Comparative Absorption of 5-Aminosalicylic Acid(5-ASA)after Administration of a 5-ASA Enema and Salazosulfapyridine(SASP)after an SASP Suppository in Japanese Volunteers
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概要
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Salazosulfapyridine(SASP)is widely used orally and rectally in the treatment of ulcerative colitis. SASP is mainly metabolized by hydrolysis and the main active metabolite, 5-aminosalicylic acid(5-ASA), has an antiinflammatory effect. In the present study, we prepared suppositories containing 6.5 mmol of SASP and an enema containing 6.5 mmol of 5-ASA. We measured the concentrations of SASP and its various metabolites, 5-ASA, sulfapyridine(SP), acetylated metabolite of SP(Ac-SP), and N-acetyl-5-ASA(Ac-5-ASA), in the serum and urine after a single administration of each preparation to healthy male volunteers. When the SASP suppository was administered, the maximum concentration(C_<max>)of SASP and Ac-5-ASA was 2.5±0.4 and 0.5±0.2μM and the time to C_<max>(T_<max>) was 5 and 12h, respectively. The C_<max> value of SP, which causes side effects, was one-half of that of the parent compound. No 5-ASA in the serum was observed. When the 5-ASA enema was administered. C_<max> and T_<max> values of 5-ASA and Ac-5-ASA were 5.8±2.0 and 13.3±3.6μM and 1 and 7h, respectively. The area under the serum concentration-time curve(AUC)of SASP was 27.4±4.8μM・h, a finding similar to that of 5-ASA after the administration of the 5-ASA enema(29.4±11.1 μM・h). The percentage of urinary recovery of SASP 24h after administration of the SASP suppository was approximately 0.2%. These results indicate that SASP administered rectally is almost completely hydrolyzed in the colon and that 5-ASA is partially absorbed from the small intestine in unchanged form. On the other hand, approximately 0.3% of 5-ASA was recovered in the urine in unchanged form after the administration of the 5-ASA enema, whereas the urinary recovery of Ac-5-ASA was more than 10%. The present findings suggest that 5-ASA has favorable absorptive properties and can be expected to have systemic action after rectal administration of a 5-ASA enema.
- 公益社団法人日本薬学会の論文
- 2002-02-01
著者
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Nabeshima Toshitaka
Department of Chemical Pharmacology, Graduate School of Pharmaceutical Sciences, Meijo University, J
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Nabeshima Toshitaka
Department Of Chemical Pharmacology Faculty Of Pharmaceutical Sciences Meijo University
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Tokui Kenji
Department Of Clinical Biochemistry Faculty Of Pharmacy Meijo University
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Nabeshima T
Nagoya Univ. Graduate School Of Medicine Nagoya Jpn
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Arakawa T
Fukuyama Univ. Hiroshima Jpn
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TOKUl Kenji
Department of Pharmacy, Nagoya Daini Red Cross Hospital
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ASAI Yoshitaka
Department of Pharmacy, Nagoya Daini Red Cross Hospital
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ARAKAWA Toshiharu
Department of Pharmacy and Nagoya Daini Red Cross Hospital
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MATSUMOTO Takatoshi
Department of Surgery, Nagoya Daini Red Cross Hospital
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Tokul Kenji
Department Of Pharmacy Nagoya Daini Red Cross Hospital
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Asai Yoshitaka
Department Of Pharmacy Nagoya Daini Red Cross Hospital
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Matsumoto Takatoshi
Department Of Surgery Nagoya Daini Red Cross Hospital
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