Sustained release beadlets containing stavudine stabilised by magnesium stearate

摘要

Extended dosage forms of stavudine are provided comprising beadlets formed by extrusion-spheronisation and coated with a seal coating. The beadlets are also coated with a modified release coating such that a hard gelatin capsule containing such beadlets will provide blood levels of stavudine over approximately 24 hours. The beadlets are prepared from a dry blend of stavudine, a spheronising agent, a suitable diluent and a stabilizing amount of magnesium stearate. The magnesium stearate, in contrast to other similar pharmaceutical adjuncts, has been found to stabilize stavudine against degradation due to hydrolysis in the presence of the limited amount of water necessary for the extrusion-spheronisation process. Also provided are hard gelatin capsules containing, in addition to the stavudine beadlets, similar beadlets containing other therapeutic agents utilised to treat retroviral infections.