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Dissolution Enhancement of Rosuvastatin Calcium by Liquisolid Compact Technique.

Kapure VJ, Pande VV, Deshmukh PK - J Pharm (Cairo) (2013)

Bottom Line: The model drug RVT, a HMG-Co A reductase inhibitor was formulated in form of directly compressed tablets and liquisolid compacts; and studied for in-vitro release characteristics at different dissolution conditions.In this technique, liquid medications of water insoluble drugs in non-volatile liquid vehicles can be converted into acceptably flowing and compressible powders.As liquisolid compacts demonstrated significantly higher drug release rates, we lead to conclusion that it could be a promising strategy in improving the dissolution of poor water soluble drugs and formulating immediate release solid dosage forms.

View Article: PubMed Central - PubMed

Affiliation: Department of Pharmaceutics and Quality Assurance, H. R. Patel Institute of Pharmaceutical Education and Research, Shirpur, Maharashtra 425405, India.

ABSTRACT
In present investigation liquisolid compact technique is investigated as a tool for enhanced dissolution of poorly water-soluble drug Rosuvastatin calcium (RVT). The model drug RVT, a HMG-Co A reductase inhibitor was formulated in form of directly compressed tablets and liquisolid compacts; and studied for in-vitro release characteristics at different dissolution conditions. In this technique, liquid medications of water insoluble drugs in non-volatile liquid vehicles can be converted into acceptably flowing and compressible powders. Formulated systems were assessed for precompression parameters like flow properties of liquisolid system, Fourior transform infra red spectra (FTIR) analysis, X-ray powder diffraction (XRPD), differential scanning calorimetry (DSC), and post compression parameters like content uniformity, weight variation, hardness and friability, disintegration test, wetting time, in vitro dissolution studies, effect of dissolution volume on drug release rate, and estimation of fraction of molecularly dispersed drug in liquid medication. As liquisolid compacts demonstrated significantly higher drug release rates, we lead to conclusion that it could be a promising strategy in improving the dissolution of poor water soluble drugs and formulating immediate release solid dosage forms.

No MeSH data available.


Related in: MedlinePlus

Effect of the dissolution volume on the initial dissolution rate of liquisolid compact (LS-1) exhibited by the liquisolid compacts and directly compressed tablets using different dissolution media.
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Related In: Results  -  Collection


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fig8: Effect of the dissolution volume on the initial dissolution rate of liquisolid compact (LS-1) exhibited by the liquisolid compacts and directly compressed tablets using different dissolution media.

Mentions: It seems that the drug dissolution rate of liquisolid compacts is significantly faster than that of the plain tablets, and it is independent of the volume of the dissolving liquid used. Furthermore, it is apparent that decreasing dissolution volumes result in a proportional decrease of the in vitro drug release rates displayed by the directly compressed tablets. According to the “diffusion layer model” dissolution theories, the dissolution rate of a drug is directly proportional to its concentration gradient (ΔC = Cs − C) in the stagnant diffusion layer formed by the dissolving liquid around the drug particles. Cs is the saturation solubility of the drug in the dissolution medium, and, thus, it is a constant characteristic property related to the drug and dissolving liquid involved. On the other hand, C, the drug concentration in the bulk of the dissolving medium, increases with decreasing volumes of dissolution fluid used. Therefore, the ΔC values existing in the three different dissolution volumes of our tests decrease with decreasing volumes of dissolution medium. Consequently such ΔC reduction is directly related to the decreased drug dissolution rates of the conventional tablets with the decreasing volumes of both the dissolution media used (Figure 8).


Dissolution Enhancement of Rosuvastatin Calcium by Liquisolid Compact Technique.

Kapure VJ, Pande VV, Deshmukh PK - J Pharm (Cairo) (2013)

Effect of the dissolution volume on the initial dissolution rate of liquisolid compact (LS-1) exhibited by the liquisolid compacts and directly compressed tablets using different dissolution media.
© Copyright Policy - open-access
Related In: Results  -  Collection

Show All Figures
getmorefigures.php?uid=PMC4590788&req=5

fig8: Effect of the dissolution volume on the initial dissolution rate of liquisolid compact (LS-1) exhibited by the liquisolid compacts and directly compressed tablets using different dissolution media.
Mentions: It seems that the drug dissolution rate of liquisolid compacts is significantly faster than that of the plain tablets, and it is independent of the volume of the dissolving liquid used. Furthermore, it is apparent that decreasing dissolution volumes result in a proportional decrease of the in vitro drug release rates displayed by the directly compressed tablets. According to the “diffusion layer model” dissolution theories, the dissolution rate of a drug is directly proportional to its concentration gradient (ΔC = Cs − C) in the stagnant diffusion layer formed by the dissolving liquid around the drug particles. Cs is the saturation solubility of the drug in the dissolution medium, and, thus, it is a constant characteristic property related to the drug and dissolving liquid involved. On the other hand, C, the drug concentration in the bulk of the dissolving medium, increases with decreasing volumes of dissolution fluid used. Therefore, the ΔC values existing in the three different dissolution volumes of our tests decrease with decreasing volumes of dissolution medium. Consequently such ΔC reduction is directly related to the decreased drug dissolution rates of the conventional tablets with the decreasing volumes of both the dissolution media used (Figure 8).

Bottom Line: The model drug RVT, a HMG-Co A reductase inhibitor was formulated in form of directly compressed tablets and liquisolid compacts; and studied for in-vitro release characteristics at different dissolution conditions.In this technique, liquid medications of water insoluble drugs in non-volatile liquid vehicles can be converted into acceptably flowing and compressible powders.As liquisolid compacts demonstrated significantly higher drug release rates, we lead to conclusion that it could be a promising strategy in improving the dissolution of poor water soluble drugs and formulating immediate release solid dosage forms.

View Article: PubMed Central - PubMed

Affiliation: Department of Pharmaceutics and Quality Assurance, H. R. Patel Institute of Pharmaceutical Education and Research, Shirpur, Maharashtra 425405, India.

ABSTRACT
In present investigation liquisolid compact technique is investigated as a tool for enhanced dissolution of poorly water-soluble drug Rosuvastatin calcium (RVT). The model drug RVT, a HMG-Co A reductase inhibitor was formulated in form of directly compressed tablets and liquisolid compacts; and studied for in-vitro release characteristics at different dissolution conditions. In this technique, liquid medications of water insoluble drugs in non-volatile liquid vehicles can be converted into acceptably flowing and compressible powders. Formulated systems were assessed for precompression parameters like flow properties of liquisolid system, Fourior transform infra red spectra (FTIR) analysis, X-ray powder diffraction (XRPD), differential scanning calorimetry (DSC), and post compression parameters like content uniformity, weight variation, hardness and friability, disintegration test, wetting time, in vitro dissolution studies, effect of dissolution volume on drug release rate, and estimation of fraction of molecularly dispersed drug in liquid medication. As liquisolid compacts demonstrated significantly higher drug release rates, we lead to conclusion that it could be a promising strategy in improving the dissolution of poor water soluble drugs and formulating immediate release solid dosage forms.

No MeSH data available.


Related in: MedlinePlus