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《Chinese Pharmacological Bulletin》 2004-10
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A pharmacokinetic study of tetramethylpyrazine in the retinal tisue of rabbits following intraperitoneal injection

DENG Xin-guo1, Hu Shi-xing 1,2, ZHANG Qing-jiong1,YANG Jin-nan1, LIN Shao-chun1, WU Jue-heng3,TANG Li-fen3,ZHONG Guo-ping4 (1.Dept of Clinical Ocular Pharmacology, Zhongshan Ophthalmic Center, Sun Yat -Sen University,Guangzhou 510060 China;2.Eye Hospital of China Academy of Tra ditional Chinese Medicine, Beijing, 100040 China;3.The Research Center of Mol ecular Medicine, Zhongshan Medical College, Sun Yat-SenUniversity; 4.Pharmaco logical Institute, Pharmacological College, Sun Yat-Sen University Guangzhou 5 10060,China)  
Aim To determine the concentration and dynamic chan ge s of tetramethylpyrazine hydrochloride in the retinal tissue following intraperi toneal injection in rabbits.Methods 44 rabbits were randomly divided into 11 groups. Tetramethylpyrazine hydrochloride (80 mg·kg -1) was given by intraperitoneal injection. After a single dose administration retinal tiss ue were harvested at different time points and the concentrations of tetramethylpyrazine hydrochloride were determined by Reversed Phase High Performance Liquid Chromatography ( RP-HPLC ). Resuslts The concentration-time data of tetramethylpyrazine hydrochloride in the retinal tissue were subjected to two-compartment open model. The pharmacokinetic parameters were: C max= 1.63 mg·g -1, T max=0.32 h, T 1/2α=0.35 h, T 1/2β= 2.50 h, CL=7.89 g·h -1.The concentration of tetramethylpyrazine hydrochl oride in retinal tissue were (1.36±0.16) mg·g -1 at 15 min and reached its maximum concentration (2.59±0.19) mg·g -1 at 30 min. Then the conc entration of tetramethylpyrazine hydrochloride in retinal tissue gradually decre ased and there were lower concentrations after 5 h. Conclusion The RP-HPLC was accurate and sensitive.Tetramethylpyrazine hydrochloride can penetrate blood-retinal barriers and enter retina tissue. These results provide an experimental data for the management of eye diseases with tetramethylpyrazine by systemic administration.
【Fund】: 广东省自然科学基金 (张清炯 0 10 765 );; 国家自然科学基金(杨锦南 3 0 3 0 0 467);; 广东省中医药管理局科学基金 (邓新国 10 40 0 64 )资助项目
【CateGory Index】: R96
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