摘要
目的 制备吲哚美辛缓释片,并考察其含量、释放度。比较其与普通吲哚美辛胶囊的药代动力学参数和生物利用度。方法 采用紫外分光光度法作为释放度和含量测定的检测方法。以HPLC法测定10名健康受试者随机交叉口服75mg自制缓释片（本品）与吲哚美辛普通胶囊（对照品）后的血药浓度,计算相应的药动学参数和相对生物利用度。结果 单剂量口服 75 mg本品与对照品的AUC分别为14.100±2.817μg/ml和14.254±2.349μm/ml;Cmax为 2.17±0.71μg/ml和3.95±0.78μm/ml;Tmax为4.1±0.7h和1.85±0.53h;MRT为7.27±0.75h和 5.20±0.74 h,本品的相对生物利用度为98.9％±10.9％。多剂量口服75mg本品（每日一次）与对照品（每日3次）的Cmin ss分别为0.257±0.094μg/ml和0.302±0.104μg/ml;Cmaxss为1.945±0.340μg/ml和1.538±0.384μg/ml;FI为1.537±0.145和1.334±0.186。结论 每日口服一次本品与每日3次对照品生物等效。
AIM Indomethacin sustained-release tablets (ISRT) were prepared. The drug release rate and drug content of the tablets were tested. The pharmacokinetic parameters and relative biovailability of ISRT were investigated. METHODS UV method was used for assaying release degree of ISRT in vitro. The HPLC method was used to monitor plasma drug concentration in vivo. The pharmacokinetics and relative bioavailability (F) of ISRT and conventional capsules (CC) were investigated in \0 healthy male subjects in random 2-way crossover design. RESULTS Single dose test showed that F of ISRT was 98. 9%±10. 9% ; AUC of ISRT and CC were 14. 100±2. 817h. μg/ml and 14. 254±2. 347 h.μg/ml; Cmax were 2. 17± 0. 71μg/ml and 3. 95±0. 78μg/ml; Tmax were 4. 1±0. 7h and 1. 85±0. 53h; MRT were 7. 27 ±0. 75 and 5. 20±0. 74, respectively. The Cmax、Tmax and MRT for the ISRT and CC were significantly different., while the AUC for the two preparations was equal. After multiple doses, Cmin ss of ISRT and CC were 0. 257±0. 094μg/ml and 0. 302±0. 104μg/ml; Cmax ss were 1. 945±0. 340μg/ml and 1. 538±0. 384μg/ml respectively; FI of ISRT and CC were 1. 537±0. 145 and 1.334±1.86. CONCLUSION The two preparations were bioequivalent.
出处
《中国药科大学学报》
CAS
CSCD
北大核心
2002年第5期383-387,共5页
Journal of China Pharmaceutical University
关键词
吲哚美辛
缓释片
释放度
含量测定
生物利用度
药物代谢动力学
紫外分光光度法
Indomethacin
Sustained- release tablets
Dissolution
Determination of content
HPLC
Pharmacokinetics
Relative bioavailability
