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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

FT-IR spectra of (a) Aerosil 200, (b) Avicel PH 102, (c) pure RVT, and (d) liquisolid system (LS-1).
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fig1: FT-IR spectra of (a) Aerosil 200, (b) Avicel PH 102, (c) pure RVT, and (d) liquisolid system (LS-1).

Mentions: Samples of Aerosil 200, Avicel PH-102, pure RVT, and liquisolid system (LS-1) were subjected to FT-IR spectroscopic analysis, and their spectra at 500–4000 cm−1 are shown in Figure 1. Characteristics peaks of aromatic N-H stretching and C=O stretching at 3364.57 cm−1 and 1556.55 cm−1 appeared, respectively. A reduction in the intensity of the characteristics absorption bands of RVT was observed in the liquisolid formulation, which might be attributed to the hydrogen bonding interaction between the carboxylic group of RVT and the hydroxyl group of the liquid vehicles; this resulted in drug dissolution enhancement.


Dissolution Enhancement of Rosuvastatin Calcium by Liquisolid Compact Technique.

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

FT-IR spectra of (a) Aerosil 200, (b) Avicel PH 102, (c) pure RVT, and (d) liquisolid system (LS-1).
© Copyright Policy - open-access
Related In: Results  -  Collection

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

fig1: FT-IR spectra of (a) Aerosil 200, (b) Avicel PH 102, (c) pure RVT, and (d) liquisolid system (LS-1).
Mentions: Samples of Aerosil 200, Avicel PH-102, pure RVT, and liquisolid system (LS-1) were subjected to FT-IR spectroscopic analysis, and their spectra at 500–4000 cm−1 are shown in Figure 1. Characteristics peaks of aromatic N-H stretching and C=O stretching at 3364.57 cm−1 and 1556.55 cm−1 appeared, respectively. A reduction in the intensity of the characteristics absorption bands of RVT was observed in the liquisolid formulation, which might be attributed to the hydrogen bonding interaction between the carboxylic group of RVT and the hydroxyl group of the liquid vehicles; this resulted in drug dissolution enhancement.

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