New formulation of in situ gelling Metolose-based liquid suppository.
Drug Dev Ind Pharm
; 37(1): 1-7, 2011 Jan.
Article
en En
| MEDLINE
| ID: mdl-21073325
CONTEXT: An in situ gelling liquid suppository is liquid at room temperature but forms a gel at body temperature. In our work, Metolose® SM-4000 (methylcellulose) is studied that basically shows thermal gelation at 68°C (2%, w/w). OBJECTIVE: The objective was to study the potency of different factors (concentration, pH, additives) to change the value of thermal gelation temperature (T (t)) for Metolose® to form an in situ gelling liquid suppository. MATERIALS AND METHODS: We studied the effect of Metolose® concentration, pH, and salts (sodium chloride, potassium chloride, sodium hydrogen carbonate, and sodium monohydrogen phosphate) on T (t) by viscosimetry. To choose the appropriate compound, in vitro drug release was examined. Rectal safety test was performed on rats in vivo after 12-hour application. RESULTS: Increasing the Metolose® concentrations (0.5-4%, w/w), T (t) can be decreased, but it also altered the consistency of gel. pH does not affect the T (t). The water-soluble salts allowed reducing the gelation temperature to 37°C. Sodium monohydrogen phosphate in 4.5% concentration was found to be the most appropriate. The impact of examined factors on in vitro drug release of piroxicam from the in situ-formed gel was characterized according to Fickian diffusion. Metolose® and the chosen salt did not cause any morphological damage on the rectal tissues. DISCUSSION: According to our study, Metolose® has the physical and chemical potential to be used as base for liquid suppositories.
Texto completo:
1
Colección:
01-internacional
Base de datos:
MEDLINE
Asunto principal:
Fosfatos
/
Supositorios
/
Piroxicam
/
Antiinflamatorios no Esteroideos
/
Geles
/
Metilcelulosa
Tipo de estudio:
Prognostic_studies
Límite:
Animals
Idioma:
En
Revista:
Drug Dev Ind Pharm
Año:
2011
Tipo del documento:
Article
País de afiliación:
Hungria
Pais de publicación:
Reino Unido