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Monodesmosides, saponin A,B and C, isolated from pericarps of Sapindus mukurossi (Enmei-hi) were shown to promote the rectal absorption of beta-lactam antibiotics in rat, using an in situ loop method and an in vivo method. In the in situ loop method, monodesmosides were solubilized with a mixture of bisdesmosides, mukurozi-saponin X, Y1 and Y2, each of which was isolated from pericarps of Sapindus mukurossi. The promoting functions of the three monodesmosides for the rectal absorption of antibiotics were comparable and also suppressed by Ca2+ ion coexisting in the administered solution. Unlike the case of N-acylcollagenpeptides, which were also previously reported as absorption promoters, no influence of osmolarity of the administered solution on the absorption promoting action was observed. Absorption of beta-lactam antibiotics from suppositories was enhanced with the aid of either of monodesmosides without solubilizing agent.

Enhanced rectal absorption of .BETA.-lactam antibiotics in rat by monodesmosides isolated from pericarps of Sapindus mukurossi (Enmei-hi)