Semi-solid dosage form of clonazepam for rapid oral mucosal absorption

Published on Jul 1, 2011in Drug Development and Industrial Pharmacy2.367
· DOI :10.3109/03639045.2010.545069
Osamu Sakata6
Estimated H-index: 6
(Hoshi University),
Yoshiharu Machida38
Estimated H-index: 38
(Hoshi University),
Hiraku Onishi14
Estimated H-index: 14
(Hoshi University)
Background: In order to obtain an alternative to the intravenous (i.v.) dosage form of clonazepam (CZ), an oral droplet formulation of CZ was developed previously; however, the droplet was physically unstable. Therefore, in the present study, it was attempted to develop an easily-handled dosage form, which was more physically stable and allowed rapid drug absorption from oral mucosa. Method: A semi-solid dosage form, composed of polyethylene glycol 1500 (PEG), CZ, and oleic acid (OA) at 37/1/2 (w/w) and named PEG/CZ/OA, and a semi-solid dosage form containing PEG and CZ at 39/1 (w/w), called PEG/CZ, were prepared. Their physical stability in air at room temperature and oral mucosal absorption in rats were investigated. Results: The semi-solid dosage forms were much more stable physically than the droplet, that is, no recrystallization of CZ was observed for at least 8 days. The effective concentration for humans and rats (20 ng/mL or more) was achieved within 30 min after buccal administration for both PE...
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