DOSAGE FORM OF DNA-APTAMER Russian patent published in 2020 - IPC A61K31/7088 A61P7/02 

FIELD: biotechnology; medicine.

SUBSTANCE: group of inventions relates to biotechnology and medicine, specifically to the preparation of a medicinal form of aptamer RA-361. Aptamer RA-361 comprises 5'-GG-TT-GG-TGT-GG-TT-GG-T-GG-TT-GG-TGT-GG-TT-GG-3', covalently modified 20 kDa PEG in 16 position in concentration 30 mg/ml with allowable limit of 35.7 mg/ml, water, potassium chloride with concentration of 10 mM, where concentration of potassium chloride does not exceed 20 mM, and physiologic saline, wherein the dosage form has pH between 7 and 7.5 and is a clear aqueous solution. Group of inventions also relates to a method for preparing a medicinal form of the aptamer, which includes obtaining modified PEG aptamer RA-361 with chromatographic purification and concentration of active substance, heating and maintaining temperature of active substance samples to 95 °C for 5 minutes with subsequent cooling of samples to room temperature at rate of 5 °C per minute and performing sterilization by means of filters with pore diameter of 0.22 mcm to obtain a pharmaceutical substance in concentration of 120–150 mg/ml, then substance is subjected to four-time dissolution in sterile physiological saline, where water is used, prepared according to ISO 3696 standard, and packed into glass bottles in laminar cabinet, then they are sealed, wherein output is a substance in volume of 10 ml, and concentration of oligonucleotide RA-361 is 30–35.7 mg/ml.

EFFECT: use of this group of inventions enables to obtain an antithrombin aptamer, which is 31-link DNA oligonucleotide, covalently modified 20 kDa PEG and having a spatial structure of the antiparallel G quadruplex type stabilized by potassium cations, which enables to preserve blood plasma coagulation.

2 cl, 6 ex, 7 tbl, 12 dwg