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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

Equilateral triangle representing simplex lattice design for 3 components (A, B, and C).
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Related In: Results  -  Collection


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fig2: Equilateral triangle representing simplex lattice design for 3 components (A, B, and C).

Mentions: Simplex Centroid Design. A simplex centroid design [22] was adopted to optimize the formulation variables. In this design three factors were evaluated by changing their concentrations simultaneously and keeping their total concentration constant. The simplex centroid design for a 3-component system (A, B, and C) is represented by an equilateral triangle in a 2-dimensional space (Figure 2). The amounts of matrixing agent carboxymethyl xyloglucan (carboxymethyl xyloglucan, X1), gelling agent (HPMC K100M, X2), and dicalcium phosphate (DCP, X3) were selected as independent variables as shown in Table 3. Percent release values of drug at 2nd hour and 8th hour were selected as dependent variables. The levels of the three factors were selected on the basis of the preliminary studies carried out before implementing the experimental design.


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)

Equilateral triangle representing simplex lattice design for 3 components (A, B, and C).
© Copyright Policy - open-access
Related In: Results  -  Collection

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

fig2: Equilateral triangle representing simplex lattice design for 3 components (A, B, and C).
Mentions: Simplex Centroid Design. A simplex centroid design [22] was adopted to optimize the formulation variables. In this design three factors were evaluated by changing their concentrations simultaneously and keeping their total concentration constant. The simplex centroid design for a 3-component system (A, B, and C) is represented by an equilateral triangle in a 2-dimensional space (Figure 2). The amounts of matrixing agent carboxymethyl xyloglucan (carboxymethyl xyloglucan, X1), gelling agent (HPMC K100M, X2), and dicalcium phosphate (DCP, X3) were selected as independent variables as shown in Table 3. Percent release values of drug at 2nd hour and 8th hour were selected as dependent variables. The levels of the three factors were selected on the basis of the preliminary studies carried out before implementing the experimental design.

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