BACKGROUND Mucosal healing has become an important goal of Crohn’s disease(CD)treat-ments.Modulen,enriched with transforming growth factor-beta 2,and budeso-nide are commonly accepted treatments for mild-moderate CD....BACKGROUND Mucosal healing has become an important goal of Crohn’s disease(CD)treat-ments.Modulen,enriched with transforming growth factor-beta 2,and budeso-nide are commonly accepted treatments for mild-moderate CD.However,their effects on the small bowel(SB)mucosa remain underexplored.AIM To prospectively assess clinical and mucosal responses to Modulen vs budesonide in adults with CD,using SB capsule endoscopy.METHODS Thirty patients were divided into two groups:Modulen+home-based diet(21 patients)and budesonide(9 patients)for an eight-week intervention followed by four weeks of follow-up.Clinical,laboratory,and endoscopic responses were evaluated.The mucosal changes were assessed through SB capsule endoscopy.RESULTS Results indicated significant clinical improvement in the Modulen group with reduced CD activity index(P=0.041)and improved inflammatory bowel disease questionnaire score(P=0.016).Moreover,Modulen was associated with a signifi-cant SB mucosal improvement,evidenced by a decrease in Lewis score(P=0.027).No significant changes were observed in calprotectin or other laboratory parame-ters.Conversely,budesonide exhibited more modest clinical effects,but it improved calprotectin,hemoglobin,and C-reactive protein levels(P=0.051,P=0.014,and P=0.038,respectively).The capsule endoscopy did not reveal a significant mucosal response in the budesonide group.CONCLUSION Both interventions have a role in CD treatment.Yet,their effects differ and may complement each other:Modulen yields clinical and mucosal improvements,while budesonide primarily leads mainly to laboratory improvements.展开更多
This study explores the clinical efficacy of budesonide combined with ambroxol inhalation therapy for neonatal pneumonia.A total of 68 neonatal pneumonia patients treated at Li County Hospital from January 2023 to Dec...This study explores the clinical efficacy of budesonide combined with ambroxol inhalation therapy for neonatal pneumonia.A total of 68 neonatal pneumonia patients treated at Li County Hospital from January 2023 to December 2024 were randomly divided into a monotherapy group and a combination group,with 34 patients in each.The monotherapy group received ambroxol inhalation therapy,while the combination group received budesonide inhalation therapy in addition to ambroxol.The recovery progress,blood gas analysis indicators,inflammatory response improvement,and overall clinical efficacy were compared between the two groups.Results showed that the combination group experienced a significantly shorter time for body temperature normalization(3.36±0.58 days vs.4.59±0.45 days),oxygen inhalation duration(4.89±0.57min vs.6.96±0.79min),disappearance of shortness of breath and cough(4.56±0.29 days vs.6.63±0.75 days),and resolution of lung wet rales(5.62±1.46 days vs.7.92±1.28 days)compared to the monotherapy group(P<0.05).Additionally,the total effective rate was significantly higher in the combination group(97.06%)than in the monotherapy group(73.52%)(P<0.05).Post-treatment,the combination group exhibited significantly better blood gas analysis and inflammatory response indicators(P<0.05).These findings suggest that budesonide combined with ambroxol inhalation therapy can effectively improve blood oxygen saturation,reduce inflammation,promote faster recovery,and enhance overall clinical efficacy,making it a reliable treatment option for neonatal pneumonia.展开更多
This article explores the significant implications of the study by Ovadia et al,which innovatively compares the efficacy of a nutritional intervention(Modulen)to conventional pharmaceutical therapy(budesonide)in promo...This article explores the significant implications of the study by Ovadia et al,which innovatively compares the efficacy of a nutritional intervention(Modulen)to conventional pharmaceutical therapy(budesonide)in promoting mucosal healing in Crohn’s disease.Highlighting the paradox of a well-established yet underutilized nutritional approach,the findings suggest that Modulen may offer comparable therapeutic benefits despite its high withdrawal rate due to adherence challenges.This advancement underscores the evolving paradigm in inflammatory bowel disease treatment,shifting focus toward non-pharmacologic alternatives that target both clinical remission and endoscopic healing.The article advocates for the development of integrative treatment strategies that balance efficacy,patient adherence,and long-term disease management,emphasizing the need for further research to refine and optimize the role of nutritional therapies in clinical practice.展开更多
BACKGROUND Respiratory viruses are increasingly detected in children with communityacquired pneumonia.Further strategies to limit antibiotic use in children with viral pneumonia are warranted.AIM To explore clinical e...BACKGROUND Respiratory viruses are increasingly detected in children with communityacquired pneumonia.Further strategies to limit antibiotic use in children with viral pneumonia are warranted.AIM To explore clinical efficacy of budesonide/formoterol inhalation powder for viral pneumonia in children and its impact on cellular immunity and inflammatory factor production.METHODS A total of 60 children with viral pneumonia were recruited:30 receiving budesonide/formoterol inhalation powder and 30 conventional symptomatic treatment.Outcome measures included peripheral blood levels of inflammatory cytokines,CD4^(+),CD8^(+),Th1,Th2,Th17 and Treg,clinical efficacy,and incidence of adverse reactions.RESULTS Compared with the control group,the observation group showed a significant reduction in interleukin-6 and high-sensitivity C-reactive protein levels after treatment.Compared with the control group,the observation group showed a significant increase in CD4^(+)/CD8^(+)and Th1/Th2 levels,and a decrease in Th17/Treg levels after treatment.The total effective rates in the observation group and the control group were 93.75%and 85.00%,respectively,which was a significant difference(P=0.003).CONCLUSION Budesonide/formoterol inhalation powder significantly improved therapeutic efficacy for viral pneumonia in children.The mechanism of action may be related to downregulation of the inflammatory response and improved cellular immune function.展开更多
Objective:To investigate the effects of budesonide on blood gas and inflammation indexes in patients with chronic obstructive pulmonary disease(COPD)during remission.Methods:Fifty-one patients with COPD in remission,a...Objective:To investigate the effects of budesonide on blood gas and inflammation indexes in patients with chronic obstructive pulmonary disease(COPD)during remission.Methods:Fifty-one patients with COPD in remission,admitted to Zhongshan Hospital of Dalian University from July 2021 to December 2022,were selected and divided into two groups based on a randomized numerical table method.The control group(25 cases)received budesonide formoterol treatment,while the observation group(26 cases)received budesonide geforce treatment.Various indexes,including clinical efficacy,blood gas indexes,inflammation indexes,St.George’s Respiratory Questionnaire(SGRQ)scores,Chronic Obstructive Pulmonary Disease Assessment Test(CAT)scores,and 6-minute Walking Distance Test(6MWD)results,were compared between the two groups.Results:After 21 days of treatment,the total clinical effectiveness rate of the observation group was higher than that of the control group,with a statistically significant difference(P<0.05).Post-treatment,the PaO2 level and pH value in both groups were higher,and the PaCO_(2) level was lower compared to pre-treatment levels.The observation group showed better improvements in these indicators than the control group,with statistically significant differences(P<0.05).SGRQ and CAT scores for both groups were lower post-treatment,with the observation group scoring lower than the control group.Additionally,the 6MWD results were farther for both groups post-treatment,with the observation group achieving greater distances than the control group,with statistically significant differences(P<0.05).Conclusion:Budesonide can effectively improve blood gas indexes in patients with COPD in remission,alleviate related clinical symptoms,reduce inflammatory responses,and promote patient recovery.The treatment efficacy is significant.展开更多
Objective:To analyze the clinical efficacy of tiotropium bromide(TB)combined with budesonide formoterol(BUD/FM)inhalation in treating chronic obstructive pulmonary disease(COPD).Methods:62 COPD patients admitted to th...Objective:To analyze the clinical efficacy of tiotropium bromide(TB)combined with budesonide formoterol(BUD/FM)inhalation in treating chronic obstructive pulmonary disease(COPD).Methods:62 COPD patients admitted to the hospital between June 2020 and December 2022 were selected as samples for this study.The patients were divided into a combination group and a conventional group using the random number table method,with 31 cases in each group.The patients in the combination group were treated with TB combined with BUD/FM inhalation,whereas the patients in the conventional group were treated with BUD/FM inhalation only.The treatment efficacy and changes in lung function indicators of both groups were compared.Results:The total efficacy of treatment in the combined group was higher than that in the conventional group,and the difference was statistically significant(P<0.05).Before treatment,there was no difference in pulmonary function indicators between the two groups(P>0.05).After three months of treatment,all lung function indicators of the combined group were higher than those of the conventional group,and the difference was statistically significant(P<0.05).Conclusion:Combining TB with BUD/FM inhalation therapy increases the efficacy of treatment for patients with COPD.Besides,it also improves lung function and leads to a better prognosis.展开更多
Objective: To analyze the clinical effect of terbutaline combined with budesonide in the treatment of chronic obstructive pulmonary disease. Methods: 500 cases of patients with chronic obstructive pulmonary disease ad...Objective: To analyze the clinical effect of terbutaline combined with budesonide in the treatment of chronic obstructive pulmonary disease. Methods: 500 cases of patients with chronic obstructive pulmonary disease admitted to the hospital from January 2022 to December 2023 were selected and divided into 250 cases in the control group and 250 cases in the observation group by randomization method, both groups received conventional symptomatic treatment, with budesonide added to the control group and terbutaline and budesonide to the observation group, and the lung function indexes, therapeutic effects and adverse drug reactions before and after treatment were compared. Results: After treatment, the level of all lung function indexes of patients in the observation group was higher than that of the control group, and the level of total effective rate of treatment was 96.40%, which was higher than that of the control group (P < 0.05), and the difference in the incidence rate of adverse reactions between the two groups was not strong (P > 0.05). Conclusion: In the clinical treatment of chronic obstructive pulmonary disease, the combined use of terbutaline and budesonide can positively improve lung function, with precise effects and few adverse reactions.展开更多
Budesonide is a corticosteroid used for the treatment of asthma via various matrices and inhalation mechanisms. An unknown peak of Budesonide aqueous formulation has been investigated during stability study wherein th...Budesonide is a corticosteroid used for the treatment of asthma via various matrices and inhalation mechanisms. An unknown peak of Budesonide aqueous formulation has been investigated during stability study wherein the impurity level observed around 0.1% well below the threshold 0.5%. The approach to identify anonymous species was adopted as first to generate the impurity in sample, isolate, enrich and was subjected to LC-MS/MS and NMR for spectral studies. Based on the spectral data the anonymous species were identified as a “Lumibudesonide’’ ((5aR,5bS,5cS,6S,7aS,7bS,10aR,11aS,11bS)-6-hydroxy-7b-(2-hydroxyacetyl)-5b,7a-dimethyl-9-propyl 1,5a,5b,5c,6,7,7a,7b,10a,11,11a,11b dodecahydrocyclopenta[2'',3'']cyclopropa [1'',2'':3', 4']benzo [1',2':4,5]indeno [1,2-d][1,3]dioxol-5(2H)-one), which is observed in photolysis of Budesonide.展开更多
To increase the solubility and adsorption of budesonide（BUD）,budesonide-loaded solid lipid nanoparticles（BUD-SLNs） were prepared and characterized in this study.Glycerin monostearate（GMS）was selected to be the m...To increase the solubility and adsorption of budesonide（BUD）,budesonide-loaded solid lipid nanoparticles（BUD-SLNs） were prepared and characterized in this study.Glycerin monostearate（GMS）was selected to be the matrix lipid material after calculation the differences of partial solubility parameters.An emulsification-ultrasound diffusion method was employed and formula was optimized in the BUD-SLNs preparation.The entrapment efficiency（ee%）of BUD-SLNs was（97.77±2.60）%, and the mean particle size was 147.3 nm（PDI=0.228）.Uniform and sphere particles were observed under TEM.The in vitro release of BUD-SLNs could be well explained by the biphasic release dynamics equation.The spectrums of DSC and X-ray diffraction indicated that BUD molecules were dispersed mainly into the lipids to form homogeneous matrix structure.Our results provide fundamental data for the application of SLNs in pulmonary delivery system.展开更多
Objective: the experiment will implement different treatment plans for patients with moderate and severe bronchial asthma, and further compare the clinical efficacy of budesonide and formoterol powder inhalation and b...Objective: the experiment will implement different treatment plans for patients with moderate and severe bronchial asthma, and further compare the clinical efficacy of budesonide and formoterol powder inhalation and budesonide suspension atomization inhalation. Methods: 100 patients with moderate to severe bronchial asthma admitted to our hospital were randomly selected as the subjects of this study. The diagnosis and treatment time range was from July 2020 to August 2021, and they were divided into groups by random design. The control group received budesonide suspension inhalation, while the observation group received budesonide formoterol powder inhalation, and the situation after four weeks of treatment was compared. Results: from the perspective of nursing quality, the lung function indexes of patients in the observation group were better than those in the control group. After treatment, FEV1 and FEV1/FVC in the observation group were (1.69±0.26) L and (65.77±0.28) %, respectively, while those in the control group were (1.13±0.19) L and (56.92±0.17) %. The comparison was statistically significant (P < 0.05). At the same time, the negative rate of bronchial dilation test in the observation group was higher than that in the control group (76.0% and 56.0%, respectively), and the difference was statistically significant. In addition, we compared the asthma control scores of patients before and after treatment, and the scores of the observation group were more advantageous after treatment, indicating that asthma symptoms were better controlled. Finally, the incidence of adverse reactions in patients was compared. There was no significant difference between the two groups, and both groups had safety guarantee. Conclusion: inhalation of Budesonide formoterol powder in the treatment of moderate and severe bronchial asthma has good efficacy, can improve the lung function index of patients, strengthen the control of asthma symptoms, and has the value of clinical promotion.展开更多
AIM： Prednisone and azathioprine represent the standard treatment for autoimmune hepatitis （AIH）. However, only 65% of the patients enter complete histological remission. Recently, budesonide （BUD） was reported t...AIM： Prednisone and azathioprine represent the standard treatment for autoimmune hepatitis （AIH）. However, only 65% of the patients enter complete histological remission. Recently, budesonide （BUD） was reported to be a promising alternative. In this study we assessed the efficacy and safety of BUD in AIH. METHODS： Eighteen patients （12 women, 6 men; mean age 45.4±21 years） with AIH were treated with BUD （Budenofalk） 3 mg thrice daily and followed up for at least 24 wk. Seven patients also had features of primary biliary cirrhosis （n = 5） or primary sclerosing cholangitis （n = 2）. Advanced liver fibrosis or cirrhosis was present in RESULTS： Fifteen （83%） patients had a complete clinical and biochemical remission. Ten patients, including five with acute hepatitis, were given BUD as first-line therapy, of which seven enter remission. Three patients, two with liver cirrhosis, did not improve. All patients with second-line therapy experienced long-term remission. A histological remission was also seen in three patients. Clinically relevant BUD-induced side effects were recorded only in patients with liver cirrhosis （n = 4）. CONCLUSION： BUD is effective in remission induction in the majority of our patients with AIH. Side effects and treatment failure was mainly observed in patients with liver cirrhosis.展开更多
AIM:To investigate the systemic availability of budesonide in a patient with Child A cirrhosis due to autoimmune hepatitis (AIH) and primary hepatocellular carcinoma,who developed serious side effects. METHODS:Serum l...AIM:To investigate the systemic availability of budesonide in a patient with Child A cirrhosis due to autoimmune hepatitis (AIH) and primary hepatocellular carcinoma,who developed serious side effects. METHODS:Serum levels of budesonide,6β-OH-budesonide and 16α-OH-prednisolon were measured by HPLC/MS/MS; portosystemic shunt-index (SI) was determined by 99mTc nuclear imaging.All values were compared with a matched control patient without side effects. RESULTS:Serum levels of budesonide were 13-fold increased in the index patient.The ratio between serum levels of the metabolites 6β-OH-budesonide and 16α-OH- prednisolone,respectively,and serum levels of budesonide was diminished (1.0 vs.4.0 for 6β-OH-budesonide,4.2 vs. 10.7 for 16α-OH-prednisolone).Both patients had portosystemic SI (5.7 % and 3.1%) within the range of healthy subjects.CONCLUSION:Serum levels of budesonide Vary uP to 13-fold in AIH Patients with Child A eirrhosis in the absenee ofrelevant Portosystemic shunting.Redueed hePatiemetabolism,as indicated by redueed metabolite-to-drugratio,rather than Portosystemie shunting may explainsystemic side effects of this drug in cirrhosis展开更多
Eosinophilic cholangitis is a rare cause of deranged obstructive liver function tests. It has been described as a great mimicker for malignant biliary strictures and bile duct obstruction. There are only case reports ...Eosinophilic cholangitis is a rare cause of deranged obstructive liver function tests. It has been described as a great mimicker for malignant biliary strictures and bile duct obstruction. There are only case reports available on treatment experience for eosinophilic cholangitis. A large proportion of patients present with biliary strictures for which they have undergone surgery or endoscopic treatment and a small proportion was given systemic corticosteroid. We share our treatment experience using budesonide which has fewer systemic side effects to prednisolone and avoids invasive management.展开更多
Large Hollow nanoparticulate aggregates（LHNAs） based on albumin nanoparticles is a promising technology for developing dry powder inhaler（DPI） with good aerodynamic properties in order to provide a new drug delive...Large Hollow nanoparticulate aggregates（LHNAs） based on albumin nanoparticles is a promising technology for developing dry powder inhaler（DPI） with good aerodynamic properties in order to provide a new drug delivery system（DDS） for the treatment of lung disease. Improved understanding of molecular interactions could lead to prepare the DDS rationally. Therefore, this investigation utilized computations and experiments to reveal the mechanisms of budesonide（BUD） interactions with bovine serum albumin（BSA） at the molecular level. The molecular dynamics（MD） simulation revealed that there were three critical stable binding sites of BUD on BSA（P1, P2, P3） mainly by hydrophobic interaction and hydrogen bond. The energy decomposition of each residue to the whole BUD-BSA complex system in P1-P3 showed that nonpolar residues in or around the binding site played an important role in the binding of BUD to BSA. The molar ratio was close to 3 in preparations in drug-loading efficiency experiment, which was confirmed to the simulation results. The details of the binding sites from computation provided a guideline for the design of the BSA nanoparticles carrying BUD, which was prepared successfully at last. Combination of the MD simulation and experiment as well as the mechanism of the molecular interaction provided a solid theoretical basis for the preparation of BSA-LHNAs for DPI in the future.展开更多
Purpose: Since intravesically administered steroid therapy may treat bladder pain syndrome/interstitial cystitis (BPS/IC) with fewer side effects than the current treatment of orally administered steroids, we investig...Purpose: Since intravesically administered steroid therapy may treat bladder pain syndrome/interstitial cystitis (BPS/IC) with fewer side effects than the current treatment of orally administered steroids, we investigated whether the intravesical infusion of budesonide foam can effectively treat BPS/IC symptoms in a rat model of tranilast-induced BPS/IC. Methods: There were 6 rat treatment groups (n = 8 per group): control + single or daily saline infusion, tranilast + single or daily saline infusion, and tranilast + single or daily budesonide infusion. All groups except for the controls were fed a tranilast supplemented diet for 5 weeks. Budesonide and saline were infused intravesically. After the BPS/IC rat model underwent single infusion treatments, we measured the paw pain threshold using the von Frey test and continuous cystometry was taken. After two weeks of daily intravesical infusions, we measured locomotor activity and serum cortisol levels;harvested bladders underwent histological analysis. Results: Both pain threshold and locomotor activity were significantly lower in the saline-infused groups receiving the tranilast diet, but there were no differences between the budesonide-infused groups and the controls. The interval between bladder contractions was significantly shorter in the tranilast group than the control or tranilast + budesonide infusion groups. The serum cortisol levels did not change. Hematoxylin-Eosin stainings of the bladder showed thickening of the bladder muscle layer and mucosal edema in the tranilast group, while the tranilast + budesonide infusion group showed only mild changes. Conclusion: Intravesical infusion of budesonide effectively treated BPS/IC symptoms in a rat model of BPS/IC.展开更多
Objective:To study the influence of budesonide and salbutamol atomization inhalation on Th17/Treg balance in patients with bronchial asthma and its correlation with airway remodeling.Methods:A total of 90 patients wit...Objective:To study the influence of budesonide and salbutamol atomization inhalation on Th17/Treg balance in patients with bronchial asthma and its correlation with airway remodeling.Methods:A total of 90 patients with bronchial asthma who received systemic treatment in our hospital between July 2013 and April 2016 were divided into control group (n=45) and observation group (n=45) according to random number table. Patients in the control group were treated with salbutamol atomization inhalation alone while those in observation group were treated with budesonide and salbutamol atomization inhalation. The Th17/Treg ratio in peripheral blood as well as serum contents of airway remodeling-related indicators was compared between two groups before and after treatment. The correlation between Th17/Treg balance and airway remodeling in patients with bronchial asthma was detected by Pearson test. Results:Before treatment, the differences in peripheral blood Th17/Treg ratio as well as serum contents of inflammatory mediators, growth factor indexes and collagen metabolism indexes were not statistically significant between two groups of patients. After treatment, peripheral blood Th17/Treg ratio in observation group was lower than that in control group, serum CRP, IL-8, IL-13 and TNF- contents in observation group were lower than those in control group, serum PDGF-BB, b-FGF and VEGF contents in observation group were lower than those in control group, and serum HA, PCⅢ and LN contents in observation group were lower than those in control group. The Th17/Treg ratio in patients with bronchial asthma after treatment was positively correlated with the levels of airway remodeling-related indexes.Conclusion:Budesonide combined with salbutamol atomization inhalation can optimize the Th17/Treg balance in patients with bronchial asthma, and Th17/Treg is directly correlated to the degree of airway remodeling.展开更多
Objective: To investigate the effects of montelukast sodium combined with budesonide on pulmonary function, inflammatory factors and immunoglobulin in children with asthma. Methods: A total of 100 children with asthma...Objective: To investigate the effects of montelukast sodium combined with budesonide on pulmonary function, inflammatory factors and immunoglobulin in children with asthma. Methods: A total of 100 children with asthma treated in our hospital from May 2013 to November 2016 were randomly divided into control group and observation group. In the control group, budesonide inhalation therapy was given. On the basis of the control group, montelukast sodium treatment was given, pulmonary function, inflammatory factors and immunoglobulin levels in the two groups before and after treatment were measured. Results:Compared with before treatment, the levels of FEV1%, FEF50%, FEF25% and PEF% in the two groups were significantly increased, those in the observation group were higher than in control group;compared with before treatment, IL-10 levels were significantly increased, TNF-α and IL-8 levels were significantly decreased in the two groups after treatment, moreover those in the observation group IL-10 levels were significantly higher than the control group, TNF-α and IL-8 were significantly lower than those in the control group, the difference was statistically significant;Compared with before treatment, IgA and IgM levels were significantly increased in both groups after treatment, IgE levels were significantly decreased, and IgA and IgM levels in the observation group were significantly higher than in the control group, IgE levels were significantly lower than the control group, the difference was statistically. Conclusion: Montelukast sodium combined with budesonide can effectively reduce the inflammation level of children with asthma, improve lung function, enhance immunity, the effect is significant, it is worth further clinical application.展开更多
Objective: To study the effects of oral cetirizine combined with budesonide inhalation on immune inflammatory response in children with acute asthma attack. Methods: Children with acute asthma attack who were treated ...Objective: To study the effects of oral cetirizine combined with budesonide inhalation on immune inflammatory response in children with acute asthma attack. Methods: Children with acute asthma attack who were treated in Beijing Luhe Hospital Affiliated to Capital Medical University between April 2014 and February 2017 were selected and randomly divided into two groups, observation group received oral cetirizine combined with budesonide inhalation therapy, and control group received budesonide inhalation therapy. The contents of CD4+T cell subsets and the expression of immune transcription factors in peripheral blood as well as the contents of CD4+T cytokines and inflammatory mediators in serum were measured after 1 week of treatment. Results: After 1 week of treatment, Th1 and Treg contents as well as BCL11B, STAT4 and SOCS3 mRNA expression in peripheral blood as well as IFN-γand IL-10 contents in serum of observation group were greatly higher than those of control group while Th2, Th17 and Th22 contents as well as STAT1 and STAT3 mRNA expression in peripheral blood as well as IL-4, IL-17, IL-22, HMGB1, Periostin, Eotaxin and ADAM33 contents in serum were greatly lower than those of control group. Conclusion: Oral cetirizine combined with budesonide inhalation is more effective than budesonide inhalation alone to modulate the immune inflammatory response in children with acute asthma attack.展开更多
This study aims to understand the absorption patterns of three different kinds of inhaled formulations via in silico modeling using budesonide(BUD)as a model drug.The formulations investigated in this study are:(i)com...This study aims to understand the absorption patterns of three different kinds of inhaled formulations via in silico modeling using budesonide(BUD)as a model drug.The formulations investigated in this study are:(i)commercially available micronized BUD mixed with lactose(BUD-PT),(ii)BUD nanocrystal suspension(BUD-NC),(iii)BUD nanocrystals embedded hyaluronic acid microparticles(BUD-NEM).The deposition patterns of the three inhaled formulations in the rats’lungs were determined in vivo and in silico predicted,which were used as inputs in GastroPlus TM software to predict drug absorption following aerosolization of the tested formulations.BUD pharmacokinetics,estimated based on intravenous data in rats,was used to establish a drug-specific in silico absorption model.The BUD-specific in silico model revealed that drug pulmonary solubility and absorption rate constant were the key factors affecting pulmonary absorption of BUD-NC and BUD-NEM,respectively.In the case of BUD-PT,the in silico model revealed significant gastrointestinal absorption of BUD,which could be overlooked by traditional in vivo experimental observation.This study demonstrated that in vitro-in vivo-in silico approach was able to identify the key factors that influence the absorption of different inhaled formulations,which may facilitate the development of orally inhaled formulations with different drug release/absorption rates.展开更多
Budesonide is a highly potent synthetic, nonhalogenated corticosteroid. The mechanism of action of corticosteroids in allergic rhinitis remains unknown, but may involve reductions in number of various mediator cells s...Budesonide is a highly potent synthetic, nonhalogenated corticosteroid. The mechanism of action of corticosteroids in allergic rhinitis remains unknown, but may involve reductions in number of various mediator cells such as basophils, eosinophils, T-helper cells, mast cells, and neutrophils. In the nasal mucosa, nasal reactivity to allergens, and release of inflammatory mediators and proteolytic enzymes. Budesonide is very effective and quikly acting as it is rapidly and almost completely absorbed after oral administration, but has poor systemic availability (about 10%) due to extensive first-pass metabolism in the liver, mainly by the cytochrome P450 isoenzyme CYP3A4.. The major metabolites, 6-β- hydroxybudesonide and 16-α-hydroxyprednisolone have less than 1% of the glucocorticoid activity of unchanged drug with a terminal half-life of about 2 - 4 hours. Polymeric films containing Eudragit RL 100: Eudragit RS: drug (7:3:1, 7: 2:1) and Ethyl cellulose: PVP: drug (7:3:1, 7:2:1) were selected for transdermal administration based on evaluation studies. These polymeric films were prepared by mercury substrate method employing PEG-400 as plasticizer. Two different penetration enhancers Urea and Dimethyl sulphoxide (DMSO) were employed in the study. The patches in each group were uniform in drug content, thickness. In Vitro drug permeation, moisture absorption and WVTR studies were carried out on these test patches. It was found that at all humidity condition the absorption increases which were linear to the moisture absorbed. In PVA and EUDRAGIT RL 100 patches the water vapor transmission rate was found to be higher at 75% RH, RT conditions. Therefore at both % RH, RT condition the PVA and EUDRAGIT RL 100 patches provides the best resistance to water vapor. Therefore, when applied to animals (in further studies) these patches may provide more occlusion to water vapor loss from skin thus making atmosphere beneath the skin more humid that aid in drug permeation.展开更多
文摘BACKGROUND Mucosal healing has become an important goal of Crohn’s disease(CD)treat-ments.Modulen,enriched with transforming growth factor-beta 2,and budeso-nide are commonly accepted treatments for mild-moderate CD.However,their effects on the small bowel(SB)mucosa remain underexplored.AIM To prospectively assess clinical and mucosal responses to Modulen vs budesonide in adults with CD,using SB capsule endoscopy.METHODS Thirty patients were divided into two groups:Modulen+home-based diet(21 patients)and budesonide(9 patients)for an eight-week intervention followed by four weeks of follow-up.Clinical,laboratory,and endoscopic responses were evaluated.The mucosal changes were assessed through SB capsule endoscopy.RESULTS Results indicated significant clinical improvement in the Modulen group with reduced CD activity index(P=0.041)and improved inflammatory bowel disease questionnaire score(P=0.016).Moreover,Modulen was associated with a signifi-cant SB mucosal improvement,evidenced by a decrease in Lewis score(P=0.027).No significant changes were observed in calprotectin or other laboratory parame-ters.Conversely,budesonide exhibited more modest clinical effects,but it improved calprotectin,hemoglobin,and C-reactive protein levels(P=0.051,P=0.014,and P=0.038,respectively).The capsule endoscopy did not reveal a significant mucosal response in the budesonide group.CONCLUSION Both interventions have a role in CD treatment.Yet,their effects differ and may complement each other:Modulen yields clinical and mucosal improvements,while budesonide primarily leads mainly to laboratory improvements.
文摘This study explores the clinical efficacy of budesonide combined with ambroxol inhalation therapy for neonatal pneumonia.A total of 68 neonatal pneumonia patients treated at Li County Hospital from January 2023 to December 2024 were randomly divided into a monotherapy group and a combination group,with 34 patients in each.The monotherapy group received ambroxol inhalation therapy,while the combination group received budesonide inhalation therapy in addition to ambroxol.The recovery progress,blood gas analysis indicators,inflammatory response improvement,and overall clinical efficacy were compared between the two groups.Results showed that the combination group experienced a significantly shorter time for body temperature normalization(3.36±0.58 days vs.4.59±0.45 days),oxygen inhalation duration(4.89±0.57min vs.6.96±0.79min),disappearance of shortness of breath and cough(4.56±0.29 days vs.6.63±0.75 days),and resolution of lung wet rales(5.62±1.46 days vs.7.92±1.28 days)compared to the monotherapy group(P<0.05).Additionally,the total effective rate was significantly higher in the combination group(97.06%)than in the monotherapy group(73.52%)(P<0.05).Post-treatment,the combination group exhibited significantly better blood gas analysis and inflammatory response indicators(P<0.05).These findings suggest that budesonide combined with ambroxol inhalation therapy can effectively improve blood oxygen saturation,reduce inflammation,promote faster recovery,and enhance overall clinical efficacy,making it a reliable treatment option for neonatal pneumonia.
文摘This article explores the significant implications of the study by Ovadia et al,which innovatively compares the efficacy of a nutritional intervention(Modulen)to conventional pharmaceutical therapy(budesonide)in promoting mucosal healing in Crohn’s disease.Highlighting the paradox of a well-established yet underutilized nutritional approach,the findings suggest that Modulen may offer comparable therapeutic benefits despite its high withdrawal rate due to adherence challenges.This advancement underscores the evolving paradigm in inflammatory bowel disease treatment,shifting focus toward non-pharmacologic alternatives that target both clinical remission and endoscopic healing.The article advocates for the development of integrative treatment strategies that balance efficacy,patient adherence,and long-term disease management,emphasizing the need for further research to refine and optimize the role of nutritional therapies in clinical practice.
基金the Wenzhou Basic Medical and Health Science and Technology Project,No.Y20210307.
文摘BACKGROUND Respiratory viruses are increasingly detected in children with communityacquired pneumonia.Further strategies to limit antibiotic use in children with viral pneumonia are warranted.AIM To explore clinical efficacy of budesonide/formoterol inhalation powder for viral pneumonia in children and its impact on cellular immunity and inflammatory factor production.METHODS A total of 60 children with viral pneumonia were recruited:30 receiving budesonide/formoterol inhalation powder and 30 conventional symptomatic treatment.Outcome measures included peripheral blood levels of inflammatory cytokines,CD4^(+),CD8^(+),Th1,Th2,Th17 and Treg,clinical efficacy,and incidence of adverse reactions.RESULTS Compared with the control group,the observation group showed a significant reduction in interleukin-6 and high-sensitivity C-reactive protein levels after treatment.Compared with the control group,the observation group showed a significant increase in CD4^(+)/CD8^(+)and Th1/Th2 levels,and a decrease in Th17/Treg levels after treatment.The total effective rates in the observation group and the control group were 93.75%and 85.00%,respectively,which was a significant difference(P=0.003).CONCLUSION Budesonide/formoterol inhalation powder significantly improved therapeutic efficacy for viral pneumonia in children.The mechanism of action may be related to downregulation of the inflammatory response and improved cellular immune function.
文摘Objective:To investigate the effects of budesonide on blood gas and inflammation indexes in patients with chronic obstructive pulmonary disease(COPD)during remission.Methods:Fifty-one patients with COPD in remission,admitted to Zhongshan Hospital of Dalian University from July 2021 to December 2022,were selected and divided into two groups based on a randomized numerical table method.The control group(25 cases)received budesonide formoterol treatment,while the observation group(26 cases)received budesonide geforce treatment.Various indexes,including clinical efficacy,blood gas indexes,inflammation indexes,St.George’s Respiratory Questionnaire(SGRQ)scores,Chronic Obstructive Pulmonary Disease Assessment Test(CAT)scores,and 6-minute Walking Distance Test(6MWD)results,were compared between the two groups.Results:After 21 days of treatment,the total clinical effectiveness rate of the observation group was higher than that of the control group,with a statistically significant difference(P<0.05).Post-treatment,the PaO2 level and pH value in both groups were higher,and the PaCO_(2) level was lower compared to pre-treatment levels.The observation group showed better improvements in these indicators than the control group,with statistically significant differences(P<0.05).SGRQ and CAT scores for both groups were lower post-treatment,with the observation group scoring lower than the control group.Additionally,the 6MWD results were farther for both groups post-treatment,with the observation group achieving greater distances than the control group,with statistically significant differences(P<0.05).Conclusion:Budesonide can effectively improve blood gas indexes in patients with COPD in remission,alleviate related clinical symptoms,reduce inflammatory responses,and promote patient recovery.The treatment efficacy is significant.
文摘Objective:To analyze the clinical efficacy of tiotropium bromide(TB)combined with budesonide formoterol(BUD/FM)inhalation in treating chronic obstructive pulmonary disease(COPD).Methods:62 COPD patients admitted to the hospital between June 2020 and December 2022 were selected as samples for this study.The patients were divided into a combination group and a conventional group using the random number table method,with 31 cases in each group.The patients in the combination group were treated with TB combined with BUD/FM inhalation,whereas the patients in the conventional group were treated with BUD/FM inhalation only.The treatment efficacy and changes in lung function indicators of both groups were compared.Results:The total efficacy of treatment in the combined group was higher than that in the conventional group,and the difference was statistically significant(P<0.05).Before treatment,there was no difference in pulmonary function indicators between the two groups(P>0.05).After three months of treatment,all lung function indicators of the combined group were higher than those of the conventional group,and the difference was statistically significant(P<0.05).Conclusion:Combining TB with BUD/FM inhalation therapy increases the efficacy of treatment for patients with COPD.Besides,it also improves lung function and leads to a better prognosis.
文摘Objective: To analyze the clinical effect of terbutaline combined with budesonide in the treatment of chronic obstructive pulmonary disease. Methods: 500 cases of patients with chronic obstructive pulmonary disease admitted to the hospital from January 2022 to December 2023 were selected and divided into 250 cases in the control group and 250 cases in the observation group by randomization method, both groups received conventional symptomatic treatment, with budesonide added to the control group and terbutaline and budesonide to the observation group, and the lung function indexes, therapeutic effects and adverse drug reactions before and after treatment were compared. Results: After treatment, the level of all lung function indexes of patients in the observation group was higher than that of the control group, and the level of total effective rate of treatment was 96.40%, which was higher than that of the control group (P < 0.05), and the difference in the incidence rate of adverse reactions between the two groups was not strong (P > 0.05). Conclusion: In the clinical treatment of chronic obstructive pulmonary disease, the combined use of terbutaline and budesonide can positively improve lung function, with precise effects and few adverse reactions.
文摘Budesonide is a corticosteroid used for the treatment of asthma via various matrices and inhalation mechanisms. An unknown peak of Budesonide aqueous formulation has been investigated during stability study wherein the impurity level observed around 0.1% well below the threshold 0.5%. The approach to identify anonymous species was adopted as first to generate the impurity in sample, isolate, enrich and was subjected to LC-MS/MS and NMR for spectral studies. Based on the spectral data the anonymous species were identified as a “Lumibudesonide’’ ((5aR,5bS,5cS,6S,7aS,7bS,10aR,11aS,11bS)-6-hydroxy-7b-(2-hydroxyacetyl)-5b,7a-dimethyl-9-propyl 1,5a,5b,5c,6,7,7a,7b,10a,11,11a,11b dodecahydrocyclopenta[2'',3'']cyclopropa [1'',2'':3', 4']benzo [1',2':4,5]indeno [1,2-d][1,3]dioxol-5(2H)-one), which is observed in photolysis of Budesonide.
基金National Basic Research Program of China (973 Program No 2009CB930300)National Integrity Innovational Technology Platform of New Drug and Research and Development (Grant No 2009ZX09310-001)
文摘To increase the solubility and adsorption of budesonide（BUD）,budesonide-loaded solid lipid nanoparticles（BUD-SLNs） were prepared and characterized in this study.Glycerin monostearate（GMS）was selected to be the matrix lipid material after calculation the differences of partial solubility parameters.An emulsification-ultrasound diffusion method was employed and formula was optimized in the BUD-SLNs preparation.The entrapment efficiency（ee%）of BUD-SLNs was（97.77±2.60）%, and the mean particle size was 147.3 nm（PDI=0.228）.Uniform and sphere particles were observed under TEM.The in vitro release of BUD-SLNs could be well explained by the biphasic release dynamics equation.The spectrums of DSC and X-ray diffraction indicated that BUD molecules were dispersed mainly into the lipids to form homogeneous matrix structure.Our results provide fundamental data for the application of SLNs in pulmonary delivery system.
文摘Objective: the experiment will implement different treatment plans for patients with moderate and severe bronchial asthma, and further compare the clinical efficacy of budesonide and formoterol powder inhalation and budesonide suspension atomization inhalation. Methods: 100 patients with moderate to severe bronchial asthma admitted to our hospital were randomly selected as the subjects of this study. The diagnosis and treatment time range was from July 2020 to August 2021, and they were divided into groups by random design. The control group received budesonide suspension inhalation, while the observation group received budesonide formoterol powder inhalation, and the situation after four weeks of treatment was compared. Results: from the perspective of nursing quality, the lung function indexes of patients in the observation group were better than those in the control group. After treatment, FEV1 and FEV1/FVC in the observation group were (1.69±0.26) L and (65.77±0.28) %, respectively, while those in the control group were (1.13±0.19) L and (56.92±0.17) %. The comparison was statistically significant (P < 0.05). At the same time, the negative rate of bronchial dilation test in the observation group was higher than that in the control group (76.0% and 56.0%, respectively), and the difference was statistically significant. In addition, we compared the asthma control scores of patients before and after treatment, and the scores of the observation group were more advantageous after treatment, indicating that asthma symptoms were better controlled. Finally, the incidence of adverse reactions in patients was compared. There was no significant difference between the two groups, and both groups had safety guarantee. Conclusion: inhalation of Budesonide formoterol powder in the treatment of moderate and severe bronchial asthma has good efficacy, can improve the lung function index of patients, strengthen the control of asthma symptoms, and has the value of clinical promotion.
文摘AIM： Prednisone and azathioprine represent the standard treatment for autoimmune hepatitis （AIH）. However, only 65% of the patients enter complete histological remission. Recently, budesonide （BUD） was reported to be a promising alternative. In this study we assessed the efficacy and safety of BUD in AIH. METHODS： Eighteen patients （12 women, 6 men; mean age 45.4±21 years） with AIH were treated with BUD （Budenofalk） 3 mg thrice daily and followed up for at least 24 wk. Seven patients also had features of primary biliary cirrhosis （n = 5） or primary sclerosing cholangitis （n = 2）. Advanced liver fibrosis or cirrhosis was present in RESULTS： Fifteen （83%） patients had a complete clinical and biochemical remission. Ten patients, including five with acute hepatitis, were given BUD as first-line therapy, of which seven enter remission. Three patients, two with liver cirrhosis, did not improve. All patients with second-line therapy experienced long-term remission. A histological remission was also seen in three patients. Clinically relevant BUD-induced side effects were recorded only in patients with liver cirrhosis （n = 4）. CONCLUSION： BUD is effective in remission induction in the majority of our patients with AIH. Side effects and treatment failure was mainly observed in patients with liver cirrhosis.
文摘AIM:To investigate the systemic availability of budesonide in a patient with Child A cirrhosis due to autoimmune hepatitis (AIH) and primary hepatocellular carcinoma,who developed serious side effects. METHODS:Serum levels of budesonide,6β-OH-budesonide and 16α-OH-prednisolon were measured by HPLC/MS/MS; portosystemic shunt-index (SI) was determined by 99mTc nuclear imaging.All values were compared with a matched control patient without side effects. RESULTS:Serum levels of budesonide were 13-fold increased in the index patient.The ratio between serum levels of the metabolites 6β-OH-budesonide and 16α-OH- prednisolone,respectively,and serum levels of budesonide was diminished (1.0 vs.4.0 for 6β-OH-budesonide,4.2 vs. 10.7 for 16α-OH-prednisolone).Both patients had portosystemic SI (5.7 % and 3.1%) within the range of healthy subjects.CONCLUSION:Serum levels of budesonide Vary uP to 13-fold in AIH Patients with Child A eirrhosis in the absenee ofrelevant Portosystemic shunting.Redueed hePatiemetabolism,as indicated by redueed metabolite-to-drugratio,rather than Portosystemie shunting may explainsystemic side effects of this drug in cirrhosis
文摘Eosinophilic cholangitis is a rare cause of deranged obstructive liver function tests. It has been described as a great mimicker for malignant biliary strictures and bile duct obstruction. There are only case reports available on treatment experience for eosinophilic cholangitis. A large proportion of patients present with biliary strictures for which they have undergone surgery or endoscopic treatment and a small proportion was given systemic corticosteroid. We share our treatment experience using budesonide which has fewer systemic side effects to prednisolone and avoids invasive management.
基金The National Natural Science Foundation of China(Grant No.81202469)Founder of new drug research fund(Grant No.20130527)
文摘Large Hollow nanoparticulate aggregates（LHNAs） based on albumin nanoparticles is a promising technology for developing dry powder inhaler（DPI） with good aerodynamic properties in order to provide a new drug delivery system（DDS） for the treatment of lung disease. Improved understanding of molecular interactions could lead to prepare the DDS rationally. Therefore, this investigation utilized computations and experiments to reveal the mechanisms of budesonide（BUD） interactions with bovine serum albumin（BSA） at the molecular level. The molecular dynamics（MD） simulation revealed that there were three critical stable binding sites of BUD on BSA（P1, P2, P3） mainly by hydrophobic interaction and hydrogen bond. The energy decomposition of each residue to the whole BUD-BSA complex system in P1-P3 showed that nonpolar residues in or around the binding site played an important role in the binding of BUD to BSA. The molar ratio was close to 3 in preparations in drug-loading efficiency experiment, which was confirmed to the simulation results. The details of the binding sites from computation provided a guideline for the design of the BSA nanoparticles carrying BUD, which was prepared successfully at last. Combination of the MD simulation and experiment as well as the mechanism of the molecular interaction provided a solid theoretical basis for the preparation of BSA-LHNAs for DPI in the future.
文摘Purpose: Since intravesically administered steroid therapy may treat bladder pain syndrome/interstitial cystitis (BPS/IC) with fewer side effects than the current treatment of orally administered steroids, we investigated whether the intravesical infusion of budesonide foam can effectively treat BPS/IC symptoms in a rat model of tranilast-induced BPS/IC. Methods: There were 6 rat treatment groups (n = 8 per group): control + single or daily saline infusion, tranilast + single or daily saline infusion, and tranilast + single or daily budesonide infusion. All groups except for the controls were fed a tranilast supplemented diet for 5 weeks. Budesonide and saline were infused intravesically. After the BPS/IC rat model underwent single infusion treatments, we measured the paw pain threshold using the von Frey test and continuous cystometry was taken. After two weeks of daily intravesical infusions, we measured locomotor activity and serum cortisol levels;harvested bladders underwent histological analysis. Results: Both pain threshold and locomotor activity were significantly lower in the saline-infused groups receiving the tranilast diet, but there were no differences between the budesonide-infused groups and the controls. The interval between bladder contractions was significantly shorter in the tranilast group than the control or tranilast + budesonide infusion groups. The serum cortisol levels did not change. Hematoxylin-Eosin stainings of the bladder showed thickening of the bladder muscle layer and mucosal edema in the tranilast group, while the tranilast + budesonide infusion group showed only mild changes. Conclusion: Intravesical infusion of budesonide effectively treated BPS/IC symptoms in a rat model of BPS/IC.
文摘Objective:To study the influence of budesonide and salbutamol atomization inhalation on Th17/Treg balance in patients with bronchial asthma and its correlation with airway remodeling.Methods:A total of 90 patients with bronchial asthma who received systemic treatment in our hospital between July 2013 and April 2016 were divided into control group (n=45) and observation group (n=45) according to random number table. Patients in the control group were treated with salbutamol atomization inhalation alone while those in observation group were treated with budesonide and salbutamol atomization inhalation. The Th17/Treg ratio in peripheral blood as well as serum contents of airway remodeling-related indicators was compared between two groups before and after treatment. The correlation between Th17/Treg balance and airway remodeling in patients with bronchial asthma was detected by Pearson test. Results:Before treatment, the differences in peripheral blood Th17/Treg ratio as well as serum contents of inflammatory mediators, growth factor indexes and collagen metabolism indexes were not statistically significant between two groups of patients. After treatment, peripheral blood Th17/Treg ratio in observation group was lower than that in control group, serum CRP, IL-8, IL-13 and TNF- contents in observation group were lower than those in control group, serum PDGF-BB, b-FGF and VEGF contents in observation group were lower than those in control group, and serum HA, PCⅢ and LN contents in observation group were lower than those in control group. The Th17/Treg ratio in patients with bronchial asthma after treatment was positively correlated with the levels of airway remodeling-related indexes.Conclusion:Budesonide combined with salbutamol atomization inhalation can optimize the Th17/Treg balance in patients with bronchial asthma, and Th17/Treg is directly correlated to the degree of airway remodeling.
文摘Objective: To investigate the effects of montelukast sodium combined with budesonide on pulmonary function, inflammatory factors and immunoglobulin in children with asthma. Methods: A total of 100 children with asthma treated in our hospital from May 2013 to November 2016 were randomly divided into control group and observation group. In the control group, budesonide inhalation therapy was given. On the basis of the control group, montelukast sodium treatment was given, pulmonary function, inflammatory factors and immunoglobulin levels in the two groups before and after treatment were measured. Results:Compared with before treatment, the levels of FEV1%, FEF50%, FEF25% and PEF% in the two groups were significantly increased, those in the observation group were higher than in control group;compared with before treatment, IL-10 levels were significantly increased, TNF-α and IL-8 levels were significantly decreased in the two groups after treatment, moreover those in the observation group IL-10 levels were significantly higher than the control group, TNF-α and IL-8 were significantly lower than those in the control group, the difference was statistically significant;Compared with before treatment, IgA and IgM levels were significantly increased in both groups after treatment, IgE levels were significantly decreased, and IgA and IgM levels in the observation group were significantly higher than in the control group, IgE levels were significantly lower than the control group, the difference was statistically. Conclusion: Montelukast sodium combined with budesonide can effectively reduce the inflammation level of children with asthma, improve lung function, enhance immunity, the effect is significant, it is worth further clinical application.
文摘Objective: To study the effects of oral cetirizine combined with budesonide inhalation on immune inflammatory response in children with acute asthma attack. Methods: Children with acute asthma attack who were treated in Beijing Luhe Hospital Affiliated to Capital Medical University between April 2014 and February 2017 were selected and randomly divided into two groups, observation group received oral cetirizine combined with budesonide inhalation therapy, and control group received budesonide inhalation therapy. The contents of CD4+T cell subsets and the expression of immune transcription factors in peripheral blood as well as the contents of CD4+T cytokines and inflammatory mediators in serum were measured after 1 week of treatment. Results: After 1 week of treatment, Th1 and Treg contents as well as BCL11B, STAT4 and SOCS3 mRNA expression in peripheral blood as well as IFN-γand IL-10 contents in serum of observation group were greatly higher than those of control group while Th2, Th17 and Th22 contents as well as STAT1 and STAT3 mRNA expression in peripheral blood as well as IL-4, IL-17, IL-22, HMGB1, Periostin, Eotaxin and ADAM33 contents in serum were greatly lower than those of control group. Conclusion: Oral cetirizine combined with budesonide inhalation is more effective than budesonide inhalation alone to modulate the immune inflammatory response in children with acute asthma attack.
基金This work was supported by National Natural Science Foundation of China(Nos.81302720 and No.81573380)Liaoning Pan Deng Xue Zhe Scholarship+1 种基金supported by the Ministry of Education,Science and Technological Development,Republic of Serbia(grant number 451-03-68/2020-14/200161)Cun D.is grateful to Liaoning Provincial Education officer’s Excellent Talents Supporting Plan for financial support.
文摘This study aims to understand the absorption patterns of three different kinds of inhaled formulations via in silico modeling using budesonide(BUD)as a model drug.The formulations investigated in this study are:(i)commercially available micronized BUD mixed with lactose(BUD-PT),(ii)BUD nanocrystal suspension(BUD-NC),(iii)BUD nanocrystals embedded hyaluronic acid microparticles(BUD-NEM).The deposition patterns of the three inhaled formulations in the rats’lungs were determined in vivo and in silico predicted,which were used as inputs in GastroPlus TM software to predict drug absorption following aerosolization of the tested formulations.BUD pharmacokinetics,estimated based on intravenous data in rats,was used to establish a drug-specific in silico absorption model.The BUD-specific in silico model revealed that drug pulmonary solubility and absorption rate constant were the key factors affecting pulmonary absorption of BUD-NC and BUD-NEM,respectively.In the case of BUD-PT,the in silico model revealed significant gastrointestinal absorption of BUD,which could be overlooked by traditional in vivo experimental observation.This study demonstrated that in vitro-in vivo-in silico approach was able to identify the key factors that influence the absorption of different inhaled formulations,which may facilitate the development of orally inhaled formulations with different drug release/absorption rates.
文摘Budesonide is a highly potent synthetic, nonhalogenated corticosteroid. The mechanism of action of corticosteroids in allergic rhinitis remains unknown, but may involve reductions in number of various mediator cells such as basophils, eosinophils, T-helper cells, mast cells, and neutrophils. In the nasal mucosa, nasal reactivity to allergens, and release of inflammatory mediators and proteolytic enzymes. Budesonide is very effective and quikly acting as it is rapidly and almost completely absorbed after oral administration, but has poor systemic availability (about 10%) due to extensive first-pass metabolism in the liver, mainly by the cytochrome P450 isoenzyme CYP3A4.. The major metabolites, 6-β- hydroxybudesonide and 16-α-hydroxyprednisolone have less than 1% of the glucocorticoid activity of unchanged drug with a terminal half-life of about 2 - 4 hours. Polymeric films containing Eudragit RL 100: Eudragit RS: drug (7:3:1, 7: 2:1) and Ethyl cellulose: PVP: drug (7:3:1, 7:2:1) were selected for transdermal administration based on evaluation studies. These polymeric films were prepared by mercury substrate method employing PEG-400 as plasticizer. Two different penetration enhancers Urea and Dimethyl sulphoxide (DMSO) were employed in the study. The patches in each group were uniform in drug content, thickness. In Vitro drug permeation, moisture absorption and WVTR studies were carried out on these test patches. It was found that at all humidity condition the absorption increases which were linear to the moisture absorbed. In PVA and EUDRAGIT RL 100 patches the water vapor transmission rate was found to be higher at 75% RH, RT conditions. Therefore at both % RH, RT condition the PVA and EUDRAGIT RL 100 patches provides the best resistance to water vapor. Therefore, when applied to animals (in further studies) these patches may provide more occlusion to water vapor loss from skin thus making atmosphere beneath the skin more humid that aid in drug permeation.
