[Lercanidipine distribution in warm-blooded animals]. / Raspredelenie lerkanidipina v organizme teplokrovnykh zhivotnykh.

THE AIM OF THE STUDY: Is to investigate the lercadipine distribution in warm-blooded animals (rats). The experimental study used rats of Wistar race. TLC, GC-MS and UV-spectrophotometry methods were used for physical and chemical analysis. Semilethal (890 mg/kg) dose of lercadipine, previously suspended in water, was injected into stomach of laboratory animals. Examined substance was isolated from the thick tissues and animals' blood by acetone, cleaned with a change of solvent and macrocolumn chromatography using 30 µm «Silasorb S-18¼ sorbent and acetonitrile-water (8:2) polar eluent. The analyte was identified by chromatographic behavior in the thin sorbent layer, retention time and set of positive ions in its mass spectrum, as well as by UV-spectrum. The analyte was determined quantitatively in bioactive matrix using UV-spectrophotometry. The methods were validated by criteria of linearity, selectivity, accuracy, precision, detection limits and quantitative determination. The main content of lercanidipine (mg/100 g) was determined in the stomach content (198.183±29.541), the stomach (195.312±21.579), the small intestine (47.096±3.947), the spleen (38.952±3.532) and the liver (26.211±2.232).

[Felodipine distribution in organisms of warm-blooded animals]. / Raspredelenie felodipina v organizme teplokrovnykh zhivotnykh.

The objective of the work was to study felodipine distribution in warm-blooded animals (rats). The methods of TLC, GC-MS, and UV spectrophotometry were used in the experiments. A lethal dose of felodipine (1.05 g/kg) preliminary suspended in water was introduced intragastric into test animals (male rats of the Wistar line). The analyzed compound was isolated from solid tissues and blood of the animals with acetone, purified by the solvent replacement, and by macrocolumn chromatography with the Silasorb S-18 sorbent of 30 µm and polar eluent, acetonitrile-water (7:3). The analyte was identified by chromatographic behavior in a thin sorbent layer, retention time, and a set of positive ions in its mass spectrum, as well as by the UV spectrum. The analyte was quantitatively detected in biological matrices using UV spectrophotometry. The method was validated by the criteria of linearity, selectivity, accuracy, precision, limits of detection, and quantitative determination. The predominant content of felodipine was detected in tissues of the stomach (312.303±25.980 µg/g), small intestine with its contents (93.235±12.310 µg/g), stomach contents (80.072±8.510 µg/g), and in the spleen (26.083±1.758 µg/g).

[Features of the determination of amlodipine in a biological material]. / Osobennosti opredeleniia amlodipina v biologicheskom materiale.

The purpose of the work is to determine the optimal conditions for isolating amlodipine, to purify it by the method of column chromatography and to develop a method for detecting it in biological material. TLC, GC-MS, low pressure column chromatography, and HPLC were used for analysis. We studied the comparative isolation of amlodipine from biological material using 13 isolating agents of organic nature, water, and aqueous solutions. The use of acetone as an insulating agent for the extraction of amlodipine from tissues of cadaver organs has been substantiated. The possibility of purification of the analyzed compound from the endogenous substances of the biomaterial is shown by the method of reversed phase chromatography in a column of the Silasorp S-18 sorbent of 30 µm. A technique has been developed for detecting amlodipine in the tissues of cadaveric organs (liver), which corresponds to the necessary parameters of linearity, selectivity, accuracy, precision and stability. The limits of detection and quantification of amlodipine by the proposed method are 0.25·10-6 and 4.0·10-6 g, respectively, in 1 g of the biomaterial.

[The distribution of amlodipine in the organism of the warm-blooded animals]. / Raspredelenie amlodipina v organizme teplokrovnykh zhivotnykh.

The objective of the present study was to elucidate the specific features of amlodipine distribution in the organism of the warm-blooded animals (rats) following a single intragastric administration of the poisonous substance at a dose of 686 mg/kg b/w/ (LD50). Amlodipine was isolated from the blood and various organs of the animals by means of acetone extraction and purified on the silica gel column (100/160 mcm) with the elution by an ethanol-hexane (7:3) mixture. The identification and the quantitative measurement of amlodipine were performed with the use of the TLC, GC-M, and UV-spectrophotometry. The study has shown that unmetabolized amlodipine was present in large amounts in the internal organs and blood of the poisoned animals. The principal organs of its accumulation were the stomach, kidneys, and blood.