替硝唑（Tinidazole）

替硝唑（Ｔｉｎｉｄａｚｏｌｅ）又名服净（Ｆａｓｉｇｙｎ），为美国Ｐｆｉｚｅｒ公司开发的硝基咪唑类药，化学名１－［２－（乙基磺基）乙基］－２－甲基－５－硝基咪唑，国内已批准生产。药理作用与甲硝唑（灭滴灵）类似，但疗效更高，疗程缩短，副作用少而轻。１药理...

Simultaneous determination of metronidazole and tinidazole in plasma by using HPLC-DAD coupled with second-order calibration

A method using HPLC-DAD coupled with second-order calibration was developed to simultaneously determine metronidazole and tinidazole in plasma samples in this paper. The second-order calibration method based on APTLD （alternating penalty trilinear decomposition） algorithm was proposed to analyze the three-way HPLC-DAD data from both standard and prediction samples, which makes it possible that calibration can be performed even in the presence of unknown interferences with a simple and green chromatographic condition and short analysis time. The results showed that good recoveries were obtained although the chromatographic and spectral profiles of the analytes of interest as well as background were partially overlapped with each other in plasma samples.

Efficacy of recombinant human osteoprotegerin combined with tinidazole in the treatment of periodontitis mice and its correlation with serum RANKL and MCP-1 levels

Objective: To investigate the effect of recombinant human osteoprotegerin combined with tinidazole on mice with periodontitis and the effect on serum RANKL and MCP-1 levels. Methods: 80 SPF-cleaned mice were randomly divided into 4 groups, 20 each, model group, tinidazole group and recombinant human osteoprotegerin group were modeled by Kimura et al., and tinidazole group received tinidazole. After intragastric administration, the recombinant human osteoprotegerin group was injected with recombinant human osteoprotegerin in the periodontal pocket according to the tinidazole group. The periodontal changes of the four groups of mice were observed and recorded, and the gingival rating was performed. Epithelial tissue morphology was observed by hematoxylin-eosin (HE) staining. Serum levels of IL-4, IL-6, RANKL and MCP-1 were measured by enzyme-linked immunosorbent assay. Results:After the intervention, the model group developed severe inflammatory reactions, including redness, hemorrhage, and deep periodontal pockets. The teeth were significantly loosened. The mice in the tinidazole group and the recombinant human osteoprotegerin group recovered substantially, and the gingival rating of the recombinant human osteoprotegerin group was better than that. The tinidazole group and the model group (P<0.05). The results of HE staining showed that the model group had edema, vasodilation and a large amount of inflammatory infiltration. The epithelial structure of the mice in the tinidazole group and the recombinant human osteoprotegerin group was intact and arranged closely and orderly. After intervention, the IL-4 in the tinidazole group and the recombinant human osteoprotegerin group was significantly higher than the model group and IL-6 was significantly lower than the model group (P<0.05), and the recombinant human osteoprotegerin group IL-4 was significantly higher after the intervention. IL-6 was significantly lower in the tinidazole group than in the tinidazole group (P<0.05). After the intervention, the tinidazole group and the recombinant human osteoprotegerin group were significantly reduced, and the recombinant human osteoprotegerin group RAKNL and MCP-1 were significantly lower than the model group (P>0.05). Conclusion: Recombinant human osteoprotegerin combined with tinidazole has a better therapeutic effect on gums and teeth in mice with periodontitis, and can lower the levels of RAKNL and MCP-1 in serum, inhibit bone resorption and protect teeth.

Effect of CYP3A4 genetic polymorphisms on pharmacokinetics of tinidazole

In the present study, we aimed to investigate the frequency of CYP3 A4*18 B genetic polymorphism in Han Chinese populations, and to assess the effect of the CYP3 A4*18 B genetic polymorphism on the pharmacokinetics of tinidazole. A total of 100 healthy volunteers from Han nationalities in China were recruited. DNA was extracted from peripheral leukocytes using a standard protocol. A PCR-RFLP method was developed to detect the alleles of CYP3 A4*18 B. A pharmacokinetic study of tinidazole was then carried out in two groups with CYP3 A4*1/*1(n = 10) and CYP3 A4*1/*18 B(n = 9) genotypes. Concentrations of tinidazole were determined using high-performance liquid chromatography in plasma samples that were collected up to 72 h after drug intake. In this study, 88 healthy volunteers were found with CYP3 A4*1/*1 genotype, and 12 were found with CYP3 A4*1/*18 B genotype. CYP3 A4*18 B/*18 B were absent from all subjects. The allele frequencies of CYP3 A4*18 B were 6%. The pharmacokinetic parameters of CYP3 A4*1/*1 genotype and CYP3 A4*1/*18 B genotype in healthy subjects were as follows: t1/2:(15.92±1.62),(15.77±1.67) h;Cmax:(18.72±3.10),(20.25±3.42) mg/L;tmax:(1.50±0.66),(1.45±0.69) h;Vd/F:(55.73±10.66),(51.30±7.75) L;CL/F:(2.44±0.47),(2.26±0.30) L·h;AUC0–∞:(424.40±82.38),(450.53±69.48) mg·h/L. Collectively, the CYP3 A4*18 B genetic polymorphism did not affect pharmacokinetics of tinidazolein healthy volunteers.

Simultaneous determination of three 5-nitroimidazoles in foodstuffs by differential pulse voltammetry and chemometrics

The voltammetric behaviour of three 5-nitroimidazoles,metronidazole,tinidazole and ornidazole,was investigated,and a method was developed for the simultaneous determination of these compounds,based on their reduction at a hanging mercury drop electrode（HMDE） in pH 8.95 buffer with differential pulse voltammetric（DPV） approach.Well defined voltammetric waves with peak potentials of -692,-640 and -652 mV were observed for these compounds,respectively.It is difficult to determine them individually from their mixtures without preseparation,for their voltammetric peaks overlapped seriously,so the chemometrics were used to resolve the overlapped voltammogram and quantify the mixtures.The proposed method was successfully applied to the determination of three 5-nitroimidazoles in milk and honey samples.