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Gastrointestinal transit and 5-ASA release from a new mesalazine extended-release formulation (2003)

Brunner, M. ; Assandri, R. ; Kletter, K. ; [et al.]

Oxford, UK : Blackwell Science Ltd

Alimentary pharmacology & therapeutics 17 (2003), S. 0

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ISSN: 1365-2036

Source: Blackwell Publishing Journal Backfiles 1879-2005

Topics: Medicine

Notes: Background : Mesalazine (5-aminosalicylic acid, 5-ASA)-containing formulations represent a cornerstone in the treatment of inflammatory bowel diseases. Recently, a new formulation has been developed to provide selective and more homogeneous release of 5-ASA compared to traditional systems.Methods : In a first study, gastrointestinal transit was followed by gamma-scintigraphy after single-dose application of tablets containing 1200 mg mesalazine to 12 healthy male volunteers. 5-ASA release was verified by the assessment of plasma pharmacokinetics. In a second, 7-day, multiple-dose study, the steady state plasma pharmacokinetics, urinary excretion and safety profile were characterized after twice-daily tablet administration to 12 healthy volunteers.Results : Tablet erosion started after 6.9 ± 1.1 h in the ascending or transverse colon. Radioactivity spread homogeneously throughout the colon, indicating the sustained release of active 5-ASA. Plasma kinetics indicated an earlier initial absorption of 5-ASA, i.e. during transit of the small intestine and ileum. Mean Cmax values (350.6 ± 322.6 ng/mL) were observed during location in the ileo-caecal region. The mean relative absorption of 5-ASA was 19.9 ± 18.2% in the small intestine and ileum and 80.1 ± 18.2% in the colon.Conclusions : The administration of the new mesalazine formulation was well tolerated, and 5-ASA was continuously released along the whole colon, a favourable prerequisite for the therapy of distally located inflammatory bowel disease.

Type of Medium: Electronic Resource

URL: http://dx.doi.org/10.1046/j.1365-2036.2003.01445.x

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Ionic Permeability on Isolated Mouse Liver Nuclei: Influence of ATP and Ca2+ (1997)

Assandri, R. ; Mazzanti, M.

Springer

The journal of membrane biology 157 (1997), S. 301 -309

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ISSN: 1432-1424

Keywords: Key words: Isolated nuclei — Ionic channels — Patch-clamp — ATP — Ca++— Channel modulation

Source: Springer Online Journal Archives 1860-2000

Topics: Biology , Chemistry and Pharmacology

Notes: Abstract. Patch-clamp experiments on isolated nuclei revealed the existence of ionic channels on the nuclear envelope, but their exact localization and function are still unknown. Recent studies have demonstrated that ATP and calcium ions play an important role in nucleocytoplasmic protein traffic. ATP is essential to allow big molecules in and out of the nucleus. However, a cytoplasmic rise of calcium ions above 300 nm decreases both ATP-dependent transport and passive diffusion through the nuclear envelope. The use of isolated nuclei placed in a saline solution provides the possibility for testing only the compounds added in the bath or in the recording pipette. In the present study, we show that ATP is responsible for an increase of nuclear ionic permeability on isolated nuclei. This result not only confirms data previously reported in in situ nuclei, but also suggests that ATP is directly involved in the modulation of passive ionic permeability. In these particular experimental conditions, calcium ions decrease the channel current starting from a concentration of 1 μm. The parallelism in the modulation action of ATP and Ca++ between nuclear pores and ionic channels present on the nuclear envelope contributes to the support of the idea that an ionic pathway is associated with the pore complex.