FIELD: pharmacy.
SUBSTANCE: invention proposes medicinal formulations of stavudine with sustained-release effect comprising granules prepared by extrusion-spheronization and covered by isolating coating. Granules involve coating for sustained releasing also. Granules are prepared by mixing stavudine, spheronizing agent, suitable solvent, magnesium stearate taken in stabilizing amount in the presence of water taken in limited amount that is necessary for carrying out extrusion-spheronization process. Invention involves also solid gelatin capsules containing similar granules containing other therapeutic agents in addition to stavudine granules that are useful for retroviral infections. It has been shown that magnesium stearate, in contrast to other similar pharmaceutical additions, stabilizes stavudine against decomposition in hydrolysis and protects granules from color change from yellow to brown. Stavudine granules with magnesium stearate don't cause reducing activity of stavudine in hydrolysis that is associated with a method for their preparing.
EFFECT: improved preparing method, valuable pharmaceutical properties of granules.
33 cl, 3 tbl, 5 ex
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Authors
Dates
2004-11-10—Published
2001-03-29—Filed