维胺酯软胶囊的人体相对生物利用度研究

 目的：研究维胺酯软胶囊与硬胶囊的人体相对生物利用度。方法：采用反相高效液相色谱法测定10名男性健康志愿者随机单剂量po维胺酯硬胶囊150mg（25mg×6粒）和软胶囊100mg（5mg×20粒）后，药物在体内的经时过程。结果：药物制成软胶囊后，药物的吸收相和消除相无明显改变，但可以显著提高口服维胺酯的生物利用度，软胶囊与硬胶囊的t_1／2ka分别为（1．457±0．508）h和（1．349±0．482）h，t_1／2ke分别为（2．378±0．871）h和（2．744±1．097）h，t_max分别为（2．612±0．778）h和（2．649±0．700）h，c_max分别为（17．496±8．992）μg·L^－1和（16．031±7．732）μg·L^－1，体内平均驻留时间（MRT）分别为（3．618±0．540）h和（3．728±0．379）h，AUC分别为（93．467±54．148）μg·h·L^－1和（89．658±45．814）μg·h·L^－1。其相对生物利用度为（169．41±29．08）％。结论：软胶囊与硬胶囊相比具有较高的生物利用度。

The relative bioavailability of soft ritaminate capsules in healthy volunteers

OBJECTIVE: To study the relative bioavailability between soft and solid capsules. METHODS: The single dose soft (100 mg) and solid (150 mg) capsules were administrated crossing over in 10 volunteers. A reversed phase high performance liquid chromatography was used to determine ritaminate level in human plasma. RESULTS: There were no significant difference in absorption and elimination phases between two preparations. The main pharmacokinetic parameters of soft and solid capsules were as follows. The absorption t_1/2 was (1.457±0.508)h and (1.349±0.482)h respectively. The elimination t_1/2 was (2.378±0.871)h and (2.744±1.097)h respectively. The time to achieve maximum plasma concentrations was (2.612±0.778)h and (2.649±0.700)h, respectively. The peak concentrations were (17.496±8.992)μg·L^-1 and (16.031±7.732)μg·L^-1 respectively. The mean retention times (MRT) were (3.618±0.540)h and (3.728±0.379)h, respectively. The area under curve (AUC) was (93.467±54.148)μg·h·L^-1 and (89.658±45.814)μg·h·L^-1 respectively. The relative bioavailability of ritaminate soft capsule to solid capsule was (169.41±29.08)%. CONCLUSION: The ritaminate soft capsules have higher bioavailability than solid ones.