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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

Swelling index for A1 to A5 formulations.
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Related In: Results  -  Collection


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fig4: Swelling index for A1 to A5 formulations.

Mentions: Swelling study results showed slow and gradual increase in swelling index with time and concentration of CM-xyloglucan, as CM-xyloglucan does not swell instantaneously as soon as it comes in contact with water as shown in Figure 4; this results in burst release due to improper swelling. Therefore, to avoid the burst release effect, we have added HPMC K100 in the small quantity. Swelling of A5 batch is highest because it contains a higher amount of polymer. If swelling is more then it increases the path length required for water to travel inside the core of tablet, which gives more sustained-release.


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)

Swelling index for A1 to A5 formulations.
© Copyright Policy - open-access
Related In: Results  -  Collection

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

fig4: Swelling index for A1 to A5 formulations.
Mentions: Swelling study results showed slow and gradual increase in swelling index with time and concentration of CM-xyloglucan, as CM-xyloglucan does not swell instantaneously as soon as it comes in contact with water as shown in Figure 4; this results in burst release due to improper swelling. Therefore, to avoid the burst release effect, we have added HPMC K100 in the small quantity. Swelling of A5 batch is highest because it contains a higher amount of polymer. If swelling is more then it increases the path length required for water to travel inside the core of tablet, which gives more sustained-release.

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