Development of pH- and enzyme-controlled, colon-targeted, pulsed delivery system of a poorly water-soluble drug: preparation and in vitro evaluation.
Drug Dev Ind Pharm
; 36(1): 81-92, 2010 Jan.
Article
em En
| MEDLINE
| ID: mdl-19640246
ABSTRACT
BACKGROUND:
As conventional pH-controlled colon-targeted system used for oral drug delivery often shows a poor performance, a more effective way to preserve poorly water-soluble drug from releasing in upper gastrointestinal tract should be researched.METHOD:
The objective of this study was to develop a novel colon-targeted drug delivery system using guar gum and Eudragit as enzyme- and pH-based materials. Lansoprazole, a poorly water-soluble drug was used as model drug. Under three different conditions, the in vitro drug release behaviors of this newly developed system was evaluated, using ß-mannanase, rat cecal content, and human fecal media to simulate the pH and enzyme during intestinal transit to the colon.RESULTS:
The released amount of lansoprazole in simulated small intestine fluid (pH 6.8) after 5 hours was less than 10% from the pH- and enzyme-controlled tablets compared with 80.01±0.3% in rat cecal content medium (pH 7.4).The degradation ability of human fecal slurries on PECCT-PT was independent of human age and gender. ß-Mannanase did not have a similar effect on the degradation of polysaccharide as rat cecal enzymes and human fecal enzymes in our study. Scanning electron microscope study indicated that the dissolution mechanism of PECCT-PT should be corrosion.CONCLUSION:
The above results indicated this system could be served as a potential carrier to deliver poorly water-soluble drug specifically to the colon.
Texto completo:
1
Coleções:
01-internacional
Base de dados:
MEDLINE
Assunto principal:
Sistemas de Liberação de Medicamentos
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Colo
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2-Piridinilmetilsulfinilbenzimidazóis
Tipo de estudo:
Prognostic_studies
Limite:
Adolescent
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Adult
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Aged
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Animals
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Child
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Child, preschool
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Female
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Humans
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Male
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Middle aged
Idioma:
En
Revista:
Drug Dev Ind Pharm
Ano de publicação:
2010
Tipo de documento:
Article