[Enhancement of rectal absorption of rifampicin by sodium para-aminosalicylate dihydrate in human subjects].
The suppositories of rifampicin (RFP) containing sodium para-aminosalicylate dihydrate (PAS-Na) were prepared in order to enhance the rectal absorption of RFP. By the addition of PAS-Na, the in vitro release of RFP from the suppositories was enhanced and the hardness of the suppositories decreased. The rectal absorption of RFP from the suppositories containing no PAS-Na (control suppositories) was significantly lower compared to oral administration of it (26%) in human subjects. When PAS-Na was added to the suppository (300 mg), both the area under the plasma concentration-time curve (AUC) and the maximum plasma concentration (Cmax) increased significantly compared to those of the control suppositories. The rectal absorption of PAS-Na itself from the suppositories seemed to be fast. PAS-Na might increase the absorption of RFP dissolved in the rectal fluid from the suppositories, but not affect the undissolved RFP.
Faculty of Pharmaceutical Sciences, Health Sciences University of Hokkaido, Japan.
R
R
Suzuki
Y
Y
Nakajima
N
N
Yagi
H
H
Kenmotsu
H
H
Sekikawa
S
S
Miyazaki
K
K
Mino
S
S
Ohwada
F
F
Kishi
N
N
Hayashi
D000284:Administration, Oral; D000328:Adult; D010131:Aminosalicylic Acid / Q000494:pharmacology*; D001682:Biological Availability; D004347:Drug Interactions; D006801:Humans; D007408:Intestinal Absorption / Q000187:drug effects*; D008297:Male; D012007:Rectum / Q000378:metabolism*; D012293:Rifampin / Q000008:administration & dosage / Q000493:pharmacokinetics*; D013488:Suppositories
D013488:Suppositories; D010131:Aminosalicylic Acid; D012293:Rifampin