Patent ID: 6514524
Filing Date: 2003-02-04
Classification: A61K,A61P

Abstract:
An orally administerable galenic formulation allowing improved absorption by the transmembrane or paracellular route in the gastrointestinal tract, comprising:at least one active ingredient which is a compound of the formula (I): in whichX is R is C1-C7 alkyl, R1, R2, and R3 each independently is C1-C7 alkyl, A is: v and w each independently is 0, 1, or 2, or A is R5 and R6, independently of each other, are hydrogen, C1-C7 alkyl, aryl of 6 to 14 carbon atoms, or heteroaryl which is furyl, thienyl, or thiazoyl, it being possible for the aryl and heteroaryl radicals to carry 1 to 3 substituents where are C1-C7 alkyl, halogen and/or trifluoromethyl, t=1âˆ’3, R4 is hydrogen, C1-C7 alkyl, CF3, aryl having from 6 to 14 carbon atoms, heteroaryl which is furyl, thienyl, or thiazoyl, it being possible for the aryl and heteroaryl radicals to carry 1 to 3 substituents which are C1-C7 alkyl, halogen and/or trifluoromethyl, M presents a monovalent metal (Na, K, Li) or a divalent metal (Ca, Mg, Sr, Zn), m=1 or 2, p=1âˆ’2 and q=1âˆ’2, p and q being such that the salt is electrically neutral, and an absorption-promoting agent having an HLB greater than 8 which is one or more lipid substances selected from polysorbates, ethers of polyoxyethylene and alkyl, esters of polyoxythylene and fatty acids, fatty alcohols, bile acids and their salts with pharmaceutically acceptable cations, esters of C1-C6 alkanols with fatty acids, esters of a polyol with fatty acids wherein said polyol comprises 2 to 6 hydroxyl groups, and polyglycolysed glycerides, and one or more pharmaceutically acceptable excipients.