Suzuki R, Nakajima Y, Yagi N, Kenmotsu H, Sekikawa H, Miyazaki S, Mino K, Ohwada S, Kishi F, Hayashi N
Faculty of Pharmaceutical Sciences, Health Sciences University of Hokkaido, Japan.
Yakugaku Zasshi. 1994 Nov;114(11):894-900. doi: 10.1248/yakushi1947.114.11_894.
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.