Development and optimization of the lyophilized tablets containing a dipeptide mimetic of the nerve growth factor using the desirability function and analysis of variance (ANOVA)

Lyophilized tablets are a promising dosage form for the delivery of thermolabile pharmaceutical substances to the oral cavity in the absence of a presystemic metabolism and ensure the convenience and use of the drug for patients with dysphagia. Therefore, for the developed and synthesized at the Zakusov Research Institute of Pharmacology, substances hexamethylenediamide bis-(N-monosukinyl-L-glutamyl-L-lysine) (GK-2), the composition and technology of the lyophilized tablet were selected. The aim of the present study is to develop the composition of the GK-2 lyophilized tablet, which has the most optimal characteristics and the manufacturing process, as well as in studying the factors and interactions of factors that have the greatest influence on the characteristics of lyophilized tablets. As a result of the studies, 81 compositions of GK-2 lyophilized tablets were developed, and the compositions obtained were characterized by disintegration time, mechanical strength, residual moisture, moisture uptake, and mass transfer resistance of water vapor. The results were compared to study the influence of compositional factors and factor interactions by analysis of variance. The most optimal composition with the best characteristics was selected using function desirability. Based on the data obtained, all the technological and physicochemical properties of lyophilized tablets were mainly influenced by the form, amount of matrix-forming filler, and the interaction of the factors presented. In addition, a conclusion was drawn on the degree of influence of each factor on the individual characteristics of lyophilized tablets. Using the desirability function, composition No. 18 is selected having the most optimal properties, characteristics and process. © 2020, Advanced Scientific Research. All rights reserved.