贝诺酯片剂的研制及生物利用度研究

通过减小药物粒径,提高贝诺酯片剂的生物利用度。在市售片以A(500mg)基础上研制了新处方片剂B(400mg)。建立贝诺酯片剂体外溶出度试验方法,即以表面活性剂溶液作溶出介质,以浆法进行溶出度测定。用HPLC法测定贝诺酯在体内的水解产物水杨酸和扑热息痛的血药浓度。结果表明药物研磨粉碎前后体外溶出速度常数分别为0.0152min-1及0.0337min^-1(P<0.001)。A及B体外平均溶出时间分别为42.25min及15.77min(P<0.001)。体内研究表明A及B水杨酸的C_max,T_p,AUC之间均无显著性差异(P>0.1)(A,B的服用量分别为4.5g及3.6g),B的相对生物利用度为125.59%。

STUDIES ON FORMULATION AND BIOAVAILABILITY OF BENORILATE TABLETS

A new new formulation tablet B was developed and compared with tablet A with thepurpose of improving the bioavailability of benorilate by rebucing its particle size,The dissolution ratein uitro was determined by paddle method and using surfactant solution medlum, The plasma concentra-tions of hydrulyzates which are salicylic acid and paracetamol from benorilate in vivo were measuted byHPLC. The dissolution rates of ground and unground drug are 0.0337 min-1 and0.0152 min-1(P< 0.001) respectively. Compared with tablet A , the cumulative dissolution percentage of B ishigher. The mean dissolution time of B and A are l5. 77 min and 42.25 min(P<0. 001)respec-tively-The study in uiuo showed that the Cmax,Tp and AUC of salicylic acid for these two formulationshave no significant difference(P>0.1), The relative bioavailability of B to A is l25.59%. Their invivo process fits one-compartment medel and first order elimination.