Comparison of the effect of tromethamine and polyvinylpyrrolidone on dissolution properties and analgesic effect of nimesulide |
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Authors: | Hamdy Abdelkader Ossama Y Abdallah Hesham S Salem |
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Institution: | (1) Department of Pharmaceutics, Faculty of Pharmacy, Minia University, Minia, Egypt;(2) Department of Pharmaceutics, Faculty of Pharmacy, Alexandria University, Alexandria, Egypt;(3) Department of Analytical Chemistry, Faculty of Pharmacy, Minia University, Minia, Egypt |
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Abstract: | The solubilizing and absorption enhancer properties towards nimesulide (ND) of tromethamine (Tris) and polyvinylpyrrolidone
(PVP) have been investigated. Solid binary systems were prepared at various drug-polymer ratios by mixing or coprecipitation,
characterized by differential scanning calorimetry, X-ray diffractometry, and Fourier transform infrared spectroscopy, and
tested for dissolution behavior. Both carriers improved drug dissolution and their performance depended on concentration of
the hydrophilic carrier in coprecipitates. Tris was more effective than PVP, despite the amorphizing power of PVP as revealed
by solid state analyses. Complete drug amorphiztion was attained at 1∶3 (wt/wt) drug: PVP, 25% (wt/wt) ND in PVP. According
to thermal behavior of ND and Tris, ND-Tris systems present a eutectic behavior. The eutectic composition was 30% ND-70% Tris
at ∼129°C. Amorphous ND-PVP and eutectic ND-Tris mixtures showed an improvement of 5.55 and 6.6 times of drug dissolution
efficiency, respectively. In vivo experiments in mice demonstrated that administration of 60 mg/kg of drug coprecipitated
with PVP or Tris resulted, respectively, in a 50% and 94% reduction of acetic acid-induced writhings in comparison with pure
drug, which, instead, was statistically ineffective as compared with the control group. Moreover, the eutectic mixture of
ND-Tris demonstrated antiwrithing potency 1.88 times higher than amorphous ND-PVP coprecipitate. Thus, the solubilizing power,
dissolution-enhancing effect, and analgesic effect enhancer ability toward the drug make Tris particularly suitable for developing
a reduced-dose, fast-release solid oral dosage form of nimesulide.
Published: August 10, 2007 |
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Keywords: | Nimesulide Polyvinylpyrrolidone Tromethamine Analgesic effect Coprecipitation |
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