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Design of fast disintegrating tablets of prochlorperazine maleate by effervescence method.

Shirsand SB, Suresh S, Para MS, Swamy PV - Indian J Pharm Sci (2009)

Bottom Line: In this method, mixtures of sodium bicarbonate and anhydrous citric acid in different ratios along with crospovidone (2-10% w/w), croscarmellose sodium (2-10% w/w) were used as superdisintegrants.Among the two promising formulations, the formulation containing 10% w/w of crospovidone and mixture of 20% w/w sodium bicarbonate and 15% w/w of citric acid emerged as the overall best formulation (t(50%) 6 min) based on drug release characteristics in pH 6.8 phosphate buffer compared to commercial conventional tablet formulation (t(50%) 17.4 min).Short-term stability studies on the promising formulations indicated that there are no significant changes in drug content and in vitro dispersion time (p<0.05).

View Article: PubMed Central - PubMed

Affiliation: Department of Pharmaceutical Technology, H. K. E. Society's College of Pharmacy, Sedam Road, Gulbarga-585 105, India.

ABSTRACT
In the present work, fast disintegrating tablets of prochlorperazine maleate were designed with a view to enhance patient compliance by effervescent method. In this method, mixtures of sodium bicarbonate and anhydrous citric acid in different ratios along with crospovidone (2-10% w/w), croscarmellose sodium (2-10% w/w) were used as superdisintegrants. Estimation of prochlorperazine maleate in the prepared tablet formulations was carried out by extracting the drug with methanol and measuring the absorbance at 254.5 nm. The prepared formulations were further evaluated for hardness, friability, drug content uniformity and in vitro dispersion time. Based on in vitro dispersion time (approximately 13-21 s), two promising formulations (one from each super-disintegrant) were tested for in vitro drug release pattern in pH 6.8 phosphate buffer, short-term stability (at 40 degrees /75% relative humidity for 3 mo) and drug-excipient interaction (IR spectroscopy). Among the two promising formulations, the formulation containing 10% w/w of crospovidone and mixture of 20% w/w sodium bicarbonate and 15% w/w of citric acid emerged as the overall best formulation (t(50%) 6 min) based on drug release characteristics in pH 6.8 phosphate buffer compared to commercial conventional tablet formulation (t(50%) 17.4 min). Short-term stability studies on the promising formulations indicated that there are no significant changes in drug content and in vitro dispersion time (p<0.05).

No MeSH data available.


Related in: MedlinePlus

In vitro cumulative percent drug release versus time profile of promising formulationsPlot showing percent cumulative release of promising prochlorperazine maleate formulations in pH 6.8 phosphate buffer. EC0 (-♦-), CCF (-▪-), ECCS4 (-▲-), ECP4 (-χ-). The values expressed are average of three readings.
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Figure 0001: In vitro cumulative percent drug release versus time profile of promising formulationsPlot showing percent cumulative release of promising prochlorperazine maleate formulations in pH 6.8 phosphate buffer. EC0 (-♦-), CCF (-▪-), ECCS4 (-▲-), ECP4 (-χ-). The values expressed are average of three readings.

Mentions: In vitro dissolution studies on the promising formulations (ECP4 and ECCS4), the control (EC0) and CCF (Stemitil 5 mg, Nicolas Piramal Health Care, Baddi, HP, India) were carried out in pH 6.8 phosphate buffer, and the various dissolution parameter values viz., percent drug dissolved in 5, 10 and 15 min (D5, D10 and D15), dissolution efficiency at 10 min (DE10min)[12], t50%, t70% and t90% are shown in Table 3 and the dissolution profiles depicted in fig. 1. This data reveals that overall, the formulation ECP4 containing 10% w/w of CP along with effervescent mixture has shown nearly three-fold faster drug release (t50% 6 min) when compared to the CCF of prochlorperazine maleate (t50% 17.4 min) and released five-times more drug than the control formulation in 10 min.


Design of fast disintegrating tablets of prochlorperazine maleate by effervescence method.

Shirsand SB, Suresh S, Para MS, Swamy PV - Indian J Pharm Sci (2009)

In vitro cumulative percent drug release versus time profile of promising formulationsPlot showing percent cumulative release of promising prochlorperazine maleate formulations in pH 6.8 phosphate buffer. EC0 (-♦-), CCF (-▪-), ECCS4 (-▲-), ECP4 (-χ-). The values expressed are average of three readings.
© Copyright Policy - open-access
Related In: Results  -  Collection

License
Show All Figures
getmorefigures.php?uid=PMC2865821&req=5

Figure 0001: In vitro cumulative percent drug release versus time profile of promising formulationsPlot showing percent cumulative release of promising prochlorperazine maleate formulations in pH 6.8 phosphate buffer. EC0 (-♦-), CCF (-▪-), ECCS4 (-▲-), ECP4 (-χ-). The values expressed are average of three readings.
Mentions: In vitro dissolution studies on the promising formulations (ECP4 and ECCS4), the control (EC0) and CCF (Stemitil 5 mg, Nicolas Piramal Health Care, Baddi, HP, India) were carried out in pH 6.8 phosphate buffer, and the various dissolution parameter values viz., percent drug dissolved in 5, 10 and 15 min (D5, D10 and D15), dissolution efficiency at 10 min (DE10min)[12], t50%, t70% and t90% are shown in Table 3 and the dissolution profiles depicted in fig. 1. This data reveals that overall, the formulation ECP4 containing 10% w/w of CP along with effervescent mixture has shown nearly three-fold faster drug release (t50% 6 min) when compared to the CCF of prochlorperazine maleate (t50% 17.4 min) and released five-times more drug than the control formulation in 10 min.

Bottom Line: In this method, mixtures of sodium bicarbonate and anhydrous citric acid in different ratios along with crospovidone (2-10% w/w), croscarmellose sodium (2-10% w/w) were used as superdisintegrants.Among the two promising formulations, the formulation containing 10% w/w of crospovidone and mixture of 20% w/w sodium bicarbonate and 15% w/w of citric acid emerged as the overall best formulation (t(50%) 6 min) based on drug release characteristics in pH 6.8 phosphate buffer compared to commercial conventional tablet formulation (t(50%) 17.4 min).Short-term stability studies on the promising formulations indicated that there are no significant changes in drug content and in vitro dispersion time (p<0.05).

View Article: PubMed Central - PubMed

Affiliation: Department of Pharmaceutical Technology, H. K. E. Society's College of Pharmacy, Sedam Road, Gulbarga-585 105, India.

ABSTRACT
In the present work, fast disintegrating tablets of prochlorperazine maleate were designed with a view to enhance patient compliance by effervescent method. In this method, mixtures of sodium bicarbonate and anhydrous citric acid in different ratios along with crospovidone (2-10% w/w), croscarmellose sodium (2-10% w/w) were used as superdisintegrants. Estimation of prochlorperazine maleate in the prepared tablet formulations was carried out by extracting the drug with methanol and measuring the absorbance at 254.5 nm. The prepared formulations were further evaluated for hardness, friability, drug content uniformity and in vitro dispersion time. Based on in vitro dispersion time (approximately 13-21 s), two promising formulations (one from each super-disintegrant) were tested for in vitro drug release pattern in pH 6.8 phosphate buffer, short-term stability (at 40 degrees /75% relative humidity for 3 mo) and drug-excipient interaction (IR spectroscopy). Among the two promising formulations, the formulation containing 10% w/w of crospovidone and mixture of 20% w/w sodium bicarbonate and 15% w/w of citric acid emerged as the overall best formulation (t(50%) 6 min) based on drug release characteristics in pH 6.8 phosphate buffer compared to commercial conventional tablet formulation (t(50%) 17.4 min). Short-term stability studies on the promising formulations indicated that there are no significant changes in drug content and in vitro dispersion time (p<0.05).

No MeSH data available.


Related in: MedlinePlus