Carbinoxamine maleate salt

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Chemical Structure| 3505-38-2 同义名 : Carbinoxamine (maleate);CarbinoxaMine Maleate;NSC 62362
CAS号 : 3505-38-2
货号 : A242556
分子式 : C20H23ClN2O5
纯度 : 99+%
分子量 : 406.86
MDL号 : MFCD00050923
存储条件:

Pure form Keep in dark place,Sealed in dry,Room Temperature

In solvent -20°C:3-6个月-80°C:12个月

溶解度 :

DMSO: 105 mg/mL(258.07 mM),配合低频超声助溶,注意:DMSO长时间开封后,会吸水并导致溶解能力下降,请避免使用长期开封的DMSO

H2O: 50 mg/mL(122.89 mM),配合低频超声助溶

动物实验配方:

PO 0.5% CMC-Na 40 mg/mL clear

生物活性
靶点
  • H1 receptor

描述 Carbinoxamine maleate is a histamine-H1 receptor blocking agent with antihistamine and anticholinergic properties[3]. Carbinoxamine maleate is an antihistamine drug with mild sedation effects, which is used to treat seasonal and perennial allergic rhinitis clinically[4]. The short half-life and bitter taste of carbinoxamine maleate (CAM) lead to poor compliance by pediatric patients who are being treated for allergic rhinitis. The homemade preparations had release behaviors similar to that of the reference in vitro and achieved sustained release in vivo. The low drug loading preparation had a higher relative bioavailability of 109% owing to its faster release and better dispersibility. The suspensions based on MCRCs (microencapsulated carbinoxamine-resin complexes) could be successfully applied to treating allergic rhinitis in children[5].
实验方案
1mg 5mg 10mg

1 mM

5 mM

10 mM

2.46mL

0.49mL

0.25mL

12.29mL

2.46mL

1.23mL

24.58mL

4.92mL

2.46mL

参考文献

[1]Ramadan AA, Mandil H. Spectrophotometric determination of carbinoxamine maleate in pharmaceutical formulations by ternary complex formation with Cu(II) and eosin. Anal Biochem. 2006 Jun 1;353(1):133-7. Epub 2006 Mar 9.

[2]Mansour AM. Determination of pseudoephedrine hydrochloride and carbinoxamine maleate in combination drug formulation by liquid chromatography. J AOAC Int. 1998 Sep-Oct;81(5):958-62.

[3]LiverTox: Clinical and Research Information on Drug-Induced Liver Injury [Internet]. Bethesda (MD): National Institute of Diabetes and Digestive and Kidney Diseases; 2012–. Carbinoxamine. 2017 Jan 16. PMID: 31643335

[4]Li P, Xiao J, Liu J, Liu R, Bi K, Li Q. Development and full validation of a liquid chromatography-tandem mass spectrometry method for determination of carbinoxamine in beagle plasma and its application to a pharmacokinetic study. J Chromatogr B Analyt Technol Biomed Life Sci. 2018 Sep 1;1093-1094:183-189

[5]Deng Y, Wang T, Li J, Sun W, He H, Gou J, Wang Y, Yin T, Zhang Y, Tang X. Studies on the in vitro ion exchange kinetics and thermodynamics and in vivo pharmacokinetics of the carbinoxamine-resin complex. Int J Pharm. 2020 Oct 15;588:119779