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Formulation and evaluation of bilayer tablet for bimodal release of venlafaxine hydrochloride.

Momin MM, Kane S, Abhang P - Front Pharmacol (2015)

Bottom Line: The selected responses, bioadhesion force (0.11-0.25 ± 0.023 g), amount of drug released in 10 h, Y10 (78.20-95.78 ± 1.24%) and bioadhesive strength, (19-24 ± 2 h) presented good correlation with the selected independent variables.Statistical analysis (ANOVA) of the optimized bilayer formulations showed no significant difference in the cumulative amount of drug release after 15 min, but significant difference (p < 0.05) in the amount of drug released after 1 hr till 12 h from optimized formulations was observed.The natural mucilage like FNM could be successfully incorporated into tablet with only 20% replacement with HPMC and it showed good bioadhesiveness and sustained drug release.

View Article: PubMed Central - PubMed

Affiliation: Department of Pharmaceutics, SVKM's Dr. Bhanuben Nanavati College of Pharmacy Mumbai, India.

ABSTRACT
The aim of the present research was to develop a bilayer tablet of venlafaxine hydrochloride for bimodal drug release. In the present investigation authors have tried to explore fenugreek mucilage (FNM) for bioadhesive sustained release layer. The attempt has been made to combine FNM with well studied bioadhesive polymers like hydroxy propyl methyl cellulose (HPMC), Carbopol, and Xanthan Gum. The formulations were evaluated for swelling Index, ex vivo bioadhesion, water uptake studies, in vitro drug release and dissolution kinetics was studied. Substantial bioadhesion force (2.4 ± 0.023 g) and tablet adhesion retention time (24 ± 2 h) was observed with FNM and HPMC combination at 80:20 ratio. The dissolution kinetics followed the Higuchi model (R (2) = 0.9913) via a non-Fickian diffusion controlled release mechanism after the initial burst. The 3(2) full factorial design was employed in the present study. The type of polymers used in combination with FNM (X1) and percent polymer replaced with FNM (X2) were taken as independent formulations variables. The selected responses, bioadhesion force (0.11-0.25 ± 0.023 g), amount of drug released in 10 h, Y10 (78.20-95.78 ± 1.24%) and bioadhesive strength, (19-24 ± 2 h) presented good correlation with the selected independent variables. Statistical analysis (ANOVA) of the optimized bilayer formulations showed no significant difference in the cumulative amount of drug release after 15 min, but significant difference (p < 0.05) in the amount of drug released after 1 hr till 12 h from optimized formulations was observed. The natural mucilage like FNM could be successfully incorporated into tablet with only 20% replacement with HPMC and it showed good bioadhesiveness and sustained drug release.

No MeSH data available.


Related in: MedlinePlus

3-D Graph for effect of independent variables on Y10.
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Figure 3: 3-D Graph for effect of independent variables on Y10.

Mentions: The independent variable, Y10, Bioadhesion force, and bioadhesion Retention Time were compared statistically using Design Expert software and polynomial equation was derived. The Figure 3 depicts the effect of polymer and type of polymer used in combination with FNM at different level. From Eqs 2–4, it can be concluded that, Xanthan Gum has a predominant effect on drug release, as compared to Carbopol and HPMC. Xanthan Gum has a negative effect on the amount of drug release Whereas, Carbopol and FNM combination does not sustain drug release significantly. Figure 3 depicts the response surface plot, showing the influence of HPMC, Xanthan Gum, and Carbopol-934P on Y10. The surface plot shows that Y10 varies as the concentration of the three polymers changes. From the contour plot (Figures 4 and 5), it can be concluded that all polymers at the selected levels with FNM significantly affect the bioadhesive strength and retention time. Figure 5 presents the corresponding contour plot, showing the relationship between various levels of the three polymers.


Formulation and evaluation of bilayer tablet for bimodal release of venlafaxine hydrochloride.

Momin MM, Kane S, Abhang P - Front Pharmacol (2015)

3-D Graph for effect of independent variables on Y10.
© Copyright Policy
Related In: Results  -  Collection

License
Show All Figures
getmorefigures.php?uid=PMC4496574&req=5

Figure 3: 3-D Graph for effect of independent variables on Y10.
Mentions: The independent variable, Y10, Bioadhesion force, and bioadhesion Retention Time were compared statistically using Design Expert software and polynomial equation was derived. The Figure 3 depicts the effect of polymer and type of polymer used in combination with FNM at different level. From Eqs 2–4, it can be concluded that, Xanthan Gum has a predominant effect on drug release, as compared to Carbopol and HPMC. Xanthan Gum has a negative effect on the amount of drug release Whereas, Carbopol and FNM combination does not sustain drug release significantly. Figure 3 depicts the response surface plot, showing the influence of HPMC, Xanthan Gum, and Carbopol-934P on Y10. The surface plot shows that Y10 varies as the concentration of the three polymers changes. From the contour plot (Figures 4 and 5), it can be concluded that all polymers at the selected levels with FNM significantly affect the bioadhesive strength and retention time. Figure 5 presents the corresponding contour plot, showing the relationship between various levels of the three polymers.

Bottom Line: The selected responses, bioadhesion force (0.11-0.25 ± 0.023 g), amount of drug released in 10 h, Y10 (78.20-95.78 ± 1.24%) and bioadhesive strength, (19-24 ± 2 h) presented good correlation with the selected independent variables.Statistical analysis (ANOVA) of the optimized bilayer formulations showed no significant difference in the cumulative amount of drug release after 15 min, but significant difference (p < 0.05) in the amount of drug released after 1 hr till 12 h from optimized formulations was observed.The natural mucilage like FNM could be successfully incorporated into tablet with only 20% replacement with HPMC and it showed good bioadhesiveness and sustained drug release.

View Article: PubMed Central - PubMed

Affiliation: Department of Pharmaceutics, SVKM's Dr. Bhanuben Nanavati College of Pharmacy Mumbai, India.

ABSTRACT
The aim of the present research was to develop a bilayer tablet of venlafaxine hydrochloride for bimodal drug release. In the present investigation authors have tried to explore fenugreek mucilage (FNM) for bioadhesive sustained release layer. The attempt has been made to combine FNM with well studied bioadhesive polymers like hydroxy propyl methyl cellulose (HPMC), Carbopol, and Xanthan Gum. The formulations were evaluated for swelling Index, ex vivo bioadhesion, water uptake studies, in vitro drug release and dissolution kinetics was studied. Substantial bioadhesion force (2.4 ± 0.023 g) and tablet adhesion retention time (24 ± 2 h) was observed with FNM and HPMC combination at 80:20 ratio. The dissolution kinetics followed the Higuchi model (R (2) = 0.9913) via a non-Fickian diffusion controlled release mechanism after the initial burst. The 3(2) full factorial design was employed in the present study. The type of polymers used in combination with FNM (X1) and percent polymer replaced with FNM (X2) were taken as independent formulations variables. The selected responses, bioadhesion force (0.11-0.25 ± 0.023 g), amount of drug released in 10 h, Y10 (78.20-95.78 ± 1.24%) and bioadhesive strength, (19-24 ± 2 h) presented good correlation with the selected independent variables. Statistical analysis (ANOVA) of the optimized bilayer formulations showed no significant difference in the cumulative amount of drug release after 15 min, but significant difference (p < 0.05) in the amount of drug released after 1 hr till 12 h from optimized formulations was observed. The natural mucilage like FNM could be successfully incorporated into tablet with only 20% replacement with HPMC and it showed good bioadhesiveness and sustained drug release.

No MeSH data available.


Related in: MedlinePlus