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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

Dissolution rate profile of optimized chitosan-eudragit RLPO coated tablet in SCF.
© Copyright Policy - open-access
Related In: Results  -  Collection


getmorefigures.php?uid=PMC4595939&req=5

fig5: Dissolution rate profile of optimized chitosan-eudragit RLPO coated tablet in SCF.

Mentions: The best formulation showing drug release corresponded to 18.96% of chitosan (pore former) and 11.3% of coating thickness of eudragit RLPO film provided the desired release as shown in Figure 5. The above quantity (X1 and X2) of formulation was substituted in (1) to obtain the predicted responses. The validity of the optimization procedure was confirmed by preparing a new batch of coating formulation with the concentration provided by the software and the observed response were found to be inside the constraints and close to the predicted responses. Thus, the factorial design was valid for predicting the optimum formulation.


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)

Dissolution rate profile of optimized chitosan-eudragit RLPO coated tablet in SCF.
© Copyright Policy - open-access
Related In: Results  -  Collection

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

fig5: Dissolution rate profile of optimized chitosan-eudragit RLPO coated tablet in SCF.
Mentions: The best formulation showing drug release corresponded to 18.96% of chitosan (pore former) and 11.3% of coating thickness of eudragit RLPO film provided the desired release as shown in Figure 5. The above quantity (X1 and X2) of formulation was substituted in (1) to obtain the predicted responses. The validity of the optimization procedure was confirmed by preparing a new batch of coating formulation with the concentration provided by the software and the observed response were found to be inside the constraints and close to the predicted responses. Thus, the factorial design was valid for predicting the optimum formulation.

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