Semi-solid dosage form of clonazepam for rapid oral mucosal absorption.
Drug Dev Ind Pharm
; 37(7): 809-14, 2011 Jul.
Article
en En
| MEDLINE
| ID: mdl-21247373
ABSTRACT
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 PEG/CZ/OA and PEG/CZ. The plasma concentration increased gradually and less varied at each time point for PEG/CZ/OA. PEG/CZ/OA was found to show more rapid and higher absorption of CZ in buccal administration than in sublingual administration.CONCLUSION:
Buccal administration with the semi-solid dosage PEG/CZ with or without OA was suggested to be a possibly useful novel dosage form as an alternative to i.v. injection.
Texto completo:
1
Banco de datos:
MEDLINE
Asunto principal:
Clonazepam
/
Composición de Medicamentos
/
Mucosa Bucal
Límite:
Animals
/
Humans
/
Male
Idioma:
En
Año:
2011
Tipo del documento:
Article