更新于：2024-11-21

Cyanocobalamin/Cyanocobalamin Co-57/Cyanocobalamin Co-58

氰钴胺/氰钴胺 CO-57/氰钴胺 CO-58

更新于：2024-11-21

概要

概要

基本信息

药物类型

小分子化药

别名

Dicopac Kit

靶点-

作用机制-

治疗领域-

在研适应症-

非在研适应症-

原研机构

G&E Healthcare Co., Ltd.

在研机构-

非在研机构

G&E Healthcare Co., Ltd.

最高研发阶段撤市

首次获批日期

美国 (1974-06-10)

最高研发阶段(中国)-

特殊审评-

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结构

分子式C63H88CoN14O14P

InChIKeyDLRXOSFAWIKARM-SYUKHSAKSA-M

CAS号68-19-9

查看全部结构式(3)

关联

100 项与氰钴胺/氰钴胺 CO-57/氰钴胺 CO-58 相关的临床结果

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100 项与氰钴胺/氰钴胺 CO-57/氰钴胺 CO-58 相关的转化医学

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100 项与氰钴胺/氰钴胺 CO-57/氰钴胺 CO-58 相关的专利（医药）

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项与氰钴胺/氰钴胺 CO-57/氰钴胺 CO-58 相关的文献（医药）

2024-04-01·International Journal of Biological Macromolecules

Hyaluronan/B12-chitosan polyelectrolyte complex for oral colistin administration

Article

作者: Sall, Tatiana S ; Anufrikov, Yuri A ; Shasherina, Anna Y ; Egorova, Tatiana S ; Skorik, Yury A ; Dubashynskaya, Natallia V ; Vlasova, Elena N ; Demyanova, Elena V ; Murashko, Ekaterina A ; Bokatyi, Anton N ; Dubrovskii, Yaroslav A

Polyelectrolyte complexes (PECs) based on polysaccharides, including hyaluronic acid (HA) and chitosan (CS), are promising delivery systems for antimicrobial agents, including oral administration of the peptide antibiotic colistin (CT). Modification of CS with different targeting ligands to improve intestinal permeability is a suitable way to improve the oral bioavailability of polyelectrolyte particles. This study describes the procedure for obtaining CT-containing PECs based on HA and CS modified with cyanocobalamin (vitamin B12). In this case, vitamin B12 is used as a targeting ligand because it is absorbed in the ileum via specific transporter proteins. The resulting PECs had a hydrodynamic size of about 284 nm and a positive ζ-potential of about 26 mV; the encapsulation efficiency was 88.2 % and the CT content was 42.2 μg/mg. The developed systems provided a two-phase drug release: about 50 % of the CT was released in 0.5-1 h, and about 60 % of the antibiotic was cumulatively released in 5 h. The antimicrobial activity of encapsulated CT was maintained at the same level as the pure drug for at least 24 h (minimum inhibitory concentration against Pseudomonas aeruginosa was 2 μg/mL for both). In addition, the apparent permeability coefficient of CT in the PEC formulation was 2.4 × 10^-6 cm/s. Thus, the incorporation of CT into HA- and vitamin B12-modified CS-based PECs can be considered as a simple and convenient method to improve the oral delivery of CT.

2024-03-01·Biochemistry (Moscow)

Association of Increased Homocysteine Levels with Impaired Folate Metabolism and Vitamin B Deficiency in Early-Onset Multiple Sclerosis

Article

作者: Abdurasulova, Irina N ; Dmitriev, Alexander V ; Tsymbalova, Evgenia A ; Bisaga, Gennadij N ; Lioudyno, Victoria I ; Scripchenko, Elena Y ; Chernyavskaya, Ekaterina A

The contents of homocysteine (HCy), cyanocobalamin (vitamin B12), folic acid (vitamin B9), and pyridoxine (vitamin B6) were analyzed and the genotypes of the main gene polymorphisms associated with folate metabolism (C677T and A1298C of the MTHFR gene, A2756G of the MTR gene and A66G of the MTRR gene) were determined in children at the onset of multiple sclerosis (MS) (with disease duration of no more than six months), healthy children under 18 years (control group), healthy adults without neurological pathology, adult patients with MS at the onset of disease, and adult patients with long-term MS. A significant increase in the HCy levels was found in children at the MS onset compared to healthy children of the corresponding age. It was established that the content of HCy in children has a high predictive value. At the same time, an increase in the HCy levels was not accompanied by the deficiency of vitamins B6, B9, and B12 in the blood. The lack of correlation between the laboratory signs of vitamin deficiency and HCy levels may be due to the polymorphic variants of folate cycle genes. An increased HCy level should be considered as a marker of functional disorders of folate metabolism accompanying the development of pathological process in pediatric MS. Our finding can be used to develop new approaches to the prevention of demyelination in children and treatment of pediatric MS.

2023-07-17·International journal of molecular sciences

Cyanocobalamin-Modified Colistin-Hyaluronan Conjugates: Synthesis and Bioactivity.

Article

作者: Sall, Tatiana S ; Murashko, Ekaterina A ; Egorova, Tatiana S ; Dubrovskii, Yaroslav A ; Dubashynskaya, Natallia V ; Skorik, Yury A ; Vlasova, Elena N ; Bokatyi, Anton N ; Nashchekina, Yuliya A ; Demyanova, Elena V

Polymeric drug delivery systems enhance the biopharmaceutical properties of antibiotics by increasing their bioavailability, providing programmable and controlled-release properties, and reducing toxicity. In addition, drug delivery systems are a promising strategy to improve the intestinal permeability of various antimicrobial agents, including colistin (CT). This study describes the modification of conjugates based on CT and hyaluronic acid (HA) with cyanocobalamin (vitamin B12). Vitamin B12 was chosen as a targeting ligand because it has its own absorption pathway in the small intestine. The resulting polysaccharide conjugates contained 95 μg/mg vitamin B12 and the CT content was 335 μg/mg; they consisted of particles of two sizes, 98 and 702 nm, with a ζ-potential of approximately -25 mV. An in vitro release test at pH 7.4 and pH 5.2 showed an ultra-slow release of colistin of approximately 1% after 10 h. The modified B12 conjugates retained their antimicrobial activity at the level of pure CT (minimum inhibitory concentration was 2 μg/mL). The resulting delivery systems also reduced the nephrotoxicity of CT by 30-40% (HEK 293 cell line). In addition, the modification of B12 improved the intestinal permeability of CT, and the apparent permeability coefficient of HA-CT-B12 conjugates was 3.5 × 10^-6 cm/s, corresponding to an in vivo intestinal absorption of 50-100%. Thus, vitamin-B12-modified conjugates based on CT and HA may be promising oral delivery systems with improved biopharmaceutical properties.

100 项与氰钴胺/氰钴胺 CO-57/氰钴胺 CO-58 相关的药物交易

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