine: In Vitro Optimization and In Vivo Evaluation. Pharmaceuticals (Basel). 2021;14(1):66.

Does Rivastigmine Tartrate require protection from moisture during long-term storage?

Yes, it is hygroscopic and susceptible to hydrolysis of the carbamate group. Store in tightly sealed containers with desiccant.

What is the recommended storage temperature for Rivastigmine Tartrate?

Store at controlled room temperature (15–25°C). Avoid excessive heat above 30°C, which accelerates degradation.

Is Rivastigmine Tartrate stable in capsule and transdermal patch formulations?

Capsules are stable with moisture-protective packaging. Patches are stable when protected from light and moisture.

How is the impurity rivastigmine N-oxide (an oxidative degradation product) monitored?

This degradation product is quantified using a stability-indicating HPLC method, ensuring it remains within pharmacopoeial limits.