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Design, Development, and Optimization of Sterculia Gum-Based Tablet Coated with Chitosan/Eudragit RLPO Mixed Blend Polymers for Possible Colonic Drug Delivery.

Nath B, Nath LK - J Pharm (Cairo) (2012)

Bottom Line: Chitosan in the mixed film coat was found to be degraded by enzymatic action of the microflora in the colon.Release kinetic data revealed that the optimized MCDDS was fitted well into first-order model, and apparent lag time was found to be 6 hours, followed by Higuchi release kinetics.In vivo study in rabbits shows delayed T max, prolonged absorption time, decreased C max, and absorption rate constant (Ka), indicating a reduced systemic toxicity of the drug as compared to other dosage forms.

View Article: PubMed Central - PubMed

Affiliation: Department of Pharmaceutical Sciences, Girijananda Chowdhury Institute of Pharmaceutical Sciences (GIPS), Azara, Assam, Guwahati 781001, India ; Girijananda Chowdhury Institute of Pharmaceutical Sciences (GIPS) Affiliated to Gauhati University, Azara, Assam, Guwahati 781017, India.

ABSTRACT
The purpose of this study is to explore the possible applicability of Sterculia urens gum as a novel carrier for colonic delivery system of a sparingly soluble drug, azathioprine. The study involves designing a microflora triggered colon-targeted drug delivery system (MCDDS) which consists of a central polysaccharide core and is coated to different film thicknesses with blends of chitosan/Eudragit RLPO, and is overcoated with Eudragit L00 to provide acid and intestinal resistance. The microflora degradation property of gum was investigated in rat caecal medium. Drug release study in simulated colonic fluid revealed that swelling force of the gum could concurrently drive the drug out of the polysaccharide core due to the rupture of the chitosan/Eudargit coating in microflora-activated environment. Chitosan in the mixed film coat was found to be degraded by enzymatic action of the microflora in the colon. Release kinetic data revealed that the optimized MCDDS was fitted well into first-order model, and apparent lag time was found to be 6 hours, followed by Higuchi release kinetics. In vivo study in rabbits shows delayed T max, prolonged absorption time, decreased C max, and absorption rate constant (Ka), indicating a reduced systemic toxicity of the drug as compared to other dosage forms.

No MeSH data available.


Related in: MedlinePlus

Changes of pH of phosphate buffer medium containing rat caecal content (–) 4%, (–) 8%, (–) 12% with and without sterculia gum (–). Each point represents the mean ± SD.
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fig1: Changes of pH of phosphate buffer medium containing rat caecal content (–) 4%, (–) 8%, (–) 12% with and without sterculia gum (–). Each point represents the mean ± SD.

Mentions: Microflora degradation studies of sterculia gum revealed that the pH of caecal-PBS was decreased markedly from pH 7.4 to 5.0 after incubation for 2 h with sterculia gum. The rate of decrease of pH was depended on the concentration of caecal contents within the 8 h of incubation (Figure 1). The decrease in pH was due to the appearance of degradation products of sterculia gum such as organic acids by the bacterial enzyme present in rat caecal contents.


Design, Development, and Optimization of Sterculia Gum-Based Tablet Coated with Chitosan/Eudragit RLPO Mixed Blend Polymers for Possible Colonic Drug Delivery.

Nath B, Nath LK - J Pharm (Cairo) (2012)

Changes of pH of phosphate buffer medium containing rat caecal content (–) 4%, (–) 8%, (–) 12% with and without sterculia gum (–). Each point represents the mean ± SD.
© Copyright Policy - open-access
Related In: Results  -  Collection

Show All Figures
getmorefigures.php?uid=PMC4595939&req=5

fig1: Changes of pH of phosphate buffer medium containing rat caecal content (–) 4%, (–) 8%, (–) 12% with and without sterculia gum (–). Each point represents the mean ± SD.
Mentions: Microflora degradation studies of sterculia gum revealed that the pH of caecal-PBS was decreased markedly from pH 7.4 to 5.0 after incubation for 2 h with sterculia gum. The rate of decrease of pH was depended on the concentration of caecal contents within the 8 h of incubation (Figure 1). The decrease in pH was due to the appearance of degradation products of sterculia gum such as organic acids by the bacterial enzyme present in rat caecal contents.

Bottom Line: Chitosan in the mixed film coat was found to be degraded by enzymatic action of the microflora in the colon.Release kinetic data revealed that the optimized MCDDS was fitted well into first-order model, and apparent lag time was found to be 6 hours, followed by Higuchi release kinetics.In vivo study in rabbits shows delayed T max, prolonged absorption time, decreased C max, and absorption rate constant (Ka), indicating a reduced systemic toxicity of the drug as compared to other dosage forms.

View Article: PubMed Central - PubMed

Affiliation: Department of Pharmaceutical Sciences, Girijananda Chowdhury Institute of Pharmaceutical Sciences (GIPS), Azara, Assam, Guwahati 781001, India ; Girijananda Chowdhury Institute of Pharmaceutical Sciences (GIPS) Affiliated to Gauhati University, Azara, Assam, Guwahati 781017, India.

ABSTRACT
The purpose of this study is to explore the possible applicability of Sterculia urens gum as a novel carrier for colonic delivery system of a sparingly soluble drug, azathioprine. The study involves designing a microflora triggered colon-targeted drug delivery system (MCDDS) which consists of a central polysaccharide core and is coated to different film thicknesses with blends of chitosan/Eudragit RLPO, and is overcoated with Eudragit L00 to provide acid and intestinal resistance. The microflora degradation property of gum was investigated in rat caecal medium. Drug release study in simulated colonic fluid revealed that swelling force of the gum could concurrently drive the drug out of the polysaccharide core due to the rupture of the chitosan/Eudargit coating in microflora-activated environment. Chitosan in the mixed film coat was found to be degraded by enzymatic action of the microflora in the colon. Release kinetic data revealed that the optimized MCDDS was fitted well into first-order model, and apparent lag time was found to be 6 hours, followed by Higuchi release kinetics. In vivo study in rabbits shows delayed T max, prolonged absorption time, decreased C max, and absorption rate constant (Ka), indicating a reduced systemic toxicity of the drug as compared to other dosage forms.

No MeSH data available.


Related in: MedlinePlus