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Triprolidine HCl monohydrate

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Chemical Structure| 6138-79-0 同义名 : 盐酸曲普利啶 ;Triprolidine Hydrochloride;Triprolidine hydrochloride monohydrate
CAS号 : 6138-79-0
货号 : A728042
分子式 : C19H25ClN2O
纯度 : 99%
分子量 : 332.868
MDL号 : MFCD00150574
存储条件:

粉末 Inert atmosphere,2-8°C

液体 -20°C:3-6个月-80°C:12个月

溶解度 :

DMSO: 105 mg/mL(315.44 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: 100 mg/mL(300.42 mM),配合低频超声助溶

动物实验配方:
生物活性
描述 Triprolidine HCl is a hydrochloride resulting from the formal reaction of equimolar amounts of triprolidine and hydrogen chloride. Its monohydrate is used for the symptomatic relief of uticaria, rhinitis, and various pruritic skin disorders. It has a role as a H1-receptor antagonist. It contains a triprolidine(1+). The absolute oral bioavailability of triprolidine (1-mg/kg dose) in the dog was low (4%). A comparison of triprolidine pharmacokinetic parameters in dogs, rabbits, rats, and humans revealed considerable similarity in elimination characteristics in these species[1]. of 0, 250, 1000, or 2000 ppm (as the free base) to groups of 60 Fischer 344 (F344) rats of each sex for up to 2 years to evaluate its potential carcinogenicity. Survival was significantly extended in triprolidine-treated males and females, particularly at the high dose. At the close of the study high-dose males and females had gained significantly less body weight than controls. Triprolidine was not carcinogenic in F344 rats[2]. The permeation rate of triprolidine in the stripped skin was greatly larger than that in the whole skin. The permeability of triprolidine was markedly increased with stripping of the mouse skin to remove the stratum corneum that acts as a barrier of skin permeation[3].
实验方案
1mg 5mg 10mg

1 mM

5 mM

10 mM

3.00mL

0.60mL

0.30mL

15.02mL

3.00mL

1.50mL

30.04mL

6.01mL

3.00mL

参考文献

[1]Findlay JW, Butz RF, Coker GG, DeAngelis RL, Welch RM. Triprolidine radioimmunoassay: disposition in animals and humans. J Pharm Sci. 1984 Oct;73(10):1339-44

[2]Greenman DL, Sheldon W, Schieferstein G, Allen R, Allaben WT. Triprolidine: 104-week feeding study in rats. Fundam Appl Toxicol. 1995 Sep;27(2):223-31

[3]Shin SC, Lee HJ. Enhanced transdermal delivery of triprolidine from the ethylene-vinyl acetate matrix. Eur J Pharm Biopharm. 2002 Nov;54(3):325-8