国产亚叶酸钙片、胶囊与进口亚叶酸钙片的人体相对生物利用度比较

Domestic calcium folinate tablets and capsules vs imported calcium folinate tablets relative bioavailability in healthy volunteers

目的 :研究 3种亚叶酸钙制剂 (国产片剂、胶囊和进口片剂 )在 12名健康志愿者体内的相对生物利用度。方法 :同体交叉试验后 ,测定血浆中亚叶酸钙浓度 ,计算主要药物动力学参数和相对生物利用度 ,并进行统计学分析。结果 :国产片、胶囊和进口片单剂量 75mg ,po后 ,Tmax 分别为 ( 2 .5±s0 .3)h ,( 2 .5± 0 .3)h和 ( 2 .4± 0 .3)h ;Cmax为 ( 654± 146) μg·L- 1,( 599± 132 ) μg·L- 1和 ( 640± 163)μg·L- 1;AUC0～∞ 为 ( 7811± 1481) μg·h·L- 1,( 70 91± 1397) μg·h·L- 1和 ( 7898± 1855) μg·h·L- 1;T12 为 ( 8.7± 0 .6)h ,( 8.6± 0 .4 )h和 ( 8.6±0 .5)h。国产片、胶囊相对生物利用度分别为 ( 10 1± 14) % ,( 93± 11) %。结论 :3种制剂生物等效。

AIM: To study the pharmacokinetics and relative bioavailability of calcium folinate domestic tablets and capsules and imported tablets in 12 healthy volunteers. METHODS: According to the crossover design, each volunteer was orally given calcium folinate tablets or capsule (75 mg). The drug concentrations in plasma were determined by RP-HPLC. RESULTS: The pharmacokinetic parameters of the domestic tablets, capsules and imported tablets were as following: T max (2.5±0.3) h,(2.5±0.3) h and (2.4±0.3) h; C max (654±146) μg·L -1 ,(599±132) μg·L -1 and (640±163) μg·L -1 ; AUC 0-∞ (7811±1855) μg·h·L -1 ,(7091±1397) μg·h·L -1 and (7898±1855) μg·h·L -1 ; T 12 (8.7± 0.6 ) h,(8.6±0.4) h and (8.6±0.5) h. The relative bioavailability of the domestic tablets and capsules was (101±14)% and (93±11)%. CONCLUSION: The result of statistical analysis shows that three formulations are bioequivalent. * Graduate of school of pharmacy, Shanghai Medical University in the class of 1999, SHANGHAI 200032, China