The effect of HPMC particle size on the drug release rate and the percolation threshold in extended-release mini-tablets
Abstract The particle size of HPMC is a critical factor that can influence drug release rate from hydrophilic matrix systems. Percolation theory is a statistical tool which is used to study the disorder of particles in a lattice of a sample. The percolation threshold is the point at which a componen...
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| Veröffentlicht in: | Drug development and industrial pharmacy 2015-01, Vol.41 (1), p.70-78 |
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| creator | Mohamed, Faiezah A. A. Roberts, Matthew Seton, Linda Ford, James L. Levina, Marina Rajabi-Siahboomi, Ali R. |
| description | Abstract
The particle size of HPMC is a critical factor that can influence drug release rate from hydrophilic matrix systems. Percolation theory is a statistical tool which is used to study the disorder of particles in a lattice of a sample. The percolation threshold is the point at which a component is dominant in a cluster resulting in significant changes in drug release rates. Mini-tablets are compact dosage forms of 1.5-4 mm diameter, which have potential benefits in the delivery of drug to some patient groups such as pediatrics. In this study, the effect of HPMC particle size on hydrocortisone release and its associated percolation threshold for mini-tablets and tablets was assessed. For both mini-tablets and tablets, large polymer particles reduced tensile strength, but increased the drug release rate and the percolation threshold. Upon hydration, compacts with 45-125 μm HPMC particles formed a strong gel layer with low porosity, reducing hydrocortisone release rates. In comparison, faster drug release rates were obtained when 125-355 µm HPMC particles were used, due to the greater pore sizes that resulted in the formation of a weaker gel. Using 125-355 µm HPMC particles increased the percolation threshold for tablets and to a greater extent for mini-tablets. This work has demonstrated the importance of HPMC particle size in ER matrices, the effects of which are even more obvious for mini-tablets. |
| doi_str_mv | 10.3109/03639045.2013.845843 |
| format | Article |
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The particle size of HPMC is a critical factor that can influence drug release rate from hydrophilic matrix systems. Percolation theory is a statistical tool which is used to study the disorder of particles in a lattice of a sample. The percolation threshold is the point at which a component is dominant in a cluster resulting in significant changes in drug release rates. Mini-tablets are compact dosage forms of 1.5-4 mm diameter, which have potential benefits in the delivery of drug to some patient groups such as pediatrics. In this study, the effect of HPMC particle size on hydrocortisone release and its associated percolation threshold for mini-tablets and tablets was assessed. For both mini-tablets and tablets, large polymer particles reduced tensile strength, but increased the drug release rate and the percolation threshold. Upon hydration, compacts with 45-125 μm HPMC particles formed a strong gel layer with low porosity, reducing hydrocortisone release rates. In comparison, faster drug release rates were obtained when 125-355 µm HPMC particles were used, due to the greater pore sizes that resulted in the formation of a weaker gel. Using 125-355 µm HPMC particles increased the percolation threshold for tablets and to a greater extent for mini-tablets. This work has demonstrated the importance of HPMC particle size in ER matrices, the effects of which are even more obvious for mini-tablets.</description><identifier>ISSN: 0363-9045</identifier><identifier>EISSN: 1520-5762</identifier><identifier>DOI: 10.3109/03639045.2013.845843</identifier><identifier>PMID: 24134563</identifier><language>eng</language><publisher>England: Informa Healthcare USA, Inc</publisher><subject>Delayed-Action Preparations - chemistry ; Delayed-Action Preparations - pharmacokinetics ; Drug Liberation ; hydrocortisone ; hypromellose ; Lactose - analogs & derivatives ; Lactose - chemistry ; Lactose - pharmacokinetics ; matrix ; Methylcellulose - analogs & derivatives ; Methylcellulose - chemistry ; Methylcellulose - pharmacokinetics ; Particle Size ; pediatric ; Tablets ; Tensile Strength</subject><ispartof>Drug development and industrial pharmacy, 2015-01, Vol.41 (1), p.70-78</ispartof><rights>2015 Informa Healthcare USA, Inc. All rights reserved: reproduction in whole or part not permitted 2015</rights><lds50>peer_reviewed</lds50><woscitedreferencessubscribed>false</woscitedreferencessubscribed><citedby>FETCH-LOGICAL-c418t-ec096890639cb55f0b3e4ae8e4caeb8a08ad5efebea3e82b2a260f32cdf5ce8a3</citedby><cites>FETCH-LOGICAL-c418t-ec096890639cb55f0b3e4ae8e4caeb8a08ad5efebea3e82b2a260f32cdf5ce8a3</cites></display><links><openurl>$$Topenurl_article</openurl><openurlfulltext>$$Topenurlfull_article</openurlfulltext><thumbnail>$$Tsyndetics_thumb_exl</thumbnail><link.rule.ids>314,780,784,27923,27924</link.rule.ids><backlink>$$Uhttps://www.ncbi.nlm.nih.gov/pubmed/24134563$$D View this record in MEDLINE/PubMed$$Hfree_for_read</backlink></links><search><creatorcontrib>Mohamed, Faiezah A. A.</creatorcontrib><creatorcontrib>Roberts, Matthew</creatorcontrib><creatorcontrib>Seton, Linda</creatorcontrib><creatorcontrib>Ford, James L.</creatorcontrib><creatorcontrib>Levina, Marina</creatorcontrib><creatorcontrib>Rajabi-Siahboomi, Ali R.</creatorcontrib><title>The effect of HPMC particle size on the drug release rate and the percolation threshold in extended-release mini-tablets</title><title>Drug development and industrial pharmacy</title><addtitle>Drug Dev Ind Pharm</addtitle><description>Abstract
The particle size of HPMC is a critical factor that can influence drug release rate from hydrophilic matrix systems. Percolation theory is a statistical tool which is used to study the disorder of particles in a lattice of a sample. The percolation threshold is the point at which a component is dominant in a cluster resulting in significant changes in drug release rates. Mini-tablets are compact dosage forms of 1.5-4 mm diameter, which have potential benefits in the delivery of drug to some patient groups such as pediatrics. In this study, the effect of HPMC particle size on hydrocortisone release and its associated percolation threshold for mini-tablets and tablets was assessed. For both mini-tablets and tablets, large polymer particles reduced tensile strength, but increased the drug release rate and the percolation threshold. Upon hydration, compacts with 45-125 μm HPMC particles formed a strong gel layer with low porosity, reducing hydrocortisone release rates. In comparison, faster drug release rates were obtained when 125-355 µm HPMC particles were used, due to the greater pore sizes that resulted in the formation of a weaker gel. Using 125-355 µm HPMC particles increased the percolation threshold for tablets and to a greater extent for mini-tablets. This work has demonstrated the importance of HPMC particle size in ER matrices, the effects of which are even more obvious for mini-tablets.</description><subject>Delayed-Action Preparations - chemistry</subject><subject>Delayed-Action Preparations - pharmacokinetics</subject><subject>Drug Liberation</subject><subject>hydrocortisone</subject><subject>hypromellose</subject><subject>Lactose - analogs & derivatives</subject><subject>Lactose - chemistry</subject><subject>Lactose - pharmacokinetics</subject><subject>matrix</subject><subject>Methylcellulose - analogs & derivatives</subject><subject>Methylcellulose - chemistry</subject><subject>Methylcellulose - pharmacokinetics</subject><subject>Particle Size</subject><subject>pediatric</subject><subject>Tablets</subject><subject>Tensile Strength</subject><issn>0363-9045</issn><issn>1520-5762</issn><fulltext>true</fulltext><rsrctype>article</rsrctype><creationdate>2015</creationdate><recordtype>article</recordtype><sourceid>EIF</sourceid><recordid>eNp9kE1v1DAQhi0EokvhHyDkI5cs_oizyQWEVkCRitpDOVsTe8y6cuLFdtSWX9-k20Xqpac5-HnfGT-EvOdsLTnrPjHZyI7Vai0Yl-u2Vm0tX5AVV4JVatOIl2S1INXCnJA3OV8zxkWn1GtyImoua9XIFbm92iFF59AUGh09u_y1pXtIxZuANPt_SONIy8zYNP2hCQNCRpqgIIXRPrzsMZkYoPgHMmHexWCpHyneFhwt2uoYG_zoqwJ9wJLfklcOQsZ3j_OU_P7-7Wp7Vp1f_Pi5_XpemZq3pULDuqbt2PxX0yvlWC-xBmyxNoB9C6wFq9BhjyCxFb0A0TAnhbFOGWxBnpKPh959in8nzEUPPhsMAUaMU9a8kZuu23RczWh9QE2KOSd0ep_8AOlOc6YX5_roXC_O9cH5HPvwuGHqB7T_Q0fJM_DlAPjRxTTATUzB6gJ3ISaXYDQ-L_XPrvj8pGGHEMrOQEJ9Hac0zgKfv_EeJCSmJQ</recordid><startdate>20150101</startdate><enddate>20150101</enddate><creator>Mohamed, Faiezah A. A.</creator><creator>Roberts, Matthew</creator><creator>Seton, Linda</creator><creator>Ford, James L.</creator><creator>Levina, Marina</creator><creator>Rajabi-Siahboomi, Ali R.</creator><general>Informa Healthcare USA, Inc</general><general>Informa Healthcare</general><scope>CGR</scope><scope>CUY</scope><scope>CVF</scope><scope>ECM</scope><scope>EIF</scope><scope>NPM</scope><scope>AAYXX</scope><scope>CITATION</scope><scope>7X8</scope></search><sort><creationdate>20150101</creationdate><title>The effect of HPMC particle size on the drug release rate and the percolation threshold in extended-release mini-tablets</title><author>Mohamed, Faiezah A. A. ; Roberts, Matthew ; Seton, Linda ; Ford, James L. ; Levina, Marina ; Rajabi-Siahboomi, Ali R.</author></sort><facets><frbrtype>5</frbrtype><frbrgroupid>cdi_FETCH-LOGICAL-c418t-ec096890639cb55f0b3e4ae8e4caeb8a08ad5efebea3e82b2a260f32cdf5ce8a3</frbrgroupid><rsrctype>articles</rsrctype><prefilter>articles</prefilter><language>eng</language><creationdate>2015</creationdate><topic>Delayed-Action Preparations - chemistry</topic><topic>Delayed-Action Preparations - pharmacokinetics</topic><topic>Drug Liberation</topic><topic>hydrocortisone</topic><topic>hypromellose</topic><topic>Lactose - analogs & derivatives</topic><topic>Lactose - chemistry</topic><topic>Lactose - pharmacokinetics</topic><topic>matrix</topic><topic>Methylcellulose - analogs & derivatives</topic><topic>Methylcellulose - chemistry</topic><topic>Methylcellulose - pharmacokinetics</topic><topic>Particle Size</topic><topic>pediatric</topic><topic>Tablets</topic><topic>Tensile Strength</topic><toplevel>peer_reviewed</toplevel><toplevel>online_resources</toplevel><creatorcontrib>Mohamed, Faiezah A. A.</creatorcontrib><creatorcontrib>Roberts, Matthew</creatorcontrib><creatorcontrib>Seton, Linda</creatorcontrib><creatorcontrib>Ford, James L.</creatorcontrib><creatorcontrib>Levina, Marina</creatorcontrib><creatorcontrib>Rajabi-Siahboomi, Ali R.</creatorcontrib><collection>Medline</collection><collection>MEDLINE</collection><collection>MEDLINE (Ovid)</collection><collection>MEDLINE</collection><collection>MEDLINE</collection><collection>PubMed</collection><collection>CrossRef</collection><collection>MEDLINE - Academic</collection><jtitle>Drug development and industrial pharmacy</jtitle></facets><delivery><delcategory>Remote Search Resource</delcategory><fulltext>fulltext</fulltext></delivery><addata><au>Mohamed, Faiezah A. A.</au><au>Roberts, Matthew</au><au>Seton, Linda</au><au>Ford, James L.</au><au>Levina, Marina</au><au>Rajabi-Siahboomi, Ali R.</au><format>journal</format><genre>article</genre><ristype>JOUR</ristype><atitle>The effect of HPMC particle size on the drug release rate and the percolation threshold in extended-release mini-tablets</atitle><jtitle>Drug development and industrial pharmacy</jtitle><addtitle>Drug Dev Ind Pharm</addtitle><date>2015-01-01</date><risdate>2015</risdate><volume>41</volume><issue>1</issue><spage>70</spage><epage>78</epage><pages>70-78</pages><issn>0363-9045</issn><eissn>1520-5762</eissn><abstract>Abstract
The particle size of HPMC is a critical factor that can influence drug release rate from hydrophilic matrix systems. Percolation theory is a statistical tool which is used to study the disorder of particles in a lattice of a sample. The percolation threshold is the point at which a component is dominant in a cluster resulting in significant changes in drug release rates. Mini-tablets are compact dosage forms of 1.5-4 mm diameter, which have potential benefits in the delivery of drug to some patient groups such as pediatrics. In this study, the effect of HPMC particle size on hydrocortisone release and its associated percolation threshold for mini-tablets and tablets was assessed. For both mini-tablets and tablets, large polymer particles reduced tensile strength, but increased the drug release rate and the percolation threshold. Upon hydration, compacts with 45-125 μm HPMC particles formed a strong gel layer with low porosity, reducing hydrocortisone release rates. In comparison, faster drug release rates were obtained when 125-355 µm HPMC particles were used, due to the greater pore sizes that resulted in the formation of a weaker gel. Using 125-355 µm HPMC particles increased the percolation threshold for tablets and to a greater extent for mini-tablets. This work has demonstrated the importance of HPMC particle size in ER matrices, the effects of which are even more obvious for mini-tablets.</abstract><cop>England</cop><pub>Informa Healthcare USA, Inc</pub><pmid>24134563</pmid><doi>10.3109/03639045.2013.845843</doi><tpages>9</tpages></addata></record> |
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| subjects | Delayed-Action Preparations - chemistry Delayed-Action Preparations - pharmacokinetics Drug Liberation hydrocortisone hypromellose Lactose - analogs & derivatives Lactose - chemistry Lactose - pharmacokinetics matrix Methylcellulose - analogs & derivatives Methylcellulose - chemistry Methylcellulose - pharmacokinetics Particle Size pediatric Tablets Tensile Strength |
| title | The effect of HPMC particle size on the drug release rate and the percolation threshold in extended-release mini-tablets |
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