中文摘要 Cefaclor是臨床上使用的第二代頭孢菌素類(Cephasporins)抗生素，為一種廣效型抗生素，它比第一代頭孢菌類抗生素對於革蘭氏陰性菌有更大的活性，更能抵抗β-lactamases的破壞，且更容易進入腦脊髓液治療。Cefaclor的口服吸收良好、食物對吸收的影響並不大。在本研究中，主要在評估兩種含量250 mg Cefaclor膠囊劑，永信藥廠生產的Kerfen膠囊劑與台灣Lilly公司生產的Keflor膠囊劑，於國人的相對生體可用率及定量法HPLC的分析結果。 12位健康受試者接受此兩種產品的隨機雙向交叉研究，每人於試驗開始口服單劑量250 mg，試驗一天，抽全程血液檢品。利用高效液相層析法(High performance liquid chromatography:HPLC)分析血漿中Cefaclor的濃度。其分析條件為：Purospher STAR RP-18e逆相層析管柱、移動相為氰甲烷 / 磷酸-水(pH3.5)=6/94(v/v)、流速1ml/min、β-Hydroxyethyl—theophylline為內部標準品、UV偵測波長265nm。分析後有良好的線性關係，其同日、異日精確性及定量極限之變異係數均在10%以內，相對回收率亦大於95%。 結果顯示，Cefaclor膠囊在國人口服後約0.72小時可達到最高血中濃度約5.55μg/ml、平均半衰期(T1/2)約為0.85小時、平均曲線下面積(AUC0-∞)約6.9μg*hr/ml。經由統計學二向變異數分析(Two-way ANOVA)結果，兩組產品的動力學參數，包括：Cmax、Tmax、T1/2、AUC0-∞及AUC0-10 等，結果發現並無統計學上的顯著差異(p>0.05)，因此可以認定KeflorⓇ膠囊劑和Kerfen膠囊劑兩藥品是生體相等性的。; Abstract Cefaclor is the second-generation cephalosporins antibiotic in clinical therapy. It has a broad antibacterial spectrum and shows better activity against Gram-negative bacteria, against the destroy of β-lactamase , and more easy cross into brand blister fluid than first-generation cephalosporins antibiotic. Cefaclor is an oral absorbed well and is not significantly affected by the presence of food. In this study, it was mainly estimating relative bioavailability in Taiwan and the analysis results of quantitative methods (HPLC) of the capsules formulations of test preparation (Kerfen, YSP) and reference preparation (Keflor, Lilly in Taiwan). Twelve healthy subjects received both products by randomized two-way crossover design. Within one day, each subject was administrated 250 mg doses before the test. The plasma samples were collected all day. The concentrations of Cefaclor in plasma samples were analyzed by high performance liquid chromatography (HPLC). The chromatographic conditions were : Purosphur STAR RP-18 column, acetonitril : water with phosphoric acid (pH 3.5) = 6 : 94 (v/v) of mobile phase, flow rate 1 ml/min, β-hydroxyethyl-theophylline as internal standard, and monitored at UV 265nm. The method showed good linearity, the intra- and inter-day validation and limit of quantification were reasonably with C.V. values less than 10%. The relative recovery was above 95%. The results showed Tawan reaching peak concentration 5.5 μg/ml at about 0.72 hours. The mean half-life (T1/2) was about 0.85 hours. The mean area under the serum concentration curve (AUC0-∞) was about 6.9 μg*hr/ml. After analyzed by two-way ANOVA statistics, there are no significant statistic different between pharmacokinetic parameter (p<0.05) of two products, including the plasma concentration (Cmax), time to peak level (Tmax), the mean half-life (T1/2), and area under the curve (AUC). It could be recommened that Keflor capsule and Kerfen capsule are bioequivalent.
