Studies On The Enantioseparation Of Several β-receptor Blocking Drugs By TLC

Many drugs or necessary-physiological compounds are chiral, and the optical isomers of these compounds are very different in physiology, in some cases, perhaps the optical isomers have unexpected side-effects.So, in order to improve drug activity, decrease side-effect and process drug manufacturing and quality controlling, supplying optically pure compounds has become an important subject in biochemistry and pharmacology. Guidelines of chiral drugs, which was published by FDA in 1992, demanded that detailed reports of racemic new drugs should be provided before entering the market in USA, which should prove physiology effects, toxicity and clinical results of isomers in drugs.In a word, the enantioseparation of racemic drugs is very important.The trend of development of chiral techniques was analyzed, and the forthcoming chiral separation methods and their advantages and disadvantages were reviewed detailedly in this paper.The enantioseparation of propranolol by TLC using D-10-camphor ammonium sulfonate as chiral ion-pair agent in the mobile phase was studied in depth. The effects of the mobile phase, temperature, pre-saturation time, pH, the concentration of ion-pair agent and humidity on separation were investigated by single-factor experiments, and the optimal chroatographic conditions were concluded; Secondly, resolution of propranolol hydrochloride enantiomers usingβ-cyclodextrin impregnated thin-layer chromatography was studied synchronously, the makeup of the mobile phase and quantity of the impregnated chiral selectors were studied, the conditions of separation were optimized, then concluded the optimal conditions of separation.In the meantime, we studied the enantioseparation of metoprolol and atenolol by TLC using D-10-camphor ammonium sulfonate as chiral ion-pair agent in the mobile phase , discussed the effects of the mobile phase, temperature, pre-saturation time, pH, the concentration of ion-pair agent and humidity on separation, and concluded respectively the optimal separation conditions of metoprolol and atenolol ;we also discussed the conditions of resolution of metoprolol and atenolol enantiomers usingβ-cyclodextrin impregnated thin-layer chromatography , such as the makeup of the mobile phase , temperature and quantity of the impregnated chiral selectors .etc.