- Chromatographic separation and spectroscopic characterization of the E/Z isomers of acrivastine
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A reverse phase high performance liquid chromatography (HPLC) method has been developed for the separation of two geometric isomers of Acrivastine using crude reaction mixture. The resolution between two isomers was found more than 2.9. The geometric isomers have been isolated by preparative HPLC and characterized by spectroscopic techniques, such as NMR, infrared, and MS. The developed method has been validated for the determination of Z-isomer in Acrivastine. The limit of detection and limit of quantification of the Z-isomer were 0.05 and 0.2 μg/ml, respectively. The developed method is precise, linear, accurate, rugged and robust for its intended use.
- Davadra, Prakash M.,Dabhi, Batuk,Singh, Manoj K.,Jain, Mukul R.,Joshi, Hitendra S.,Bapodra, Atul H.
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- Method for preparing acrivastine
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The invention belongs to the field of pharmaceutical synthesis, and relates to a method for preparing acrivastine. The method comprises the steps of adopting an acriva ethyl ester compound as a raw material, dissolving the acriva ethyl ester compound into an organic solvent medium, adding an inorganic base for alkaline hydrolysis, and completing alkaline reaction to obtain a hydrolysate of the acriva ethyl ester compound; decompressing concentrating the hydrolysate of the acriva ethyl ester compound until stopping flowing, and obtaining a concentrate; and adding water into the obtained concentrate, cooling to be ranged from 20 DEG C to 30 DEG C, acidizing to enable pH (Potential of Hydrogen) to be ranged from 5.0 to 7.0, crystallizing through a temperature differential method, filtering and drying to obtain an acrivastine crude product. The method is simple to operate, low in cost, free of using an organic solvent, environmentally friendly and easy for industrial production, and the obtained acrivastine is high in yield, high in purity and stable in quality.
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Paragraph 0041-0041
(2017/05/18)
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- A method for preparing arab League cuts down Si Ding (by machine translation)
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The invention belongs to the field of organic chemical synthesis and specifically relates to a preparation method of acrivastine. The preparation method comprises the following steps: by taking p-methyl benzoyl hydrazone and alpha-halogenated pyridine as raw materials, carrying out palladium-catalyzed coupling reaction to obtain an intermediate for synthesizing acrivastine; and further preparing acrivastine. By carrying out non-palladium borate-catalyzed coupling reaction, the preparation method is mild in reaction condition; dangerous butyl lithium is not used, so that the risk in plant production is reduced; the reaction is short in time required and high in efficiency; and the raw materials are cheap and easily available and the cost is lowered. The preparation method provided by the invention provides a novel safe, economic and efficient preparation path for preparation of acrivastine.
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Paragraph 0038; 0039; 0041; 0044
(2017/07/20)
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- 3-{6-[3-Pyrrolidino-1-(4-tolyl)prop-1-enyl]-2-pyridyl}acrylic acid and pharmaceutically acceptable salts thereof
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This disclosure describes a compound of Formula I STR1 (including its pharmaceutically acceptable salts and esters) which has potent antihistamine activity which is substantially free from sedative effects and which has little or no anticholinergic effects.
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- Triprolidine radioimmunoassay: Disposition in animals and humans
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A hapten derivative of triprolidine, bearing an acrylic acid side chain ortho to the pyridine ring nitrogen atom, was synthesized and coupled to bovine serum albumin. Immunization of New Zealand White rabbits with the resulting drug-protein conjugate resulted in the production of antisera capable of binding a radioiodinated tyramine conjugate of the triprolidine hapten derivative at high antiserum dilutions (1:70,000-1:150,000). These antisera were used to develop a radioimmunoassay (RIA) for triprolidine in human plasma with a sensitivity limit of 0.1 ng/mL (0.01 ng of actual mass). The known hydroxymethyl and carboxyl metabolites of triprolidine cross-reacted weakly (2 and 0.05%, respectively) with this antiserum. The RIA could be used for the direct analysis of triprolidine in human and rabbit plasma, but not for rat or dog plasma, presumably due to the presence of other interfering substances (possibly metabolites). The validity of the RIA procedure in human plasma was demonstrated by comparative analysis of a number of samples by quantitative TLC (r = 0.985, slope = 1.076). The assay was employed to describe the pharmacokinetics of triprolidine in the rabbit (t( 1/2 ,β) = 1.7 h). The assay had adequate sensitivity to detect low circulating drug concentrations in humans after therapeutic oral doses and also substantiated previous disposition experiments with triprolidine in humans (t( 1/2 ,β = 2.27 h). TLC analysis demonstrated that 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 human revealed considerable similarity in elimination characteristics in these species.
- Findlay,Butz,Coker,et al.
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p. 1339 - 1344
(2007/10/02)
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