The increased consumption of azithromycin during the COVID-19 pandemic may have led to its presence in the waterways. This study aims to evaluate the effect of this situation on aquatic bacteria. Methodology: Over a f...The increased consumption of azithromycin during the COVID-19 pandemic may have led to its presence in the waterways. This study aims to evaluate the effect of this situation on aquatic bacteria. Methodology: Over a four-month period following the official recognition of the COVID-19 outbreak in Yaoundé, water samples were collected from four rivers selected on the basis of their vicinity to care centers for COVID-19. Bacteria within azithromycin’s spectrum of activity were isolated, and the antibiotic’s efficacy was tested against the most frequently isolated species. The influence of COVID-19 incidence and other external factors was also assessed. Results: The most frequently isolated bacteria were Bacillus spp., Enterococcus spp., Listeria spp. and Staphylococcus epidermidis. These strains exhibited varying levels of sensitivity to azithromycin, ranging from 0% to 100%. The observed resistance rates were 12.5%, 14.29%, 16.67%, and 0%, respectively. Neither COVID-19 incidence, proximity to hospitals, nor rainfall significantly influenced bacterial resistance rates to azithromycin (P > 0.05). These resistance levels may be attributed to the relatively short exposure of bacteria to azithromycin at the sampled locations, as well as the impact of agricultural and livestock-related chemicals, such as biocides and antibiotics, present in the watershed. Conclusion: These results highlight the need to integrate into anti-COVID-19 activities, the monitoring of bacteria’s sensitivity in aquatic environments.展开更多
Introduction: The WHO recommends mass administration of azithromycin 30 mg/kg to eradicate yaws and 20 mg/kg to eliminate trachoma. We evaluated the effectiveness of azithromycin at 20 and 30 mg/Kg, and the number of ...Introduction: The WHO recommends mass administration of azithromycin 30 mg/kg to eradicate yaws and 20 mg/kg to eliminate trachoma. We evaluated the effectiveness of azithromycin at 20 and 30 mg/Kg, and the number of cycles of mass administration on the treatment and interruption of yaws transmission in the Mbaïki health district in the Central African Republic. Methods: Following a yaws prevalence survey, azithromycin was administered as a mass treatment in four yaws endemic communities in the Mbaïki health district. Azithromycin 30 mg/kg was administered in one cycle in Kenengué and three cycles spaced three months apart in Bambou. In Kapou and Bangui-Bouchia, azithromycin was administered at a dose of 20 mg/kg in one cycle and three cycles, respectively, spaced three months apart. Before the mass treatment round, confirmed yaw cases were selected and followed for seven months. The primary endpoint was serological cure seven months after the first treatment cycle. Secondary endpoints were clinical cure at four weeks after the first treatment cycle and serological cure at four months after the first treatment cycle. A non-inferiority margin (∆) of 10% was used. Results: A total of 92 participants aged 1 to 90 years, including 52 men, were included in the study. The frequently encountered skin lesions were ulcers (65.22%) and were localized to the lower limbs (59.78%). Clinical cure was not obtained in Bangui-Bouchia and Kapou (∆ = 17.1% and 30.8%). Serological cure at four and seven months was not obtained in Kapou (∆ equal to 17.9% and 13.8% respectively). Conclusion: This study confirms the effectiveness of azithromycin 30 mg/kg in a single dose for the treatment of yaws. However, the study suggests that for yaws eradication programs, two to three cycles of mass administration of azithromycin at 20 or 30 mg/kg spaced three months apart, with therapeutic coverage greater than 90% are essential.展开更多
3＇-N-demethylazithromycin is an impurity in azithromycin drug. It is derived by demethyl- ation of azithromycin, i. e. , azithromycin loses a methyl group on the 3＇-N position. In this study, bulk product was purifi...3＇-N-demethylazithromycin is an impurity in azithromycin drug. It is derived by demethyl- ation of azithromycin, i. e. , azithromycin loses a methyl group on the 3＇-N position. In this study, bulk product was purified with chromatographic separation. It was observed that 3＇-N-demethylaz- ithromycin was also a precursor of other impurities. Simultaneously, another derivative was synthe- sized, i. e. , 3＇-N-demethyl-3＇-N-formylazithromycin. Reaction conditions were optimized with the HPLC method and good-quality and high-yield derivative product was achieved. The structures of de- rivatives were identified by 1H-NMR and MS.展开更多
A universal quantitative model was developed to determine the azithromycin content in granules using near infrared （NIR） diffuse reflectance spectroscopy. The diffuse reflection spectra were recorded with the integr...A universal quantitative model was developed to determine the azithromycin content in granules using near infrared （NIR） diffuse reflectance spectroscopy. The diffuse reflection spectra were recorded with the integrating sphere at 8 cm-1 resolution in 4000–12 000 cm-1 spectral range. During each measurement, 32 co-added scans were performed. This quantitative model was constructed with 103 batches of azithromycin granules from 21 different manufacturers. The azithromycin content ranges from 3.0% to 24.5%. The root mean square error of prediction （RMSEP） of model was 0.613. In addition, the quantitative model was evaluated in terms of specificity, linearity, accuracy, and precision according to ICH guidelines. In conclusion, it is feasible to construct a universal quantitative model for azithromycin granules by choosing suitable training set samples and selecting an appropriate wavelength range. The quantitative model could be applied in the quick assay of azithromycin granules produced by domestic manufacturers （content： 3.0%–24.5%）.展开更多
Aim In order to improve the solubility of azithromycin, the objectives of the present study were to screen an appropriate salt for azithromycin by comparing acute hepatic and renal toxicities in animals, and study the...Aim In order to improve the solubility of azithromycin, the objectives of the present study were to screen an appropriate salt for azithromycin by comparing acute hepatic and renal toxicities in animals, and study the pharmacokinetics of final chosen azithromycin salt. Methods Various salts of azithromycin, such as glutamate, citrate, hydrochloride, sulphate, dihydrogen phosphate, lactobionate, tartrate, and aspartate were given intravenously to Sprague Dawley rats at a dose of 10 mg once daily for 14 consecutive days via tail vein. The acute hepatic and renal indicators were measured before and after administration. A pharmacokinetic study was performed on 12 healthy human volunteers. The subjects were equally divided into two groups by a randomized crossover design. Azithromycin glutamate injection was administered by intravenous infusion or intramuscular injection at a single dose of 500 mg, respectively. Azithromycin concentrations in plasma were determined by microbial inhibition zone assay, and the pharmacokinetic parameters were calculated using a practical pharmacokinetic software 3P87 program. Results Azithromycin glutamate was least toxic to the liver and kidney of the rats, thus being selected as a final salt for parenteral preparation of azithromycin. Pharmacokinetic results showed that the area under the plasma concentration-time curves （AUC0-120h） were 21.47 ± 1.57 h·μg·mL^-1 for intravenous infusion, and 19.36 ± 2.44 h·μg·mL^-1 for intramuscular injection. The absolute bioavailability of intramuscular injection was 92.59%. Conclusion Azithromycin glutamate is suitable for the future clinical application, and its pharmacokinetics is characterized in human volunteers in the present study.展开更多
A high-performance liquid chromatography （HPLC） system was used in the reversed phase mode for the determination ofbenzalkonium chloride （BKC） in azithromycin viscous ophthalmic drops. A Venusil-XBP（L）-C18 （150...A high-performance liquid chromatography （HPLC） system was used in the reversed phase mode for the determination ofbenzalkonium chloride （BKC） in azithromycin viscous ophthalmic drops. A Venusil-XBP（L）-C18 （150 mm×4.6 mm, 5 gm） column was used at 50℃. The mobile phase consisted of a mixture of methanol-potassium phosphate （16：5, v/v）. Two sample preparation methods were compared. The results suggested that, compared with an extraction procedure, a deproteinization procedure was much quicker and more convenient. Using the deproteinization procedure for sample preparation, calibration curves were linear in the range 5.0-50μg/ml. The within-day and inter-day coefficients of variation were less than 10%. The average recoveries were determined as 96.70%, 98.52%, and 97.96% at concentrations of 10.0, 30.0, and 50.0 μg/ml, respectively. Variability in precision did not exceed 5%. In conclusion, this HPLC method using a simple sample treatment procedure appears suitable for monitoring BKC content in azithromycin viscous ophthalmic drops.展开更多
AIM： To evaluate whether adding azithromycin to firstline Helicobacter pylori （H pylorl） eradication improved eradication and reduced side effects. METHODS： Eligible articles were identified by searches of electro...AIM： To evaluate whether adding azithromycin to firstline Helicobacter pylori （H pylorl） eradication improved eradication and reduced side effects. METHODS： Eligible articles were identified by searches of electronic databases. We included all randomized trials that compared azithromycin-containing with standard triple-therapy regimens for first-line treatment of H pylori infection. Statistical analysis was performed with Review Manager 5.0.10. Sub-analyses were also performed. RESULTS： We identified 14 randomized trials （1431 patients）. Pooled Hpylori eradication rates were 72.01% （95% CI： 58.09%-85.93%） and 69.78% （95% CI： 66.47%-73.09%） for patients with or without azithromycin by intention-to-treat analysis, and the odds ratio （OR） was 1.17 （95% CI： 0.64-2.14）. The occurrence of side effects differed significantly and was 15.81% （95% CI： 12.50%-19.12%） and 25.20% （95% CI： 21.44%-28.96%） for treatment with or without azithromycin, respectively, and the summary OR was 0.58 （95% CI： 0.41-0.82）. Furthermore, the azithromycin-containing group had a lower occurrence of diarrhea, nausea and taste disturbance. CONCLUSION： Our review suggests that azithromycincontaining triple-therapy regimens could be equally effective in eradication of Hpylori compared with standard first-line triple-therapy regimens.展开更多
Azithromycin and Chinese medicine forsythia are often used together to treat pediatric mycoplasma infections in China. We aimed to investigate the pharmacokinetic interaction of Forsythia suspensa extract and azithrom...Azithromycin and Chinese medicine forsythia are often used together to treat pediatric mycoplasma infections in China. We aimed to investigate the pharmacokinetic interaction of Forsythia suspensa extract and azithromycin after single and co-intravenous administration in rats. Male Sprague-Dawley rats received single(Forsythia suspensa extract or azithromycin) treatment or co-administration of Forsythia suspensa extract and azithromycin. Blood samples were collected at scheduled times, and drug concentrations were determined by HPLC-UV or HPLC-MS/MS methods. Both non-compartmental analyses and nonlinear mixed-effects modeling approaches were applied to fit pharmacokinetic data and evaluate the impact of co-administration. Pharmacokinetic analysis showed that the area under the curve of azithromycin and forsythiaside increased, and clearance decreased significantly(P < 0.05),after co-administration. The in vivo behavior of both azithromycin and forsythiaside could be appropriately described by the two-compartmental model. The final population pharmacokinetic model indicated that co-administration decreased the central volume of azithromycin and forsythiaside clearance significantly. Co-administration of Forsythia suspensa extract and azithromycin significantly decreased the clearance and increased exposure for both drugs. Pharmacokinetic data suggest that drug co-administration may increase efficiency.展开更多
AIM： To investigate eradication rates, patient compliance and tolerability of a 1-wk Azithromycin-based quadruple therapy versus the 2-wk conventional therapy. METHODS： A total of 129 Hpylori-positive patients were ...AIM： To investigate eradication rates, patient compliance and tolerability of a 1-wk Azithromycin-based quadruple therapy versus the 2-wk conventional therapy. METHODS： A total of 129 Hpylori-positive patients were randomized to either omeprazole 20 mg, bismuth subcitrate 240 mg, azithromycin 250 mg, and metronidazole 500 mg, all twice daily for 1-wk （B-OAzM） or omeprazole 20 mg, bismuth subcitrate 240 mg, amoxicillin lg, and metronidazole 500 mg all twice daily for 2-wk （B-OAM）. Hpylori infection was defined at entry by histology and rapid urease test and cure of infection was determined by negative urea breath test. RESULTS： Hpylori eradication rates produced by B-OAzM and B-OAM were 74.1% and 70.4% respectively based on an intention to treat analysis, and 78.1% versus 75.7% respectively based on a per-protocol analysis. The incidence of poor compliance was lower, although not significantly so, in patients randomized to B-OAzM than for B-OAM （3.5% versus 4.3%） but intolerability was similar in the two groups （ 35% versus 33.3%）. CONCLUSION： 1-wk azithromycin based quadruple regimen achieves an Hpylori eradication rate comparable to that of standard 2-wk quadruple therapy, and is associated with comparable patient compliance and complications.展开更多
Raman spectroscopy has been proven a noninvasive technique with high potential in pharmaceutical industry. In this study, micro Raman technique and chemometric tools were used for identification of azithromycin (AZM) ...Raman spectroscopy has been proven a noninvasive technique with high potential in pharmaceutical industry. In this study, micro Raman technique and chemometric tools were used for identification of azithromycin (AZM) tablets by different manufacturers and quantitative analysis of the active pharmaceutical ingredient (API) in the samples. Support vector machine (SVM), Bayes classifier and K-nearest neighbour (KNN) were employed for identification, partial least squares (PLS) regression was used for quantitative determination, and interval partial least squares (iPLS) and Monte Carlo based uninformative variable elimination (MC-UVE) methods were used to select informative variables for improving the models. The results show that all the samples can be classified into groups by manufacturers with high accuracy, and the correlation coefficient between the predicted API concentrations and reference values is as high as 0.96. Therefore, micro Raman spectroscopy coupled with chemometrics may be a fast and powerful tool for identification and quantitative determination of pharmaceutical tablets.展开更多
Azithromycin loaded fumaryl diketopiperazine(FDKP)dry powder inhalation was designed and prepared for the treatment of community-acquired pneumonia.The solubility of FDKP and stability of azithromycin solution was inv...Azithromycin loaded fumaryl diketopiperazine(FDKP)dry powder inhalation was designed and prepared for the treatment of community-acquired pneumonia.The solubility of FDKP and stability of azithromycin solution was investigated.Formulation of azithromycin loaded FDKP microparticle was investigated and optimized by the single factor experiment.High-pressure homogenization and spray drying conditions were also optimized to prepare the particles by spray drying azithromycin dissolved FDKP microparticle suspension at pH 4.5.The in vitro antibacterial efficiency and in vitro dispersion performance was also investigated to confirm the antibacterial efficiency,dispersion and deposition behavers.FDKP/azithromycin mass ratio(3:2)was the optimized formulation of azithromycin loaded FDKP microparticle with the maximal drug loading efficiency.High-pressure homogenization and spray drying conditions were also optimized.The in vitro antibacterial results indicated that only with the antibiotic concentration higher than mutant prevention concentration could totally inhibit the reproduction of bacteria.In vitro dispersion performance of azithromycin loaded FDKP microparticles(AZM@FDKP-MPs)also shows remarkable improvement of dispersion and deposition behavers of AZM.AZM@FDKP-MPs dry powder inhalation as a targeting delivery route has better potential for lung infection treatment.展开更多
文摘The increased consumption of azithromycin during the COVID-19 pandemic may have led to its presence in the waterways. This study aims to evaluate the effect of this situation on aquatic bacteria. Methodology: Over a four-month period following the official recognition of the COVID-19 outbreak in Yaoundé, water samples were collected from four rivers selected on the basis of their vicinity to care centers for COVID-19. Bacteria within azithromycin’s spectrum of activity were isolated, and the antibiotic’s efficacy was tested against the most frequently isolated species. The influence of COVID-19 incidence and other external factors was also assessed. Results: The most frequently isolated bacteria were Bacillus spp., Enterococcus spp., Listeria spp. and Staphylococcus epidermidis. These strains exhibited varying levels of sensitivity to azithromycin, ranging from 0% to 100%. The observed resistance rates were 12.5%, 14.29%, 16.67%, and 0%, respectively. Neither COVID-19 incidence, proximity to hospitals, nor rainfall significantly influenced bacterial resistance rates to azithromycin (P > 0.05). These resistance levels may be attributed to the relatively short exposure of bacteria to azithromycin at the sampled locations, as well as the impact of agricultural and livestock-related chemicals, such as biocides and antibiotics, present in the watershed. Conclusion: These results highlight the need to integrate into anti-COVID-19 activities, the monitoring of bacteria’s sensitivity in aquatic environments.
文摘Introduction: The WHO recommends mass administration of azithromycin 30 mg/kg to eradicate yaws and 20 mg/kg to eliminate trachoma. We evaluated the effectiveness of azithromycin at 20 and 30 mg/Kg, and the number of cycles of mass administration on the treatment and interruption of yaws transmission in the Mbaïki health district in the Central African Republic. Methods: Following a yaws prevalence survey, azithromycin was administered as a mass treatment in four yaws endemic communities in the Mbaïki health district. Azithromycin 30 mg/kg was administered in one cycle in Kenengué and three cycles spaced three months apart in Bambou. In Kapou and Bangui-Bouchia, azithromycin was administered at a dose of 20 mg/kg in one cycle and three cycles, respectively, spaced three months apart. Before the mass treatment round, confirmed yaw cases were selected and followed for seven months. The primary endpoint was serological cure seven months after the first treatment cycle. Secondary endpoints were clinical cure at four weeks after the first treatment cycle and serological cure at four months after the first treatment cycle. A non-inferiority margin (∆) of 10% was used. Results: A total of 92 participants aged 1 to 90 years, including 52 men, were included in the study. The frequently encountered skin lesions were ulcers (65.22%) and were localized to the lower limbs (59.78%). Clinical cure was not obtained in Bangui-Bouchia and Kapou (∆ = 17.1% and 30.8%). Serological cure at four and seven months was not obtained in Kapou (∆ equal to 17.9% and 13.8% respectively). Conclusion: This study confirms the effectiveness of azithromycin 30 mg/kg in a single dose for the treatment of yaws. However, the study suggests that for yaws eradication programs, two to three cycles of mass administration of azithromycin at 20 or 30 mg/kg spaced three months apart, with therapeutic coverage greater than 90% are essential.
基金Supported by the Major Projects of National Science & Technology(2009ZX09313-027)
文摘3＇-N-demethylazithromycin is an impurity in azithromycin drug. It is derived by demethyl- ation of azithromycin, i. e. , azithromycin loses a methyl group on the 3＇-N position. In this study, bulk product was purified with chromatographic separation. It was observed that 3＇-N-demethylaz- ithromycin was also a precursor of other impurities. Simultaneously, another derivative was synthe- sized, i. e. , 3＇-N-demethyl-3＇-N-formylazithromycin. Reaction conditions were optimized with the HPLC method and good-quality and high-yield derivative product was achieved. The structures of de- rivatives were identified by 1H-NMR and MS.
基金National Science and Technology Major Project of the Ministry of Science and Technology of China (Grant No.2010ZX09401-403)
文摘A universal quantitative model was developed to determine the azithromycin content in granules using near infrared （NIR） diffuse reflectance spectroscopy. The diffuse reflection spectra were recorded with the integrating sphere at 8 cm-1 resolution in 4000–12 000 cm-1 spectral range. During each measurement, 32 co-added scans were performed. This quantitative model was constructed with 103 batches of azithromycin granules from 21 different manufacturers. The azithromycin content ranges from 3.0% to 24.5%. The root mean square error of prediction （RMSEP） of model was 0.613. In addition, the quantitative model was evaluated in terms of specificity, linearity, accuracy, and precision according to ICH guidelines. In conclusion, it is feasible to construct a universal quantitative model for azithromycin granules by choosing suitable training set samples and selecting an appropriate wavelength range. The quantitative model could be applied in the quick assay of azithromycin granules produced by domestic manufacturers （content： 3.0%–24.5%）.
文摘Aim In order to improve the solubility of azithromycin, the objectives of the present study were to screen an appropriate salt for azithromycin by comparing acute hepatic and renal toxicities in animals, and study the pharmacokinetics of final chosen azithromycin salt. Methods Various salts of azithromycin, such as glutamate, citrate, hydrochloride, sulphate, dihydrogen phosphate, lactobionate, tartrate, and aspartate were given intravenously to Sprague Dawley rats at a dose of 10 mg once daily for 14 consecutive days via tail vein. The acute hepatic and renal indicators were measured before and after administration. A pharmacokinetic study was performed on 12 healthy human volunteers. The subjects were equally divided into two groups by a randomized crossover design. Azithromycin glutamate injection was administered by intravenous infusion or intramuscular injection at a single dose of 500 mg, respectively. Azithromycin concentrations in plasma were determined by microbial inhibition zone assay, and the pharmacokinetic parameters were calculated using a practical pharmacokinetic software 3P87 program. Results Azithromycin glutamate was least toxic to the liver and kidney of the rats, thus being selected as a final salt for parenteral preparation of azithromycin. Pharmacokinetic results showed that the area under the plasma concentration-time curves （AUC0-120h） were 21.47 ± 1.57 h·μg·mL^-1 for intravenous infusion, and 19.36 ± 2.44 h·μg·mL^-1 for intramuscular injection. The absolute bioavailability of intramuscular injection was 92.59%. Conclusion Azithromycin glutamate is suitable for the future clinical application, and its pharmacokinetics is characterized in human volunteers in the present study.
基金Project (No. 2008BAI55B03) supported by the Key Project of the National Science and Technology Pillar Program, China
文摘A high-performance liquid chromatography （HPLC） system was used in the reversed phase mode for the determination ofbenzalkonium chloride （BKC） in azithromycin viscous ophthalmic drops. A Venusil-XBP（L）-C18 （150 mm×4.6 mm, 5 gm） column was used at 50℃. The mobile phase consisted of a mixture of methanol-potassium phosphate （16：5, v/v）. Two sample preparation methods were compared. The results suggested that, compared with an extraction procedure, a deproteinization procedure was much quicker and more convenient. Using the deproteinization procedure for sample preparation, calibration curves were linear in the range 5.0-50μg/ml. The within-day and inter-day coefficients of variation were less than 10%. The average recoveries were determined as 96.70%, 98.52%, and 97.96% at concentrations of 10.0, 30.0, and 50.0 μg/ml, respectively. Variability in precision did not exceed 5%. In conclusion, this HPLC method using a simple sample treatment procedure appears suitable for monitoring BKC content in azithromycin viscous ophthalmic drops.
文摘AIM： To evaluate whether adding azithromycin to firstline Helicobacter pylori （H pylorl） eradication improved eradication and reduced side effects. METHODS： Eligible articles were identified by searches of electronic databases. We included all randomized trials that compared azithromycin-containing with standard triple-therapy regimens for first-line treatment of H pylori infection. Statistical analysis was performed with Review Manager 5.0.10. Sub-analyses were also performed. RESULTS： We identified 14 randomized trials （1431 patients）. Pooled Hpylori eradication rates were 72.01% （95% CI： 58.09%-85.93%） and 69.78% （95% CI： 66.47%-73.09%） for patients with or without azithromycin by intention-to-treat analysis, and the odds ratio （OR） was 1.17 （95% CI： 0.64-2.14）. The occurrence of side effects differed significantly and was 15.81% （95% CI： 12.50%-19.12%） and 25.20% （95% CI： 21.44%-28.96%） for treatment with or without azithromycin, respectively, and the summary OR was 0.58 （95% CI： 0.41-0.82）. Furthermore, the azithromycin-containing group had a lower occurrence of diarrhea, nausea and taste disturbance. CONCLUSION： Our review suggests that azithromycincontaining triple-therapy regimens could be equally effective in eradication of Hpylori compared with standard first-line triple-therapy regimens.
文摘Azithromycin and Chinese medicine forsythia are often used together to treat pediatric mycoplasma infections in China. We aimed to investigate the pharmacokinetic interaction of Forsythia suspensa extract and azithromycin after single and co-intravenous administration in rats. Male Sprague-Dawley rats received single(Forsythia suspensa extract or azithromycin) treatment or co-administration of Forsythia suspensa extract and azithromycin. Blood samples were collected at scheduled times, and drug concentrations were determined by HPLC-UV or HPLC-MS/MS methods. Both non-compartmental analyses and nonlinear mixed-effects modeling approaches were applied to fit pharmacokinetic data and evaluate the impact of co-administration. Pharmacokinetic analysis showed that the area under the curve of azithromycin and forsythiaside increased, and clearance decreased significantly(P < 0.05),after co-administration. The in vivo behavior of both azithromycin and forsythiaside could be appropriately described by the two-compartmental model. The final population pharmacokinetic model indicated that co-administration decreased the central volume of azithromycin and forsythiaside clearance significantly. Co-administration of Forsythia suspensa extract and azithromycin significantly decreased the clearance and increased exposure for both drugs. Pharmacokinetic data suggest that drug co-administration may increase efficiency.
文摘AIM： To investigate eradication rates, patient compliance and tolerability of a 1-wk Azithromycin-based quadruple therapy versus the 2-wk conventional therapy. METHODS： A total of 129 Hpylori-positive patients were randomized to either omeprazole 20 mg, bismuth subcitrate 240 mg, azithromycin 250 mg, and metronidazole 500 mg, all twice daily for 1-wk （B-OAzM） or omeprazole 20 mg, bismuth subcitrate 240 mg, amoxicillin lg, and metronidazole 500 mg all twice daily for 2-wk （B-OAM）. Hpylori infection was defined at entry by histology and rapid urease test and cure of infection was determined by negative urea breath test. RESULTS： Hpylori eradication rates produced by B-OAzM and B-OAM were 74.1% and 70.4% respectively based on an intention to treat analysis, and 78.1% versus 75.7% respectively based on a per-protocol analysis. The incidence of poor compliance was lower, although not significantly so, in patients randomized to B-OAzM than for B-OAM （3.5% versus 4.3%） but intolerability was similar in the two groups （ 35% versus 33.3%）. CONCLUSION： 1-wk azithromycin based quadruple regimen achieves an Hpylori eradication rate comparable to that of standard 2-wk quadruple therapy, and is associated with comparable patient compliance and complications.
文摘Raman spectroscopy has been proven a noninvasive technique with high potential in pharmaceutical industry. In this study, micro Raman technique and chemometric tools were used for identification of azithromycin (AZM) tablets by different manufacturers and quantitative analysis of the active pharmaceutical ingredient (API) in the samples. Support vector machine (SVM), Bayes classifier and K-nearest neighbour (KNN) were employed for identification, partial least squares (PLS) regression was used for quantitative determination, and interval partial least squares (iPLS) and Monte Carlo based uninformative variable elimination (MC-UVE) methods were used to select informative variables for improving the models. The results show that all the samples can be classified into groups by manufacturers with high accuracy, and the correlation coefficient between the predicted API concentrations and reference values is as high as 0.96. Therefore, micro Raman spectroscopy coupled with chemometrics may be a fast and powerful tool for identification and quantitative determination of pharmaceutical tablets.
基金supported by the Ministry of Science and Technology of China(No.2017ZX09101001-005-003)the National Natural Science Foundation of China(Nos.81501579,81673364 and 81972892)+2 种基金the Natural Science Foundation of Jiangsu Province(No.BK20150702)the Science and Technology Development Fund of Nanjing Medical University(No.2016NJMU105)Project Fundedby the Priority Academic Program Development of Jiangsu Higher Education Institutions(No.KYCX170674)。
文摘Azithromycin loaded fumaryl diketopiperazine(FDKP)dry powder inhalation was designed and prepared for the treatment of community-acquired pneumonia.The solubility of FDKP and stability of azithromycin solution was investigated.Formulation of azithromycin loaded FDKP microparticle was investigated and optimized by the single factor experiment.High-pressure homogenization and spray drying conditions were also optimized to prepare the particles by spray drying azithromycin dissolved FDKP microparticle suspension at pH 4.5.The in vitro antibacterial efficiency and in vitro dispersion performance was also investigated to confirm the antibacterial efficiency,dispersion and deposition behavers.FDKP/azithromycin mass ratio(3:2)was the optimized formulation of azithromycin loaded FDKP microparticle with the maximal drug loading efficiency.High-pressure homogenization and spray drying conditions were also optimized.The in vitro antibacterial results indicated that only with the antibiotic concentration higher than mutant prevention concentration could totally inhibit the reproduction of bacteria.In vitro dispersion performance of azithromycin loaded FDKP microparticles(AZM@FDKP-MPs)also shows remarkable improvement of dispersion and deposition behavers of AZM.AZM@FDKP-MPs dry powder inhalation as a targeting delivery route has better potential for lung infection treatment.
