Effect of Roxithromycin on Airway Inflammation in Patients with Chronic Obstructive Pulmonary Disease at Stable Phase / 中国药师

Objective:To investigate the effect of roxithromycin on airway inflammation in chronic obstructive pulmonary disease ( COPD) patients at stable phase to provide evidence for the clinical diagnosis and treatment .Methods:Totally 46 cases of outpatients with stable COPD were divided into the observation group and the control group .The control group received the conventional treatment , while the observation group was treated with roxithromycin capsules 150mg.d-1 additionally, and the treatment course was 10 months. The sputum, serum cytokines γ-IFN, IL-8 and TNF-αlevels, sputum leukocyte , neutrophil count and adverse reactions were observed and compared between the groups .Results:After the 5-month treatment, the levels of γ-IFN, IL-8 and TNF-αcytokines in serum and sputum in the observation group were significantly lower than those before the treatment (P<0.05) and in the control group (P<0.05).After the 10-month treatment, the above indices in the observation were further decreased when compared with those after the 5-month treatment (P<0.05), which were notably lower than those in the control group (P<0.05).There was only one case of ad-verse drug reactions in the observation group , and the patient was out of the study .Conclusion:Long-term use of roxithromycin at low dose can reduce cytokines in serum and sputum and inflammatory cell count in sputum in stable COPD patients , which exhibits the effect on airway inflammation to some extent .

Pharmacokinetic comparison of roxithromycin under normoxic and hypoxic conditions in rats by UPLC/MS/MS / 中国药理学通报

Aim To study and compare the pharmaco-kinetic parameters of roxithromycin under normoxic and hypoxic rats. Methods A highly effective and rapid ultra-performance liquid chromatography with tandem mass spectrometry ( UPLC-MS/MS) method with posi-tive electrospray ionization source was successfully de-veloped and validated for quantification of roxithromy-cin in rat plasma. Sprague-Dawley rats were randomly divided into the hypoxia and normoxic groups. Each rat obtained a single dose of roxithromycin with 10 mg · kg-1 via intragastric administration. The pharmacoki-netic parameter comparison between normoxic and hy-poxic groups was calculated by SPSS software using in-dependent sample t test method. Results The main pharmacokinetic parameters of roxithromycin between the normoxic and hypoxic rats were:the AUC(0-t) 7 576 and 3 761 μg·h·L-1 , MRT(0-t) 5. 6 and 7. 7 h, T1/2 3. 4 h and 3. 9 h, CL 1. 5 and 3. 0 L · h-1 · kg-2 , tmax3. 1 and 3. 4 h, Cmax 1 116 and 372 μg·L-1 , re-spectively. The levels of Cmax and AUC of roxithromy-cin in hypoxic rats were statistically lower than those in normoxic rats. Conclusion The exposure level of rox-ithromycin in hypoxic rats markedly decreased. Our re-sults may provide an important experimental basis to adjust the dosage for roxithromycin in hypoxic clinical practice.

The effect of long term low dose roxithromycin on the chest CT imaging and clinical symptoms change of bronchiectasis stable patients / 中国生化药物杂志

Objective To explore the clinical effect and lung CT change of long-term used of low-dose roxithromycin in treatment for bronchial expansion patients in stable phase. Methods 94 cases collected in the Department of Respiration, The Second Hospital Affiliated to Suzhou University from February 2011 to December 2012 were diagnosed as bronchiectasis, 34 cases in control group were given oral treatment for ambroxol 30 mg, three times one day, 60 cases in treatment group were added roxithromycin 75 mg on basis of control group, two times one day. Patients in two groups were both treated for 6 months. The therapeutic effect and the score of life quality and dyspnea scores in two groups were observed, and the changes of CT data were compared before and after treatment. Results After treatment, the life quality score and dyspnea score of two groups were all improved, but the treatment group was signiifcantly higher than the control group (P<0.05). The effective rate in treatment group was 86.67%, which was signiifcantly higher than 70.59%in the control group (P<0.05). After treatment, chest CT imaging score of patients in treatment group were improved, signiifcantly better than that in the control group (P<0.05). Conclusion Long-term low dose administration of roxithromycin can control and stable bronchiectasis symptoms, and improve signs and symptoms .

Influence of treating with roxithromycin on airway inflammation in patients with asthma who smoke / 重庆医学

Objective To investigate the influence and effect of treating with low dose roxithromycin on airway inflammation in asthma who have been smoking patients .Methods Forty-six patients with mild to moderate asthma who had been smoking were assigned to group A and group B randomly .The patients in group A received inhaling salmeterol/fluticasone(50/250 μg) ,one puff bid ,2 times/day .The patients in group B treated with oral roxithromycin dispersible tablet 0 .15 g/d combining with inhaling salme-terol/fluticasone(50/250 μg) ,one puff bid ,2 times/day .The patients of two groups had been treated for 4 weeks .The lung func-tion ,cells and interleukin-8(IL-8) in induced sputum of patients in the two groups were measured before and after treatment .Results There was negative correlation between the FEV 1% and the number of eosinophile granulocyte ,neutrophil and the concentration of IL-8 in induced sputum of the patients(P<0 .01) .The number of neutrophil ,eosinophile granulocyte and the level of IL-8 of the patients in group B decreased more than those in the group A after 4 weeks of treatment(P<0 .05) .Furthermore the PEF and FEV1% of the patients in group B were ameliorated significantly than those in group A (P<0 .01) .Conclusion The treatment of roxithromycin combining with salmeterol/fluticasone on patients with asthma who smoke can not only reduce the number of eosino-phile granulocyte ,neutrophil and the level of IL-8 in induced sputum significantly ,but also ameliorate the PEF and FEV1% of them significantly .

The treatment effects by combinative supplementation of formoterol, indomethacin and roxithromycin on cancer cachexia mice / 肠外与肠内营养

Objective: To observe the effect of the combinative supplementation of Formoterol, Indomethacin and Roxithromycin on cancer cachexia (CC) and to study the mechanism. Methods: Male BALB/c mice bearing colon 26 adenocarcinoma for 9 days were served as models of cancer cachexia. The mice were divided into nine groups. Physiological conditions, body weight and food intake were documented every day. Serum levels of cytokine and nutritional markers were detected 7 days after treatment. Results: Tumor-bearing caused a wasting of non-tumor body weight and gastrocnemius muscle. Serum tumor necrosis factor-α, (TNF-α) and interleukin-6 (IL-6) levels were significantly elevated accompanied with nutrition depletion in tumor-bearing mice. After treatment with combinative supplementation of Formoterol, Indomethacin and Roxithromycin, left gastrocnemius weight and serum glucose were improved and the levels of TNF-α and triglyceride were down-regulated. Conclusion: Formoterol, Indomethacin and Roxithromycin had their own positive effects to CC mice. Drugs combinationin in tumor-bearing mice with cancer cachexia could produce synergistic action.

The protective effect of oral roxithromycin on lung function in chronic obstructive pulmonary disease / 中国医师进修杂志

Objective To evaluate the effect of oral roxithromyein on lung function in chronic obstructive pulmonary disease (COPD) and analyse the probable mechanism. Methods Fifty patients with COPD were divided randomly into treatment group (25 eases) and control group (25 eases). The control group was treated with base therapy, and the treatment group was treated with oral roxithromycin beside base therapy, 0.15 g, twice one day for one year. Then the changes of peripheral blood neutrophil and lung function was observed before and after treatment, and the times of acute exacerbation were statistically analyzed.Results There was significant difference in the changes of peripheral blood neutrophil in treatment group (P<0.05). The ratio of forced expiratory volume in one second and forced vital capacity (FEV_1/FVC),FEV_1% pred, peak expiratory flow, maximal vital volume had no obvious change in treatment group (P>0.05), but had obvious decrease in control group (P<0.05 ). There was significant difference in the changes of lung function in two groups(P<0.05 ). The times of acute exacerbation were 10(40%) in treatment group and 19 (76%) in control group, and the times of need to be in hospital were 6 (24%) and 13 (52%)respectively. There were significant difference (P<0.05). Conclusion Long-term oral roxithromyein can protect the lung function of COPD patients, the probable mechanism is that roxithromyein inhibit the neutrophil's function.

Roxithromycin Suppresses MUC5B/8 Mucin Genes and Mucin Production in Airway Epithelial Cells / 대한이비인후과학회지

BACKGROUND AND OBJECTIVES: Macrolide antibiotics are known to inhibit mucus hypersecretion in patients with chronic airway diseases, but its action mechanism is unclear. Several reports demonstrated that macrolides significantly inhibited gene expression of MUC2, MUC4 and MUC5AC in the airway epithelial cells, but little is known about its inhibitory effect for the other important airway mucins. In upper airway tracts, MUC5B and MUC8 are other important secreted mucin genes. Therefore, this study was aimed to investigate the effects of roxithromycin on the IL-1beta-induced gene expression and mucin production of MUC5B and MUC8 in NCI-H292 cells and cultured human nasal polyp epithelial cells. SUBJECTS AND METHOD: The effects of roxithromycin on the IL-1beta-induced MUC5B and MUC8 expression were analyzed by reverse transcription-polymerase chain reaction and enzyme-linked immunosorbent assay. RESULTS: Roxithromycin attenuated the IL-1beta-induced MUC5B and MUC8 gene expression and mucin production with a dose-dependent pattern in NCI-H292 epithelial cells and cultured human nasal polyp epithelial cells. CONCLUSION: Roxithromycin exerts direct inhibitory effects on the gene expression of MUC5B and MUC8 in airway epithelial cells. These novel findings may explain the clinical efficacy of 14-membered macrolides in the treatment of chronic airway inflammations.

Analysis of Uncertainty of Measurement in the Determination of Roxithromycin Dispersible Tablets by HPLC / 中国药房

OBJECTIVE: To find out the critical influential factors of measurement in the determination of Roxithromycin dispersible tablets. METHODS: Mathematic model of HPLC was established to analyze the effects of many uncertain factors on measurement results. Combined standard uncertainty and expanded standard uncertainty were calculated. RESULTS: The expanded uncertainty was 1.6% and the results of determination could be expressed as (96.8?1.6)%. CONCLUSION: The established analytical method is applicable to the uncertainty analysis in the content determination of Roxithromycin dispersible tablets by HPLC.

Effect of Ambroxol on Plasma Concentration and Pharmacokinetic Parameters of Roxithromycin / 中国药房

OBJECTIVE:To evaluate the effect of ambroxol on plasma concentration and pharmacokinetic parameters of roxithromycin when healthy volunteers received roxithromycin and ambroxol. METHODS: In double-period cross-over experiment, 24 healthy male volunteers received roxithromycin tablets or roxithromycin tablets combined with ambroxol tablets. Serial venous blood samples were collected at different time points after drug administration. Plasma concentrations of roxithromycin were measured by LC-MS. The pharmacokinetic parameters of roxithromycin were calculated and analyzed by variance analysis. Drug interaction was detected by 90% confidence interval. RESULTS: Main pharmacokinetic parameters of roxithromycin tablets and drug combination were as follows: tmax(1.67?0.32)h vs. (1.67?0.41)h; Cmax(10.26?2.82) mg?L-1 vs. (10.86?3.19) mg?L-1; AUC0～72(110.19?35.18) mg?h?L-1 vs. (113.42?38.72)mg?h?L-1; AUC0～∞(111.70?36.23) mg?h?L-1 vs. (115.04?39.98) mg?h?L-1. CONCLUSION:? Ambroxol has no effect on the plasma concentration and pharmacokinetics of roxithromycin in healthy volunteers.

Effect of Macrolide on the MUC4 Gene Expression in Human Airway Epithelial Cells / 대한이비인후과학회지

BACKGROUND AND OBJECTIVES: Mucin gene expression and mucin secretion are highly increased by inflammatory airway diseases such as asthma, chronic bronchitis and rhinosinusitis. Macrolide antibiotics is considered one of the effective drugs inhibiting mucus secretion for chronic bronchitis and rhinosinusitis with nasal polyp. However, the anti-secretory effect of macrolide is not clear. This study was designed to investigate whether macrolide can suppress interleukin-1beta (IL-1beta)-induced MUC4 gene expression and mucin secretion in the cultured human nasal polyp epithelial cells and NCI-H292 epithelial cells. SUBJECTS AND METHOD: Nasal polyps were obtained from 20 patients with chronic rhinosinusitis with nasal polyp during endoscopic sinus surgery. We observed the effect of roxithromycin on the IL-1beta-induced MUC4 gene and mucin secretion by reverse transcriptase-polymerase chain reaction (RT-PCR) with enzyme-linked immunosorbent assay (ELISA) method. RESULTS: Roxithromycin attenuated the IL-1beta-induced MUC4 mRNA expression and mucin secretion with a dose dependent pattern in both of the cultured human nasal polyp epithelial cells and NCI-H292 epithelial cells. CONCLUSION: This result suggests that roxithromycin may be considered as an effective anti-hypersecretory agent for its down-regulation of the MUC4 gene.

Bioequivalence of Roxithromycin Tablets in Healthy Volunteers / 中华医院感染学杂志

OBJECTIVE To study the relative bioequivalence of two sorts of domestic roxithromycin tablets. METHODS The randomized and crossover study was conducted in 18 healthy volunteers. After a single dose of the drugs given, their plasma drug concentration was determined by microbioassay. RESULTS Both the two sorts of domestic roxithromycin tablets were fitted to one compartment model. The main pharmacokinetic parameters of the tested and reference roxithromycin were as follows: C_ max (10.869?2.671) ?g/ml and (11.250?3.097)?g/ml; T_ max (1.7?0.8)h and (1.6?0.8) h; t_ 1/2 (13.407?2.391)h and (12.496?2.231) h; AUC_ 0-tn (127.097?32.971)?g?ml~ -1 ?h and (134.429?35.783) ?g?ml~ -1 ?h;AUC_ 0-∞ (136.556?33.958)?g?ml~ -1 ?h and (143.483? 38.052 ) ?g?ml~ -1? h; F_ 0-tn and F_ 0-∞ were (95.79?17.46)% and (96.58?16.66)%, respectively. CONCLUSIONS The results of analysis showed that the tested and reference formulations are bioequivalent.

Preparation and Quality Evaluation of Roxithromycin Microspheres / 中国药房

OBJECTIVE:To optimize the preparation technology of roxithromycin microspheres.METHODS:The microspheres of roxithromycin were prepared by the emulsion-solvent diffusion method with ethylcellulose used as capsule wall material.The preparation technology of microspheres was optimized by orthogonal experiment taking encapsulation efficiency as index with the ratio of roxithromycin to ethylcellulose(A),the concentration of ethylcellulose(B)and the ratio of water phase to oil phase(C)as factors.The appearance,particle diameter,drug-loading amount,encapsulation efficiency,in vitro release and bitter smell were studied.RESULTS:The optimal preparation conditions were as follows:A was 1∶1,B was 30 ?g?mL-1 and C was 4∶1.The microspheres obtained were round and well-distributed with mean diameter of 75.0～90.0 ?m,drug-loading amount of 45%～46%,encapsulation efficiency of over 90% and sustained release for over 13 hours.No bitter taste of the roxithromycin-ethylcellulose microspheres was felt by the majority of subjects.CONCLUSION:The roxithromycin microspheres made by optimization technology was bitter-masked and sustained release.

Study on Bioequiavailability in Human Body between Domestic and Imported Roxithromycin / 中国药房

OBJECTIVE:To study the bioequiavailability of domestic roxithromycin tablets and imported ones.METH?ODS:20male healthy volunteers took single dose of150mg roxithromycin tablet orally in a random crossover design,blood concentrations were determined by LC-MS.RESULTS:The main pharmacokinetic parameters of domestic and imported tablets were determined respectively as follows,AUC 0～72 were(72.81?23.85)(mg?n)/L and(72.63?20.86)(mg?h)/L,AUC 0～∞ were(74.41?24.45)(mg?h)/L and(74.42?24.45)(mg?h)/L,C max were(6.46?1.51)mg/L and(6.58?1.55)mg/L,t max were(1.9?0.5)h and(1.8?0.5)h,t 1/2 were(13.56?1.35)h and(14.18?1.50)h,the relative bioavailability of the homemade tablet to imported one was(99.8?11.2)%.CONCLUSIONS:Domestic and imported roxithromycin are bioequivalent.

Effects of roxithromycin on NF-?B activity and bronchial hyperresponsiveness of asthma rats / 中国临床药理学与治疗学

AIM: To investigate the effect of roxithromycin on the NF-?B activity,the airway inflammation and bronchial hyperresponsiveness of asthma rats.METHODS: Thirty male adult Sprague-Dawley rats were randomly divided into the control group(Group C,n=10),asthma group(Group A,n=10) and roxithromycin group(Group R,n=10).The asthma model was induced by ovalbumin and Al(OH)3.The airway reactivity was detected and then rats in each group were sacrificed after 24 hours for the last provocation.The concentrations of IL-4,IL-5 and IFN-? in bronchoalveolar lavage fluid(BALF) were measured by ELISA,and the activity of NF-?B protein in bronchial epithelium was detected by immunohistochemistry.RESULTS: Compared with Group C,the airway reactivity in Group A was increased(P

Roxithromycin inhibited airway inflammation through pathway of inducible nitric oxide synthase and nitric oxide in rat asthmatic model / 中国药理学通报

Aim To investigate the effect of roxithromycin on expression of inducible nitric oxide synthase (iNOS) and content of nitric oxide(NO) and cytokines(IL-4,IFN-?) in bronchiole epithelial cell of asthmatic rats.Methods Twenty four male Sprague-Dawley rats were randomly divided into three groups,namely control group,asthmatic group and roxithromycin group. The numbers of total cell and eosinophils cell in bronchoalveolar lavage fluid (BALF) were counted. The expression of inducible nitric oxide synthase was detected by immunohistochemistry method,and iNOS mRNA was detected by reverse transcription-lolymerse chain reaction (RT-PCR). The activity of iNOS and content of NO in lung homogenates were measured by spectrophotometry.The concentrations of IL-4 and IFN-? were detected by sandwich enzyme-linked immunosorbent assay (ELISA).Results The numbers of eosinophils cell and the ratios of eosinophils to total cell in BALF of asthmatic group[(7.28?1.65)?108?L-1,(7.73?1.54)%]were significantly higher than those of control group[(3.76?0.97)?108?L-1,(1.27?0.60)%],but those of roxithromycin group[(5.68?0.95)?108?L-1,(5.54?1.53)%]were lower compared with asthmatic group. The concentration of IL-4,activity of iNOS and content of NO in lung homogenates of asthmatic group were significantly higher than those of control group,while those of roxithromycin group were lower compared with asthmatic group. The concentration of IFN-? in lung homogenats of asthmatic group was significantly lower than that of control group,while that of roxithromycin group were higher compared with asthmatic group. The absorbance of iNOS protein expression in bronchiole epithelial cell and mRNA expression in lung homogenats of asthmatic group[(0.25?0.06),(0.52?0.14)]were markedly increased compared with control group[(0.14?0.05),(0.33?0.05)],while those of roxithromycin group[(0.15?0.03),(0.35?0.07)]were decreased compared with asthmatic group.Conclusions Roxithromycin can affect the concentrations of IL-4,IFN-? and the pathway of iNOS/NO in airway of asthma rat,through which inhibit asthmatic airway inflammation reaction.

Study of mutant prevention concentrations of macrolide-resistant Streptococcus pneumoniae / 第三军医大学学报

Objective To detect the mutant prevention concentration (MPC) of macrolide resistant Streptococcus pneumoniae, to amplify the resistance gene of Streptococcus pneumoniae mutants selected in the mutant selection window (MSW), and to investigate the mechanism in the resistance of Streptococcus pneumoniae to macrolides. Methods The Streptococcus pneumoniae strain ATCC49619 was enriched in broth, and the bacterial concentrations were adjusted to 1010 colony forming units per milliliter. The minimal inhibitory concentration (MIC), MIC for 99 % of input cells (MIC99), provisional MPC (MPCpr), and MPC of roxithromycin and azithromycin for Streptococcus pneumoniae were determined by agar plate dilution method. The ermB and mefA of Streptococcus pneumoniae mutants selected in the MSW were obtained by PCR method and sequencing. Results The MPCs of roxithromycin and azithromycin for ATCC49619 were 0.80 ?g/ml and 0.51 ?g/ml, and the MPC/MIC99 were 5.0 and 3.9. The ermB gene was detected in Streptococcus pneumoniae mutants selected in the MSW. Conclusion Adjustment of the drug dose may limit the enrichment of macrolide-resistant Streptococcus pneumoniae mutant. The mechanism in the resistance of Streptococcus pneumonia to macrolides may be associated with ermB genes carried.

Effect of Roxithromycin and Intranasal Fluticasone Spray in Reducing Symptoms of Chronic Sinusitis, Polyp Size and IL-4 in Allergic Patients

Nasal polyp is an intractable condition usually associated with chronic hyperplastic sinusitis with allergic rhinitis. IL-4 is known to contribute to the inflammatory reaction by enhancing binding of inflammatory cells in the nasal polyp. The objectives of this study were to evaluate the effect of roxithromycin (300 mg daily) and intranasal fluticasone spray (200 microgram daily ) in reducing symptoms of chronic sinusitis and polyp size and to compare pre - and post-treatment secretion of IL-4. Twenty-four patients with chronic sinusitis with nasal polyp and allergic rhinitis were selected and allocated into 3 groups ; roxythromycin, fluticasone propionate and combined use group. Statistically significant decrease in symptoms was observed in both the roxythromycin and fluticasone propionate groups. Significant improvement of rhinorrhea and postnasal drip was observed in the combined use group. The polyp size decreased significantly in all three groups. IL-4 secretion decreased significantly in the combined use group after treatment. Long term medication of roxithromycin and intranasal fluticasone spray were effective in reducing symptoms and polyp size in chronic sinusitis with allergic rhinitis. They were also effective in reducing IL-4.

Determination of Roxithromycin by Liquid Chromatography/Mass Spectrometry after Multiple-Dose Oral Administration in Broilers

A highly sensitive and specific method for the determination of roxithromycin in broiler tissues by LC/MS was developed and validated. A dichloromethane extract of the sample was separated on C18 reversed-phase column with acetonitrile-50 mM ammonium acetate (80:20, v/v) as the mobile phase and analyzed by LC/MS via atmospheric pressure ionization/electrospray ionization interface. The limit of detection and limit of quantitation were 1 ng/g and 5 ng/g. The method has been successfully applied to determine for roxithromycin in various tissues of broilers. Residue concentrations were associated with administered dose. At the termination of treatment, roxithromycin was found in all collected samples for both dose groups. Liver was detected to have the highest residual concentration of roxithromycin. Residue concentrations of roxithromycin were lower than its LOQ in all tissues from both dose groups 10 days after the treatment of roxithromycin mixed with drinking water at a dose rate of 15 mg/L or 60 mg/L to each broiler for 7 days.

Roxithromycin Treatment of Tsutsugamushi Disease (Scrub Typhus) in Children

PURPOSE: Although chloramphenicol and doxycycline have been used for the treatment of tsutsugamuchi disease, a difficulty exists in determining which drugs to use in treating children because of potential complications such as aplastic anemia or teeth discoloration. We evaluated the effect of roxithromycin, a macrolide antibiotic, on tsutsugamushi disease in children. METHODS: A retrospective analysis was conducted on 39 children with tsutsugamuchi disease(scrub typhus) who were treated with doxycycline(DC), chloramphenicol(CM), or roxythromycin(RM) between 1991 and 2000. We divided the patients into a DC-treated group(DC group; 16 children), a CM-treated group(CM group; 14 children), and RM-treated group(RM group; 9 children) and compared these groups. RESULTS: Most cases(97%) developed in October and November. Fever and rash were observed in all 39 cases and an eschar was noted in 36 cases(92%). No statistical differences could be found between the three groups in mean age, duration of fever before admission, white blood cell(WBC) count, and complications including abnormal liver enzymes. In most cases defervescence after treatment was within 24 hours(34 cases, 87%), and during 24-48 hours in two cases in the DC group, one in the CM group, and two in the RM group(no statistical difference). CONCLUSION: Roxythromycin was as effective as conventional doxycycline or chloramphenicol, in children with scrub typhus and may be safer to use.

Effect of Macrolides on the Interleukin-1beta-mediated MUC2/5AC Genes Expression and Mucin Secretion in Human Airway Epithelial Cells

BACKGROUND AND OBJECTIVES: Macrolide is a relatively effective drug in chronic bronchiolitis and chronic sinusitis with mucous hypersecretion. However, the anti-secretory effect of macrolide is not clear. The aim of this study was to evaluate the effect of macrolide on the interleukin -1beta (IL-1beta)-induced MUC2/5AC genes expression and mucin secretion. Matrials and Methods: We observed effects of roxithromycin and clarithromycin on the IL-1beta-induced MUC2/5AC genes expression and mucin secretion in cultured human airway NCI-H292 epithelial cells. The steady state mRNA levels of MUC2/5AC and mucin secretion were determined by reverse transcriptase-polymerase chain reaction (RT-PCR) and enzyme-linked immunosorbent assay. RESULTS: Roxithromycin attenuated the IL-1beta-mediated MUC2/5AC genes expression and mucin secretion. When roxithromycin treated before exposure to IL-1beta and after exposure to IL-1beta in cultured cells, both treatment methods inhibited the IL-1beta-induced MUC2/5AC genes expression and mucin secretion. However, clarithromycin did not suppress the IL-1beta-mediated MUC2/5AC genes expression and mucin secretion. CONCLUSION: This result suggests that roxithromycin inhibits the IL-1beta-mediated mucin secretion through inhibition of MUC2/5AC genes expression.