Preparation method of rifapentine-carried polycaprolactone microspheres

Abstract

The invention discloses a preparation method of rifapentine-carried polycaprolactone microspheres. The preparation method comprises steps as follows: rifapentine crude drugs and polycaprolactone 20 are jointly dissolved in dichloromethane, the mixture is subjected to ultrasonic treatment, and an oil phase is formed; the formed oil phase is dropwise added to a 2% polyvinyl alcohol water solution, mechanically stirred at the rotating speed of 3,000 rpm for 30 min, sealed, left to stand for 30 min and continuously stirred at the rotating speed of 100 rpm for 3 h, and an emulsion is formed; centrifugal treatment is performed, obtained solids are washed with distilled water, centrifugal separation and washing are performed again, finally, drying is performed in a freezing vacuum drier, and the rifapentine-carried polycaprolactone microspheres are obtained and put at the temperature of subzero 4 DEG C in the dark place for storage. The prepared rifapentine-carried polycaprolactone microspheres have round and complete shapes, have a micropore structure on the surface, are good in particle size dispersity and high in drug loading capacity, have a good slow release function and can be used for long-acting interventional therapy of tuberculosis of bones and joints.

Description

technical field [0001] The invention belongs to the field of preparation of drug-loaded microspheres, in particular to a preparation method of polycaprolactone-loaded rifapentine microspheres. Background technique [0002] Bone and joint tuberculosis has seriously affected the health and quality of life of patients for a long time. Oral or intravenous preparations are often used for systemic administration during the treatment process, but it is difficult to achieve effective drug concentrations. Local drugs will disappear quickly with blood circulation and self-metabolism. The local drug loading system can adjust the release rate of the drug, reduce the side effects of the drug, maintain the effective drug concentration for a long time, and improve the curative effect. [0003] Degradable drug-loaded microspheres have been proven to be a highly efficient, low-toxic drug sustained-release control system, and have recently attracted extensive attention from researchers. The...

AI Technical Summary

Problems solved by technology

[0004] At present, there are few studies on the use of polycaprolactone to load rifapentine to construct long-acting microsphere sustained-release systems, and the preparation of products has poor effect, low drug loading, and poor antibacterial properties.