醋酸曲安奈德/硅凝胶药膜的制备及体外释放度观察

Preparation of triamcinolone acetonide acetate/silicone gel sheets and observation of its release in vitro

目的:制备醋酸曲安奈德/硅凝胶药膜,观察其体外释放度和释药均一性,以选择释药量符合临床治疗需要的药膜类型。方法:实验于2004-11-10/2005-01-15于第三军医大学高原医学系中心实验室进行。利用醋酸曲安奈德药物原粉与硅凝胶混合,在150°C高温硫化2h,分别制备醋酸曲安奈德/硅凝胶A,B,C3种药膜,含药量分别为:0.83,1.11,1.39mg/cm2。各观察时间点样品体外释放度的测定采用高效液相色谱方法(测定样品吸收度,根据标准曲线计算其释放量,得出释放百分比),并观察药膜释药均一性。结果:①醋酸曲安奈德/硅凝胶药膜体外释放度:A,B,C3种药膜的释药趋势基本相同,硅凝胶释药呈稳定释放趋势,符合Higuichi方程;14d时的体外释放度分别达到18.18%,19.38%,22.38%。C型药膜14d内释药约为20～30mg,药膜释药可达到0.3～0.4mg/cm2。②药膜释药均一性:同型药膜各部分释药在同时间段中的相对标准偏差<3%。结论:从不同药物添加量中,发现C型药膜的释药剂量较为符合临床处方剂量,制膜时使得药膜药物含量达到约1.5mg/cm2时释放量符合临床治疗剂量的要求。

AIM:To prepare triamcinolone acetonide acetate(TAA)/silicone gel sheets(SGS) and observe its in vitro release and uniformity of drug delivery so as to choose types of drug gel sheets accordant with the requirement of clinical treatment. METHODS:The experiment was finished in central laboratory of Department of High Altitude Medicine,Third Military Medical University from November 10,2004 to January 15,2005.Three different types of TAA/SGS,type A,type B,type C,which contained TAA 0.83 mg/cm2,1.11 mg/cm2,1.39 mg/cm2,were prepared by the TAA powder and SGS at 150 ℃for approximately 2 hours.The in vitro release at different time was detected by high performance liquid chromatography(the absorptivity was detected,and the release was calculated based on the standard curve so as to get release percent of TAA in SGS).The uniformity of drug delivery of the drug gel sheets was also observed. RESULTS:①The in vitro release of TAA/SGS:The three types of TAA/SGS almost had the same trend of drug delivery.The stabilized release trend of TAA/SGS was accordant with Hiquichi equation.The in vitro release percents of A,B,C types of TAA/SGS at 14 days were 18.18%,19.38%and 22.38%respectively.The drug delivery of type C TAA/SGS ranged from 20 to 30 mg within 14 days,and the drug delivery rate of drug gel sheets achieved 0.3 to 0.4 mg/cm2.②The uniformity of drug delivery of TAA/SGS:The relative standard deviation was less than 3%in different parts of the same type of drug gel sheets. CONCLUSION:From the different additive doses of drugs,it is found that the drug delivery rate of type C of TAA/SGS is more accordant with the dose of clinical prescription,as compared with the two other types of TAA/SGS,that is,the drug delivery rate about 1.5 mg/cm2 is accordant with the dose of clinical requirement.