【摘要】 以乳酸—乙醇酸共聚物为载体,利用复乳—液中蒸发法制备生长激素释放肽-6(GHRP-6)微球。结果为包封率达100%,平均粒径3.45μm,回收率79%;在37℃p、H 7.0的生理等渗缓冲液中,首日释药19.19%,后以平均日释药3.23%的速度释药25 d。分别对分组家兔肌肉注射GHRP-6微球(2 mg/kg)、GHRP-6(2 mg/kg)、空微球和生理盐水,37 d后,GHRP-6微球组家兔累积增重分别比GHRP-6组、空微球组和生理盐水组高56.34%(P<0.01)、86.68%(P<0.01)和78.41%(P<0.01);采用RIA法测定家兔血清IGF-Ⅰ浓度,注射10 d后,GHRP-6微球组血清IGF-Ⅰ水平较注射前升高41.06%(P<0.05),注射20 d后,分别比GHRP-6组、空微球组和生理盐水组高27.53%(P>0.05)、123.88%(P<0.05)和275.66%(P<0.01)。试验结果表明:GHRP-6乳酸乙醇酸共聚物微球表现出明显的缓释特点,具有显著的促生长作用,有望发展成为新型长效制剂。更多还原

【Abstract】 Sustained-releasing GHRP-6 microspheres were prepared by double emulsion-in liquid evaporation process,using biodegradable polylactic-co-glycolicacid as carrier and the drug release test of the microspheres was detected in vitro.The entrapment efficiency was 100%,mean particle size 3.45 μm and the yield above 79%.In Ph 7.0 physiological isotonic buffer solution,after 19.19% of GHRP-6 was released on the first day,the microspheres released at a rate of 3.23% per day for more than 25 d(r=0.877).Rabbits were divided into four groups with 8 rabbits in each group randomly.Rabbits were treated with GHRP-6 microspheres(2 mg/kg of BW),GHRP-6(2 mg/kg of BW),empty microspheres and saline by muscular injection.37 days later,the mean accumulative weight gain of rabbits injected with GHRP-6 microspheres was 56.34%(P<0.01),86.68%(P<0.01),78.41%(P<0.01)higher than that of rabbits injected with GHRP-6,empty microspheres and saline,respectively.Before and after injection,concentrations of serum IGF-Ⅰ of rabbits were detected by radioimmunoassay(RIA) using a human IGF1 RIA kit.Concentrations of serum IGF-Ⅰ increased 41.06%(P<0.05)in GHRP-6 microspheres group on the tenth day,27.53%(P>0.05),123.88%(P<0.05),275.66%(P<0.01)higher than those groups injected with GHRP-6,empty microspheres and saline respectively.更多还原