Pharmacokinetic parameters and a theoretical study about metabolism of BR-AEA (a salbutamol derivative) in rabbit

Soriano-Ursúa, Marvin A.; Correa‐Basurto, José; Romero-Huerta, Juan; Elizalde-Solis, Octavio; Galicia‐Luna, Luis A.; Trujillo‐Ferrara, José G.

doi:10.3109/14756360903179450

Cited by 7 publications

(1 citation statement)

References 29 publications

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“…The drug content from the different organs was estimated using high-performance liquid chromatography. 36 The known quality of salbutamol within the plasma was withdrawn into microtubes and an internal standard (terbutaline sulphate) was added. Then, this was centrifuged, and the supernatant was separated and injected into a C18 column (50 μm, 70 A).…”

Section: Tissue Distribution Targeting Efficiency and Pharmacokinetmentioning

confidence: 99%

<p>An Efficient, Lung-Targeted, Drug-Delivery System To Treat Asthma Via Microparticles</p>

Sreeharsha

Venugopala

Nair

et al. 2019

DDDT

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Background: Chronic diseases such as diabetes, asthma, and heart disease are the leading causes of death in developing countries. Public health plays an important role in preventing such diseases to improve individuals' quality of life. Conventional dosage schemes used in public health to cure various diseases generally lead to undesirable side effects and renders the overall treatment ineffective. For example, a required concentration of drug cannot reach the lungs using conventional methods to cure asthma. Microspheres have emerged as a confirmed drug-delivery system to cure asthma. Method: In this paper, a salbutamol-loaded poly lactic acid-co-glycolic acid-polyethylene glycol (PLGA-PEG) microsphere (SPP)-based formulation was prepared using a Buchi B-90 nanospray drier. Face-centered central composite design (CCD) was applied to optimize the spray-drying process. Results: The drug content and product yield were found to be 72%±0.8% and 86%±0.4%, respectively; drug release (91.1%) peaked for up to 12 hrs in vitro. Microspheres obtained from the spray dryer were found to be shriveled. The experiments were carried out and verified using various groups of rabbits. In our study, the particle size (8.24 µm) was observed to be an essential parameter for drug delivery. The in vivo results indicated that the targeting efficacy and drug concentration in the lung was higher with the salbutamolloaded PLGA-PEG SPP formulation (1,410.1±10.11 µg/g, 15 mins), as compared to the conventional formulation (92±0.56 µg/g, 10 min). The final product was stable under 5°C±2°C , 25°C±2°C, and 40°C±2°C/75%±5% relative humidity. In addition, these co-polymers have a good safety profile, as determined by testing on human alveolar basal epithelium A549 cell lines. Conclusion: Our results prove that microspheres are an alternative drug-delivery system for lung-targeted asthma treatments used in public health.

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Section: Tissue Distribution Targeting Efficiency and Pharmacokinetmentioning

confidence: 99%

<p>An Efficient, Lung-Targeted, Drug-Delivery System To Treat Asthma Via Microparticles</p>

Sreeharsha

Venugopala

Nair

et al. 2019

DDDT

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Boron-Containing Compounds for Prevention, Diagnosis, and Treatment of Human Metabolic Disorders

Rodríguez-Vera

et al. 2022

Biol Trace Elem Res

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Cell-based and in-silico studies on the high intrinsic activity of two boron-containing salbutamol derivatives at the human β2-adrenoceptor

Soriano-Ursúa¹,

McNaught-Flores²,

Nieto-Alamilla³

et al. 2012

Bioorganic & Medicinal Chemistry

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Pharmacokinetic parameters and a theoretical study about metabolism of BR-AEA (a salbutamol derivative) in rabbit

Abstract: (2010) Pharmacokinetic parameters and a theoretical study about metabolism of BR-AEA (a salbutamol

Cited by 7 publications

References 29 publications

<p>An Efficient, Lung-Targeted, Drug-Delivery System To Treat Asthma Via Microparticles</p>

<p>An Efficient, Lung-Targeted, Drug-Delivery System To Treat Asthma Via Microparticles</p>

Boron-Containing Compounds for Prevention, Diagnosis, and Treatment of Human Metabolic Disorders

Cell-based and in-silico studies on the high intrinsic activity of two boron-containing salbutamol derivatives at the human β2-adrenoceptor

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