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

Nicholls, Andrew; Harris-Collazo, Raul; Huang, Michael; Hardiman, Yun; Jones, Richard J.; Moro, Luigi

doi:10.1177/0300060513476588

Cited by 19 publications

(18 citation statements)

References 13 publications

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“…Finally, the technology used in the dosage form development can also influence the colonic bioavailability of drugs. Useris® and Entocort EC® are currently approved budesonide products for the treatment of UC and CD, respectively (35). Useris® is a multi-matrix (MMX)-based delayed-release tablets, which ensures the drug release in the colon, while Entocort EC® is a capsule which releases the drug in the ileum to treat CD.…”

Section: Formulation Factorsmentioning

confidence: 99%

Colon-Targeted Oral Drug Delivery Systems: Design Trends and Approaches

2015

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Abstract. Colon-specific drug delivery systems (CDDS) are desirable for the treatment of a range of local diseases such as ulcerative colitis, Crohn's disease, irritable bowel syndrome, chronic pancreatitis, and colonic cancer. In addition, the colon can be a potential site for the systemic absorption of several drugs to treat non-colonic conditions. Drugs such as proteins and peptides that are known to degrade in the extreme gastric pH, if delivered to the colon intact, can be systemically absorbed by colonic mucosa. In order to achieve effective therapeutic outcomes, it is imperative that the designed delivery system specifically targets the drugs into the colon. Several formulation approaches have been explored in the development colon-targeted drug delivery systems. These approaches involve the use of formulation components that interact with one or more aspects of gastrointestinal (GI) physiology, such as the difference in the pH along the GI tract, the presence of colonic microflora, and enzymes, to achieve colon targeting. This article highlights the factors influencing colon-specific drug delivery and colonic bioavailability, and the limitations associated with CDDS. Further, the review provides a systematic discussion of various conventional, as well as relatively newer formulation approaches/technologies currently being utilized for the development of CDDS.

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Section: Formulation Factorsmentioning

confidence: 99%

Colon-Targeted Oral Drug Delivery Systems: Design Trends and Approaches

2015

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“…27 Apart from the differences in the site and rate of drug release, the different oral budesonide formulations share similar pharmacokinetic characteristics [table 1]. 21,28–34 Likewise, the two rectal formulations share similar pharmacokinetics, although the foam is characterized by less proximal spread and takes longer time to reach peak plasma concentration [table 1]. …”

Section: Pharmacokineticsmentioning

confidence: 99%

“…The pharmacokinetics information for the rectal formulations are based on studies conducted on patients with left-sided UC. 21,28–34 † Data presented as mean (SD) or mean (range) Abbreviations: AUC: area under the plasma drug concentration time curve, Cmax: peak plasma concentration, Tmax: time to peak plasma concentration, Tlag: time to detect drug concentration in the plasma …”

Section: Figurementioning

confidence: 99%

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Budesonide for the treatment of ulcerative colitis

Abdalla

Herfarth

2016

Expert Opinion on Pharmacotherapy

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Introduction Budesonide is a synthetic corticosteroid characterized by enhanced topical potency and limited systemic bioavailability. Its use in ulcerative colitis (UC) was limited to rectal preparations until recently when the new oral budesonide formulation incorporating the multi-matrix system technology was introduced. The purpose of this review is to evaluate the current role of oral and rectal budesonide in managing UC patients Areas Covered In this paper, we described the chemical structure and pharmacologic characteristics of the different oral and rectal budesonide preparations, provided a summary of the published trials that evaluated the efficacy and safety of budesonide in UC, and discussed the current status of its use in this population Expert Opinion Budesonide is effective in inducing remission in a subset of patients with mild-moderate UC. Nevertheless, the current evidence suggests inferiority of oral budesonide to 5-aminosalisylates (5-ASA) and systemic steroids, whereas rectal applications are comparable to other rectal steroid preparations but still inferior to rectal 5-ASA. In clinical practice, several issues need clarification including, its exact position in the line of induction agents; the role of combining budesonide and 5-ASAs; the role of combining oral and rectal budesonide; and the role of budesonide in maintenance therapy.

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“…The resulting major metabolites of BDS are 6OH‐BDS and 16OH‐PREDN. The human pharmacokinetics (PK) of BDS have been evaluated by various routes of administration, including intravenous, oral, pulmonary, nasal inhalation, and rectal . Renal elimination of unchanged BDS is low because of its extensive biotransformation in the liver.…”

Section: Introductionmentioning

confidence: 99%

Effect of hyperhydration on the pharmacokinetics and detection of orally administered budesonide in doping control analysis

Αθανασιάδου

Vonaparti

Dokoumetzidis

et al. 2019

Scandinavian Med Sci Sports

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The aim of the present study was to investigate if hyperhydration could influence the excretion and subsequent detection of budesonide (BDS) and its main metabolites (6β‐hydroxy‐budesonide and 16α‐hydroxy‐prednisolone) during doping control analysis by leading to concentrations below the WADA reporting level (30 ng/mL). The influence of hyperhydration on the plasma and urinary pharmacokinetic (PK) profiles of BDS and metabolites was also examined. Seven healthy physically active non‐smoking Caucasian males participated in a 15‐day clinical study. BDS was administered orally at a single dose of 9 mg on Days 1, 7, and 13. Hyperhydration was applied in the morning on two consecutive days, that is, 0 and 24 hours after first fluid ingestion. Water and a commercial sports drink were used as hyperhydration agents (20 mL/kg body weight). Results showed no significant difference (P > 0.05, 95% CI) on plasma or urinary PK parameters under hyperhydration conditions for all the analytes. However, significant differences (P < 0.05, 95% CI) due to hyperhydration were observed on the urinary concentrations of BDS and metabolites. To compensate the dilution effect due to hyperhydration, different adjustment methods were applied based on specific gravity, urinary flow rate, and creatinine. All the applied methods were able to adjust the concentration values close to the baseline ones for each analyte; however, specific gravity was the optimum method in terms of effectiveness and practicability. Furthermore, no masking of the detection sensitivity of BDS or its metabolites was observed due to hyperhydration either in plasma or urine samples.

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

Cited by 19 publications

References 13 publications

Colon-Targeted Oral Drug Delivery Systems: Design Trends and Approaches

Colon-Targeted Oral Drug Delivery Systems: Design Trends and Approaches

Budesonide for the treatment of ulcerative colitis

Effect of hyperhydration on the pharmacokinetics and detection of orally administered budesonide in doping control analysis

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