ABSTRACT
This study is to establish and validation in vivo models of moxifloxacin based on the theory of physiologically based pharmacokinetics (PBPK), and then to predict the distribution of moxifloxacin in human venous return and organ such as lung, spleen and so on. The efficacy of moxifloxacin and its pharmaceutical preparations were quantified by comparing the pharmacokinetic parameters with the minimum inhibitory concentration of related pathogenic bacterium. The results showed that the anti-infection efficacy of pharmaceutical moxifloxacin preparation in the corresponding organs was basically the same. The PBPK model of moxifloxacin preparations can be more accurately described the pharmacokinetic of anti-infective drugs in human, it is suitable for the efficacy evaluation of anti-infective drugs and provides a strong basis for the corresponding scientific research and scientific supervision.
ABSTRACT
Research on polymer impurities has always been important in the quality control of cephalosporins. Research on polymers in cephalosporins that lack active amino groups on the C-7 side chain has not been reported. Therefore, our study used cefazolin sodium, which is widely used in the clinic, as an example. The polymer in cefazolin sodium and its product "cefazolin sodium pentahydrate for injection" was analyzed by column switching liquid chromatography-high resolution mass spectrometry. Two polymer impurity peaks were detected and the possible structures of these polymers were suggested. Through two-dimensional liquid chromatography, the chromatographic peaks following Sephadex gel chromatography and high-performance gel chromatography were compared to those obtained by reverse high-performance liquid chromatography (HPLC) for cefazolin sodium as reported in the Chinese Pharmacopoeia. The HPLC method proves more suitable for polymer detection than Sephadex gel chromatography and high-performance gel chromatography. The method of polymer detection for cefazolin sodium was established using the method of related substances HPLC as described in the Chinese Pharmacopoeia.
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To establish a method for the determination of polymer impurities in cefixime raw materials and preparations, a cefixime degradation solution containing polymer impurities was prepared by forced polymerization. Polymer impurities in the degradation solution were separated and identified by high performance gel chromatography and the column switching-LC-MSn method. A new RP-HPLC method for cefixime polymer was established and validated with a Phenomenex Gemini-C18 column using a mobile phase gradient elution of 0.5% formic acid-water solution and 0.5% formic acid-acetonitrile solution. The results showed that when using this high performance gel chromatography method some small molecular weight impurities were co-eluted with the polymers, resulting in a poor specificity and poor quantitative accuracy. But when using the RP-HPLC method, three polymer impurities were detected with good specificity, sensitivity and robustness, including two cefixime dimers, and dehydrate dimer. Therefore, the described RP-HPLC method is suitable for the quality control of polymer impurities in cefixime, and cefixime degradation solution can be used as suitable solution for analysis of cefixime polymers.
ABSTRACT
To establish a method for the determination of polymer impurities in ceftazidime raw materials and preparations, a ceftazidime degradation solution containing polymer impurities was prepared by forced polymerization. Polymer impurities in the degradation solution were separated and identified by high performance gel chromatography and the column switching-LC-MSn method. A new RP-HPLC method for ceftazidime polymer was established and validated with a Phenomenex Gemini-C18 column using a mobile phase gradient elution of 0.02 mol·L-1 phosphate buffer, methanol and acetonitrile. The results showed that when using this high performance gel chromatography method some small molecular weight impurities were co-eluted with the polymers, resulting in a poor specificity and poor quantitative accuracy. But when using the RP-HPLC method, four polymer impurities were detected in the 25-45 min time range with good specificity, sensitivity and robustness, including two ceftazidime dimers, trimers, and derivatives. Therefore, the described RP-HPLC method is suitable for the quality control of polymer impurities in ceftazidime, and ceftazidime degradation solution can be used as suitable solution for analysis of ceftazidime polymers.
ABSTRACT
Objective To observe the curative effect of mouse nerve growth factor and its influence on levels of BDNF,IGF-1,and IL-33 in patients with acute cerebral infarction.Methods Totally 106 cases of patients with acute cerebral infarction were chosen as the research objects between October 2015 and February 2017 in Fourth People's Hospital of Langfang City.According to digital list method,the patients were randomly divided into treatment group and control group,53 cases in each group.The patients in two groups were treated with conventional medicine of acute cerebral infarction,and the patients in treatment group were added to mNGF on the basis of conventional drugs,im injection,18 μg each time,once daily.The patients in control group were not added to NGF treatment,and the patients in two groups were treated for 14 d.Before and after treatment,the degrees of neural function defect in two groups were scored according to NIH Stroke Scale (NIHSS),serum levels of brain-derived neurotrophic factor (BDNF),insulin-like growth factor-1 (IGF-1) and interleukin-33 (IL-33) were determinated using enzyme-linked immunosorbent method.Results Compared with those before treatment,NIHSS scores decreased (P ＜ 0.05) after 14 d of treatment in two groups,but the reduced value in treatment group was obviously higher than that in control group (P ＜ 0.05).After treatment,the total effective rate (93.4％) of treatment group was better than that of control group (46.6％),and the difference was statistically significant (P ＜ 0.05).Compared with before treatment,serum levels of BDNF and IGF-1 rised (P ＜ 0.05),IL-33 decreased (P ＜ 0.05) after 14 d of treatment in two groups,but the changes in treatment group were significantly greater than those in control group (P ＜ 0.05).Conclusion mNGF can effectively reduce the severity of nervous functional defects,and effectively increase expression levels of BDNF and IGF 1 and decreasedexpression level ofIL-33.
ABSTRACT
Objective To observe the curative effect of mouse nerve growth factor and its influence on levels of BDNF,IGF-1,and IL-33 in patients with acute cerebral infarction.Methods Totally 106 cases of patients with acute cerebral infarction were chosen as the research objects between October 2015 and February 2017 in Fourth People's Hospital of Langfang City.According to digital list method,the patients were randomly divided into treatment group and control group,53 cases in each group.The patients in two groups were treated with conventional medicine of acute cerebral infarction,and the patients in treatment group were added to mNGF on the basis of conventional drugs,im injection,18 μg each time,once daily.The patients in control group were not added to NGF treatment,and the patients in two groups were treated for 14 d.Before and after treatment,the degrees of neural function defect in two groups were scored according to NIH Stroke Scale (NIHSS),serum levels of brain-derived neurotrophic factor (BDNF),insulin-like growth factor-1 (IGF-1) and interleukin-33 (IL-33) were determinated using enzyme-linked immunosorbent method.Results Compared with those before treatment,NIHSS scores decreased (P ＜ 0.05) after 14 d of treatment in two groups,but the reduced value in treatment group was obviously higher than that in control group (P ＜ 0.05).After treatment,the total effective rate (93.4％) of treatment group was better than that of control group (46.6％),and the difference was statistically significant (P ＜ 0.05).Compared with before treatment,serum levels of BDNF and IGF-1 rised (P ＜ 0.05),IL-33 decreased (P ＜ 0.05) after 14 d of treatment in two groups,but the changes in treatment group were significantly greater than those in control group (P ＜ 0.05).Conclusion mNGF can effectively reduce the severity of nervous functional defects,and effectively increase expression levels of BDNF and IGF 1 and decreasedexpression level ofIL-33.
ABSTRACT
Powder X-ray diffraction (PXRD) technology combined with cluster analysis method was used to classify 75 batches of crystalline ceftriaxone sodium into subtypes, the crystalline characteristics of each subtype were measured with scanning electron microscope (SEM). By comparing some parameters of these subtypes correlated to crystallization process of ceftriaxone sodium, such as salification rate, water content in different subtypes, as well as by studying different lattice stabilities, different compatibilities with rubber closures during accelerated stability tests, the key point to improve the quality of domestic ceftriaxone sodium was disclosed. The results of this paper indicated that the fine structure of the products could be controlled well by improving the salification and crystallization process. As a result, the subtype II of ceftriaxone sodium with high stability can be produced.
Subject(s)
Ceftriaxone , Chemistry , Classification , Crystallization , Microscopy, Electron, Scanning , Powders , Water , X-Ray DiffractionABSTRACT
One kind of new cefazolin sodium hydrate crystal was obtained in the isopropyl alcohol - water system. There are two symmetry independent molecules in the asymmetric unit, both being well ordered in the lattice, and ten independent water positions but generally four to six (mean five) water molecules and one sodium ion present in the unit cell structure. Huge solvent tunnels can be found. Again there are two general regions of water molecules, those in the large solvent tunnels and those in proximity of the sodium ion and the tetrazole moieties of the drug molecule. The physical and chemical characteristics of the new cefazolin sodium hydrate crystal are similar to that of the alpha-form cefazolin sodium crystal, and the new crystal has better chemical stability than amorphous cefazolin sodium powder.