摘要
目的:制备阿司匹林缓释片,评价人体内动力学、相对生物利用度及血药浓度。方法:以羟丙甲纤维素,聚丙烯酸树脂Ⅱ为释放阻滞剂制备缓释片,转篮法测释放度,高效液相色谱法测10名男性健康志愿者交叉po50mg肠溶片和缓释片后的血药浓度,数据经3P87软件微机处理。结果:体外释药:肠溶片t50=2.4h,缓释片t50=4.5h。释药9h以上。单剂量po肠溶片和缓释片cmax分别为(7.96±1.65)μg·ml-1和(3.03±0.22)μg·ml-1(P<0.01)。t1/2R分别为(2.89±0.93)h和(7.81±2.16)h。(P<0.01)。AUC0～24h为(64.53±8.86)μg·h·ml-1和(66.49±12.55)μg·h·ml-1(P>0.05),相对生物利用度为(103.49±12.32)%。多剂量po肠溶片和缓释片cmin分别为(0.54±0.20)μg·ml-1和(1.25±0.27)μg·ml-1(P<0.01)。cmax分别为(6.86±1.09)μg·ml-1和(3.29±0.41)μg·ml-1(P<0.01)。FI分别为(1.73±0.16)和(0.86±0.23)(P<0.01)。结论:该缓释片处方合理,工艺简单,适合于工业化生产,为预防和治疗血栓形成提供一个新的剂型。
OBJECTIVE:To prepare aspirin sustained release tablets and study the pharmacokinetics and relative bioavailability in volunteers.METHODS:Hypromellose and poplyacrglic resin Ⅱ were used as blocking agent for the preparation of sustained release tablets.The release experiments were performed in a rotating shaker.The aspirin in concentrations in serum were assayed by HPLC mothod.A single oral does of sustained release tablets and enteric coated tablet were given to 10 volunteers respectively in an open randomized cross over test.3P87 was used to process main pharmacokinetic parameters.RESULTS:The sustained release of tablet and enteric coated tablets in vitro,t 50 was 4.5 h and 2.4 h respectively.The drug in sustained release tablets was released over 9 h.The main parameters of daily dose were as following. c max of enteric tablets and sustained release tablets were (7.96±1.65)μg·ml -1 and (3.03±0.22)μg·ml -1 ( P <0.01). t 1/2K (2.89±0.93) h and (7.81±2.16)h.( P <0.01). AUC 0～24h (64.53±8.86)μg·h·ml -1 and (66.49±12.55)μg·h·ml -1 ( P >0.05).The relative bioavailability of sustained release tablets was (103.49±12.32)%.The main parameters of cumulative dose in body, c min of enteric coated tablets and sustained release tablets were (0.54±0.20)μg·ml -1 and (1 25±0.27)μg·ml -1 ( P <0.01)。 c max (6.86±1.09)μg·ml -1 and (3.29±0.41)μg·ml -1 ( P <0.01)。FI(1.73±0.16) and (0.86±0.23),respectively ( P <0.01).CONCLUSION:The sustained release tablets may play an important role in prevention and treatment of thrombogenesis as the result of its reasonable formulation and simple technology.
出处
《中国药学杂志》
EI
CAS
CSCD
北大核心
2000年第2期110-113,共4页
Chinese Pharmaceutical Journal
关键词
阿司匹林
缓释片
药代动力学
aspirin,sustained release tablets,pharmacokinetics
