Memantine HCl

Синонимы: 1-Amino-3,5-dimethyladamantane hydrochloride, 3,5-Dimethyl-1-adamantanamine hydrochloride, Memantine hydrochloride, Namenda, Axura, Ebixa, D-145

Memantine HCl is the hydrochloride salt of memantine, a low-affinity uncompetitive antagonist of the NMDA receptor. Unlike other adamantane derivatives such as amantadine, memantine carries two methyl groups on the adamantane cage, a modification that fine-tunes its binding kinetics and improves tolerability. First approved in Europe in the 1990s and later in the United States under the brand Namenda, it has become a mainstay in the management of moderate-to-severe Alzheimer’s disease.

In terms of chemical behavior, memantine HCl is a white crystalline solid that is freely soluble in water and in ethanol, but practically insoluble in nonpolar solvents. Its pKa of approximately 10.3 means the amine is protonated at physiological pH, which limits passive diffusion across membranes but supports its use as a well-behaved salt form for oral solid dosage. The molecule is stable under ordinary storage conditions, though it should be protected from excessive moisture and heat.

For formulators, the salt form offers advantages over the free base: better aqueous solubility, improved handling, and more consistent dissolution profiles. It is commonly used in immediate-release tablets, extended-release capsules, and oral solutions. The active pharmaceutical ingredient is also investigated in combination products and in generic development programs targeting the growing dementia care market.

Функция

• NMDA receptor antagonism: Memantine binds preferentially to the open channel of the NMDA receptor, reducing pathological glutamate signaling without interfering with normal synaptic transmission.
• Нейропротекция: By dampening excitotoxicity, it helps protect neurons from calcium overload and subsequent damage.
• Symptomatic improvement in Alzheimer’s: Clinically, it slows cognitive and functional decline in moderate-to-severe stages of the disease.
• Modulation of glutamatergic transmission: The drug’s fast on/off kinetics allow it to act as a buffer against excessive glutamate, which may contribute to its cognitive benefits.
• Adjunct in other neurological conditions: Research continues into its potential in Parkinson’s disease, neuropathic pain, and obsessive-compulsive disorder, though these uses remain investigational.

Source & Standardization

• Source: Synthetic, derived from adamantane through a multi-step process.
• Standardization: Complying with USP/EP monograph specifications; assay 98.0%–102.0% on dried basis.
• Forms: Crystalline powder; also available as micronized grades for improved blend uniformity.
• Приложения: Oral solid dosage forms, extended-release formulations, and fixed-dose combinations.

Технические характеристики

Documentation & Supply

• Monthly capacity: 5 metric tons
• Срок выполнения заказа: 3–5 рабочих дней (товары, имеющиеся в наличии)
• Documentation: COA, MSDS, TDS, and regulatory support available upon request
• Packaging: 25 kg fiber drum with double polyethylene liner; custom packaging options for small-scale trials

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