Pharmakokinetische Daten für verschiedene 5-Aminosalicylsäure- und Budesonidpräparate

Klotz, Ulrich

doi:10.1007/bf03042028

Cited by 13 publications

(3 citation statements)

References 45 publications

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“…This formulation releases budesonide as it passes through the small intestine (pH > 5.5), delivering the steroid to the distal ileum and allowing treatment of terminal ileal or right-sided colonic Crohn‘s disease. 5,9,10 However, in contrast to Crohn's disease, UC typically involves the colon (and usually the left colon): 11 a pattern of disease that requires more distal distribution of budesonide than can be achieved by Entocort EC®.…”

Section: Introductionmentioning

confidence: 99%

Bioavailability profile of Uceris MMX extended-release tablets compared with Entocort EC capsules in healthy volunteers

Nicholls¹,

Harris-Collazo

Huang

et al. 2013

J Int Med Res

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Objective: To compare the pharmacokinetics of the extended-release MMX Õ formulation of budesonide (Uceris Õ ) with that of Entocort Õ EC, an extended (controlled ileal) release formulation of budesonide. Methods:Using an open-label, randomized, three-period crossover, Latin square design, healthy male or female volunteers received single doses of 6 mg Uceris Õ , 9 mg Uceris Õ or 9 mg Entocort Õ EC. Standard pharmacokinetic parameters were assessed. Results: The study included 12 subjects. The 9 mg Uceris Õ and 9 mg Entocort Õ EC formulations had comparable area under the concentration-time curve (AUC) data, but 9 mg Uceris Õ had a notably longer time to first appearance in plasma (median T lag , 6 h versus 1 h, respectively), and a delayed time to maximum concentration (median T max , 15 h versus 5 h, respectively) compared with 9 mg Entocort Õ EC. The ratio of log-transformed AUC 0-last (Uceris Õ /Entocort Õ EC) was 91% (90% confidence interval [CI] 77%, 108%) and the corresponding maximum concentration ratio was 79% (90% CI 63%, 100%). Conclusion: Uceris was associated with a similar extent (AUC) of systemic exposure to budesonide compared with that following Entocort. However, for Uceris, the pharmacokinetic profile was delayed, a pattern consistent with greater colonic delivery of the active substance.

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Section: Introductionmentioning

confidence: 99%

Bioavailability profile of Uceris MMX extended-release tablets compared with Entocort EC capsules in healthy volunteers

Nicholls¹,

Harris-Collazo

Huang

et al. 2013

J Int Med Res

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“…As previously mentioned, the bioavailability of budesonide when delivered as an enema is approximately 15% [7]. However, the budesonide enema and foam seem to be able to reach the splenic flexure and sigmoid colon after rectal application [12,13].…”

Section: Rectal Administration Of Budesonidementioning

confidence: 94%

“…Oral contraceptives do not affect the plasma levels of budesonide and at the same time budesonide does not affect the plasma levels of oral contraceptives. When administered as an enema, the bioavailability of budesonide is also low, at approximately 15% [7].…”

Section: Pharmacology Of Budesonidementioning

confidence: 99%

Budesonide: Teaching an Old Dog New Tricks for Inflammatory Bowel Disease Treatment

Angelucci

Malesci

Danese

2008

CMC

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Crohn's disease and ulcerative colitis are chronic relapsing inflammatory bowel diseases with extremely great variability in presentation and clinical course. For many decades, corticosteroids and aminosalicylates have been the mainstay of the treatment for both Crohn's disease and ulcerative colitis, for the induction and maintenance of remission, respectively. The main limiting factors for the repeated use of corticosteroids or the use as a maintenance treatment are the very high prevalence of systemic side effects, together with the possibility of developing dependency on and/or resistance to the drug, which are reported in more than one third of patients with inflammatory bowel disease. In the last decade, a number of corticosteroids with enhanced topical activity and low systemic activity have been developed. Among them, budesonide and beclomethasone dipropionate are the most used for the treatment of the inflammatory bowel diseases. Indeed, budesonide is the drug of choice for the treatment of ileo(-cecal) active Crohn's disease with mild-to-moderate activity, due to controlled ileal release. Budesonide foam and/or enemas are also efficacious in the treatment of left-sided/distal ulcerative colitis. Gastro-resistant, extended release tablets characterized by a multimatrix structure (i.e. MMX-budesonide), have also been developed to allow uniform release along the length of the colon. This paper reviews the mechanism-of-action, safety and efficacy of budesonide in the treatment of inflammatory bowel disease.

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Therapie gastrointestinaler Erkrankungen

Mueller¹

Praktische Arzneitherapie

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Pharmakokinetische Daten für verschiedene 5-Aminosalicylsäure- und Budesonidpräparate

Cited by 13 publications

References 45 publications

Bioavailability profile of Uceris MMX extended-release tablets compared with Entocort EC capsules in healthy volunteers

Bioavailability profile of Uceris MMX extended-release tablets compared with Entocort EC capsules in healthy volunteers

Budesonide: Teaching an Old Dog New Tricks for Inflammatory Bowel Disease Treatment

Therapie gastrointestinaler Erkrankungen

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