Abstract
Novelty: A sustained release formulation of acetazolamide (at least 25% w/w) is claimed. It comprises spherical binder-free pellets coated with a release-controlling substance. Acetazolamide is a carbonic anhydrase inhibitor and is used to treat glaucoma.
Biology: A clinical study was performed on ten volunteers (aged 60-74) in two groups, given either a capsule or a conventional tablet (control) every 24 hrs. Hourly blood samples taken over 24hrs showed acetazolamide levels (assayed by HPLC) in plasma = 5pg/ml, rising steadily to 11 pg/ml after 9 hrs. Conventional tablets showed two sharp peaks at 2 and 14 hrs. Another study, with the two groups interchanged and younger (aged 19-27) volunteers, gave substantially the same results.
Chemistry: The acetazolamide, in the form of spherical binder-free pellets (preferably 79-82% w/w), acts as its own binder and is coated with a sustained release controlling membrane of ethyl cellulose or similar material. Details of ten manufacturing steps of pellet cores and film coating solution are also given.