Development of the Composition and Technology for Obtaining a Model of an Injection Form of an Indolocarbazole Derivative

被引：0
|
作者：
Nikolaeva, L. L. [1 ,2 ]
Lantsova, A. V. [1 ]
Sanarova, E. V. [1 ]
Orlova, O. L. [1 ]
Oborotov, A. V. [1 ]
Ignatieva, E. V. [1 ]
Shprakh, Z. S. [1 ,2 ]
Kulbachevskaya, N. Yu. [1 ]
Konyaeva, O. I. [1 ]
机构：
[1] Minist Hlth Russia, Blokhin Natl Res Ctr Oncol, 24 Kashirskoe Shosse, Moscow 115478, Russia
[2] Sechenov Univ, Minist Hlth Russia, 8-2 Trubetskaya St, Moscow 119991, Russia
来源：
PHARMACEUTICAL CHEMISTRY JOURNAL | 2023年 / 57卷 / 06期
关键词：
indolocarbazole derivative; solution; solubilizers; lyophilization; DRUG;
D O I：
10.1007/s11094-023-02962-6
中图分类号：
R914 [药物化学];
学科分类号：
100701 ;
摘要：
The indolocarbazole derivative LCS-1269 has a multitarget mechanism of action on tumors and blocks vasculogenic mimicry. The hydrophobic character of LCS-1269 hampers the development of an injectable dosage form (IDF), the need for which was determined in series of in vitro and in vivo biological experiments. The purpose of this study was to select an excipient composition for creating a model IDF of LCS-1269 with high antitumor activity and low toxicity and to develop the technology for LCS-1269 IDF production. Acomposition of a model IDF of LCS-1269 including EtOH (95%), Kollidon 17 PF, and polysorbate 80 and the technology for obtaining a true solution were developed during preliminary experimental studies. The selected model was lyophilized to exclude EtOH from the composition and to increase the shelf life of the compound.
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收藏
页码：874 / 878
页数：5
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