Limits...
Formulation and evaluation of liquisolid compacts for olmesartan medoxomil.

Prajapati ST, Bulchandani HH, Patel DM, Dumaniya SK, Patel CN - J Drug Deliv (2013)

Bottom Line: The objective of the present investigation was to develop liquisolid compacts for olmesartan medoxomil to improve the dissolution rate.The interaction between drug and excipients was characterized by DSC and FT-IR studies, which showed that there is no interaction between drug and excipients.The dissolution studies for liquisolid compacts and conventional formulations were carried out, and it was found that liquisolid compacts with 80% w/w of Acrysol EL 135 to the drug showed significant higher drug release rates than conventional tablets.

View Article: PubMed Central - PubMed

Affiliation: Department of Pharmaceutics, Shri Sarvajanik Pharmacy College, Near Arvind Baug, Mehsana, Gujarat 384001, India.

ABSTRACT
Olmesartan medoxomil is an angiotensin type II receptor blocker, antihypertensive agent, administered orally. It is highly lipophilic (log P 5.5) and a poorly water-soluble drug with absolute bioavailability of 26%. The poor dissolution rate of water-insoluble drugs is still a major problem confronting the pharmaceutical industry. The objective of the present investigation was to develop liquisolid compacts for olmesartan medoxomil to improve the dissolution rate. Liquisolid compacts were prepared using Acrysol El 135 as a solvent, Avicel PH 102, Fujicalin and Neusilin as carrier materials, and Aerosil as coating material in different ratios. The interaction between drug and excipients was characterized by DSC and FT-IR studies, which showed that there is no interaction between drug and excipients. The powder characteristics were evaluated by different flow parameters to comply with pharmacopoeial limits. The dissolution studies for liquisolid compacts and conventional formulations were carried out, and it was found that liquisolid compacts with 80% w/w of Acrysol EL 135 to the drug showed significant higher drug release rates than conventional tablets. Amongst carriers used Fujicalin and Neusilin were found to be more effective carrier materials for liquid adsorption.

No MeSH data available.


(a) The angle of slide of Avicel and Aerosil with Acrysol EL 135. (b) The angle of slide of Fujicalin and Aerosil with Acrysol EL 135. (c) The angle of slide of Neusilin and Aerosil with Acrysol EL 135.
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fig2: (a) The angle of slide of Avicel and Aerosil with Acrysol EL 135. (b) The angle of slide of Fujicalin and Aerosil with Acrysol EL 135. (c) The angle of slide of Neusilin and Aerosil with Acrysol EL 135.

Mentions: Angle of slide determination is an important step in the formulation of liquisolid tablets. The relationship of angle of slide with corresponding φ of Avicel, Fujicalin, Neusilin, and φCo of Aerosil for Acrysol EL 135 liquid vehicle are shown in Figures 2(a), 2(b), and 2(c), respectively. The φCa and φCo for liquid vehicles were used to calculate Lf. The Lf was then used to decide the optimum amount of carrier and coating materials required to ensure dry-looking, free-flowing and compactible powdered systems. The lowest liquid factor was obtained for Avicel PH 102, and accordingly, the amount of carrier was higher than other formulations. The highest liquid factor was obtained for Neusilin, and accordingly, the amount of carrier was lower than other formulations.


Formulation and evaluation of liquisolid compacts for olmesartan medoxomil.

Prajapati ST, Bulchandani HH, Patel DM, Dumaniya SK, Patel CN - J Drug Deliv (2013)

(a) The angle of slide of Avicel and Aerosil with Acrysol EL 135. (b) The angle of slide of Fujicalin and Aerosil with Acrysol EL 135. (c) The angle of slide of Neusilin and Aerosil with Acrysol EL 135.
© Copyright Policy - open-access
Related In: Results  -  Collection

Show All Figures
getmorefigures.php?uid=PMC3818897&req=5

fig2: (a) The angle of slide of Avicel and Aerosil with Acrysol EL 135. (b) The angle of slide of Fujicalin and Aerosil with Acrysol EL 135. (c) The angle of slide of Neusilin and Aerosil with Acrysol EL 135.
Mentions: Angle of slide determination is an important step in the formulation of liquisolid tablets. The relationship of angle of slide with corresponding φ of Avicel, Fujicalin, Neusilin, and φCo of Aerosil for Acrysol EL 135 liquid vehicle are shown in Figures 2(a), 2(b), and 2(c), respectively. The φCa and φCo for liquid vehicles were used to calculate Lf. The Lf was then used to decide the optimum amount of carrier and coating materials required to ensure dry-looking, free-flowing and compactible powdered systems. The lowest liquid factor was obtained for Avicel PH 102, and accordingly, the amount of carrier was higher than other formulations. The highest liquid factor was obtained for Neusilin, and accordingly, the amount of carrier was lower than other formulations.

Bottom Line: The objective of the present investigation was to develop liquisolid compacts for olmesartan medoxomil to improve the dissolution rate.The interaction between drug and excipients was characterized by DSC and FT-IR studies, which showed that there is no interaction between drug and excipients.The dissolution studies for liquisolid compacts and conventional formulations were carried out, and it was found that liquisolid compacts with 80% w/w of Acrysol EL 135 to the drug showed significant higher drug release rates than conventional tablets.

View Article: PubMed Central - PubMed

Affiliation: Department of Pharmaceutics, Shri Sarvajanik Pharmacy College, Near Arvind Baug, Mehsana, Gujarat 384001, India.

ABSTRACT
Olmesartan medoxomil is an angiotensin type II receptor blocker, antihypertensive agent, administered orally. It is highly lipophilic (log P 5.5) and a poorly water-soluble drug with absolute bioavailability of 26%. The poor dissolution rate of water-insoluble drugs is still a major problem confronting the pharmaceutical industry. The objective of the present investigation was to develop liquisolid compacts for olmesartan medoxomil to improve the dissolution rate. Liquisolid compacts were prepared using Acrysol El 135 as a solvent, Avicel PH 102, Fujicalin and Neusilin as carrier materials, and Aerosil as coating material in different ratios. The interaction between drug and excipients was characterized by DSC and FT-IR studies, which showed that there is no interaction between drug and excipients. The powder characteristics were evaluated by different flow parameters to comply with pharmacopoeial limits. The dissolution studies for liquisolid compacts and conventional formulations were carried out, and it was found that liquisolid compacts with 80% w/w of Acrysol EL 135 to the drug showed significant higher drug release rates than conventional tablets. Amongst carriers used Fujicalin and Neusilin were found to be more effective carrier materials for liquid adsorption.

No MeSH data available.