FUNDAMENTAL AND CLINICAL STUDIES ON BRL 28500 (CLAVULANIC ACID-TICARCILLIN) IN THE FIELD OF PLASTIC AND RECONSTRUCTIVE SURGERY
BRL 28500, a formulation of the antimicrobial agent ticarcillin (TIPC) and the β-lactamase inhibitor clavulanic acid (CVA), was evaluated to establish its distribution to the skin, antibacterial activity and clinical effect. Following intravenous administration of BRL 28500 1.6g to patients who were...
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| Published in | CHEMOTHERAPY Vol. 34; no. Supplement4; pp. 1091 - 1100 |
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| Main Authors | , , , , |
| Format | Journal Article |
| Language | English Japanese |
| Published |
Japanese Society of Chemotherapy
1986
公益社団法人 日本化学療法学会 |
| Online Access | Get full text |
| ISSN | 0009-3165 1884-5894 |
| DOI | 10.11250/chemotherapy1953.34.Supplement4_1091 |
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| Abstract | BRL 28500, a formulation of the antimicrobial agent ticarcillin (TIPC) and the β-lactamase inhibitor clavulanic acid (CVA), was evaluated to establish its distribution to the skin, antibacterial activity and clinical effect. Following intravenous administration of BRL 28500 1.6g to patients who were about to be subject to full thickness skin grafts under general anesthesia, TIPC and CVA showed high serum and skin concentration levels. The maximum level of TIPC and CVA in the serum was observed 30 minutes after injection, the value was 109.58μg/ml and 5.44μg/ml respectively. However the maximun level in the skin was observed 1 hour after injection, TIPC value was 20.60μg/g and CVA value was 1.30μg/g. The ratio of the skin level to the serum concentration 1 hour after administration was 29%(20.60/70.79) for TIPC and 39%(1.30/3.33) for CVA. The antibacterial activity of BRL 28500 against 106 clinical isolates of Staphylococcus aureus was 2 tubes superior to TIPC and 2 to 4 tubes superior to piperacillin. In clinical studies, BRL 28500 was administered at a dose of 3.2g to 6.4g per day for 4 to 21 days to 16 patients with skin infections. The clinical effect of BRL 28500 was excellent in 2, good in 13 and poor in 1 case. No adverse reactions were observed and in laboratory findings, only one patient who had a history of liver insufficiency, showed a tentative elevation of S-GOT, S-GPT and total bilirubin level. |
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| AbstractList | BRL 28500, a formulation of the antimicrobial agent ticarcillin (TIPC) and the β-lactamase inhibitor clavulanic acid (CVA), was evaluated to establish its distribution to the skin, antibacterial activity and clinical effect. Following intravenous administration of BRL 28500 1.6g to patients who were about to be subject to full thickness skin grafts under general anesthesia, TIPC and CVA showed high serum and skin concentration levels. The maximum level of TIPC and CVA in the serum was observed 30 minutes after injection, the value was 109.58μg/ml and 5.44μg/ml respectively. However the maximun level in the skin was observed 1 hour after injection, TIPC value was 20.60μg/g and CVA value was 1.30μg/g. The ratio of the skin level to the serum concentration 1 hour after administration was 29%(20.60/70.79) for TIPC and 39%(1.30/3.33) for CVA. The antibacterial activity of BRL 28500 against 106 clinical isolates of Staphylococcus aureus was 2 tubes superior to TIPC and 2 to 4 tubes superior to piperacillin. In clinical studies, BRL 28500 was administered at a dose of 3.2g to 6.4g per day for 4 to 21 days to 16 patients with skin infections. The clinical effect of BRL 28500 was excellent in 2, good in 13 and poor in 1 case. No adverse reactions were observed and in laboratory findings, only one patient who had a history of liver insufficiency, showed a tentative elevation of S-GOT, S-GPT and total bilirubin level. BRL 28500, a formulation of the antimicrobial agent ticarcillin (TIPC) and the β-lactamase inhibitor clavulanic acid (CVA), was evaluated to establish its distribution to the skin, antibacterial activity and clinical effect.Following intravenous administration of BRL 28500 1.6g to patients who were about to be subject to full thickness skin grafts under general anesthesia, TIPC and CVA showed high serum and skin concentration levels. The maximum level of TIPC and CVA in the serum was observed 30 minutes after injection, the value was 109.58μg/ml and 5.44μg/ml respectively. However the maximun level in the skin was observed 1 hour after injection, TIPC value was 20.60μg/g and CVA value was 1.30μg/g. The ratio of the skin level to the serum concentration 1 hour after administration was 29%(20.60/70.79) for TIPC and 39%(1.30/3.33) for CVA.The antibacterial activity of BRL 28500 against 106 clinical isolates of Staphylococcus aureus was 2 tubes superior to TIPC and 2 to 4 tubes superior to piperacillin.In clinical studies, BRL 28500 was administered at a dose of 3.2g to 6.4g per day for 4 to 21 days to 16 patients with skin infections. The clinical effect of BRL 28500 was excellent in 2, good in 13 and poor in 1 case.No adverse reactions were observed and in laboratory findings, only one patient who had a history of liver insufficiency, showed a tentative elevation of S-GOT, S-GPT and total bilirubin level. BRL 28500はβ-lactamase阻害剤であるclavulanic acid (CVA) とticarcillin (TIPC) を1:15 (力価比) の割合で配合した注射用抗生物質である。本剤の皮膚内濃度, 抗菌力, 臨床効果などを検討し以下の成績を得た。全身麻酔下に植皮術を受けた患者に, BRL 28500 1.6gをone shotで静注した後のTIPC, CVAの皮膚内濃度は, 血中濃度が30分値にピークを有したのに対して, 1時間値にピークがあり, それぞれ20.6±6.07μg/g, 1.30±0.55μg/gに達し, 以後1.23時間, 1.17時間のT1/2をもって減少した。皮膚への移行はTIPCで血中濃度の29%, CVAで39%と良好であった。臨床分離のS. aureus 106株のうち88.7%はβ-lactamase産生株で, TIPC, PIPCには高度耐性株が存在したが, BRL 28500はTIPCに対して2段階, PIPCに対して2～4段階強い抗菌活性を示した。β-lactamase産生94株中77株 (81.9%) がTIPCに対して100μg/ml以上のMICを示したが, CVAを配合したBRL 28500に対しては約2段階小さい値のMICとなった。術後潰瘍4例, 熱傷潰瘍3例, II度熱傷2例, 化膿性汗腺炎2例, 難治性瘻孔2例, 術後膿瘍1例, 肺梗塞に伴う呼吸器感染症1例, 下顎骨骨髄炎1例, 褥瘡1例の計17例にBRL 28500を3～21日 (平均8.2日), 総投与量8.0～124.8g (平均29.6g) を投与した。判定不能の1例を除いた16例中, 著効2例 (12.5%), 有効13例 (81.3%), 無効1例 (6.2%) で有効率は93.8%であった。副作用として投与前に肝機能障害を有した1例にGOT, GPTの一時的上昇を認めたが, 投与中止後4日目に正常値となった。その他には重篤な副作用は認めなかった。 |
| Author | SUGANO, HIROYUKI YOSHIDA, TETSUNORI HOMMA, KEN-ICHI HONDA, KOUICHI OHURA, TAKEHIKO |
| Author_FL | 菅野 弘之 本田 耕一 大浦 武彦 吉田 哲憲 本間 賢一 |
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| References | 3) 吉田哲憲, 大浦武彦, 本間賢一, 菅野弘之, 野崎敏彦, 他: Cofotaximeの皮膚移行についての検討. Chemotherapy 34 (2): 165-170, 1986 4) HUNTER, P. A.; K. COLEMAN, J. FISHER & D. TAYLOR: In vitro synergistic properties of clavulanic acid, with ampicillin, amoxycillin and ticarcillin. J. Antimicrob. Chemother. 6: 445-470, 1980 1) O'CALLAGHAN, C. H. A. MORRIS, S. M. KIRBY & A. H. SHINGLER: Novel method for detection of β-lactamase by using a chromogenic cephalosporin substrate. Antimicrob. Agents Chemother. 1 (4): 283-288, 1972 2) 吉田哲憲, 沖本雄一郎, 大浦武彦, 飯田和典, 斎玲藤: 形成外科領域におけるTicarcillinの基礎的・臨床的検討. Chemotherapy 25 (9): 2681-2689, 1977 5) 第33回日本化学療法学会総会, 新薬シンポジウムBRL 28500, 東京, 1985 |
| References_xml | – reference: 5) 第33回日本化学療法学会総会, 新薬シンポジウムBRL 28500, 東京, 1985 – reference: 2) 吉田哲憲, 沖本雄一郎, 大浦武彦, 飯田和典, 斎玲藤: 形成外科領域におけるTicarcillinの基礎的・臨床的検討. Chemotherapy 25 (9): 2681-2689, 1977 – reference: 3) 吉田哲憲, 大浦武彦, 本間賢一, 菅野弘之, 野崎敏彦, 他: Cofotaximeの皮膚移行についての検討. Chemotherapy 34 (2): 165-170, 1986 – reference: 1) O'CALLAGHAN, C. H. A. MORRIS, S. M. KIRBY & A. H. SHINGLER: Novel method for detection of β-lactamase by using a chromogenic cephalosporin substrate. Antimicrob. Agents Chemother. 1 (4): 283-288, 1972 – reference: 4) HUNTER, P. A.; K. COLEMAN, J. FISHER & D. TAYLOR: In vitro synergistic properties of clavulanic acid, with ampicillin, amoxycillin and ticarcillin. J. Antimicrob. Chemother. 6: 445-470, 1980 |
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| Title | FUNDAMENTAL AND CLINICAL STUDIES ON BRL 28500 (CLAVULANIC ACID-TICARCILLIN) IN THE FIELD OF PLASTIC AND RECONSTRUCTIVE SURGERY |
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