Study On The Synthesis And Performance Of New Pharmaceutical Excipients-amino Acids And Meglumine Surfactants

Amino acid and meglumine surfactants are surfactants synthesized with biological substances as substrates.They have good surface properties and can be used as preservatives,antibacterial agents and solubilizers.Especially in terms of pharmaceutical excipients,it can improve the bioavailability of drugs.Nowadays,the synthetic methods of synthetic amino acids and meglumine surfactants are too single,and the synthesis process has many problems such as low yield and environmental pollution.Therefore,a new synthetic route for amino acids and meglumine surfactants has been developed.It is of great significance.In this paper,six series of amino acid and meglumine surfactants are designed,a total of thirty compounds,which are named glycine series,sarcosine series,alanine series,threonine series according to the different names of the small molecule compounds involved in the synthesis.Amino acid series,valine series and meglumine series.First,sodium caprylate,sodium laurate,sodium myristate,sodium palmitate and sodium stearate are used as starting materials to react with epichlorohydrin under the catalysis of tetrabutylammonium bromide to form long-carbon chain glycidyl esters.And then under alkaline conditions,the long-carbon chain glycidyl ester is ring-opened with glycine,sarcosine,alanine,threonine,valine,and meglumine to undergo condensation reactions to form new amino acids connected by C-N bonds and glucose For methylamine surfactants,infrared spectroscopy is used in the experiment to detect the reaction process of the product,infer the progress of the reaction,and characterize the characteristics of the product.The surface properties,cytotoxicity and Krafft points of the synthesized thirty amino acids and meglumine surfactants were measured.(1)Use a contact angle/interfacial tension tester to measure the surface tension and obtain the critical micelle concentration(CMC value).The surface performance results show that the CMC value of the same series of surfactants decreases with the increase of the carbon chain length.Compared with the standard products,the products have excellent surface activity.When the carbon chain length is greater than 16 amino acids and meglumine surfactants because of poor water solubility,their surface tension values cannot be measured.(2)Use human skin fibroblast HSF cells to culture and test the cytotoxicity of surfactants.The cytotoxicity results showed that the same series of surfactants became more cytotoxic as the carbon chain length increased.The toxicity results of amino acids with a carbon chain length of less than 16 and meglumine surfactants were significantly reduced compared with the standard products.(3)Measure the Krafft point by observing the transparent state of the system in a mixture of ice and water.The results show that meglumine surfactants have the best water solubility.Under low temperature conditions,meglumine surfactants with a carbon chain length of 8-18 have good hydrophilic properties;amino acid surfactants have good hydrophilic properties when the carbon chain length is less than 16,and vice versa.The properties deteriorate and the hydrophilic properties decrease.