Application of Solid Dispersion Technology to Obtain a Model of Injectable Dosage Form of Indolocarbazole Derivative

Introduction. N. Blokhin National Medical Research Center of Oncology the Ministry Health Russia synthesized an original derivative indolocarbazole with carbohydrate residue xylose, which has a pronounced cytotoxic and anti-angiogenic activity. The substance LCS-1269 is amorphous powder that almost insoluble in water, causes difficulties development injectable dosage form (IDP). To solve this problem, technological approach to obtain solid dispersion (SD) been proposed. Aim. develop model IDP based on SD. Materials methods. We used Chemical Synthesis Laboratory Oncology. Emuxol 268, Kolliphor® P 188, Soluplus®, Lutrol® F68, Kollidon® 12 17, soybean phosphatidylcholine unsaturated S PC saturated PC-3 were investigated as carriers active substance. SD was obtained by solvent removal: dissolved acetone, carrier − chloroform, solutions mixed, transferred into bottle evaporated under vacuum (50 ± 5 mbar) desiccator at water bath temperature 65 2 °С. aqueous solution dry mass using different auxiliary substances or their mixtures: for injection, ethanol 95 %, benzyl alcohol, Kollisolv® PEG 400, MONTANOX™ 80. increase stability, lyophilized Edwards Minifast DO.2 freeze dryer. Results discussion. 17 chosen material It found clear concentration 0.5 % formed dissolving then gradually diluting alcohol mixture injection. In case, ratio components developed IDF LCS : 1 40 32 127. As result freeze-drying water-ethanol lyophilizate easily soluble 10 obtained. Conclusion. An hydrophobic submitted biological studies evaluate its effectiveness.