坐薬の必要挿入時間と途中排出に関する薬物体内動態論的考察

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Drug informations on a suitable insertion duration of suppositories and on a deal with the problem of the loss from rectal are essential for the proper therapy of patients. In the present study, we collected the data on drug disposition after administration of commercially available suppositories which had systemic pharmacological effects, and then analized pharmacokinetically on the problems of the insertion duration of them and the loss from rectal. The rectal absorption rate and the cumulative absorption ratio of drugs from commercially available suppositories were estimated by the deconvolution analysis. The plasma concentration data after rectal and intravenous administration were obtained in nine kinds of drugs, which were ampicilline, ketoprophene, indomethacine, acetoaminophene, phenobarbital, donperidone, bromazepam, buprenorphine and morphine. It was shown that the completion time of the absorption of drug from the suppositories varied largely from 50 min for ampicilline to 8 hours for donperidone. Comparing the time periods required to reach to 50% in the cumulative absorption ratio in those drugs, the fastest time was found in ampicilline (15 min), and the slowest was in aminophylline (90 min). These findings make it possible to the persue counseling for the patients on the proper insertion duration of each suppositories. The simulation of the time course of blood drug concentration after the loss of suppositories from rectal and the supplement of them was successfully performed, suggesting that the optimal drug concentration could be controled by the rational supplemental dose. In conclusion, the drug information based on the deconvolution analysis can be useful to instruct a rational use of suppositories to the pharmacist and/or the patients.
日本医療薬学会の論文
1993-06-21

坐薬の必要挿入時間と途中排出に関する薬物体内動態論的考察

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