Bioavailability of Orally Administered Micronised Fluticasone Propionate

Falcoz, Christine; Oliver, Ruth; McDowall, Jo E.; Ventresca, Pietro; Bye, Alan; Daley‐Yates, Peter T.

doi:10.2165/00003088-200039001-00002

Cited by 58 publications

(38 citation statements)

References 4 publications

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“…In studies by Kerwin et al (16) and Bernstein et al (18), Fp AUC 0-t and C max increased approximately dose proportionally across the dose levels tested (Fp MDPI 12.5, 25, 50, 100, 200, and 400 mcg). (19,20). The results of these previously published studies and of the present study suggest more efficient delivery of Fp and salmeterol via the MDPI device compared with the DPI device.…”

Section: Discussionsupporting

confidence: 71%

The pharmacokinetics, safety, and tolerability of single, high-strength doses of fluticasone propionate and fluticasone propionate/salmeterol delivered via a novel multidose dry powder inhaler in adolescents and adults with persistent asthma

et al. 2017

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Objective: Characterize fluticasone propionate (Fp) and combination fluticasone propionate and salmeterol (FS) pharmacokinetic and safety profiles, delivered via a novel, inhalation-driven, multidose dry powder inhaler (MDPI). Methods: This multicenter, open-label, four-period crossover, single-dose study randomized patients aged ࣙ12 years with persistent asthma to Fp MDPI 200 mcg, FS MDPI 200/12.5 mcg, Fp dry powder inhaler (DPI) 500 mcg (250 mcg × 2 inhalations), or FS DPI 500/50 mcg. Blood samples for determination of Fp and salmeterol pharmacokinetic parameters including C max , AUC 0-t , AUC 0-inf , t max , and t ½ were collected predose through 36 h postdose (14 time points). Safety assessments comprised adverse events, vital signs, and physical examinations. The institutional review board approved the study protocol. Results: The pharmacokinetic analysis set and safety population each included 40 patients. Fp systemic exposure (C max , AUC 0-t , and AUC 0-inf ) was highest for Fp DPI 500 mcg and similar for Fp MDPI 200 mcg, FS MDPI 200/12.5 mcg, and FS DPI 500/50 mcg. Fp geometric mean t ½ values were similar across treatments. Salmeterol C max was 20% lower and AUC 0-t and AUC 0-inf were approximately 50% lower with FS MDPI versus FS DPI. Median t max and geometric mean t ½ were similar between FS MDPI and FS DPI. Adverse events were similar across treatments with no relevant changes in vital signs, physical examinations, or hematology test results. Conclusions: Fp MDPI and FS MDPI produced similar or lower systemic exposure to Fp and salmeterol, despite lower doses, versus conventional DPI devices, suggesting improved efficiency due to formulation and device differences.

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Section: Discussionsupporting

confidence: 71%

The pharmacokinetics, safety, and tolerability of single, high-strength doses of fluticasone propionate and fluticasone propionate/salmeterol delivered via a novel multidose dry powder inhaler in adolescents and adults with persistent asthma

et al. 2017

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“…Some 99% of the dose swallowed is inactivated by first-pass metabolism, 17 and there is negligible oropharyngeal absorption. 18 Also, when the study was planned, we were aware that the formulation containing the HFA propellant would be replacing the CFC product, and no data on delivery of the HFA product in young children were available.…”

Section: Product Selectionmentioning

confidence: 99%

Lung bioavailability of hydrofluoroalkane fluticasone in young children when delivered by an antistatic chamber/mask

Khan

Tang

Hochhaus

et al. 2006

The Journal of Pediatrics

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“…FP is well tolerated having a low potential to cause adverse systemic effects. Compared to first-generation topical corticosteroids such as betamethasone, the compound yields little hypothalamic-pituitary-adrenal axis effects reflecting the high quotient between topical activity and systemic activity due to its lipophilicity [24,25] and its hepatic metabolism to the inactive moiety 17ß-carboxylic acid [26,27]. In a clinical trial investigating the propensity for systemic absorption, 25 g FP 0.05% cream were allotted twice daily under occlusion for 5 days in one group, and 12.5 g FP 0.05% cream were applied twice daily without occlusion for 21 days in the other group.…”

Section: Potential For Systemic Adverse Eventsmentioning

confidence: 99%

Safety and Efficacy of Fluticasone Propionate in the Topical Treatment of Skin Diseases

Roeder

Schaller

Schäfer‐Korting

et al. 2004

Skin Pharmacol Physiol

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Fluticasone propionate – the first carbothioate corticosteroid – has been classified as a potent anti-inflammatory drug for dermatological use. It is available as 0.05% cream and 0.005% ointment formulations for the acute and maintenance treatment of patients with dermatological disorders such as atopic dermatitis, psoriasis and vitiligo. This glucocorticoid is characterized by high lipophilicity, high glucocorticoid receptor binding and activation, and a rapid metabolic turnover in skin. Although skin blanching following fluticasone propionate exceeds that of corticosteroids of medium strength, several clinical trials demonstrate a low potential for cutaneous and systemic side-effects, even in difficult-to-treat areas like the face, the eyelids and intertriginous areas. Even among paediatric patients with atopic dermatitis, fluticasone propionate proved to be safe and effective. These pharmacological and clinical properties are reflected by the high therapeutic index of this glucocorticoid.

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Bioavailability of Orally Administered Micronised Fluticasone Propionate

Cited by 58 publications

References 4 publications

The pharmacokinetics, safety, and tolerability of single, high-strength doses of fluticasone propionate and fluticasone propionate/salmeterol delivered via a novel multidose dry powder inhaler in adolescents and adults with persistent asthma

The pharmacokinetics, safety, and tolerability of single, high-strength doses of fluticasone propionate and fluticasone propionate/salmeterol delivered via a novel multidose dry powder inhaler in adolescents and adults with persistent asthma

Lung bioavailability of hydrofluoroalkane fluticasone in young children when delivered by an antistatic chamber/mask

Safety and Efficacy of Fluticasone Propionate in the Topical Treatment of Skin Diseases

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