Bambuterol 20mg tablets

Silver nanoparticles (AgNPs) were found to significantly quench the fluorescence of bambuterol hydrochloride (BAM) and its active metabolite terbutaline sulfate (TER). The intrinsic fluorescence intensity of each of BAM (at 264/292 nm) and TER (at 276/306 nm) decreased by the gradual addition of AgNPs. Quenching of the steady state fluorescence of BAM and TER probably resulted from the energy transfer to the photo-excited state of AgNPs. The estimated Stern–Volmer quenching constant at several temperature settings proved that the quenching mechanism of the two drugs was dynamic quenching in case of BAM while it was static quenching in case of TER. The number of binding sites, binding constants, and corresponding thermodynamic parameters depending on the interaction system were estimated at 293, 313, and 333 °K and the results obtained were interpreted.

Abstract licence: CC BY 4.0

Selective butyrylcholinesterase inhibitors are considered promising drug candidates for the treatment of Alzheimer’s disease. In this work, one rivastigmine–bambuterol hybrid (MTR-1) and fourteen of its analogues were synthesized, purified, and characterized. In vitro cholinesterase assays showed that all the compounds were more potent inhibitors of BChE when compared to AChE. Further investigations indicated that MTR-3 (IC50(AChE) > 100,000 nM, IC50(BChE) = 78 nM) was the best compound in the series, showing high butyrylcholinesterase selectivity and inhibition potency, the potential to permeate the blood–brain barrier, and longer-lasting BChE inhibition than bambuterol. These compounds could be used to discover novel specific BChE inhibitors for the treatment of Alzheimer’s disease.

Abstract licence: CC BY 4.0

Bambuterol is a long-acting anti-asthmatic prodrug which releases terbutaline. Terbutaline is an agonist of the β2-adrenergic receptors which is formed by decarbamoylation of bambuterol by butyrylcholinesterase. Inhibition of the latter, as well as activation of β2-AR, are of interest for the treatment of Alzheimer's disease (AD). Combining these two activities, bambuterol could express a good clinical efficacy against AD. The present work firstly confirmed the capacity of bambuterol to display in cellulo neuroprotective activities, reduction of Tau hyperphosphorylation and preservation of synapses in rat hippocampal neuronal cultures intoxicated with Aβ peptides. Further, bambuterol, in the form of a liposomal gel, showed a good bioavailability in CNS after intranasal administration, which should reduce any side effects linked to peripheral terbutaline release. Indeed, even if the latter is more selective than other β2-mimetics towards bronchial β2-AR, cardiovascular effects (tachycardia, arrhythmias…) could occur upon cardiac β1-AR activation. Finally, intranasal administration of low doses of bambuterol gel in mice intoxicated with Aβ peptides, prevented long-term spatial memory impairment and showed beneficial effects on the survival of neurons and on synapse preservation.

Abstract licence: CC BY-NC-ND 4.0

Quantitative 1H-NMR became an increasingly important issue in pharmaceutical analytical chemistry. This study used NMR spectroscopy to assay the bronchodilator drug terbutaline sulfate and its pro-drug bambuterol hydrochloride in pure form and pharmaceutical preparations. The technique proceeded using deuterium oxide (D2O) as an 1H-NMR solvent and phloroglucinol anhydrous as an internal standard (IS). Comparatively, to the phloroglucinol signal at 5.9 ppm, the resulting quantitative signals of the studied drugs were corrected. The terbutaline singlet signal at 6.3 ppm was chosen for quantification, while the bambuterol quantitative singlet signal was at 2.9 ppm. The two drugs were rectilinear over the concentration range of 1.0–16.0 mg/mL. LOD values were 0.19 and 0.21 mg/mL while LOQ values were 0.58 and 0.64 mg/mL for terbutaline and bambuterol respectively. The developed method has been validated according to the International Conference of Harmonization (ICH) regarding linearity, accuracy, precision, specificity, and robustness. A greenness profile assessment was applied, and the method proved to be green. The method enables the assay of the two drugs in pure drug and pharmaceutical preparations. The method also enables the assay of the two drugs in the presence of each other; thus, it is considered a stability-indicating method where terbutaline is an acid degradation product of bambuterol.

Abstract licence: CC BY 4.0

This study proposes a new approach for the in-vitro evaluation of antioxidant profile of adrenergic drugs using high-performance thin-layer chromatography coupled with image analysis techniques (HPTLC-IA). In this regard, stationary phases of different polarity (Silica gel and RP-8, RP-18 W, CN and DIOL) were selected to simulate different environments and interactions that adrenergic drugs might encounter in the human body. Antioxidant activity was quantified using both DPPH• and ABTS⁺• radical scavenging assays on all five stationary phases. Image processing and analysis was used to quantitatively compare the free radical scavenging potential of the analyzed compounds after converting the RGB image into different color channels, namely the green channel for the DPPH test, and the red channel for ABTS. Chromatographic data were processed using multivariate analysis. Results revealed that highly polar compounds, that is norepinephrine, etilefrine, metaraminol and midodrine exhibited strong interactions with silica gel but limited retention on reversed-phase, while lipophilic derivatives, namely naphazoline, xylometazoline, clenbuterol and bambuterol demonstrated strong affinity for non-polar and moderately polar phases, predicting good membrane penetration and blood-brain barrier permeability. Interestingly, some β-agonists (bambuterol, fenoterol, buphenine and irsoxsuprine) with polar groups showed unexpectedly weak silica gel retention, highlighting their dominant lipophilic contributions. Regarding the antioxidant activity, the results showed that phase interactions with the stationary phase significantly influenced the activity of adrenergic drugs. Thus, the polar phases (silica gel, DIOL) enhanced radical scavenging activity, whereas non-polar phases often reduced it. The developed HPTLC-IA method, integrating selective stationary phases and two-radical assays, offers a novel and cost-effective approach for screening the possible variation of antioxidant activity of drugs after their interaction with physiological media constituents.

Abstract licence: CC BY-NC-ND

Abstract A straightforward, environmentally friendly, and precise isocratic RP-HPLC technique was developed and validated for simultaneous determination of bambuterol hydrochloride (BBL) and montelukast sodium (MTK). An Agilent chromatograph equipped with an Inertsil C18 column (250 × 4.6 mm, 5 µm) was utilized, and chromatographic separation was achieved using a mobile phase comprising ethanol and 0.025 M phosphate buffer at pH 3.0 in a 70:30 v/v ratio. The method, adhering to ICH requirements, was validated for linearity ranges of 1.00–100.00 µg/mL and 2.00–100.00 µg/mL for BBL and MTK, respectively. The validated method was successfully applied to quantify BBL and MTK in a pharmaceutical tablet dosage form, with mean recovery percentages of 100.92 ± 1.08 and 99.39 ± 1.41, respectively, indicating satisfactory accuracy. Dissolution patterns of the pharmaceutical tablet dosage form were studied in a 900 mL 0.5% sodium lauryl sulfate dissolution medium. Various assessment tools, including Analytical Eco-scale, GAPI, AGREE, RGB 12, and the green-specific model D-CHEMS-1, were employed to evaluate the health and safety hazards of the developed methods. The RP-HPLC method demonstrated sustainability, greenness, simplicity, and effectiveness, successfully determining both drugs in their dosage form and dissolution media.

Abstract licence: CC BY 4.0