PROCESS FOR PREPARATION OF SOLID DISPERIONS AND DEPOSITS AS WELL AS OF SOLID MEDICINAL FORMS WITH DIHYDROPYRIDINE TYPE CALCIUM ANTAGONISTS

摘要

There is described a process for the preparation of solid dispersions and deposits with dihydropyridine type calcium antagonists containing as the active substance one or more 1,4-dihydropyridine derivatives such as nitrendipine, nimodipine and lacidipine and as a carrier one or more water-soluble derivatives of mono-, di-, oligo- and polysaccharides, and, if required, also polymer substances, which are swellable in contact with water, selected from polacrilin potassium, sodium starch glycolate and/or cross-linked carboxy methyl cellulose, and anionogenic or non-ionogenic type surfactants selected from sodium lauryl sulfate, poloxamers and/or higher fatty acids polyoxyethylene sorbitan esters, whereat from the dispersion, preferably a solution and/or suspension of active substance(s), and if required one or more water-soluble adjuvants, selected from mono, di and oligosaccharides, and surfactants selected from sodium lauryl sulfate, poloxamers and/or polyoxyethylene sorbitan esters of higher fatty acids with 12 to 18 carbon atoms, in a solvent selected from lower aliphatic alcohols with 1 to 4 carbon atoms, preferably ethanol and 1-propanol and if required in mixture with water, the solvent is removed by spraying of dispersion under the stream of the heat air and if required to the carrier, selected from one or more of the water-soluble mono, di, oligo and polysaccharides and if required the water-swellable polymer substances from the group of disintegrators, and the anionic or nonionic surfactants. Furthermore, there is described a process for the preparation of solid medicinal forms of dihydropyridine type calcium antagonists, whereat the mentioned solid dispersions and (or) deposits are mixed in a suitable manner with disintegrators and lubricant, and if required the other adjuvants such as carriers and binders, and then by such a mixture there are formed preferably tablets and capsules.