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Optimization of Carboxymethyl-Xyloglucan-Based Tramadol Matrix Tablets Using Simplex Centroid Mixture Design.

Madgulkar AR, Bhalekar MR, Padalkar RR, Shaikh MY - J Pharm (Cairo) (2012)

Bottom Line: The formulated tablets showed anomalous release mechanism and followed matrix drug release kinetics, resulting in regulated and complete release from the tablets within 8 to 10 hours.The polymer carboxymethyl xyloglucan and HPMC K100M had significant effect on drug release from the tablet (P > 0.05).The statistical models developed for optimization were found to be valid.

View Article: PubMed Central - PubMed

Affiliation: Department of Pharmaceutics, AISSMS College of Pharmacy, Kennedy Road, Pune 411001, Maharashtra, India.

ABSTRACT
The aim was to determine the release-modifying effect of carboxymethyl xyloglucan for oral drug delivery. Sustained release matrix tablets of tramadol HCl were prepared by wet granulation method using carboxymethyl xyloglucan as matrix forming polymer. HPMC K100M was used in a small amount to control the burst effect which is most commonly seen with natural hydrophilic polymers. A simplex centroid design with three independent variables and two dependent variables was employed to systematically optimize drug release profile. Carboxymethyl xyloglucan (X 1), HPMC K100M (X 2), and dicalcium phosphate (X 3) were taken as independent variables. The dependent variables selected were percent of drug release at 2nd hour (Y 1) and at 8th hour (Y 2). Response surface plots were developed, and optimum formulations were selected on the basis of desirability. The formulated tablets showed anomalous release mechanism and followed matrix drug release kinetics, resulting in regulated and complete release from the tablets within 8 to 10 hours. The polymer carboxymethyl xyloglucan and HPMC K100M had significant effect on drug release from the tablet (P > 0.05). Polynomial mathematical models, generated for various response variables using multiple regression analysis, were found to be statistically significant (P > 0.05). The statistical models developed for optimization were found to be valid.

No MeSH data available.


Related in: MedlinePlus

Dissolution profile for batches F1 to F7.
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fig5: Dissolution profile for batches F1 to F7.

Mentions: Hence, it was decided to optimize the amount of CM-xyloglucan between 180 to 200 mg per tablet in order to have a sustained and complete release of drug at the end of eight to twelve hours. The amounts of matrixing agent carboxymethyl xyloglucan (CM-xyloglucan, X1), gelling agent (HPMC K100M, X2), and dicalcium phosphate (DCP, X3) were selected as independent variables. A statistical model incorporating 7 interactive terms was used to evaluate the responses:(3)Y=b0+b1X1+b2X2+b3X3+b8X1X2+b23X2X3+  b13X1X3+b83X1X2X3,where Y is the dependent variable, b0 is the arithmetic mean response of the 7 runs, and bi is the estimated coefficient for the factor Xi. The main effects (X1, X2, and X3) represent the average result of changing one factor at a time from its low to high value. The interaction terms (X1X2, X2X3, X1X3, and X1X2X3) show how the response changes when two or more factors are simultaneously changed. The rel2 Hr and rel8 Hr, respectively, for all 7 batches (F1–F7) showed a wide variation (Figure 5). The data clearly indicate that the values of drug release are strongly dependent on the selected independent variables.


Optimization of Carboxymethyl-Xyloglucan-Based Tramadol Matrix Tablets Using Simplex Centroid Mixture Design.

Madgulkar AR, Bhalekar MR, Padalkar RR, Shaikh MY - J Pharm (Cairo) (2012)

Dissolution profile for batches F1 to F7.
© Copyright Policy - open-access
Related In: Results  -  Collection

Show All Figures
getmorefigures.php?uid=PMC4595968&req=5

fig5: Dissolution profile for batches F1 to F7.
Mentions: Hence, it was decided to optimize the amount of CM-xyloglucan between 180 to 200 mg per tablet in order to have a sustained and complete release of drug at the end of eight to twelve hours. The amounts of matrixing agent carboxymethyl xyloglucan (CM-xyloglucan, X1), gelling agent (HPMC K100M, X2), and dicalcium phosphate (DCP, X3) were selected as independent variables. A statistical model incorporating 7 interactive terms was used to evaluate the responses:(3)Y=b0+b1X1+b2X2+b3X3+b8X1X2+b23X2X3+  b13X1X3+b83X1X2X3,where Y is the dependent variable, b0 is the arithmetic mean response of the 7 runs, and bi is the estimated coefficient for the factor Xi. The main effects (X1, X2, and X3) represent the average result of changing one factor at a time from its low to high value. The interaction terms (X1X2, X2X3, X1X3, and X1X2X3) show how the response changes when two or more factors are simultaneously changed. The rel2 Hr and rel8 Hr, respectively, for all 7 batches (F1–F7) showed a wide variation (Figure 5). The data clearly indicate that the values of drug release are strongly dependent on the selected independent variables.

Bottom Line: The formulated tablets showed anomalous release mechanism and followed matrix drug release kinetics, resulting in regulated and complete release from the tablets within 8 to 10 hours.The polymer carboxymethyl xyloglucan and HPMC K100M had significant effect on drug release from the tablet (P > 0.05).The statistical models developed for optimization were found to be valid.

View Article: PubMed Central - PubMed

Affiliation: Department of Pharmaceutics, AISSMS College of Pharmacy, Kennedy Road, Pune 411001, Maharashtra, India.

ABSTRACT
The aim was to determine the release-modifying effect of carboxymethyl xyloglucan for oral drug delivery. Sustained release matrix tablets of tramadol HCl were prepared by wet granulation method using carboxymethyl xyloglucan as matrix forming polymer. HPMC K100M was used in a small amount to control the burst effect which is most commonly seen with natural hydrophilic polymers. A simplex centroid design with three independent variables and two dependent variables was employed to systematically optimize drug release profile. Carboxymethyl xyloglucan (X 1), HPMC K100M (X 2), and dicalcium phosphate (X 3) were taken as independent variables. The dependent variables selected were percent of drug release at 2nd hour (Y 1) and at 8th hour (Y 2). Response surface plots were developed, and optimum formulations were selected on the basis of desirability. The formulated tablets showed anomalous release mechanism and followed matrix drug release kinetics, resulting in regulated and complete release from the tablets within 8 to 10 hours. The polymer carboxymethyl xyloglucan and HPMC K100M had significant effect on drug release from the tablet (P > 0.05). Polynomial mathematical models, generated for various response variables using multiple regression analysis, were found to be statistically significant (P > 0.05). The statistical models developed for optimization were found to be valid.

No MeSH data available.


Related in: MedlinePlus