Process for the production of solid preparacoes conservaveis of active substances hardly soluble in water, in particular sensitive medicines

摘要

A solid, stable, pharmaceutical preparation is prepared by dissolving the active substance and a physiologically acceptable, water-dispersable cellulose derivative separately or together in an inert non-aqueous solvent (or, in the case of separate solutions, in two miscible non-aqueous solvents), combining the solutions if two are used, removing the solvent and drying the residue to give a fine dispersion of the active substance in the cellulose derivative. Suitable cellulose derivatives are methyl-, hydroxy-, propyl- and hydroxypropylmethylcellulose. Examples relate to preparations comprising Vitamins D2 and D3, Vitamin D3-cholesterol, 1a , 7a -diacetyl-thio-17a -methyl testo-sterone, ethinyl estradiol and chloramphenicol. Additives, e.g. antioxidants and fluidity and grinding improvers such as highly dispersed silicic acid, CaCO3, and calcium, aluminium and magnesium silicates may be included in the preparations, which may be tableted and made up into any conventional solid formulation.