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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 A1 to A5.
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Related In: Results  -  Collection


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fig3: Dissolution profile for batches A1 to A5.

Mentions: The percentage drug release at second hour for A1 to A5 formulations was in the range of 87.90% to 53.39%, respectively, as shown in Figure 3, while only A3 to A5 formulations were able to retard drug release up to 7 to 8 hours. It was found from the initial trials that 150 to 250 mg of polymer is required for sustaining drug release up to 8 hours, while only A3 to A5 formulations were able to retard drug release up to 7 to 8 hours. But at 150 mg concentration (A3 batch) release was sustained up to 7 hours so that minimum level should be slightly more than 150 mg, while for 200 and 250 mg concentration release was almost similar, hence, 200 mg was decided as a higher level of the polymer.


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 A1 to A5.
© Copyright Policy - open-access
Related In: Results  -  Collection

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

fig3: Dissolution profile for batches A1 to A5.
Mentions: The percentage drug release at second hour for A1 to A5 formulations was in the range of 87.90% to 53.39%, respectively, as shown in Figure 3, while only A3 to A5 formulations were able to retard drug release up to 7 to 8 hours. It was found from the initial trials that 150 to 250 mg of polymer is required for sustaining drug release up to 8 hours, while only A3 to A5 formulations were able to retard drug release up to 7 to 8 hours. But at 150 mg concentration (A3 batch) release was sustained up to 7 hours so that minimum level should be slightly more than 150 mg, while for 200 and 250 mg concentration release was almost similar, hence, 200 mg was decided as a higher level of the polymer.

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