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Formulation and optimization of sustained release tablets of venlafaxine resinates using response surface methodology.

Madgulkar AR, Bhalekar MR, Kolhe VJ, Kenjale YD - Indian J Pharm Sci (2009)

Bottom Line: Compressed matrices exhibited the anomalous release mechanism, as the value of release rate exponent (n) varied between 08109 and 08719, resulting in regulated and complete release until 20 h.Validation of optimization study, performed using five confirmatory runs, indicated very high degree of prognostic ability of response surface methodology, with mean percentage error as 1.152+/-1.88%.Regulated drug release study indicates that the hydrophilic and hydrophobic matrix tablets of venlafaxine resinate prepared using hydroxypropylmethylcellulose and ethylcellulose, can successfully be employed as a once-a-day oral controlled release drug delivery system.

View Article: PubMed Central - PubMed

Affiliation: AISSMS College of Pharmacy, Kennedy Road, Near RTO, Pune-411 001, India.

ABSTRACT
The aim of the current study was to design sustained release matrix tablets of venlafaxine hydrochloride using ion exchange resin with the incorporation of hydrophilic and hydrophobic polymer combinations. Venlafaxine HCl was loaded onto Indion 244 by batch method and then resinate were wet granulated with ethyl cellulose and blended with hydroxypropylmethylcellulose and compressed. A central composite design for 2 factors at 3 levels each was employed to systematically optimize drug release profile at 2 h and at 18 h. Hydroxypropylmethylcellulose and ethylcellulose were taken as the independent variables. Response surface plots and contour plots were drawn, and optimum formulations were selected by feasibility and grid searches. Resinate shows inadequate sustained release profile. Compressed matrices exhibited the anomalous release mechanism, as the value of release rate exponent (n) varied between 08109 and 08719, resulting in regulated and complete release until 20 h. Validation of optimization study, performed using five confirmatory runs, indicated very high degree of prognostic ability of response surface methodology, with mean percentage error as 1.152+/-1.88%. Regulated drug release study indicates that the hydrophilic and hydrophobic matrix tablets of venlafaxine resinate prepared using hydroxypropylmethylcellulose and ethylcellulose, can successfully be employed as a once-a-day oral controlled release drug delivery system.

No MeSH data available.


Influence of HPMC and EC on the release at 2 h.HPMC is hydroxypropylmethylcellulose and EC is ethylcellulose. A) Response surface and B) contour plot; X1= A:Amount of HPMC, X2= B:Amount of EC
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Figure 0005: Influence of HPMC and EC on the release at 2 h.HPMC is hydroxypropylmethylcellulose and EC is ethylcellulose. A) Response surface and B) contour plot; X1= A:Amount of HPMC, X2= B:Amount of EC

Mentions: Figs. 5 and 6 portray the 3 dimensional response surface plots and the corresponding contour plots for the studied response properties viz rel2h and rel18h, respectively. Fig. 5, shows that release after 2 h varies in a nearly linear descending pattern with a change in the amount of polymers. Fig. 6 also exhibits a near linear trend of release after 18 h, but in ascending order. As there is no confounding of the contour lines in figs. 5 or 6, both the polymers seem to contribute independently towards drug release. For all of the 5 checkpoint formulations, the results of the dissolution parameters showed in Table 4. Table 5 lists the compositions of the checkpoints, their predicted and experimental values of all the response variables, and the percentage error in prognosis.


Formulation and optimization of sustained release tablets of venlafaxine resinates using response surface methodology.

Madgulkar AR, Bhalekar MR, Kolhe VJ, Kenjale YD - Indian J Pharm Sci (2009)

Influence of HPMC and EC on the release at 2 h.HPMC is hydroxypropylmethylcellulose and EC is ethylcellulose. A) Response surface and B) contour plot; X1= A:Amount of HPMC, X2= B:Amount of EC
© Copyright Policy - open-access
Related In: Results  -  Collection

License
Show All Figures
getmorefigures.php?uid=PMC2865810&req=5

Figure 0005: Influence of HPMC and EC on the release at 2 h.HPMC is hydroxypropylmethylcellulose and EC is ethylcellulose. A) Response surface and B) contour plot; X1= A:Amount of HPMC, X2= B:Amount of EC
Mentions: Figs. 5 and 6 portray the 3 dimensional response surface plots and the corresponding contour plots for the studied response properties viz rel2h and rel18h, respectively. Fig. 5, shows that release after 2 h varies in a nearly linear descending pattern with a change in the amount of polymers. Fig. 6 also exhibits a near linear trend of release after 18 h, but in ascending order. As there is no confounding of the contour lines in figs. 5 or 6, both the polymers seem to contribute independently towards drug release. For all of the 5 checkpoint formulations, the results of the dissolution parameters showed in Table 4. Table 5 lists the compositions of the checkpoints, their predicted and experimental values of all the response variables, and the percentage error in prognosis.

Bottom Line: Compressed matrices exhibited the anomalous release mechanism, as the value of release rate exponent (n) varied between 08109 and 08719, resulting in regulated and complete release until 20 h.Validation of optimization study, performed using five confirmatory runs, indicated very high degree of prognostic ability of response surface methodology, with mean percentage error as 1.152+/-1.88%.Regulated drug release study indicates that the hydrophilic and hydrophobic matrix tablets of venlafaxine resinate prepared using hydroxypropylmethylcellulose and ethylcellulose, can successfully be employed as a once-a-day oral controlled release drug delivery system.

View Article: PubMed Central - PubMed

Affiliation: AISSMS College of Pharmacy, Kennedy Road, Near RTO, Pune-411 001, India.

ABSTRACT
The aim of the current study was to design sustained release matrix tablets of venlafaxine hydrochloride using ion exchange resin with the incorporation of hydrophilic and hydrophobic polymer combinations. Venlafaxine HCl was loaded onto Indion 244 by batch method and then resinate were wet granulated with ethyl cellulose and blended with hydroxypropylmethylcellulose and compressed. A central composite design for 2 factors at 3 levels each was employed to systematically optimize drug release profile at 2 h and at 18 h. Hydroxypropylmethylcellulose and ethylcellulose were taken as the independent variables. Response surface plots and contour plots were drawn, and optimum formulations were selected by feasibility and grid searches. Resinate shows inadequate sustained release profile. Compressed matrices exhibited the anomalous release mechanism, as the value of release rate exponent (n) varied between 08109 and 08719, resulting in regulated and complete release until 20 h. Validation of optimization study, performed using five confirmatory runs, indicated very high degree of prognostic ability of response surface methodology, with mean percentage error as 1.152+/-1.88%. Regulated drug release study indicates that the hydrophilic and hydrophobic matrix tablets of venlafaxine resinate prepared using hydroxypropylmethylcellulose and ethylcellulose, can successfully be employed as a once-a-day oral controlled release drug delivery system.

No MeSH data available.