Influence of amino-acid spectrum of peptide organic drugs on drug therapy effectiveness

Abstract

Using modern analytical equipment and justified and developed methodological approaches and calculations amino-acid composition of the domestic peptide drugs cortexin, retinalamin, pineamin has been studied. For the first time the exact amounts of each amino-acid out of 17 have been discovered in the specified drug products as well as the fact that cortexin has additional non-proteinogenic ornithine amino acid, retinalamin has taurine, pineamin has ornithine and taurine while cerebrolysin does not contain free amino acid cystine. It has been determined that among the cortexin amino acids 65% of them constitute L-glutamic and L-aspartic acids that together with ornithine specify bioenergetic characteristics of the drug. Absolute amount of every amino acid in cortexin in comparison with cerebrolysin (in an amount of 1 mg of the organic drug) is reasonably larger, in particular amount of aspartic, glutamic acids and tyrosine is 6,5–7 times larger, amount of serine is 9 times larger and amount of arginine is 12 times larger. Stability of amino acid spectrum of every domestic peptide drug has been achieved that is stable notwithstanding lot and time of manufacturing. For reasonable results interpretation and cortexin pharmacokinetics evaluation cerebrolysin was chosen as a reference product. Choosing of Cerebrolysin as a comparator with cortexin is explained by the fact that another medication close by indications and the structure does not exist, although in degree of preparedness the cerebrolysin is hydrolyzate, that is the final product of the process, which is an important stage of its production. At the same time, peptide medications of domestic production – cortexin, retinalamin and pineamin which having a two-component – the original peptide substance and a stabilizer (amino acid glycine), are really transferred hydrolysis process on the patient’s metabolism. Years of experience in applying cortexin was revealed no changes in metabolism when intramuscular administration, due to the minimal amount of medication (10 mg), constant availability and accessibility of aminopeptidases, short duration of the preparation.

Keywords

peptide drug products / amino-acid spectrum / cortexin / retinalamin / pineamin / cerebrolysin / pharmacokinetics / neuroprotection / ultra-performance liquid chromatography

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