摘要
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一１（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Ｃｍａｘ，Ｔｐ，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％。
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.
出处
《药学学报》
CAS
CSCD
北大核心
1994年第9期707-712,共6页
Acta Pharmaceutica Sinica
关键词
贝诺酯
水扬酸
生物利用度
片剂
Benorilate
Salicylic acid
Paracetamol
Surfactant
Bioavailability
