Galantamine Hydrobromide

Galantamine Hydrobromide

Tên sản phẩm Galantamine Hydrobromide
Số CAS 1953-04-4
Hình thức Bột tinh thể màu trắng đến trắng ngà
Thông số kỹ thuật ≥98,01% TP3T (HPLC)
Công thức phân tử C17H22BrNO3
Trọng lượng phân tử 368.27 g/mol
Độ hòa tan Soluble in water, ethanol; slightly soluble in acetone
Gói 25 kg fiber drum, inner polyethylene bags

Galantamine Hydrobromide Structure

Từ đồng nghĩa: Galantamine hydrobromide, (4aS,6R,8aS)-4a,5,9,10,11,12-Hexahydro-3-methoxy-11-methyl-6H-benzofuro[3a,3,2-ef][2]benzazepin-6-ol hydrobromide, Galanthamine hydrobromide, Lycoremine hydrobromide, Nivalin, Razadyne

Galantamine hydrobromide is a tertiary alkaloid salt derived from the Amaryllidaceae family, structurally characterized by a benzofuro[3a,3,2-ef][2]benzazepine core with a methoxy substituent at C3 and a hydroxyl group at C6. This unique framework distinguishes it from other cholinesterase inhibitors and underpins its dual mechanism of action—both as a reversible acetylcholinesterase inhibitor and a positive allosteric modulator of nicotinic acetylcholine receptors. The hydrobromide salt enhances aqueous solubility and stability, making it the preferred form for pharmaceutical formulations.

Originally isolated from snowdrop (Galanthus woronowii) and daffodil (Narcissus pseudonarcissus) bulbs, galantamine has transitioned from a natural product to a synthetically accessible active pharmaceutical ingredient (API). Today, commercial production relies on optimized semi-synthetic or fully synthetic routes, ensuring high purity and consistent supply. The compound is typically available as a white to off-white crystalline powder, with a purity of ≥98.0% as determined by HPLC. It is freely soluble in water and ethanol, facilitating formulation into oral dosage forms such as tablets, capsules, and oral solutions.

In the pharmaceutical industry, galantamine hydrobromide is primarily indicated for mild to moderate Alzheimer’s disease, where it improves cognitive function and global clinical status. Beyond its established use, ongoing research explores its potential in other neurological conditions, including vascular dementia, schizophrenia, and autism spectrum disorders. Its ability to modulate nicotinic receptors also attracts interest in smoking cessation and alcohol dependence therapies. For B2B customers, LyvBio supplies galantamine hydrobromide under strict quality control, supported by comprehensive documentation and reliable logistics.

Cấu trúc và tính chất hóa học

Galantamine hydrobromide belongs to the Amaryllidaceae alkaloid class, featuring a fused tetracyclic skeleton that includes a benzofuran ring. The C3 methoxy group and C6 hydroxyl are critical for its interaction with cholinesterase enzymes and nicotinic receptors. The hydrobromide salt form is obtained by reacting the free base with hydrobromic acid, yielding a stable, crystalline solid with a molecular weight of 368.27 g/mol. It exhibits good thermal stability under recommended storage conditions (2–8°C, protected from light and moisture). The compound’s solubility profile supports both immediate-release and sustained-release formulations, and its chiral centers necessitate stereoselective synthesis or resolution to ensure enantiomeric purity.

Cơ chế tác dụng

  • Acetylcholinesterase inhibition: Galantamine reversibly inhibits acetylcholinesterase, reducing the breakdown of acetylcholine in the synaptic cleft and enhancing cholinergic neurotransmission.
  • Nicotinic receptor modulation: It acts as a positive allosteric modulator at nicotinic acetylcholine receptors, amplifying the response to endogenous acetylcholine and potentially improving synaptic plasticity.
  • Bảo vệ thần kinh: Preclinical studies suggest galantamine may reduce amyloid-beta aggregation and oxidative stress, though clinical relevance is still under investigation.
  • Anti-inflammatory effects: Modulation of microglial activity and cytokine release has been observed in experimental models, indicating potential broader neurological benefits.

Tiêu chuẩn chất lượng

Tham số Thông số kỹ thuật
Assay (HPLC, on dried basis) ≥98,01 TP3T
Xác định IR, HPLC retention time conforms to standard
Hình thức Bột tinh thể màu trắng đến trắng ngà
Mất mát khi sấy khô ≤0.5%
Hàm lượng tro sau khi đốt ≤0.1%
Kim loại nặng ≤10 ppm
Các chất liên quan Total impurities ≤1.0%

Cung ứng và Tài liệu

  • Công suất: Annual production capacity of 5 metric tons, with flexible batch sizes from 1 kg to 500 kg.
  • Thời gian thực hiện: 3-5 business days (stock items)
  • Tài liệu hướng dẫn: COA, MSDS, TDS, and regulatory support (CEP, DMF) provided for each batch.
  • Bao bì: 25 kg fiber drums with double polyethylene liners; custom packaging for small quantities.

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