Formulation and Evaluation of Liquisolid Compacts for Olmesartan Medoxomil
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 confront...
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Published in: | Journal of Drug Delivery Vol. 2013; no. 2013; pp. 283 - 291 |
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Cairo, Egypt
Hindawi Limiteds
01-01-2013
Hindawi Puplishing Corporation Hindawi Publishing Corporation John Wiley & Sons, Inc |
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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. |
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AbstractList | 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. 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. |
Audience | Academic |
Author | Chhaganbhai N. Patel Dashrath M. Patel Shailesh T. Prajapati Suresh K. Dumaniya Hitesh H. Bulchandani |
AuthorAffiliation | 1 Department of Pharmaceutics, Shri Sarvajanik Pharmacy College, Near Arvind Baug, Mehsana, Gujarat 384001, India 2 Department of Pharmaceutical Chemistry, Shri Sarvajanik Pharmacy College, Near Arvind Baug, Mehsana, Gujarat 384001, India |
AuthorAffiliation_xml | – name: 1 Department of Pharmaceutics, Shri Sarvajanik Pharmacy College, Near Arvind Baug, Mehsana, Gujarat 384001, India – name: 2 Department of Pharmaceutical Chemistry, Shri Sarvajanik Pharmacy College, Near Arvind Baug, Mehsana, Gujarat 384001, India |
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Cites_doi | 10.1016/S0378-5173(01)00867-5 10.1111/j.1524-6175.2002.01051.x 10.1021/js970346g 10.1124/dmd.105.008888 10.2165/00003495-200262090-00005 10.2478/v10298-012-0061-2 10.1111/j.1365-2125.1988.tb03318.x 10.1016/j.ijpharm.2007.03.034 |
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Contributor | Prajapati, Shailesh T Patel, Chhaganbhai N Bulchandani, Hitesh H Patel, Dasharath M Dumaniya, Suresh K |
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Copyright | Copyright © 2013 Shailesh T. Prajapati et al. COPYRIGHT 2013 John Wiley & Sons, Inc. Copyright © 2013 Shailesh T. Prajapati et al. 2013 |
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References | (3) 2007; 341 (4) 2005; 8 (5) 1998; 87 (2) 2001; 229 (7) 2002; 4 (1) 1988; 25 (9) 2012; 434 (10) 2012; 45 (6) 2002; 62 (8) 2006; 34 9649356 - J Pharm Sci. 1998 Jul;87(7):867-72 16501004 - Drug Metab Dispos. 2006 May;34(5):862-9 15946594 - J Pharm Pharm Sci. 2005 Jan 12;8(1):18-25 11604272 - Int J Pharm. 2001 Oct 23;229(1-2):193-203 12368570 - J Clin Hypertens (Greenwich). 2002 Sep-Oct;4(5):325-31 17498898 - Int J Pharm. 2007 Aug 16;341(1-2):26-34 22677418 - Int J Pharm. 2012 Sep 15;434(1-2):122-32 3358900 - Br J Clin Pharmacol. 1988 Mar;25(3):387-96 12076183 - Drugs. 2002;62(9):1345-53; discussion 1354-6 2 3 5 8 |
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Snippet | Olmesartan medoxomil is an angiotensin type II receptor blocker, antihypertensive agent, administered orally. It is highly lipophilic (log P 5.5) and a poorly... Olmesartan medoxomil is an angiotensin type II receptor blocker, antihypertensive agent, administered orally. It is highly lipophilic (log P 5.5) and a poorly... |
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Title | Formulation and Evaluation of Liquisolid Compacts for Olmesartan Medoxomil |
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