Acamprosate Calcium

Acamprosate Calcium

製品名 Acamprosate Calcium
CAS番号 77337-73-6
分子式 C10H20CaN2O8S2
分子量 400.48 g/mol
外観 白色からオフホワイトの結晶性粉末
分析(HPLC) 98.0% – 102.0% (on dried basis)
乾燥減量 ≤ 0.5%
重金属 10 ppm以下
溶解度 Soluble in water, practically insoluble in ethanol
パッケージ 25 kg net in fiber drum with double PE liner

Acamprosate Calcium Structure

同義語: Calcium acetylhomotaurinate, N-Acetylhomotaurine calcium salt, Acamprosate calcium, Calcium 3-(acetylamino)propane-1-sulfonate, Campral

Acamprosate calcium is a synthetic molecule that belongs to the class of acetylated amino sulfonic acids. Its structure features a taurine backbone (2-aminoethanesulfonic acid) modified with an acetyl group on the nitrogen, and a calcium ion that balances the sulfonate charge. This unique combination yields a compound with high polarity and water solubility, enabling rapid dissolution in physiological fluids. The presence of both sulfonate and amide functionalities allows for specific interactions with neuronal membranes, particularly modulating glutamatergic and GABAergic systems.

First approved in Europe in the late 1980s for the management of alcohol dependence, acamprosate calcium has since become a standard pharmacotherapy, supported by extensive clinical evidence. It is commercially available as enteric-coated tablets under brand names such as Campral, and is also supplied as an active pharmaceutical ingredient (API) for generic formulations. The compound is synthesized through a multi-step process involving acetylation of homotaurine followed by calcium salt formation, yielding a highly pure, crystalline product that meets stringent pharmacopeial standards (USP/EP).

In the pharmaceutical industry, acamprosate calcium is valued not only for its established efficacy but also for its favorable safety profile and tolerability. Ongoing research explores its potential in other neurological conditions, such as tinnitus and neuroprotection, further driving demand for high-quality API. Our product is manufactured under cGMP conditions, ensuring consistent quality and regulatory compliance for formulation into solid oral dosage forms.

化学構造と性質

Acamprosate calcium is the calcium salt of N-acetylhomotaurine, with the molecular formula C10H20CaN2O8S2 and a molecular weight of 400.48 g/mol. The molecule consists of two molecules of N-acetylhomotaurine (each comprising a three-carbon chain with a sulfonate group at one end and an acetylamino group at the other) coordinated to a central calcium ion. This structure confers high aqueous solubility (greater than 100 mg/mL) and low lipophilicity, limiting passive diffusion across biological membranes. The compound is stable under normal storage conditions but should be protected from moisture and excessive heat. Its crystalline form is typically a white to off-white powder, and it exhibits polymorphism, with the most stable form being the monohydrate. The calcium salt is essential for its pharmacological activity, as the free acid form is less stable and less soluble.

作用機序

  • Glutamate modulation: Acamprosate calcium reduces glutamatergic neurotransmission by antagonizing NMDA receptors and inhibiting presynaptic glutamate release, thereby dampening the hyperexcitatory state associated with alcohol withdrawal.
  • GABAergic enhancement: It positively modulates GABA-A receptors, increasing inhibitory tone in the central nervous system, which helps restore the balance between excitatory and inhibitory signaling.
  • Calcium channel interaction: The calcium ion may influence neuronal calcium homeostasis, contributing to its neuroprotective effects and reducing alcohol craving.
  • Effect on taurine system: As a taurine analog, acamprosate may interfere with taurine transport and modulate osmotic stress, although the exact role in its therapeutic effect is still under investigation.

品質仕様

パラメータ 仕様
外観 白色からオフホワイトの結晶性粉末
Assay (HPLC, on dried basis) 98.0% – 102.0%
乾燥減量 ≤ 0.5%
重金属 10 ppm以下
関連物質 Total impurities ≤ 0.5%
残留溶剤 Meets USP/EP requirements
Microbial Limits Total aerobic count ≤ 1000 CFU/g

供給および書類

  • 容量: 5 metric tons per month, scalable upon demand.
  • リードタイム: 3~5営業日(在庫品)
  • ドキュメント: COA, MSDS, TDS, DMF (if required), and regulatory support.
  • パッケージ: 25 kg net in fiber drums with double polyethylene liners, or as per customer request.

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  • リブバイオ株式会社. — メールアドレス: info@lyvbio.com

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