ABSTRACT
Background: Arformoterol, the (R, R) enantiomer of the racemic (R, R / S, S) diastereomer, formoterol, is a short and long acting ?2 agonist bronchodilator. Levosalbutamol, the (R, R) enantiomer of racemic diastereomer (R, R / S, S) salbutamol, has a greater affinity for the ?2 receptor. Occupation of ?2 receptors by agonists result in the activation of the Gs-adenylyl cyclase-cAMP-PKA pathway, followed by phosphorylative events leading to bronchial smooth muscle relaxation. The aim of this pharmacoepidemiological study was to analyse the prescription patterns, and prescription content analysis, of arformoterol, levosalbutamol, formoterol or salbutamol, in non-severe asthma exacerbation in tertiary care hospitals, not needing hospitalization.Methods: It was a multi-centre, retrospective, observational and analytical study of 100 asthmatic patients’ hospital medical records, treated with 3 doses of arformoterol, levosalbutamol, formoterol or salbutamol nebulization, followed by peak expiratory flow rates (PEFR) measurement at the baseline and 6 minutes, after each dose; along with adverse effects recording. The number of prescriptions of 100 patients was recorded, the percentage of prescriptions was calculated, and the prescription content analysis was done.Results: PEFR of the patients showed significant increase after the first, second and third doses of bronchodilator nebulisation, with negligible adverse effects. Salbutamol was most commonly prescribed (45 prescriptions, 45%), followed by levosalbutamol (35 prescriptions, 35%), formoterol (15 prescriptions, 15%) and arformoterol (5 prescriptions, 5%). All aspects of prescription content analysis showed 100% completeness.Conclusions: Arformoterol was more effective, but equally safe, as compared to levosalbutamol, formoterol and salbutamol. Prescription frequency of salbutamol was followed by levosalbutamol, formoterol and arformoterol. Prescription content analyses showed 100% completeness.
ABSTRACT
Background: The objective of the study was to compare the efficacy between levosalbutamol and ipratropium combination over levosalbutamol nebulisation in reversing airflow obstruction and improve oxygenation, evaluated using the pulmonary asthma score, SaO2, and PEFR in mild and moderate asthma.Methods: A prospective, randomized, study was performed in RMMCH pediatric emergency department. Children between 6 and 12 years of age who presented with mild to moderate asthma exacerberations were enrolled in the study. They were randomly allocated into two different groups: one nebulised with levosalbutamol alone and another with addition of ipratropium bromide to levosalbutamol. Baseline Peak expiratory flow rate and Final absolute values or change from baseline 60-120 minutes after the inhalation are measured. Patients were evaluated using the pulmonary score.Results: After treatment there is improvement in the mean pulmonary asthma scores and PEFR percentage in A+B group than A group, but it is not statistically significant (p value >0.05). There is statistically significant improvement in pulmonary asthma score and PEFR in each of the groups after nebulisation and pulmonary asthma score has a sensitivity of 66.7% and 65.6% in diagnosing severity of asthma in relation to PEFR.
ABSTRACT
OBJECTIVE: To select excipients and optimize preparation for the ambroxol hydrochloride/levosalbutamol sulfate dry powder inhalation. METHODS: Drug and different excipients in the same ratio were prepared by spray drying to obtain a certain particle size as drug particles or carriers for dry powder inhalation, respectively. Study and compare the parameters of powders of the dry powder inhaler, such as the angle of repose, moisture content, and emptying rate, etc, to screen the excipient of the vectors. Afterward, Box-Behnken design method was adopted to optimize of preparation parameters. RESULTS: When lactose-high branched cyclodextrin compounds were used as composite carriers, their powder properties meet the requirements of dry powder inhaler, such as the repose angle was 39.69 degrees, the bulk density was 0.37 g·mL-1, the tap density was 0.66 g·mL-1, the evacuation rate of drug-carrier powders in capsules was 93.12%, and the water content was 0.10% and the simulated lung deposition rate was 14.63%. The preparation parameters, such as sample concentration, inlet air temperature, nozzle diameter parameters, theirs values were 50 mg·mL-1, 110℃, 1 mm, respectively, were opmized by Box-Behnken design method, which could obtain the carrier particle size of 30.33 μm. CONCLUSION: Lactose-high branched cyclodextrin complexes can be used as carrier for levosalbutamol sulfate-ambroxol hydrochloride compound dry powder inhaler, which could meet the requirements of dry powder inhaler by spray-drying preparation method.
ABSTRACT
Abstracts: Background: This study compared the efficacy of levosalbutamol alone and ipratropium bromide alone with levosalbutamol and ipratropium bromide combined, through inhalational route in stable patients of chronic obstructive pulmonary disease (COPD). The study was carried out in 102 patients of COPD. Levosalbutamol inhalation was administered to 33 patients and ipratropium bromide inhalation was given to 31 patients.38 patients were treated with combination of levosalbutamol and ipratropium bromide inhalation. Pulmonary functions were noted before and after 15, 30, 60,120,180 and 240 minutes of inhalation of these drugs. Bronchodilation was significantly more in patients treated with combination therapy as compared to patients treated with single drug separately. The effect was more sustained in combination therapy as it started declining after 120 minutes with levosalbutamol, after 180 minutes in ipratropium bromide and after 240 minutes with combination therapy. So it was concluded that combination therapy with levosalbutamol and ipratropium bromide is better in management of COPD patients than using either of agents alone.
ABSTRACT
A novel, simple, accurate and precise RP-HPLC method for simultaneous determination of levosalbutamol sulfate and theophylline has been developed and validated. Separation was achieved on a Phenomenex; C18 column (250 mm × 4.6 mm i.d., 5 µm) using methanol: 10 mM TBAHS(tetrabutyl ammonium hydrogen sulfate) (50:50, v/v) as mobile phase at flow rate of 1.0 mL.min-1. The UV detection wavelength was 274 nm. The linearity is obeyed over a concentration range of 0.5-150 µg.mL-1 with correlation coefficient of 0.999 for both the drugs. The proposed method was validated by determining accuracy, precision, stability and system suitability parameters. The method was found to be robust. Specificity of the method was determined by subjecting the drugs to various stress conditions like acid, alkali, oxidation, thermal and photolytic degradation. The method was used successfully for the simultaneous determination of levosalbutamol sulfate and theophylline in syrup dosage form.
Desenvolveu-se e validou-se método de RP-HPLC novo, simples, exato e preciso de determinação simultânea do sulfato de levossalbutamol e teofilina.. A separação foi efetuada em uma coluna Phenomenex; C18 (250 mm x 4,6 mm d.i., 5 µm) utilizando metanol: TBAHS (hidrogenossulfato de tetrabutilamônio) 10 mM (50:50, v/v) como fase móvel, com fluxo de 1,0 mL.min-1. O comprimento de onda de detecção no UV foi 274 nm. Observou-se linearidade na faixa de concentração de 0,5-150 µg mL-1, com coeficiente de correlação de 0,999 para ambos os fármacos. O método proposto foi validado determinando-se exatidão, precisão, estabilidade e parâmetros de adequação do sistema. O método mostrou-se robusto. A especificidade do método foi determinada submetendo os fármacos a várias condições de estresse, como ácido, álcali, oxidação, degradação térmica e fotolítica. O método foi usado com sucesso para a determinação simultânea do sulfato de levossalbutamol e teofilina na forma de xarope.
Subject(s)
Theophylline/analysis , Chromatography, High Pressure Liquid/methods , Levalbuterol/analysis , Dosage FormsABSTRACT
A simple, rapid and accurate RP-HPLC method was developed for the determination of levosalbutamol in pure and tablet dosage form by RP-HPLC method using C18 BDS column (Phenomenex, 250 x 4.6 mm, 5 μm) in isocratic mode. The mobile phase consisted of Acetonitrile and buffer in the ratio of 20:80 (v/v) was used and maintain the pH 3. The flow rate was maintained at 1 mL/min and the injection volume was 20 μL . Detection wavelength with UV detector at 276 nm and run time was kept 10 min. The retention time of levosalbutamol was 5.4 min. The method was linear over the concentration range 7-12 μg/ml. The recovery was found to be 100.44± 0.27%. The validation of method was carried out utilizing ICH-guidelines. The described HPLC method was successfully employed for the analysis of pharmaceutical formulations.
ABSTRACT
Objective. To compare efficacy and tolerability of levosalbutamol (Group 1) and racemic salbutamol (Group 2) for the treatment of acute exacerbation of asthma in children age 5 to 18 yr. Methods. A randomized double blind clinical study involving 60 children was undertaken between October ’06 to December ’07. Results. The following baseline clinical characteristic were recorded initially and after giving 3 nebulizations at 20 min intervals in the Ist hour of presentation viz respiratory rate (RR), heart rate (HR), oxygen saturation in room air SPO2, PEFR (peak expiratory flow rate), serum K+ level and asthma score. In Group 1 patients (levosalbutamol), there was significant increment in SPO2 and PEFR (P<0.05) values with decrease in tachypnea and asthma score while no significant difference was found in pre and post treatment HR & Serum K+ levels. In Group 2 patients although there was clinical improvement in terms of SPO2, PEFR, RR and asthma score, it resulted in significant tachycardia and decrease in K+ levels. Conclusion. Levosalbutamol appears to be more efficacious than racemic salbutamol in terms of improvement in PEFR, SPO2 and asthma score while deleterious effects of tachycardia and fall in serum K+ were seen with racemic salbutamol.