目的 制备稳定的氟比洛芬酯脂微球注射液。方法 通过单因素考察及正交实验优化筛选得到氟比洛芬酯脂微球的最佳处方和工艺,并研究所得制剂的离心稳定常数Ke、粒径、ζ电位、pH值等性质。结果 确定氟比洛芬酯脂微球注射液的处方组成及工艺为:10%的注射用大豆油、1.2%的蛋黄卵磷脂、0.6%的F68、0.4%的油酸、2.0%的甘油和90%的注射用水。均质前调节pH为8.0,80 MPa均质6次,于121 ℃灭菌15 min,灭菌后仍能保持良好的稳定性,制得脂微球注射液氟比洛芬酯的含量为95.59%。结论 该处方工艺可行,制得的脂微球稳定性良好。
Abstract
To prepare stable flurbiprofen axetil lipid microsphere for intravenous injection.METHODS The optional formulation and prepared procedure were obtained through the single factor and crosscut design of experiment, and the stability constant of centrifugation Ke, particle size, Zeta potential, the pH of the product were studied. RESULTS The optional formulation and procedure were 10% soybean oil for intravenous injection,1.2% soybean lecithin, 0.6% F68,0.4% oleic acid,2.0% glycerol and 90% water for injection. pH was adjusted to 8.0 before homogenization and the sample was homogenized at a pressure of 80 MPa for 6 times. Finally, the lipid microspheres were sterilized for 15 min by sterilizing at 121 ℃ and exhibited good stability after sterilization.The content of Flurbiprofen Axetil lipid microspheres was 95.59%.CONCLUSION The preparation process is feasible to prepare lipid microsphere with good physical stability.
关键词
氟比洛芬酯 /
脂微球 /
处方筛选 /
工艺优化 /
稳定性
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Key words
flurbiprofen axetil /
lipid microsphere /
formulation optimization /
process optimization /
stability
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中图分类号:
R944
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参考文献
[1] YU G H, LIU S Z, REN H P.Research overview of flurbiprofen axetil injecction for analgesia. Chin J Cancer Prev Treat(中华肿瘤防治杂志),2007,14(20):1595-1598. [2] RAO J J,MCCLEMENTS D J.Formation of flavor oil microemulsions, nanoemulsions and emulsions:Influence of composition and preparation method. J Agric Food Chem(农业化学与食品化学杂志),2011,59(9):5026-5035.[3] LIU A,CHEN H,TANG X.Preparation and physical stability of astragaloside IV lipid microspheres for injection. J Chin Pharm(中国药学杂志), 2009, 7(4):290-297.[4] YE L M,SU B,WANG D K,et al. Preparation and physico-chemical property of cyclosporine submicroemulsion .Chin J New Drugs(中国新药杂志), 2009, 18 (4):360-364.[5] ZHU H Q,PANG X J,WANG S L.Studies on the formulation and preparation technique of xingnaojing parenteral emulsion . Chin Pharm J(中国药学杂志), 2005, 3(2):53-57.[6] LIN D H,HAN C W,LI J M. Study on preparation and physical stability of submicroemulsion of oleum curcumae extracted from Rhizoma curcumae Royle . J Yantai Univ(Nat Sci Eng Ed)(烟台大学学报:自然科学与工程版),2007, 20 (4):283-286.[7] LUO R C,WANG S L,ZHOU X T,et al.Preparation and characteristics of parenteral submicroemulsion containing propofool and lidocaine hydrochloride. Chin Pharm J(中国药学杂志),2008,6(2):30-35.[8] LI Y,WU Z H,YU B.Preparation and evaluation of nitroglycerin submicron emulsion for intravenous administration.Chin Pharm J(中国药学杂志), 2010,41(7):509-512.[9] CHEN J P,RONG R,LI J W,et al. Formulation optimization and characterization of nimodipine submicron emulsion for intravenous injection . Chin Pharm J(中国药学杂志),2008,6(5):234-238. [10] MIZUSHIMA Y,UCHIDA K,MASUMOTO S,et al. Ester of flurbiprofen and emulsion containing the same:Japan,84304097.3.1984-12-27.[11] TIAN L L,TANG X,HE B.Preparation and in vitro and in vivi evaluation of etoposide submicro-emulsion for intravenous injection.Acta Pharm Sin(药学学报),2007,42(8):892-897.
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