本文選題：頭孢地尼　切入點(diǎn)：液相色譜-串聯(lián)質(zhì)譜法　出處：《鄭州大學(xué)》2014年碩士論文

【摘要】：頭孢地尼是一種新的廣譜口服半合成抗菌藥物,是一種口服氨基噻唑頭孢菌素,對(duì)腸道革蘭氏陽(yáng)性和革蘭氏陰性細(xì)菌均有效。對(duì)β內(nèi)酰胺酶不穩(wěn)定是許多頭孢菌素的弱點(diǎn),相對(duì)而言,頭孢地尼對(duì)β內(nèi)酰胺酶比較穩(wěn)定,甚至對(duì)許多耐青霉素和某些頭孢菌素的細(xì)菌依然敏感,頭孢地尼對(duì)耳、鼻竇、咽喉和皮膚常見(jiàn)細(xì)菌感染有效。本研究將以廣州市白云山光華制藥股份有限公司生產(chǎn)的頭孢地尼膠囊為參比制劑,考察廣東省先強(qiáng)藥業(yè)有限公司生產(chǎn)的頭孢地尼片和分散片在健康人體中的相對(duì)生物利用度及生物等效性。目的：采用高效液相串聯(lián)質(zhì)譜建立測(cè)定人血漿中頭孢地尼的方法學(xué)并評(píng)價(jià)頭孢地尼膠囊(廣州市白云山光華制藥股份有限公司生產(chǎn))、頭孢地尼片(廣東省先強(qiáng)藥業(yè)有限公司)、頭孢地尼分散片(廣東省先強(qiáng)藥業(yè)有限公司)在健康人體中的生物等效性。方法：采用隨機(jī)、自身前后三交叉的實(shí)驗(yàn)設(shè)計(jì),24名健康男性受試者單劑量口服100mg三種不同的頭孢地尼口服制劑,采用高效液相色譜串聯(lián)質(zhì)譜法測(cè)定,并使用DAS2.1軟件計(jì)算藥代動(dòng)力學(xué)參數(shù)及相對(duì)生物利用度,評(píng)價(jià)廣東省先強(qiáng)藥業(yè)有限公司生產(chǎn)的頭孢地尼片和分散片在健康人體中的生物等效性。結(jié)果：采用高效液相色譜串聯(lián)質(zhì)譜法,頭孢地尼的線性范圍為11.50-2300.00ng.mL-1,批內(nèi)、批間精密度(RSD)均小于10%。受試制劑(頭孢地尼片,A藥；頭孢地尼分散片,B藥)與參比制劑(頭孢地尼膠囊,R藥)的主要藥動(dòng)學(xué)參數(shù)分別為：Tmax分別為(3.0±0.8)、(3.2±0.9)和(3.5±0.7)h； Cmax分別為(548.96±184.58)、(607.09±236.38)和(570.18±172.37)ng·mL-1；t1/2分別為(2.0士0.3)、(1.9±0.4)和(1.9±0.3)h；梯形法算得AUCo-t分別為(2755.30±956.10)、(3037.50-±1014.40)和(2756.40±804.10)ng·h·m1-1,AUCo-∞分別為(2857.90±1011.60)、(3143.80±1038.40)和(2862.10±821.20)ng·h·m1-1。頭孢地尼片(A藥)和頭孢地尼分散片(B藥)分別以參比制劑為對(duì)照,用面積法AUCo-t估算的受試制劑的相對(duì)生物利用度分別為(104.2±37.5)%和(111.8±30.3)%。結(jié)論：建立的分析方法靈敏、快速、準(zhǔn)確,可以用于本研究。受試制劑與參比制劑具有生物等效性。
[Abstract]:Cefdinil is a new broad-spectrum oral semi-synthetic antibiotic, an oral aminothiazole cephalosporin, which is effective against both Gram-positive and Gram-negative bacteria in the intestinal tract. Instability of 尾 -lactamases is a weakness of many cephalosporins. Cefdinil is relatively stable to 尾 -lactamases, and even sensitive to penicillin and some cephalosporins. Common bacterial infections in throat and skin are effective. The cefdini capsule produced by Guangzhou Baiyun Mountain Guanghua Pharmaceutical Co., Ltd will be used as reference preparation. To investigate the relative bioavailability and bioequivalence of cefodipine tablets and dispersible tablets produced by Xianqiang Pharmaceutical Co., Ltd., Guangdong Province. Objective: to establish a method for the determination of cefodide in human plasma by high performance liquid chromatography tandem mass spectrometry (HPLC-MS). The methodology and evaluation of cefdini capsules (Guangzhou Baiyunshan Guanghua Pharmaceutical Co., Ltd.) production of Cefdini tablets (Guangdong Province Xianqiang Pharmaceutical Co., Ltd., Cefdini dispersible tablets (Guangdong Province Xianqiang Pharmaceutical Co., Ltd. Bioequivalence in healthy humans. Methods: random, A single dose of 100mg was administered to 24 healthy male subjects and three different kinds of cefdinir were used to determine it by high performance liquid chromatography-tandem mass spectrometry (HPLC / MS). The pharmacokinetic parameters and relative bioavailability were calculated by DAS2.1 software. To evaluate the bioequivalence of cefodinil tablets and dispersible tablets produced by Xianqiang Pharmaceutical Co., Ltd in Guangdong Province in healthy volunteers. Results: the linear range of cefdinil in healthy volunteers was 11.50-2300.00ng.mL-1 by HPLC tandem mass spectrometry (HPLC / MS). RSDs were less than 10. The main pharmacokinetic parameters of cefdinir dispersible tablets) and reference preparations (cefdinil capsule R) were: Tmax: 3. 0 鹵0. 8 鹵0. 9 鹵0. 9) and 3. 5 鹵0. 7 h; Cmax: 548. 96 鹵18. 58. 58. 58. 09 鹵236.38) and 570. 18 鹵0. 3 鹵0. 3 鹵0. 3 AUCo-t and 1. 9 鹵0. 3; trapezoidal method, AUCo-t = 2755.30 鹵956.10, 3037.50- 鹵1014.40, AU56.40 鹵AU56.40 鹵804.10)ng h, respectively. 鈭，

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