Preparation And Elvaution Of Thermally Cross-Linked Chitosan Clarithromycin Mucoadhesive Microspheres
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Author:
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UPLOADED BY-ADMIN, H. D. KORADIA, V. A. PATEL, H. V. PATEL, K. N. PATEL
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Abstract:
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Clarithromycin, an effective antibiotic, for the eradication of H. pylori. Clarithromycin
requires mucoadhesive controlled release formulation owing to short residence time of the
conventional dosage form in the stomach. Chitosan is one of the polysaccharides which show
antimicrobial and bio compatible behavior. Chitosan obtained by deacetylation of chitin (a
naturally occurring polymer) has been shown to possess mucoadhesive properties owing to
the molecular attractive forces formed by electrostatic interaction between positively charged
chitosan and negatively charged mucosal surfaces.
Mucoadhesive chitosan micro spheres of Clarithromycin were prepared by thermal crosslinking
in presence of citric acid at high temperature. Formulations were characterized for
percentage yield, particle size, surface morphology, percent drug content, swelling kinetics,
in vitro mucoadhesion and in vitro drug release. Microspheres were discrete, spherical, free
flowing and of larger particle size.
Percent yield of microspheres was varied from 58.01 to 75 %. Percentage drug content
was varied from 4.097 to 14.77 %. Percentage drug content was increased with increase in
drug concentration. Smaller size microspheres (370 µm) were obtained when drug concentration
was lower (1:4 D/P ratio). Swelling index and Percentage mucoadhesion were decrease
as the D/P ratio was increased. Clarithromycin release from chitosan microspheres was characterized
by an initial rapid release of drug followed by a slow release.
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Keyword:
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Clarithromycin, Chitosan, H. pylori, Mucoadhesive micro spheres
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DOI:
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