| 摘要 |
<p>PCT No. PCT/EP93/00055 Sec. 371 Date Jul. 13, 1994 Sec. 102(e) Date Jul. 13, 1994 PCT Filed Jan. 12, 1993 PCT Pub. No. WO93/13760 PCT Pub. Date Jul. 22, 1993The pharmaceutical formulation in the form of an effervescent and/or disintegrating tablet or of instant granules contains at least one active ingredient having an irritating taste and at least one matrix which delays the release of the active ingredient and is present as an intimate mixture with the active ingredient particles or covers said particles and is applied to a carrier. The formulation releases at most 65%, preferably at most 50%, of the active ingredient in aqueous solution at room temperature within about 2 min but more than 70%, preferably at least 80%, of the active ingredient within max. 20 min, preferably max. 15 min, in 0.1N HCl at 38 DEG C. The matrix preferably contains at least one fatty ester and/or one wax, preferably having a melting point between 30 DEG and 45 DEG C., in particular between 32 DEG and 35 DEG C., and/or at least one cellulose derivative and/or at least one polymethacrylate. In particular, the active ingredient is present in an amount of less than 60 mg, preferably less than 10 mg, and the matrix is present in an amount of 1 to 10, preferably 3 to 5, times the amount of active ingredient per tablet or granule dose. For the treatment of diarrhoea by means of loperamide, the matrix additionally contains a mixture which serves to compensate for the electrolyte loss in the body and an amount of alkali metal and/or alkaline earth metal salts, preferably of organic salts, and of chlorides.</p> |
