Synthesis And Preliminary Pharmacological Evaluation Of Essential Amino Acids Chelated Calcium

As a new type of calcium supplement, amino acid calcium compound possessessuper chemical and biological stability, higher biological value and better calciumsupplement effect. L-phenylalanine chelated calcium complex and L-phenylalanine&L-leucine chelated calcium complex were prepared in the water system. Thepharmacology of the finished product was preliminary evaluated.The process conditions of preparing phenylalanine chelated calcium complex in thewater system were determined through single-factor experiments. The effect offactors such as the molar ratio of phenylalanine to calcium, the pH value, the reactiontemperature and the reaction time to the chelating rate were investigated, and theoptimal parameters were obtained by uniform design. The optimum conditions arereaction temperature40°C, reaction time182min, the molar ratio of phenylalanine tocalcium4.3and pH9.0. Under the best conditions, the experimental result gavechelating rate87.40%, which was17.12%lower than the prediction value104.52%.The preparation conditions of L-phenylalanine&L-leucine chelated calciumcomplex were optimized by uniform design. Then the optimal parameters wereobtained as follows: reaction temperature40°C, reaction time240min, the molarratio of phenylalanine to calcium4.21and pH9.0. Under the best conditions, theexperimental result gave chelating rate65.42%, which was4.98%lower than theprediction value68.85%.The infrared spectrum characterization and thermogravimetric analysis confirmedthe existence of L-phenylalanine-Ca2+chelates and L-phenylalanine&leucine-Ca2+chelates in the products. Parts of their qualifications have been detected.The oral acute toxicity test and micronucleus test of bone marrow PCE cell havebeen carried out, and the results illustrate that the finished products synthesized aresafe, nonhazardous, and have no mutagenicity to somatic cell.Pharmacokinetics experiment shows that peak time of phenylalanine calcium highdose group, low dose group, L-phenylalanine&L-leucine calcium group and glucosecalcium group are respectively1h,3.5h,3h and5h. The concentration of all the amino acid calcium groups is falling smoothly after they achieved the peak time. Thecalcium absorption level of amino acid calcium groups is higher than the glucosecalcium.Pharmacodynamics experiment shows that the influence of amino acid calcium onthe weight is relevant to the feeding dose and amino acid composition. Theconcentration of calcium in blood has no significant differences (P>0.05). Thelength, weight and calcium content of rat femurs are all with significant differenceswhen compared with that in the finished product group (P <0.05). The absorptioneffect of amino acid calcium synthesized in this test is better than glucose calcium atthe same dosage.