Rectal absorption of ozagrel from suppositories in rabbits.
Rectal absorption of ozagrel (a selective thromboxane synthetase inhibitor) from suppositories was studied in rabbits. Two kinds of suppositories were prepared, one was from ozagrel powder (OPS, ozagrel powder suppository), and the other from ozagrel tablet (OTS, ozagrel tablet suppository). Ozagrel from OPS was absorbed quickly with a Tmax value of 26.3 +/- 7.5 min, and the peak plasma level was significantly higher than that involving intravenous infusion or oral dose (50.3 +/- 6.7 vs. 32.8 +/- 5.4 or 9.9 +/- 1.2 micrograms/ml), indicating that OPS may be a useful dosage form rather than injection. OTS was absorbed less rapidly than OPS, but the AUCs of both suppositories were similar. Because OTS was prepared using an ozagrel tablet, it is fairly easy to get an equal content in each suppository. Therefore, OTS is not only an experimentally interesting dosage form, like OPS, but is also a practical preparation for clinical use.
Zheng
N X
NX
Department of Hospital Pharmacy, Toyama Medical and Pharmaceutical University, Japan.
Adachi
I
I
Horikoshi
I
I
Kanamoto
I
I
D000042:Absorption; D000284:Administration, Oral; D000285:Administration, Rectal; D000818:Animals; D002851:Chromatography, High Pressure Liquid; D007275:Injections, Intravenous; D008297:Male; D008689:Methacrylates / Q000008:administration & dosage / Q000378:metabolism / Q000493:pharmacokinetics*; D011817:Rabbits; D012007:Rectum / Q000378:metabolism*; D013488:Suppositories; D013930:Thromboxane-A Synthase / Q000037:antagonists & inhibitors*
D008689:Methacrylates; D013488:Suppositories; D013930:Thromboxane-A Synthase; C034364:ozagrel