Oral bioavailability and pharmacokinetics of sildenafil citrate dry foam tablets in rats

Sawatdee, Somchai; Atipairin, Apichart; Yoon, Attawadee Sae; Srichana, Teerapol; Changsan, Narumon; Suwandecha, Tan; Chanthorn, Wirot; Phoem, Atchara Nuphet

doi:10.1080/2331205x.2018.1510821

Cited by 7 publications

(7 citation statements)

References 22 publications

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“…The exposure-time courses of ivabradine (Zhang et al, 2016), sildenafil (Sawatdee et al, 2018), dofetilide (Smith et al, 1992), and pimobendan (Asakura et al, 1993) were previously studied in Sprague-Dawley rats (200-300g) and showed slightly different pharmacokinetic properties compared to the larger Han-Wistar (450-600g) used here ( Figure 6). This highlights the necessity of exposure-time courses obtained in the actual animal strain for model development.…”

Section: Exposure-time Courses Of Test Compoundsmentioning

confidence: 88%

An Integrative Approach for Improved Assessment of Cardiovascular Safety Data

Wallman

Scheuerer

Martel

et al. 2021

J Pharmacol Exp Ther

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Section: Exposure-time Courses Of Test Compoundsmentioning

confidence: 88%

An Integrative Approach for Improved Assessment of Cardiovascular Safety Data

Wallman

Scheuerer

Martel

et al. 2021

J Pharmacol Exp Ther

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“…Group II: (TAM) received only tamoxifen (90 mg/kg i.p.). 7 Group III: (TAM + SIL) received Sildenafil (40 mg/kg, orally for five consecutive days), 16,27 tamoxifen were injected 1 h after last injection. Group IV: (TAM + IRR) rats exposed to LDR (0.5 Gy) after 24 h tamoxifen were injected.…”

Section: Experimental Designmentioning

confidence: 99%

Nrf2 and NF‐қB interplay in tamoxifen‐induced hepatic toxicity: A promising therapeutic approach of sildenafil and low‐dose γ radiation

Karam

Galal

Lotfy

2023

Environmental Toxicology

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Tamoxifen-induced hepatotoxicity is an inevitable side effect during breast cancer treatment. Low-dose gamma irradiation (IRR) shows many beneficial effects by stimulating various biological processes. This study evaluates the possible effect of sildenafil and low-dose gamma radiation on liver damages as new treatment strategies.Group I (control), group II: (tamoxifen), group III: (tamoxifen + Sildenafil), group IV:(tamoxifen+ irradiation) and group V: (tamoxifen +Sildenafil + irradiation). Rats were sacrificed after 5 h from tamoxifen injection. Results showed that tamoxifen caused elevation in serum AST, ALT and ALP as well hepatic ROS, iNOS, MDA, Keap-1 and NF-Kb, in addition to diminution in hepatic Nrf2 and HO-1. Exposure to low-dose gamma radiation and sildenafil amended the alterations in the measured parameters in serum and tissue. Moreover, all results were confirmed by histopathological examination. In conclusion, sildenafil and low-dose gamma radiation can mitigate the toxicity induced by tamoxifen in liver tissues. Hence, this treatment could be further evaluated as a new approach for alleviating various liver disorders.

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“…Statistically important reduction in absorption rate is observed whereas sildenafil is co-administered with high fat meal (delayed t max by 1 h in fed state compared to 30–120 min t max in fasted state, 90% confidence intervals CI: 0.7 ± 1.5 using ANOVA appropriate design) as well as in mean C max (−29% in fed state, 90% CI: 19 ± 38) [ 60 ]. The combination of food effects with the diminished bioavailability due to extensive first path metabolism [ 60 ], has led contemporary researchers to focus on upgrading the existing oral dosage formulations [ 96 , 97 , 98 , 99 , 100 ] and even apply alternative routes of administration i.e., intranasal, transdermal and intravenously [ 101 , 102 , 103 ].…”

Section: Alternative Administration Schemesmentioning

confidence: 99%

“…The material was then mixed with croscarmellose sodium, magnesium stearate and compressed into tablets [ 117 ]. The final formulation was administrated orally to male Wistar rats and resulted in systemic bioavailability of 1.5 and 1.9 times higher than that of commercial version of sildenafil film-coated tablet and sildenafil powder of 20 mg/kg sildenafil, respectively [ 100 ]. Comparing to the sublingual delivery system mentioned above the bioavailability of the dry foam tablets was lower [ 98 ] due to the rich blood supply of the sublingual vessels and the hepatic first pass metabolism escape or due to the physiological variation between the animal species.…”

Section: Alternative Administration Schemesmentioning

confidence: 99%

Sildenafil 4.0—Integrated Synthetic Chemistry, Formulation and Analytical Strategies Effecting Immense Therapeutic and Societal Impact in the Fourth Industrial Era

et al. 2021

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Sildenafil is a potent selective, reversible inhibitor of phosphodiesterase type 5 (PDE5) approved for the treatment of erectile dysfunction and pulmonary arterial hypertension. Whilst twenty years have passed since its original approval by the US Food and Drug Administration (USFDA), sildenafil enters the fourth industrial era catalyzing the treatment advances against erectile dysfunction and pulmonary hypertension. The plethora of detailed clinical data accumulated and the two sildenafil analogues marketed, namely tadalafil and vardenafil, signify the relevant therapeutic and commercial achievements. The pharmacokinetic and pharmacodynamic behavior of the drug appears complex, interdependent and of critical importance whereas the treatment of special population cohorts is considered. The diversity of the available formulation strategies and their compatible administration routes, extend from tablets to bolus suspensions and from per os to intravenous, respectively, inheriting the associated strengths and weaknesses. In this comprehensive review, we attempt to elucidate the multi-disciplinary elements spanning the knowledge fields of chemical synthesis, physicochemical properties, pharmacology, clinical applications, biopharmaceutical profile, formulation approaches for different routes of administration and analytical strategies, currently employed to guide the development of sildenafil-based compositions.

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Oral bioavailability and pharmacokinetics of sildenafil citrate dry foam tablets in rats

Cited by 7 publications

References 22 publications

An Integrative Approach for Improved Assessment of Cardiovascular Safety Data

An Integrative Approach for Improved Assessment of Cardiovascular Safety Data

Nrf2 and NF‐қB interplay in tamoxifen‐induced hepatic toxicity: A promising therapeutic approach of sildenafil and low‐dose γ radiation

Sildenafil 4.0—Integrated Synthetic Chemistry, Formulation and Analytical Strategies Effecting Immense Therapeutic and Societal Impact in the Fourth Industrial Era

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