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采用离心造粒粉末层积法制备艾拉莫德(1)载药丸芯,再用流化床底喷包衣技术进行隔离层和缓释层包衣,得到1缓释微丸。采用单因素试验优化了片芯中微晶纤维素与乳糖的比例和黏合剂浓度、缓释层包衣液中致孔剂的种类和浓度、缓释层增重及载药率等对微丸释药行为有影响的因素。以大鼠为模型,对比了市售片剂和自制缓释微丸口服后的药动学行为。结果表明,市售片剂和自制的1缓释微丸的t_(max)为(4.8±1.0)和(9.6±2.2)h,c_(max)为(7 147±1 352)和(3 825±830)ng/ml,MRT为(7.6±1.3)和(12.1±2.3)h,AUC_(0→∞)为(50 788±13 086)和(48 927±5 923)ng·h·ml~(-1)。提示自制缓释微丸具有明显的缓释效果,相对生物利用度为(87.6±11.6)%。
Centrifugal granulation powder stratification method was used to prepare Ilamod (1) loaded pellets, and then the fluidized bed bottom spray coating technique was used to coat the release layer and the sustained release coating to obtain 1 sustained release pellets. The ratio of microcrystalline cellulose to lactose and the concentration of binder in the core were optimized by single factor test. The type and concentration of porogen in sustained-release coating solution, the weight gain and drug loading rate of sustained- Drug release behavior influencing factors. The rat model was used to compare the pharmacokinetics of the commercially available tablets and homemade sustained-release pellets after oral administration. The results showed that the t max of commercial tablets and self-made 1 sustained-release pellets were (4.8 ± 1.0) and (9.6 ± 2.2) h, and the max was 7 147 ± 1 352 and 3 825 ± 0.30 ng / ml, MRT was (7.6 ± 1.3) and (12.1 ± 2.3) h, AUC 0 ~ ∞ was 50 788 ± 13 086 and 48 927 ± 5 923 ng · h · ml ~ (-1). It is suggested that the sustained-release pellets have a sustained release effect and the relative bioavailability is (87.6 ± 11.6)%.