• 专利标题:   Preparing moxidectin microsphere useful in preparation of moxidectin microspheres injection, comprises adding moxidectin, and polylactic acid into dichloromethane solvent, dispersing, adding first emulsion into polyvinyl alcohol and Tween 80 aqueous solution, centrifuging, collecting and drying.
  • 专利号:   CN114848598-A, CN114848598-B
  • 发明人:   ZHANG M, LIANG Y, ZHANG Y, MENG Z, WANG W, MENG L
  • 专利权人:   HEBEI MEIHE PHARM CO LTD
  • 国际专利分类:   A61K031/365, A61K047/04, A61K047/26, A61K047/32, A61K047/34, A61K009/10, A61K009/16, A61P031/04
  • 专利详细信息:   CN114848598-A 05 Aug 2022 A61K-009/16 202285 Chinese
  • 申请详细信息:   CN114848598-A CN10593308 27 May 2022
  • 优先权号:   CN10593308

▎ 摘  要

NOVELTY - Preparing moxidectin microsphere, comprises (a) adding moxidectin, polylactic acid and graphene into dichloromethane solvent, dispersing to obtain oil phase, where mass ratio of moxidectin and polylactic acid is 1:1-10, and mass ratio of graphene and polylactic acid is 1:250-1000; (b) dropping oil phase into aqueous solution of polyvinyl alcohol and Tween 80(Polysorbate 80) 1:1 (wt./wt.) under stirring to obtain first emulsion, where mass ratio of polyvinyl alcohol and Tween 80(Polysorbate 80) in aqueous solution is 1:0.8-1.2; (c) adding first emulsion into polyvinyl alcohol and Tween 80(Polysorbate 80) aqueous solution, stirring for 4-5 hours at a speed of 500-1000 revolutions/minute, removing organic solvent to obtain second emulsion, where mass concentration of polyvinyl alcohol in polyvinyl alcohol and Tween 80(Polysorbate 80) aqueous solution is 0.1-4%; and (d) centrifuging second emulsion and collecting centrifuged microspheres and drying. USE - The moxidectin microspheres is useful in the preparation of moxidectin microspheres injection (claimed). ADVANTAGE - The method improves the encapsulation rate and process recovery rate of moxidectin microspheres. The moxicillin microspheres have a smooth and smooth appearance, and particle size distribution of 0.01-40 μm, narrow distribution range and uniform size, which meets the requirements of pharmacy, and the medicine load of moxicillin is ≥ 30%, has high drug loading and good stability, which is in line with the characteristics of animal long-acting preparations, and provides an ideal raw material for the application of moxidectin sustained-release microinjection in veterinary clinical processes. DETAILED DESCRIPTION - An INDEPENDENT CLAIM is also included for a moxidectin microsphere, prepared as mentioned above.