The oral systemic availability of fluticasone propionate in man– preliminary data [letter]

Bye, Alan

doi:10.1111/j.1365-2125.1993.tb04212.x

Cited by 8 publications

(6 citation statements)

References 6 publications

Supporting

Mentioning

Contrasting

Order By: Relevance

“…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: 72%

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

View full text Add to dashboard Cite

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.

show abstract

Section: Discussionsupporting

confidence: 72%

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

View full text Add to dashboard Cite

show abstract

“…Fluticasone propionate is practically insoluble in water but is soluble in a number of non‐polar organic solvents. The oral bioavailability using labelled and unlabelled drug is less than 1% primarily due to incomplete absorption and pre‐systemic metabolism in the gut and liver 56 . In contrast, the majority of fluticasone delivered into the lungs is absorbed systemically.…”

Section: Glucocorticosteroids In the Treatment Of Ibdmentioning

confidence: 99%

“…The oral bioavailability using labelled and unlabelled drug is less than 1% primarily due to incomplete absorption and pre-systemic metabolism in the gut and liver. 56 In contrast, the majority of¯uticasone delivered into the lungs is absorbed systemically. Binding of uticasone propionate to human GCS receptors is 18 times greater than dexamethasone, nearly twice that of beclomethasone 17-monopropionate (the active metabolite of beclomethasone dipropionate), and over three times that of budesonide.…”

Section: Local Effects Of Glucocorticosteroidsmentioning

confidence: 99%

Review article: issues in oral administration of locally acting glucocorticosteroids for treatment of inflammatory bowel disease

Friend

1998

Aliment Pharmacol Ther

View full text Add to dashboard Cite

Inflammatory bowel diseases are treated in some cases by local administration of anti‐inflammatory drugs. Local delivery of drugs in the colon following oral administration may lead to improved efficacy/side‐effect profiles and may improve patient compliance. This review covers a number of issues important in the design of oral delivery systems of glucocorticosteroids for local therapy of colonic inflammation. The choice of specific glucocorticosteroids is based on the drug’s physicochemical and pharmacological properties. The conditions under which an orally administered glucocorticosteroid (or other drug) must be delivered to treat ulcerative colitis are also discussed. These conditions include variations in local pH, transit throughout the gastrointestinal tract, the potential role of gut microflora, and drug dissolution in both the healthly and diseased large intestine. The effective delivery of topically‐active glucocorticosteroids in ulcerative colitis and Crohn’s colitis patients is complex, but if successful could improve their usefulness.

show abstract

“…Restriction diets, however, have not been successful in adults. 15 A PPI can be helpful as the already affected oesophageal mucosa could be further damaged by acid exposure. Furthermore, the pathological diagnosis of EE should be established after a patient has been on PPI therapy for at least four weeks.…”

Section: Discussionmentioning

confidence: 99%

Eosinophilic oesophagitis: an unsuspected aetiology for dysphagia in an HIV-positive patient

Batog¹,

Psevdos

Paniz-Mondolfi

et al. 2010

Int J STD AIDS

View full text Add to dashboard Cite

Patients with HIV/AIDS are often afflicted with oesophageal disorders. Opportunistic infections such as candidiasis, herpes simplex, cytomegalovirus, mycobacterial infections, Kaposi sarcoma or lymphoma involving the oesophagus, motility disorders and reflux oesophagitis are the usual culprits. Eosinophilic oesophagitis (EE), a recently recognized entity, is an important cause of dysphagia, food impaction and chest discomfort. We report the case of an HIV-infected man who had persistent dysphagia for six months despite treatment with proton pump inhibitor. He was diagnosed with EE after having endoscopic evaluation and biopsy of his oesophagus and was successfully treated with swallowed fluticasone. This case represents the first reported case of EE in an HIV-infected individual.

show abstract

The oral systemic availability of fluticasone propionate in man– preliminary data [letter]

Cited by 8 publications

References 6 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

Review article: issues in oral administration of locally acting glucocorticosteroids for treatment of inflammatory bowel disease

Eosinophilic oesophagitis: an unsuspected aetiology for dysphagia in an HIV-positive patient

Contact Info

Product

Resources

About