The development of new technology of the dosage form for intravenous administration indolocarbazole derivative LHS-1208

Abstract

Objective. Aim of this work was to create a stable liposomal dosage form of native hydrophobic antitumor compound from the group of indolocarbazoles-LHS-1208. Materials and methods. Quantitative analysis of the drug content in liposomes was determined by spectrophotometry with a standard sample at λ = 320 ± 2 nm. The encapsulation was investigated as the ratio of LHS-1208 concentration in the liposomal dispersion after extrusion through nylon membrane filters 0.22 µm "Pall" to concentration LHS-1208 in liposomal dispersions before filtration. pH of the liposome was determitaned by the method of potentiometry. The size of liposomes was evaluated by nanosizer. Cytotoxic activity was studied by MTT-test.

Betulin-3,28-diphosphate as a Component of Combination Cytostatic Drugs for the Treatment of Ehrlich Ascites Carcinoma In Vitro and In Vivo Experiments

“…As a rule, highly water-soluble substances have severe systemic toxic effects. The modern trend of pharmacotherapy is to use well-proven drugs in new dosage forms or new methods of administration, such as selective delivery when the dose of cytostatics can be dramatically reduced [ 4 , 5 , 6 ]. The inexpensive cytostatics such as hydrazine sulfate (HS), Sehydrin and 5-fluorouracil (5-FU), characterized by a low median lethal dose (LD 50 ) value close to 0.32 mg/kg, are of interest as a component of a new dosage form in clinical practice [ 7 , 8 ].…”

Antitumor Drugs Based on Indolocarbazol Derivatives

“…To date, preclinical trials of an injectable dosage form LHS-1208 containing dimethyl sulfoxide and a solubilizer Kollidon 17PF as a co-solvent of the hydrophobic active substance, have been completed [94]. For this compound, a liposome-based DF was also developed in the form of a lyophilisate for the preparation of an injection emulsion [95].…”

Features pharmaceutical development lyophilisate GK-2 for parenteral use

“…Стерильность и апирогенность должны соблюдаться на всех этапах технологического процесса -от подготовки ВВ и оборудования до предупреждения Оригинальные статьи контаминации в сушильной камере и во время укупорки [5,6]. При изучении технологических свойств лиофилизата для приготовления инъекций на основе ГК-2 можно сделать вывод: лиофилизат обладает оптимальными технологическими и биофармацевтическими свойствами, что позволяет говорить об успешной фармацевтической разработке.…”