Dry powder inhalation for sildenafil citrate: formulation and performance tests

Taízia Dutra Silva; Ana Carolina Guimarães Ribeiro; Raquel Braga Dutra Gonçalves; Jackson Antonio Lamounier Camargos Resende; Cristina Duarte Vianna-Soares

doi:10.1590/s2175-97902026e24570

Authors

Taízia Dutra Silva Department of Pharmaceutical Products, Faculty of Pharmacy, Federal University of Minas Gerais, Belo Horizonte, MG, Brazil , Federal University of Minas Gerais
Ana Carolina Guimarães Ribeiro Department of Pharmaceutical Products, Faculty of Pharmacy, Federal University of Minas Gerais, Belo Horizonte, MG, Brazil , Federal University of Minas Gerais
Raquel Braga Dutra Gonçalves Department of Medicine, Iguaçu University, Itaperuna, RJ, Brazil , Universidade Iguaçu
Jackson Antonio Lamounier Camargos Resende Department of Inorganic Chemistry, Federal University Fluminense, Niteroi, RJ, Brazil , Fluminense Federal University
Cristina Duarte Vianna-Soares Department of Pharmaceutical Products, Faculty of Pharmacy, Federal University of Minas Gerais, Belo Horizonte, MG, Brazil , Federal University of Minas Gerais

DOI:

https://doi.org/10.1590/s2175-97902026e24570

Keywords:

Pulmonary arterial hypertension, Sildenafil, Micronization, Dry powder inhalation, Delivered dose uniformity, Aerodynamic size distribution

Abstract

Pulmonary arterial hypertension (PAH) is a severe disease responsible for high mortality in the affected population. Due to the limitations in treatment as severe adverse effects, high cost, we aimed to develop a simple therapeutic option for pulmonary administration, using a vasodilator sildenafil citrate (SILC) in a dry powder inhalation using lactose as carrier. A formulation of micronized SILC was prepared after 30 min wet grinding of the active with the aid of a vibration shear-mill. Solid characterization by laser diffraction and X-ray powder diffraction was assessed for active. Performance tests such as delivered-dose uniformity (DDU) and aerodynamic particle size distribution (APSD), using Dosage Unit Sampling Apparatus and Andersen Cascate Impactor, respectively, were performed. The micronization of SILC resulted in a medium size of 4.54 µm and a 50^th percentile of 2.93 µm. For DDU, the total amount delivered ranged from 92.42 to 109.05% of the targeted dose, in agreement with the specified range (75.0-125.0%). For ASPD, a fine particle fraction of 35% was satisfactorily obtained. This formulation is simple and promising therapeutic option for the treatment of PAH with the advantage of being easily produced using less complex carrier matrix or equipment, in a short time.

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References

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Dry powder inhalation for sildenafil citrate: formulation and performance tests

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