Sildenafil citrate monohydrate–cyclodextrin nanosuspension complexes for use in metered-dose inhalers

Sawatdee, Somchai; Phetmung, Hirihattaya; Srichana, Teerapol

doi:10.1016/j.ijpharm.2013.07.023

Cited by 35 publications

(24 citation statements)

References 38 publications

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“…[18,19] Moreover, volatile oils can be transformed to their CD complex solid powders against evaporation. [20,21] Recently, CDs have become a potential excipient for pulmonary delivery to improve bioavailability of peptides, [22] enhance the solubility and bioavailability of water-insoluble drugs [23][24][25][26] and decrease drug doses. [27] Furthermore, CDs can improve drug absorption after pulmonary delivery.…”

Section: Introductionmentioning

confidence: 99%

Pulmonary delivery of tea tree oil-β-cyclodextrin inclusion complexes for the treatment of fungal and bacterial pneumonia

Li¹,

Zhu

Zhang

et al. 2017

Journal of Pharmacy and Pharmacology

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Section: Introductionmentioning

confidence: 99%

Pulmonary delivery of tea tree oil-β-cyclodextrin inclusion complexes for the treatment of fungal and bacterial pneumonia

Li¹,

Zhu

Zhang

et al. 2017

Journal of Pharmacy and Pharmacology

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“…Dosing of sildenafil for pulmonary administration was performed according to Sawatdee and co-authors with 20 µg sildenafil per puff. 6,7 Lactose monohydrate, which was used as a carrier, was reduced by a grinding mill (Fritsch, Germany) for 3 h to obtain micronized particles (particle size ranged from 1-5 μm for use as a fine carrier). The coarse lactose monohydrate particles (50-100 μm) were used from the original material.…”

Section: Preparation Of Sildenafil Citrate Dry Powder Inhalermentioning

confidence: 99%

“…[3][4][5] Currently, sildenafil has been developed as an inhaler to treat pulmonary hypertension for delivered to the lung included of dry powder inhaler (DPI), metered-dose inhaler and nebulizer for avoiding unwanted systemic side-effects and rapid drug action. [6][7][8][9][10][11] There are previously report sildenafil citrate complexed with α-cyclodextrin to enhance the solubility of sildenafil as a linear function of cyclodextrin concentration. 12 The complex of sildenafil citrate and α-cyclodextrin is one-to-one complex formation.…”

Section: Introductionmentioning

confidence: 99%

Development of Spray-Dried Sildenafil Citrate -α-cyclodextrin Complexes for Use in Dry Powder Inhalers

Atipairin

Sawatdee

2020

IJPI

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Background: Sildenafil citrate is a drug used in the treatment of pulmonary hypertension. The development of sildenafil citrate complexed with α-cyclodextrin as dry powder inhaler (DPI) should enhance its solubility in the lung. Methods: Sildenafil citrate was dissolved with α-cyclodextrin solution at pH 4.5 to obtain inclusion complexes. The complex solution was spray-dried to make spheroidal powder. The sildenafil DPI formulations were mixed with coarse lactose and fine lactose as carriers and then filled in capsule no. 2. Three different ratios of course to fine lactose were used (1:1 (#1), 2:1 (#2) and 3:1 (#3)) to optimize the performance and aerosol properties. The fine particle fraction (FPF), mass median aerodynamic diameter (MMAD) and geometric standard deviation (GSD) were used to evaluate the in vitro drug delivery performance in the lung by in vitro. Results: The proportion of sildenafil in formulations #1, #2, #3 was 100.2% ± 0.1%, 100.1% ± 0.2% and 98.9% ± 0.1%, respectively. The aerosol properties of the best formulation (#2) were as follows: an ED of 85.5 ± 0.5%, an FPF of 56.6 ± 2.3%, an MMAD of 3.2 ± 0.6 µm and a GSD of 1.02±0.01. Conclusion: Sildenafil citrate complexed with α-cyclodextrin was successfully developed for a DPI by using coarse and fine lactose monohydrate in a 2:1 ratio.This is an open access article distributed under the terms of the Creative Commons Attribution-NonCommercial-ShareAlike 4.0 License, which allows others to remix, tweak, and build upon the work non-commercially, as long as the author is credited and the new creations are licensed under the identical terms.

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“…SILC is a compound of the pyrazolopyrimidinyl-methyl piperazine class used not only for erectile dysfunction treatment but also for pulmonary arterial hypertension (Escribano, Jimínez, Calzada, 2005;American College of Cardiology Foundation;American Heart Association, 2009;Galiè et al, 2010, Sawatdee, Phetmung, Srichana, 2013.…”

Section: Introductionmentioning

confidence: 99%

Development and validation of alternative methods by non-aqueous acid-base titration and derivative ultraviolet spectrophotometry for quantification of sildenafil in raw material and tablets

Silva

Toledo

Vianna-Soares

2017

Braz. J. Pharm. Sci.

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Sildenafil citrate (SILC) is a potent phosphodiesterase-5 inhibitor used for erectile dysfunction and pulmonary hypertension. This study shows two simple, fast and alternative analytical methods for SILC determination by non-aqueous titration and by derivative ultraviolet spectrophotometry (DUS) in active pharmaceutical ingredient and/or dosage forms. The quantitation method of SILC active pharmaceutical ingredient by non-aqueous acid-base titration was developed using methanol as solvent and 0.1 mol/L of perchloric acid in acetic acid as titrant. The endpoint was potentiometrically detected. The non-aqueous titration method shows satisfactory repeatability and intermediate precision (RSD 0.70-1.09%). The neutralization reaction occurred in the stoichiometric ratio 1:1 in methanol. The determination of SILC active pharmaceutical ingredient or dosage forms by DUS was developed in the linear range from 10 to 40 µg/mL, in 0.01 mol/L HCl, using the first order zero-peak method at λ 256 nm. The DUS method shows selectivity toward tablets excipients, appropriate linearity (R 2 0.9996), trueness (recovery range 98.86-99.30%), repeatability and intermediate precision in three concentration levels (RSD 1.17-1.28%; 1.29-1.71%, respectively). Therefore, the methods developed are excellent alternatives to sophisticated instrumental methods and can be easily applied in any pharmaceutical laboratory routine due to simple and fast executions.Uniterms: Sildenafil citrate. Vasodilator. Derivative ultraviolet spectrophotometry. Non-aqueous acidbase titrimetry. Sildenafil citrate/quality control.

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Sildenafil citrate monohydrate–cyclodextrin nanosuspension complexes for use in metered-dose inhalers

Cited by 35 publications

References 38 publications

Pulmonary delivery of tea tree oil-β-cyclodextrin inclusion complexes for the treatment of fungal and bacterial pneumonia

Pulmonary delivery of tea tree oil-β-cyclodextrin inclusion complexes for the treatment of fungal and bacterial pneumonia

Development of Spray-Dried Sildenafil Citrate -α-cyclodextrin Complexes for Use in Dry Powder Inhalers

Development and validation of alternative methods by non-aqueous acid-base titration and derivative ultraviolet spectrophotometry for quantification of sildenafil in raw material and tablets

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