Montelukast Sodium Tablets Research Articles

Efficacy and Safety of Montelukast Sodium Tablets Combined with Budesonide Suspension in the Treatment of Patients with Bronchial Asthma

Efficacy and Safety of Montelukast Sodium Tablets Combined with Budesonide Suspension in the Treatment of Patients with Bronchial Asthma

Clinical study of traditional Chinese medicine fumigation in the treatment of allergic rhinitis

Objective: To study the clinical effect of traditional Chinese medicine fumigation on treating allergic rhinitis.Methods: 80 cases of patients with allergic rhinitis in our hospital from August 2020 to August 2021 were selected and then randomly divided into two groups. In this research, the combination of montelukast sodium tablets and cetirizine was used in the control group. Traditional Chinese medicine fumigation was given in addition to oral medication in the treatment group.Results: The total effective rate of the clinical treatment in the treatment group was higher than that in the control group, and the difference was statistically significant (p < .05). It took less time to relieve nasal itching, runny nose, nasal congestion, and sneezing in the treatment group than in the control group, and the difference was statistically significant (p < .05). Besides, the symptoms were much more relieved in the treatment group than in the control group, and the difference was statistically significant.Conclusions: Traditional Chinese medicine fumigation shows a remarkable clinical effect on the treatment of allergic rhinitis, and it is worthy of clinical application.

Quality by Design Approach for Design, Development and Optimization of Orally Disintegrating Tablets of Montelukast Sodium

Background: The goal of this research was to use the Quality by Design (QbD) approach to develop orally disintegrating tablets of Montelukast sodium, a leukotriene receptor antagonist used to treat asthma. Characterizing the reference product, defining the quality target product profile (QTPP), identifying critical quality attributes (CQAs), and performing initial testing are all parts of the QbD approach and relating the critical material attributes (CMAs) and critical process parameter (CPP) to drug product CQAs, as a result to develop the design space and defining control strategy. Method: Montelukast sodium tablets were designed using direct compression technique. Formulation were designed by using (DOE software v 13.2) 23 full factorial design in which three variables namely croscarmellose sodium (CCS), microcrystalline cellulose (MCC) and magnesium stearate were varied at two levels by considering one center point. Results: The disintegration time and in vitro dissolution were considered as responses and the prepared tablets have been evaluated for various quality control tests. Formulation F5 was considered as optimized as it showed minimum disintegration time and maximum drug release profile. Conclusion: The CMAs classified as high or medium risk in the initial risk assessment were mitigated to low risk based on the experimentation. Finally, a control strategy was defined giving better control over drug product development.

Discussion on the Curative Effect of Feilike Mixture Combined with Montelukast Sodium Tablets in the Treatment of Senile Cough after Infection

Discussion on the Curative Effect of Feilike Mixture Combined with Montelukast Sodium Tablets in the Treatment of Senile Cough after Infection

Development and Validation of Reverse Phase High Performance Liquid Chromatography Method for In-vitro Dissolution Testing of Bilastine and Montelukast Sodium Tablets

The objective of this experimental work is to develop and validate a reverse-phase high-performance liquid chromatographic (RP-HPLC) method, which is capable of quantitative estimation of Bilastine (BLS) and Montelukast (MTK) content present in dissolution media accurately and precisely. A simple, fast, specific, rugged, and reproducible analytical method was developed and validated on a Shimadzu Highperformance liquid chromatography (HPLC) system. A Hypersil BDS C18-Column (100 mm x 4.6mm, 3 µm) and 0.1%v/v Triethylamine buffer (pH-3.0): Acetonitrile used as mobile phase with flow rate 1.0 mL/min in gradient mode. The column oven temperature and sample cooler temperature were set to 40°C and 25°C, respectively. The injection volume was 10 µL, and chromatograms were recorded at 220 nm. The run time for 1 sample analysis was 13 minutes. The optimized conditions for dissolution testing include USP type-II apparatus at 75 rpm with 900 mL, 0.5% w/v sodium lauryl sulfate media at 37.0 ± 0.5°C and collected after 45 minutes. Under the above conditions, the retention time (RT) of Bilastine and Montelukast was 1.84 and 7.23 minutes, respectively, without any interference of dissolution media or any other degradant at the RT of both drugs. The calibration curve was linear with R2 value of 0.99984 and 0.99988 for BLS and MTK, respectively. The sample was found stable in dissolution media beyond 12 hours. The analytical method was validated as per International Council for Harmonisation (ICH) guidelines with respect to specificity, precision, linearity, accuracy, stability in aqueous solution, and robustness. The proposed method was found useful for the routine analysis of dissolution samples for quality control purposes.

Effects of montelukast sodium tablets combined with pulmicort aerosol in the treatment of children with asthma and its influence on EOS, IL-4, IgE, TNF-α

Objective To investigate the effect of montelukast sodium tablets combined with pulmicort aerosol in the treatment of children with asthma, and its influence on eosinophil (EOS), interleukin-4 (IL-4), immunoglobulin E (IgE), tumor necrosis factor-α (TNF-α). Methods From March 2018 to March 2019, 142 children with asthma admitted to Hangzhou Dajiangdong Hospita were randomly divided into observation group (71 cases) and control group (71 cases) according to the digital table.The patients in the observation group were treated with montelukast sodium tablets combined with pulmicort aerosol, while patients in the control group were treated with pulmicort aerosol.Both two groups were treated for 2 weeks.The levels of EOS, IL-4, IgE and TNF-α, day and night asthma symptom scores and blood gas analysis indicators before and after treatment were compared between the two groups. Results The total effective rate of the observation group (91.55%) was higher than that of the control group (74.65%) (χ2=7.220, P<0.05). After treatment, the scores of asthma symptoms in day[(0.38±0.12)points] and night[(0.42±0.14)points] in the observation group were lower than those in the control group[(0.87±0.19)points and (0.93±0.25)ponts](t=18.373, 14.998, all P<0.05). After treatment, the levels of EOS[(0.38±0.09)×109/L], IL-4[(13.89±3.25)ng/L], IgE[(109.35±16.57)kU/L] and TNF-α[(1.25±0.12)ng/L] in the observation group were lower than those in the control group[(0.73±0.13)×109/L, (18.36±2.70)ng/L, (164.53±23.51)kU/L and (1.49±0.15)ng/L](t=18.652, 8.914, 16.165, 10.528, all P<0.05). Conclusion Montelukast sodium tablets combined with pulmicort aerosol is effective in the treatment of children with asthma.It can reduce the levels of EOS, IL-4, IgE and TNF-α, alleviate the symptoms of daytime and night asthma. Key words: Asthma; Eosinophils; Interleukin-4; Immunoglobulin E; Tumor necrosis factor-a; Montelukast sodium; Pulmicort aerosol; child

Clinical and inflammatory phenotypic features of asthmatic patients sensitive to cold stimulation

To explore the clinical symptoms, lung function and airway inflammation phenotype characteristics of asthmatic patients who are sensitive to cold stimulation. Eighty patients with newly diagnosed bronchial asthma or with mild to moderate acute exacerbation of previously diagnosed bronchial asthma but without regular treatment were selected. According to whether cold air stimulation could induce respiratory symptoms such as cough and wheeze, the patients were divided into cold-insensitive group (45 cases) and cold-sensitive group (35 cases). All the patients were treated with inhaled corticosteroid (ICS), long-acting β2 receptor agonist (LABA; salmeterol xinafoate and fluticasone propionate powder for inhalation, 50 μg/250 μg, twice daily) and montelukast sodium tablets (10 mg, once daily); short-acting β2 receptor agonist (SABA) and/or systemic glucocorticoid (prednisone acetate tablets, 10 mg, once daily; or injection of methylprednisolone sodium succinate, 40 mg) were given if necessary. Asthma Control Test (ACT) score before treatment and at 3 months of treatment was used to assess the clinical symptoms such as cough and wheeze; spirometry was performed to determine lung function impairment and recovery. Blood and induced sputum cell counts were examined to determine the characteristics of airway inflammation. The two groups were comparable for age, gender, BMI, proportion of smokers and allergic rhinitis before treatment. The cold-sensitive patients experienced significantly more frequent acute exacerbations than the cold-insensitive patient within 1 year before the visit (P &lt; 0.05), but the use of SABA and glucocorticoid for symptom control during the treatment did not differ significantly between the two groups (P &gt; 0.05). The ACT scores of the cold-sensitive group were significantly lower than those of the cold-insensitive group both before and after the treatment (P &lt; 0.01). Compared with the cold-insensitive patients, the cold-sensitive patients had more obvious impairment of FEV1/FVC% and FEV1%pred before treatment (P &lt; 0.01), and also showed poorer recovery after treatment (P &lt; 0.05). The percentages of eosinophils in blood and induced sputum samples did not differ significantly between the two groups either before and after the treatment, but the percentage of neutrophils was significantly higher in the cold-sensitive group (P &lt; 0.01). In the induced sputum samples collected before treatment, the cell populations consisted mainly of eosinophilic subtype (60%) and neutrophilic subtype (20%) in the cold-insensitive group; in the cold-sensitive patients, the sputum neutrophilic subtype cells increased significantly to 42.86% (P=0.03) and the eosinophilic subtype cells were lowered to 31.43% (P=0.01). The cold-sensitive asthmatic patients experience frequent recurrent and/or aggravated symptoms and have obvious lung function impairment. Different from that in patients with classic asthma, the airway inflammatory phenotype in these patients is characterized by the domination by neutrophilic subtype.

Comparison of therapeutic efficacy of antihistaminics and combinations of montelukast with allergic rhinitis

Allergic Rhinitis is basically a chronic disease that decreases quality of life. Antihistaminics have been used for the first time in allergic rhinitis. In the search for an alternative treatment in resistant allergic rhinitis, Montelukasts and their combinations have been used. Randomized double-blind controlled study. In our study, the effect on the quality of life of the compounds used recently be compared after 3 months of treatment. In this study, 7 groups of 40 patients, 18-65 years old were planned for each group. The number of females and males was equal in each group (20). The patients in group A and group B will be called for checks after 3 months of medical treatment in the C-D-E-F-G-H group without treatment for 3 months. The patients in Group C received 10 mg Rupatadin Fumarate tablets orally (1 * 1 single dose) before bedtime, 5 mg Levosetirizine Dihydrochloride tablets in the patients in Group D orally (1 * 1 single dose) before bedtime, 10 mg Montelukast Sodium tablets in patients in Group E Before oral (1 * 1 single dose), patients in Group F 5 mg Desloratadin + 10 mg Montelukast Sodium tablets orally (1 * 1 single dose) before bedtime, and patients in Group G Levocetirizine Dihydrochloride + 10 mg Montelukast Sodium tablet orally before bedtime (1 * 1 single dose) will be given. These treatments will continue for 3 months without interruption. The Rinokonjucivations Quality of Life Questionnaire (RQLQ) will be completed with a total of 28 questions. No significant superiority of the Rupatadine molecule to levocetirizine was detected. The score of the Montelukast areas was significantly low when compared to the Rupatadine and Levosetirizine groups. Combined Montelukastes were found to be much more effective than single antihistaminics and single montelukast. There was no difference in quality of life between the combined Montelukast. Antihistaminics are the first treatment option in patients with allergic rhinitis,In resistant cases, combinations with montelukast should be used.

Efficacy of oral montelukast combined with budesonide suspension inhalation in the treatment of children with cough variant asthma and its effect on inflammatory cytokines

Objective To investigate the effect of montelukast combined with budesonide suspension inhalation in the treatment of children with cough variant asthma(CVA), and its effect on inflammatory cytokines. Methods 96 patients with CVA were selected, and they were randomly divided into observation group(n=48) and control group(n=48) according to the digital table.The control group was treated with routine western medicine only. On the basis of the control group, the observation group was treated with aerosol inhalation of budesonide suspension and montelukast sodium tablets. The children in the two groups were treated for 3 months, then the treatment effect was evaluated. Results The total effective rate in the observation group was 95.8%, which was significantly higher than 77.1% in the control group(χ2=4.914, P 0.05). After treatment, the levels of IL-8, IL-6 and TNF-α in the two groups were significantly lower than before treatment(t=2.09, 3.13, 2.97, all P 0.05). There were no serious adverse reactions in the treatment group, and the treatment cycle was completed successfully. Conclusion Montelukast combined with budesonide suspension inhalation in the treatment of children with CVA can significantly improve pulmonary ventilation function, reduce cough symptoms, it is safe and effective, which is worthy of clinical reference. Key words: Montelukast; Budesonide suspension; Asthma; Chemokines

Observation on clinical effects of tuina plus montelukast sodium tablets for children with cough variant asthma

To observe the clinical effects of tuina plus oral administration of montelukast sodium tablets for children with cough variant asthma (CVA). A hundred and six children with CVA were randomly divided into a treatment group and a control group, 53 cases in each group. The treatment group was treated with Tuina therapy plus oral administration of montelukast sodium tablets, and the control group was treated only by oral administration of montelukast sodium tablets. Tuina treatment was given three times per week. 5 mg of montelukast sodium tablets was given orally before bedtime every night. The therapeutic effects were assessed after the treatment of four weeks in both groups. The total effective rates were 92.5% in the treatment group and 77.4% in the control group. The difference in the total effective rate between the two groups was statistically significant (P<0.05). The therapeutic effect of tuina plus montelukast sodium tablets for children with CVA is better than that of oral administration of montelukast sodium tablets alone.

Effect of Montelukast combined with Budesonide Nasal Spray for treatment of children allergic rhinitis and its effect on serum IgE

Objective To observe the curative effect of Montelukast combined with Budesonide Nasal Spray for treatment of children allergic rhinitis and its effect on serum IgE. Methods The 90 cases of children with allergic rhinitis were selected.Randomly divided into three groups A,B,C. Montelukast Sodium Tablets to A group,B group received Budesonide Nasal Spray,C group received Montelukast Sodium Tablets combined with Budesonide Nasal Spray.All were treated for 28 days. Respectively,before treatment and after,the quality of life scores and nasal symptoms scores were compared, and serum IgE were detected. Results The total effective rate of group C was 93.3%, better than the A group (83.3%) and B group (80%). The difference was statistically significant(P<0.05). The scores of clinical symptoms and quality of life of the 3 groups after treatment were significantly improved(P<0.05). But the C group compared with A group, B group improved more significantly(P<0.05). The 3 groups after the treatment of serum IgE content compared with before treatment were significantly decreased compared with before treatment,the differences were statistically significant(P<0.05), and C group than in A group,B group decreased significantly(P<0.05). Serious adverse reactions in 3 groups were not found. Conclusions The curative effect of Montelukast combined with Budesonide nasal spray in treatment of allergic rhinitis is better, and can reduce the serum level of IgE, and improve the quality of life of children, reduce the risk of asthma. Key words: allergic rhinitis; children; montelukast; budesonide nasal spray; serum IgE

THE THERAPEUTIC EVALUATION AND MECHANISM ON TREATING BRONCHIAL HYPER-RESPONSIVENESS COUGH BY ZIYINQINGRE PRESCRIPTION.

Objective:Discussing the effects of Ziyinqingre prescription on the level of airway resistance (Rrs), airway response threshold (Dmin), airway conductance (sGrs) and the level of inflammatory cytokines interleukin-4 (IL-4) and interferon-γ (IFN-γ) of the bronchial hyper-responsiveness (BHR) cough patients.Method:84 subjects diagnosed as BHR were randomly divided into 42 Chinese Traditional medicine group and 42 control group. The Chinese Traditional Medicine group received Ziyinqingre prescription twice a day and the control group received 10mg Montelukast Sodium tablets once a day for two weeks. Observe the clinical symptoms improvement and the changes of the level of the Rrs, Dmin, sGrs and IL-4, IFN-γ.Results:After receiving the medicine, the symptoms of the Chinese medicine group were obviously alleviated, the outcome was more satisfied than that of the control group. Compared with the control group, the level of Dmin increased and sGrs level decreased more obviously (P<0.05); the level of IL-4 decreased and IFN^level increased more obviously in the Chinese medicine group (P<0.05).Conclusion:Ziyinqingre prescription can not only improve BHR patients’ symptoms, but reduce the level of bronchial responsiveness, which proved a better curative effect of Chinese medicine. The mechanism is probably due to relieving the airway inflammation by keeping the balance between Th1 and Th2 cells.

Formulation Design of Bilayer Dual-Release Tablet composition of Fexofenadine HCl and Montelukast Sodium

The purpose of this study was to develop dual-release bilayer tablets of fexofenadine HCl and montelukast sodium (MKS) to treat the individuals getting symptoms of asthma and allergic rhinitis at late night and early morning which may lead to breathing and respiratory problem. The bilayer tablet was designed to contain fexofenadine for the immediate release and MKS for the extended release matrix. MKS and fexofenadine tablets were prepared separately by direct compression method. The optimized tablets were compressed to obtain bilayer tablets. The tablets were evaluated for various physicochemical parameters and dissolution study. Further, the bilayer tablets were subjected to accelerated stability study. The fexofenadine tablet showing more than 75% release in 15 min and MKS tablet showing more than 90% release at the end of 7 h with 2 h of initial lag time were compressed one above the other to obtain bilayer tablet. The similar release pattern was observed with the bilayer tablets as that of individual tablets. The bilayer tablets were found to be stable at the end of 6 months storage period as per ICH guidelines. Both the layers of the bilayer formulation showed desired drug release at the end of time period, these could be effective formulations in late night and early morning symptoms of asthma and allergic rhinitis.

Formulation and In-vitro Evaluation of Chewable Tablets of Montelukast Sodium

The objective of the present study is to develop chewable tablets containing different pharmaceutical compositions with simple manufacturing procedures using different excipients. Mannitols, L-HPC 11, Aspartame, Crospovidone, Crospovidone, Aerosil, and Magnesium Stearate are used as excipients for effective formulation of anti-asthmatic drug Montelukast. Montelukast is a selective, orally acting leukotriene receptor antagonist that is used for the treatment of asthma and seasonal allergic rhinitis. Montelukast chewable tablets were prepared by Direct Compression methods using suitable excipients. The chewable tablets were better presented using artificial sweetener Aspartame as flavouring agent. A total of forteen formulations were prepared and the granules were evaluated for pre-compression parameters. The formulated tablets were evaluated for post-compression parameters .The results showed that all the physical parameters were within the acceptable limits. The in vitro release study of all the formulations showed good release. The study concludes that aforementioned excipients can be used to design chewable montelukast sodium tablets.

A Randomized, Comparative, Multicentric Clinical Trial to Assess the Efficacy and Safety of Zileuton Extended-Release Tablets With Montelukast Sodium Tablets in Patients Suffering From Chronic Persistent Asthma

Leukotriene (LT) modifiers are anti-inflammatory drugs that are useful as an add-on therapy with first-line asthma-controller medications. This group includes LT synthesis inhibitors (eg, Zileuton) and receptor antagonists (eg, Montelukast), whose direct comparative clinical data are not available. This study was conducted to assess the comparative efficacy and safety of orally administered Zileuton extended-release (ER) with Montelukast sodium in patients suffering from chronic persistent asthma. Patients of 18-65 years of age with mild to moderate chronic stable asthma were randomized to treatment with Zileuton ER 2400 mg/d or Montelukast 10 mg/d for 12 weeks. Peak expiratory flow rate (PEFR) and asthma symptoms (cough, wheeze, chest tightness, and shortness of breath each on a 4-point scale) were assessed on monthly scheduled out-patient visits. Safety assessments by clinical and laboratory parameters were carried out during the course of the study. Among 210 patients eligible for efficacy assessment, PEFR improved by 64.8 ± 52.8 (95% confidence interval: 54.8-74.7) L/min with Zileuton ER (n = 109) and 40.6 ± 47.5 (31.3-49.9) L/min with Montelukast (n = 101; P < 0.001), whereas percent improvements were 27.0% (22.6%-31.5%) versus 18.4% (14.1%-22.7%), respectively (P = 0.006). Zileuton ER lead to ≥12% PEFR improvements in 74 of 109 [67.9% (59.1%-76.7%)] patients, whereas the same was noted in 52 of 101 [51.5% (41.7%-61.2%)] patients receiving Montelukast (P = 0.015). The reduction in the mean overall symptom intensity score was also significantly better with Zileuton ER [-5.0 ± 2.1 (4.6-5.4) versus -4.2 ± 2.3 (3.8-4.7)] (P = 0.018); however, the same was not observed for the decline in the individual symptom scores. A lesser but not significantly different adverse event rate was reported in the Zileuton ER group than the Montelukast group with the commonest events being headache and gastrointestinal effects in both the groups. Thus, Zileuton ER seems to be more efficacious than Montelukast and well tolerated for the treatment of mild to moderate chronic persistent asthma in adult patient population. Further studies can elucidate the comparative treatment benefits of these LT modifiers in asthma management.

Formulation and in vitro and in vivo evaluation of film-coated montelukast sodium tablets using Opadry&amp;reg; yellow 20A82938 on an industrial scale

Purpose:The aim of this study was to formulate stable film-coated montelukast sodium (MS) tablets using Opadry® yellow 20A82938 (Montikast® tablets) and to evaluate their in vitro and in vivo release profile.Methods:MS core tablets were manufactured using a direct compression method. Opadry yellow 20A82938 aqueous coating dispersion was used as the film-coating material. Dissolution of the film-coated tablets was tested in 900 mL of 0.5% sodium lauryl sulfate solution and the bioequivalence of the tablets was tested by comparing them with a reference formulation – Singulair® tablets. In vitro–in vivo correlation was evaluated. The stability of the obtained film-coated tablets was evaluated according to International Conference on Harmonisation of Technical Requirements for Registration of Pharmaceuticals for Human Use guidelines.Results:The efficiency of the film coating was determined by subjecting the coated tablets to gastric pH and drug release was analyzed using high-performance liquid chromatography. The coated tablets had no obvious defects. MS release met the study criterion of not less than 80% dissolved after 30 minutes in 0.5% sodium lauryl sulfate solution. Statistical comparison of the main pharmacokinetic parameters clearly indicated no significant difference between test and reference in any of the calculated pharmacokinetic parameters. Level A correlation between in vitro drug release and in vivo absorption was found to be satisfactory.Conclusion:These findings suggest that aqueous film coating with Opadry yellow 20A82938 is an easy, reproducible, and economical approach for preparing stable MS film-coated tablets without affecting the drug-release characteristics.

Effect Of integrated traditional Chinese and western medicine on Th1/Th2 cytokines level in children with asthma

To discuss the effect of integrated traditional Chinese and Western medicine on Th1/Th2 cytokines level in children with asthma. Children with asthma were randomly divided into control group and treatment group. The control group was given Montelukast Sodium tablets for 4 mg (2-5 years old) or 5 mg (6-14 years old), once every night before sleeping. At the same time, the treatment group was given Pingchuan water decoction additionally for one tie per day, in four to six-divided doses for eight weeks. On the other hand, groups of health children were selected as blank control. Before and after treatment, the level of IL-4, IL-13 and IFN-gamma were detected by elisa from 3 mL of venous blood. Before treatment, IL-4 and IL-13 in two groups were obviously higher than healthy group, but IFN-gamma was lower (P < 0.01, P < 0.05). After eight weeks, IL-4 and IL-13 in treatment group went down, but IFN-gamma increased. And there were significant different compared with the control group (P < 0.05). Treating children asthma by integrated traditional Chinese and western medicine can obviously reduce IL4 and IL-13, increase IFN-gamma, and therefore lighten the airway inflammation, prevent asthma attacks effectively.