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Oral compositions having improved absorption in the gastrointestinal tract - containing an absorption promoter with a hydrophile - lipophile balance over 8
Oral compositions having improved absorption in the gastrointestinal tract - containing an absorption promoter with a hydrophile - lipophile balance over 8
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机译:胃肠道吸收改善的口服组合物-含有具有亲水性的吸收促进剂-亲脂性平衡超过8
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摘要
Medicaments for oral administration having hydrophilic or ionizable active ingredients, an absorption promoter having an HLB (hydrophile-lipophile balance) of over 8 that is a lipidic material. The lipidic material is selected from one or more of the following: polysorbates, alkylethers, polyoxyethylene ethers, fatty acid polyoxyethylene esters, fatty acids, fatty alcohols, biliary acids and their salts, 1-6C alkanol esters with fatty acids, fatty acid 2-6 OH polyol esters, and polyglycosylated glycerides, in association with one or more pharmaceutical excipients, except for pharmaceutical forms containing captopril. The active material is preferably calcium acamprosate, metformin or metformin hydrochloride. The compositions preferably contain 0.001 - 10 % by weight of the absorption promoter, especially 0.1 - 2 %. The compositions may further contain an agent to control the kinetic liberation of the active material, especially glycerol palmostearates, glycerol behenates, hydrogenated castor oil, and their mixtures. ACTIVITY : The bio-availability of calcium acetylhomotaurinate (calcium acamprosate) was determined in beagle dogs using various formulations containing 333 mg of active material. For control purposes, a standard coated tablet formulation was used. Compositions of the invention contained 1 % soya lecithin, or 34 % lactose, together with Gelucire 44/14 (RTM). Taking the control as 100 %, the compositions of the invention gave maximum values of plasmatic acamprosate of 138 % and 146 % respectively.
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