Oxcarbazepine

同義語： 10-Oxo-10,11-dihydro-5H-dibenz[b,f]azepine-5-carboxamide, GP 47680, Oxcarbazepinum, Trileptal, OXC

Oxcarbazepine is a dibenzazepine carboxamide derivative that has established itself as a key API in the antiepileptic market. Chemically, it is the 10-keto analogue of carbamazepine, a structural modification that eliminates the formation of the toxic epoxide metabolite and gives the molecule a cleaner metabolic profile. First approved in Denmark in 1990 and later introduced in the United States in 2000, it has since become a standard option for partial-onset seizures, both as monotherapy and adjunctive therapy.

The compound acts primarily through its active metabolite, the S-monohydroxy derivative (MHD), which blocks voltage-gated sodium channels and stabilizes neuronal membranes. This mechanism underlies its anticonvulsant effect and has also driven interest in its use for bipolar disorder and neuropathic pain. Unlike many older antiepileptics, oxcarbazepine offers linear pharmacokinetics and fewer drug-drug interactions, making it easier to manage in polytherapy regimens.

Commercial production of oxcarbazepine typically starts from 10-methoxy-5H-dibenz[b,f]azepine or related dibenzazepine intermediates, followed by acylation and oxidation steps. The final API is isolated as a white to off-white crystalline powder, with pharmacopoeial monographs (USP, EP) specifying tight limits on related substances and residual solvents. Formulators value its favorable solubility profile in organic solvents, which facilitates wet granulation and tablet compression.

In the global marketplace, oxcarbazepine is traded as a high-purity API with an assay of 98.0%–102.0% on the dried basis. It is routinely supplied with full regulatory documentation, including CEP and DMF support, to meet the requirements of generic drug manufacturers and research organizations. The compound’s well-characterized safety profile and established clinical history continue to sustain steady demand across both mature and emerging markets.

機能

• Anticonvulsant activity: Blocks voltage-gated sodium channels via the active MHD metabolite, reducing neuronal hyperexcitability.
• Mood stabilization: Used as an adjunct in bipolar disorder, particularly in patients who cannot tolerate carbamazepine.
• Neuropathic pain relief: Effective in trigeminal neuralgia and other neuropathic pain syndromes.
• Favorable pharmacokinetics: Linear elimination and minimal autoinduction compared with carbamazepine.
• Reduced metabolic interactions: Avoids the epoxide pathway, lowering the risk of serious adverse effects.

Source & Standardization

• 出典: Synthetic, derived from dibenzazepine intermediates.
• Manufacturing: Multi-step chemical synthesis followed by recrystallization and milling.
• Standardization: Complies with USP and EP monographs; assay 98.0%–102.0% (HPLC).
• Forms: White to off-white crystalline powder.
• 用途: Antiepileptic drug products, generic formulations, research on sodium channel blockers.

仕様

資料・供給

• 月間処理能力: 5–8 metric tons
• リードタイム: 3～5営業日（在庫品）
• ドキュメント: COA, MSDS, available upon request
• パッケージ: 25 kg fiber drum with double polyethylene liner, or as per customer requirements

見積依頼

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