In:
International bulletin of Veterinary Medicine, Saint-Petersburg State University of Veterinary Medicine, Vol. 3 ( 2020), p. 58-64
Abstract:
At present, the class of rhodanine com-pounds containing 4-oxo-2-thioxo-1,3-thiazolidine residues is very promising in the development of medical and veterinary drugs. The purpose of the work is to develop a chemical compound 3- (2-phenylethyl) -2-thioxo-1,3 thiazolidin-4-one (XC-3-2-FE-2-TO-1,3T-4-OH) based on clathrate with β- cyclodextrin (CD) - a supramolecular com-pound (CMC) with improved biopharmaceu-tical properties (solubility and bioavailabil-ity). The lattice clathrates KhS-3-2-FE-2-TO-1,3T-4-OHa with CD were synthesized at the ratios of their masses 1: 5 and 1:10. CMC is a crystalline powder of white with a yellow tint with a particle size of less than 100 nm. For the first time, a method was developed for the quantitative determination of CHS-3-2-FE-2-TO-1,3T-4-OHa in the blood plasma of dogs by high performance liquid chromatography (HPLC). In the range of 0.2-4.0 μg / ml, the calibration curve is linear for ChS-3-2-FE-2-TO-1,3T-4-OH, while the regression equation is described by y = 3.977 + 30.343 × X, s the coefficient of accuracy of the approximation equal to R2 = 0.999. The lower limit of quantitative detec-tion is 10 ng / ml. The average maximum concentrations (Cmax) of ChC-3-2-FE-2-TO-1,3T-4-OHa in the blood plasma of dogs with it, as well as in the form of a clathrate single oral administration, respectively, were 0.66 ± 0, 25 and 3.03 ± 0.82 μg / ml (P≤0.05). The average values of the parame-ter AUC (0 → t) with the introduction of ChS-3-2-FE-2-TO-1,3T-4-On and its clath-rate with CD, respectively, were 4.07 ± 2.15 μg × h / ml and 24.58 ± 5.66 μg × h / ml (P≤0.05). According to a pharmacokinetic study, the best bioavailability (DB) is pos-sessed by the C-3-2-FE-2-TO-1,3T-4-OHa clathrate with CD in a ratio of 1: 5, the ob-tained DB value is 6.4 times higher than the same the value of the original compound. It was concluded that, in terms of biopharma-ceutical properties, the most promising agent for medical and veterinary use is the XC-3-2-FE-2-TO-1,3T-4-OHa clathrate with CD with a mass ratio of 1: 5 and an average par-ticle size of 40.5 nm
Type of Medium:
Online Resource
ISSN:
2072-2419
Uniform Title:
РАЗРАБОТКА АКТИВНОГО КЛАТРАТА 3-(2 –ФЕНИЛЭТИЛ)-2-ТИОКСО-1,3 ТИАЗОЛИДИН-4-ОНА С β -ЦИКЛОДЕКСТРИНОМ И ИЗУЧЕНИЕ ЕГО БИОДОСТУПНОСТИ
DOI:
10.17238/issn2072-2419.2020.3
DOI:
10.17238/issn2072-2419
DOI:
10.17238/issn2072-2419.2020.3.58
Language:
Unknown
Publisher:
Saint-Petersburg State University of Veterinary Medicine
Publication Date:
2020