Obtaining a Water-soluble Form of Hydrophobic Indolelocarbazole Derivative Using Solubilizer Complex

Introduction. LHS-1269 is an indolocarbazole derivative with high antitumor activity. Due to the hydrophobic properties of active substance, use organic co-solvents – dimethyl sulfoxide (DMSO) and ethanol required obtain injectable dosage form (DP). However, inclusion solvents in composition DF carries a potential risk side effects as result drug. Aim. Selection auxiliary substances for obtaining aqueous solution indolecarbazole derivative, which allows minimizing concentration DF. Materials methods. The object study substance series 010320, produced Chemical Synthesis Laboratory N. Blokhin National Medical Research Center Oncology. following were used model compositions: Kollidon® 17 PF, Kollisolv® PEG-400, Kolliphor® P 188, Montanox™ 20, DMSO (p.a.), 95 % (standardized according pharmacopoeia quality standard ФС.2.2.0019.18 State Pharmacopoeia Russian Federation). Analytical scales OHAUS Plus AP 100S laboratory AND DL-120 weighing substances. dissolution mixing components was carried out on IKA® C-MAG HS 4 magnetic stirrer. Results discussion. In course study, 2 groups compositions obtained estimated, comprising complex two or more solubilizer. first group formulations contained at 5 concentrations from 0 15 %. second included As result, it found that addition 188 reduces content this case, further decrease ethanol, turbidity precipitation are observed. Reducing achieved by using combination 20 solubilizer (20 %), PEG-400 %) (5 %). total without observed when compensating solvent introducing additional benzene (2 Conclusion. research, solubilizers selected, allowing compound minimum solvents.