Pharmacokinetic and Bioavailability Study of Aspirin Phospholipid Complex Self-microemulsion in Rats in vivo / 中国药房

ABSTRACT

OBJECTIVE:To study the pharmacokinetics behaviors and the bioavailability of aspirin phospholipid complex self-microemulsion in rats in vivo. METHODS:12 SD rats were randomly divided into aspirin suspension group(10 mg/kg)and as-pirin phospholipid complex self-microemulsion group (10 mg/kg),6 in each group. Rats were intragastrically administrated,and blood sample 0.6 mL was taken from jugular vein before administration and after 0.083,0.25,0.5,0.75,1.0,2.0,3.0,4.0,6.0, 8.0,12.0 h of administration. HPLC was used to determine the concentration of salicylic acid in rats'plasma. DAS 2.0 pharmacoki-netic software was adopted to calculate the pharmacokinetic parameters and relative bioavailability. RESULTS:The pharmacokinetic processes of both aspirin suspension and aspirin phospholipid complex self-microemulsion were in line with one-compartment mod-el. The salicylic acid of cmax of rats in aspirin suspension group and aspirin phospholipid complex self-microemulsion group were (1.904 ± 0.208),(6.457 ± 1.091) μg/mL;AUC0-12 h were (12.860 ± 1.327),(47.270 ± 12.860) μg/(h·mL);tmax were (2.167 ± 0.983),(0.917±0.540)h,respectively. Compared with aspirin suspension,salicylic acid of cmax and AUC0-12 h of aspirin phospholip-id complex self-microemulsion in rats in vivo were significantly increased (P<0.01),while tmax was significantly decreased (P<0.05);the relative bioavailability was 367.57%. CONCLUSIONS:Making aspirin into phospholipid complex self-microemulsion can improve the gastrointestinal absorption,with high relative bioavailability.