Gastrointestinal transit and 5‐ASA release from a new mesalazine extended‐release formulation

Abstract

SUMMARYBackground: 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.

Gastrointestinal transit, release and plasma pharmacokinetics of a new oral budesonide formulation

“…The MMX® matrix has a polymeric structure and was designed to slowly and homogenously release the active drug at a controlled rate throughout the whole colon for the oral treatment of IBD with a more distal location than the ileo-caecal region. This formulation has been successfully employed for the delivery of aminosalicylate [7].…”

“…The study medication for both studies was provided by Cosmo S.p.A., Lainate (MI), Italy, and consisted of round, film-coated, gastro-resistant, extended-release tablets, with multimatrix structure (MMX®) [7], a diameter of 10 mm, a weight of 330 mg, and each containing 9 mg budesonide. Tablets were designed for slow and graded budesonide release in the colon, and consisted of an inner lipophilic matrix in which the active ingredient was dispersed, an outer hydrophilic matrix generated by in situ hydration of selected polymer chains and a third amphiphilic matrix promoting the inert matrix wettability.…”

“…Venous blood samples (10 mL) were collected from an arm vein at predose on days 2, 4, 6 and 7, and at the following time points after the last dose on the 7th treatment day: 0 (predose), 2,3,4,5,6,7,8,10,12,16,20,24,30,36 and 48 h. Plasma samples, obtained by centrifugation were stored at ≤ − 20 ° C until analysis.…”

Systemic Absorption of Rifamycin SV MMX Administered as Modified-Release Tablets in Healthy Volunteers

“…The tablets are formulated using a multimatrix structure (MMX), which allows the delivery of the active ingredient directly to the colon, as has already been demonstrated by different pharmacoscintigraphic studies (7,8). By this technology, the maximum local bioavailability of the active ingredient is achieved in the colonic region and the biological effect is optimized.…”

“…MMX formulations were investigated in healthy volunteers with the aim of obtaining information on the gastrointestinal transit, disintegration, and release of various drugs delivered in the colonic region. Colonic delivery was clearly demonstrated by pharmacoscintigraphic investigations (7,8).…”