General Information

Brinzolamide Impurities and Brinzolamide 

Daicel Pharma synthesizes Brinzolamide impurities of exceptional quality, such as Methyl (S)-N-((4-hydroxy-2-(3-methoxypropyl)-1,1-dioxido-3,4-dihydro-2H-thieno[3,2-e][1,2]thiazin-6-yl)sulfonyl)acetimidate, Methyl (S)-N-((2-(3-methoxypropyl)-1,1-dioxido-4-(tosyloxy)-3,4-dihydro-2H-thieno[3,2-e][1,2]thiazin-6-yl)sulfonyl)acetimidate, (4R)-4-Hydroxy-2-(3-methoxypropyl)-3,4-dihydro-2H-thieno[3,2-e][1,2] thiazine-6-sulfonamide 1,1 dioxide, (4S)-6-chloro-2-(3-methoxypropyl)-3,4-dihydro-2H-thieno[3,2-e] [1,2] thiazine-4-ol- 1,1 dioxide, and so on. These impurities are crucial to assess the purity, reliability, and safety of an active pharmaceutical ingredient, Brinzolamide. Besides, Daicel Pharma provides a custom synthesis of Brinzolamide impurities to meet clients’ demands for delivery worldwide.

Brinzolamide [CAS: 138890-62-7] is a sulfonamide derivative, acts as an inhibitor of the carbonic anhydrase enzyme. It is an antiglaucoma medication. Brinzolamide reduces high intraocular pressure caused by open-angle glaucoma, which can lead to optic nerve damage and vision loss if left untreated.

Brinzolamide: Use and Commercial Availability  

Brinzolamide lowers intraocular pressure (IOP) in patients. It inhibits carbonic anhydrase II (CA-II), suppresses aqueous humor formation, and reduces IOP. Brinzolamide is a reversible CA-II inhibitor. Brinzolamide is available under the trade name Azopt.

Brinzolamide Structure and Mechanism of Action

The chemical name of Brinzolamide is (4R)-2H-Thieno[3,2-e]-1,2-thiazine-6-sulfonamide, 4-(ethylamino)-3,4-dihydro-2-(3-methoxypropyl)- 1,1-dioxide. Its chemical formula is C₁₂H₂₁N₃O₅S₃, and its molecular weight is approximately 383.5 g/mol.

Brinzolamide decreases aqueous humor secretion, possibly by slowing the formation of bicarbonate ions and reducing intraocular pressure. This reduction is beneficial in treating conditions such as open-angle glaucoma.

Brinzolamide Impurities and Synthesis

Brinzolamide may contain impurities, such as related compounds and residual solvents, form during the manufacturing process¹ or storage. They may impact the safety and efficacy of the drug product. Some common Brinzolamide impurities include degradation products, isomers, and residual solvents. It is essential to control and monitor these impurities through various methods, such as developing appropriate manufacturing processes, using high-quality raw materials, implementing proper storage conditions, and conducting regular analytical testing during manufacturing and throughout its shelf life to ensure the quality of the drug product. These measures help to ensure that the drug product is safe and effective for patients.

Daicel Pharma offers a Certificate of Analysis (CoA) for Brinzolamide impurity standards, such as Methyl (S)-N-((4-hydroxy-2-(3-methoxypropyl)-1,1-dioxido-3,4-dihydro-2H-thieno[3,2-e][1,2]thiazin-6-yl)sulfonyl)acetimidate, Methyl (S)-N-((2-(3-methoxypropyl)-1,1-dioxido-4-(tosyloxy)-3,4-dihydro-2H-thieno[3,2-e][1,2]thiazin-6-yl)sulfonyl)acetimidate, (4R)-4-Hydroxy-2-(3-methoxypropyl)-3,4-dihydro-2H-thieno[3,2-e][1,2] thiazine-6-sulfonamide 1,1 dioxide, (4S)-6-chloro-2-(3-methoxypropyl)-3,4-dihydro-2H-thieno[3,2-e] [1,2] thiazine-4-ol- 1,1 dioxide, and so on, generated from an analytical facility compliant with cGMP standards. The CoA includes a comprehensive characterization report comprising data from techniques like 1H NMR, 13C NMR, IR, MASS, and HPLC purity². Furthermore, on request, we can provide additional data like 13C-DEPT and CHN. Daicel Pharma can prepare unknown Brinzolamide impurities or degradation products. A complete characterization report accompanies every delivery.