In vitro drug release profiles and mucoadhesive property of bioadhesive microspheres of metronidazole.
- Author:
Jing-lin HUANG
1
;
Jin-fang LU
Author Information
- Publication Type:Journal Article
- MeSH: Acrylates; Animals; Anti-Infective Agents; administration & dosage; pharmacology; Cell Adhesion; Delayed-Action Preparations; Female; Fluorocarbons; chemistry; Gastric Mucosa; physiology; Metronidazole; administration & dosage; pharmacology; Microspheres; Rats; Rats, Sprague-Dawley
- From: Acta Pharmaceutica Sinica 2002;37(3):226-228
- CountryChina
- Language:Chinese
-
Abstract:
AIMTo prepare bioadhesive microspheres of metronidazole (Metro) with prolonging resident time in the stomach and sustaining drug release.
METHODSThe microspheres were prepared by a drying-in-liquid method. The appearance, particle size and drug release in vitro were examined. The factors influencing bioadhesive property and drug release, such as ethyl cellulose (EC)/carbopol 934P (CP) ratio, particle size and Metro content were investigated.
RESULTSThe average diameter of the Metro-EC-CP microspheres was 559.9 microns. The release profiles of metronidazole were shown to fit to first-order equations well. With the increase of CP content in the Metro-EC-CP microspheres, the microspheres showed better mucoadhesion and faster drug release. The drug release rate decreased with the increase of particle size and the decrease of Metro content.
CONCLUSIONThe Metro-EC-CP microspheres have a sound mucoadhsive property and sustained drug release when the ratio of EC and CP was 17:3 and Metro content was 25%. The drug release was shown to last for 8 h in 0.1 mol.L-1 hydrochloric acid.
