EFFECT OF ANTACID ON GASTROINTESTINAL ABSORPTION OF FLEROXACIN IN HEALTHY HUMANS
We investigated the effect of aluminum hydroxide, an antacid, on the gastrointestinal absorption of fleroxacin in six healthy male volunteers. Two hundred milligrams of fleroxacin was given orally to fasting subjects with and without 1g of dried aluminum hydroxide gel. The peak serum concentrations...
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| Published in | CHEMOTHERAPY Vol. 38; no. Supplement2; pp. 344 - 349 |
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| Main Authors | , , , , , , , , , , |
| Format | Journal Article |
| Language | English Japanese |
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Japanese Society of Chemotherapy
1990
公益社団法人 日本化学療法学会 |
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| ISSN | 0009-3165 1884-5894 |
| DOI | 10.11250/chemotherapy1953.38.Supplement2_344 |
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| Abstract | We investigated the effect of aluminum hydroxide, an antacid, on the gastrointestinal absorption of fleroxacin in six healthy male volunteers. Two hundred milligrams of fleroxacin was given orally to fasting subjects with and without 1g of dried aluminum hydroxide gel. The peak serum concentrations of unchanged drug were slightly reduced from 2.37 to 1.81μg/ml by concurrent administration of aluminum hydroxide, but no significant changes were found in the area under the serum concentration-time curve, time at which peak serum concentrations were achieved, and elimination half-life in serum. Furthermore, urinary excretion of fleroxacin and total drug over 48 h slightly decreased from 67.2 and 77.6 to 60.3 and 68.3%, respectively. We therefore concluded that the effect of aluminum hydroxide on the gastrointestinal absorption of fleroxacin was less than on other quinolonecarboxylic acid antimicrobial agents. |
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| AbstractList | We investigated the effect of aluminum hydroxide, an antacid, on the gastrointestinal absorption of fleroxacin in six healthy male volunteers. Two hundred milligrams of fleroxacin was given orally to fasting subjects with and without 1g of dried aluminum hydroxide gel.The peak serum concentrations of unchanged drug were slightly reduced from 2.37 to 1.81μg/ml by concurrent administration of aluminum hydroxide, but no significant changes were found in the area under the serum concentration-time curve, time at which peak serum concentrations were achieved, and elimination half-life in serum. Furthermore, urinary excretion of fleroxacin and total drug over 48 h slightly decreased from 67.2 and 77.6 to 60.3 and 68.3%, respectively. We therefore concluded that the effect of aluminum hydroxide on the gastrointestinal absorption of fleroxacin was less than on other quinolonecarboxylic acid antimicrobial agents.
Fleroxacinの胃腸管吸収に及ぼす制酸剤 (乾燥水酸化アルミニウムゲル) の影響を, 6名の健常成人男子志願者において検討した。Fleroxacin 200mgを空腹時に服用した場合の最高血清中濃度は, 乾燥水酸化アルミニウムゲル1gの同時併用により, 2.37から1.81μg/mlへと有意に低下したが, 血清中濃度曲線下面積, 最高血清中濃度到達時間及び血清中半減期に有意な変化は見られなかった。さらに服用後48hまでの尿中fleroxacinの排泄率は67.2から60.3%へ, 代謝物も含めた尿中総排泄率は77.6から68.3%へとそれぞれわずかに低下した。他のキノロンカルボン酸系抗菌剤と比較して, fleroxacinの胃腸管吸収に及ぼす水酸化アルミニウムの影響は少ないものと結論された。 We investigated the effect of aluminum hydroxide, an antacid, on the gastrointestinal absorption of fleroxacin in six healthy male volunteers. Two hundred milligrams of fleroxacin was given orally to fasting subjects with and without 1g of dried aluminum hydroxide gel. The peak serum concentrations of unchanged drug were slightly reduced from 2.37 to 1.81μg/ml by concurrent administration of aluminum hydroxide, but no significant changes were found in the area under the serum concentration-time curve, time at which peak serum concentrations were achieved, and elimination half-life in serum. Furthermore, urinary excretion of fleroxacin and total drug over 48 h slightly decreased from 67.2 and 77.6 to 60.3 and 68.3%, respectively. We therefore concluded that the effect of aluminum hydroxide on the gastrointestinal absorption of fleroxacin was less than on other quinolonecarboxylic acid antimicrobial agents. |
| Author | SAITO, SHIZUKI YOSHIDA, MASAKI SHIBA, KOHYA KUSAJIMA, HISAO SHIMADA, JINGORO UCHIDA, HIROSHI KAJI, MASANOBU HORI, SEIJI ISHIDA, RYOZO SAITO, ATSUSHI SAKAI, OSAMU |
| Author_FL | 加地 正伸 柴 孝也 草嶋 久生 酒井 紀 斉藤 静樹 吉田 正樹 内田 広 堀 誠治 石田 了三 斎藤 篤 嶋田 甚五郎 |
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| References | 8) MAESEN F P V, DAVIES B I, GERAEDTS W H, SUMAJOW C A: Ofloxacin and antacids. J Antimicrob Chemother 19: 709-712, 1987 14) NIX D E, WATSON W A, LENER M E, FROST R W, KROL G, GOLDSTEIN H, LETTIERI J, SCHENTAG J J Effects of aluminum and magnesium antacids and ranitidine on the absorption of ciprofloxacin. Clin Pharmacol Ther 46: 700-705, 1989 6) PREHEIM L C, CUEVAS T C, ROCCAFORTE J S, MELLENCAMP M A, BITTNER M J: Ciprofloxacin and antacids. Lancet II: 48, 1986 4) NAKASHIMA M, KANAMARU M, UEMATSU T, TAKIGUCHI A, MIZUNO A, ITAYA T, KAWAHARA F, OOIE T, SAITO S, UCHIDA H, MASUZAWA K: Clinical pharmacokinetics and tolerance of fleroxacin in healthy male volunteers. J Antimicrob Chemother 22 (Suppl. D): 133-144, 1988 15) WELLING P G: Interactions affecting drug absorption. Clin Pharmacokinet 9: 404-434, 1984 7) FLEMING L W, MORELAND T A, STEWART W K, SCOTT A C: Ciprofloxacin and antacids. Lancet II: 294, 1986 16) OKAZAKI O, KURATA T, TACHIZAWA H: Studies on the mechanism of pharmacokinetic interaction of aluminum hydroxide, an antacid, with new quinolones in rats. 薬物動態3: 387-394, 1988 9) RUBINSTEIN E, SEGEV S Drug interactions of ciprofloxacin with other non-antibiotic agents. Am. J Med 82 (Suppl. 4A): 119-123, 1987 1) HIRAI K, AOYAMA H, HOSAKA M, OOMORI Y, NIWATA Y, SUZUE S, IRIKURA T: In vitro and in vivo antibacterial activity of AM-833, a new quinolone derivative. Antimicrob Agents Chemother 29: 1059-1066, 1986 12) GRASELA T H JR, SCHENTAG J J, SEDMAN A J, WILTON J H, THOMAS D J, SCHULTZ R W, LEBSACK M E, KINKEL A W: Inhibition of enoxacin absorption by antacids or ranitidine Antimicrob Agents Chemother 33: 615-617, 1989 10) SHIBA K, SAITO A, MIYAHARA T, TACHIZAWA H, FUJIMOTO T: Effect of aluminum hydroxide, an antacid, on the pharmacokinetics of new quinolones in humans. 薬物動態3: 717-722, 1988 2) KUSAJIMA H, ISHIKAWA N, MACHIDA M, UCHIDA H, IRIKURA T Pharmacokinetics of a new quinolone, AM-833, in mice, rats, rabbits, dogs, and monkeys. Antimicrob Agents Chemother 30: 304-309, 1986 13) NIX D E, WILTON J H, SCHENTAG J J, PARPIA S H, NORMAN A, HARVEY R: Inhibition of norfloxacin absorption by antacids and sucralfate. Rev Infect Dis 11 (Suppl. 5): S1096, 1989 3) 川原富美男, 大家毅, 永津芳雄, 内田広: 新キノロン系抗菌剤Fleroxacinのヒト及び各種実験動物における代謝. Chemotherapy 38 (S-2): 122-134, 1990 5) HOFFKEN G, BORNER K, GLATZEL P D, KOEPPE P, LODE H: Reduced enteral absorption of ciprofloxacin in the presence of antacids. Eur J Clin Microbiol 4: 345, 1985 11) PARPIA S H, NIX D E, HEJMANOWSKI L G, GOLDSTEIN H R, WILTON J H, SCHENTAG J J: Sucralfate reduces the gastrointestinal absorption of norfloxacin. Antimicrob Agents Chemother 33: 99-102, 1989 |
| References_xml | – reference: 4) NAKASHIMA M, KANAMARU M, UEMATSU T, TAKIGUCHI A, MIZUNO A, ITAYA T, KAWAHARA F, OOIE T, SAITO S, UCHIDA H, MASUZAWA K: Clinical pharmacokinetics and tolerance of fleroxacin in healthy male volunteers. J Antimicrob Chemother 22 (Suppl. D): 133-144, 1988 – reference: 5) HOFFKEN G, BORNER K, GLATZEL P D, KOEPPE P, LODE H: Reduced enteral absorption of ciprofloxacin in the presence of antacids. Eur J Clin Microbiol 4: 345, 1985 – reference: 16) OKAZAKI O, KURATA T, TACHIZAWA H: Studies on the mechanism of pharmacokinetic interaction of aluminum hydroxide, an antacid, with new quinolones in rats. 薬物動態3: 387-394, 1988 – reference: 8) MAESEN F P V, DAVIES B I, GERAEDTS W H, SUMAJOW C A: Ofloxacin and antacids. J Antimicrob Chemother 19: 709-712, 1987 – reference: 2) KUSAJIMA H, ISHIKAWA N, MACHIDA M, UCHIDA H, IRIKURA T Pharmacokinetics of a new quinolone, AM-833, in mice, rats, rabbits, dogs, and monkeys. Antimicrob Agents Chemother 30: 304-309, 1986 – reference: 12) GRASELA T H JR, SCHENTAG J J, SEDMAN A J, WILTON J H, THOMAS D J, SCHULTZ R W, LEBSACK M E, KINKEL A W: Inhibition of enoxacin absorption by antacids or ranitidine Antimicrob Agents Chemother 33: 615-617, 1989 – reference: 11) PARPIA S H, NIX D E, HEJMANOWSKI L G, GOLDSTEIN H R, WILTON J H, SCHENTAG J J: Sucralfate reduces the gastrointestinal absorption of norfloxacin. Antimicrob Agents Chemother 33: 99-102, 1989 – reference: 7) FLEMING L W, MORELAND T A, STEWART W K, SCOTT A C: Ciprofloxacin and antacids. Lancet II: 294, 1986 – reference: 10) SHIBA K, SAITO A, MIYAHARA T, TACHIZAWA H, FUJIMOTO T: Effect of aluminum hydroxide, an antacid, on the pharmacokinetics of new quinolones in humans. 薬物動態3: 717-722, 1988 – reference: 15) WELLING P G: Interactions affecting drug absorption. Clin Pharmacokinet 9: 404-434, 1984 – reference: 9) RUBINSTEIN E, SEGEV S Drug interactions of ciprofloxacin with other non-antibiotic agents. Am. J Med 82 (Suppl. 4A): 119-123, 1987 – reference: 3) 川原富美男, 大家毅, 永津芳雄, 内田広: 新キノロン系抗菌剤Fleroxacinのヒト及び各種実験動物における代謝. Chemotherapy 38 (S-2): 122-134, 1990 – reference: 13) NIX D E, WILTON J H, SCHENTAG J J, PARPIA S H, NORMAN A, HARVEY R: Inhibition of norfloxacin absorption by antacids and sucralfate. Rev Infect Dis 11 (Suppl. 5): S1096, 1989 – reference: 14) NIX D E, WATSON W A, LENER M E, FROST R W, KROL G, GOLDSTEIN H, LETTIERI J, SCHENTAG J J Effects of aluminum and magnesium antacids and ranitidine on the absorption of ciprofloxacin. Clin Pharmacol Ther 46: 700-705, 1989 – reference: 1) HIRAI K, AOYAMA H, HOSAKA M, OOMORI Y, NIWATA Y, SUZUE S, IRIKURA T: In vitro and in vivo antibacterial activity of AM-833, a new quinolone derivative. Antimicrob Agents Chemother 29: 1059-1066, 1986 – reference: 6) PREHEIM L C, CUEVAS T C, ROCCAFORTE J S, MELLENCAMP M A, BITTNER M J: Ciprofloxacin and antacids. Lancet II: 48, 1986 |
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| SubjectTerms | Fleroxacin 制酸剤 吸収 水酸化アルミニウム |
| Title | EFFECT OF ANTACID ON GASTROINTESTINAL ABSORPTION OF FLEROXACIN IN HEALTHY HUMANS |
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