Preparation and pharmacokinetics in beagle dogs of ganershu sustained-release pellets
Identifieur interne : 000168 ( Main/Merge ); précédent : 000167; suivant : 000169Preparation and pharmacokinetics in beagle dogs of ganershu sustained-release pellets
Auteurs : Jin-Huo Pan ; Jian-Chun Wang ; Zhi-Tao Jiang ; Ting Zhang ; Shao-Bo Ge ; Ye-Xia Zhang ; Xin Jin ; Guo-Jun YanSource :
- Pharmacognosy Magazine [ 0973-1296 ] ; 2014.
Abstract
The active ingredients of Ganershu compound recipe, which are effective for hepatitis treatment in liver protection and transaminase reduction. However, the active ingredients of Ganershu compound recipe are poor absorption, which conduct it has a low oral bioavailability.
We prepared Ganershu sustained-release pellets (GSPs) by fluidized-bed on central composite design-response surface methodology and increase its bioavailability in beagle dogs.
In this study, GSPs were successfully prepared. The Drug-loaded pellets and sustained-release coated were carried out in fluidized-bed machine. GSP was optimized for fitting release, roundness, and the overall desirability by central composite design-response surface methodology.
To optimize cumulative release profile, the outermost ethyl cellulose coating layer and the hydroxypropyl methyl cellulose (HPMC) swelling layer were employed, which were respectively given coating levels in terms of weight gain of 22% and 6%, the concentration of HPMC is 4.5% (g/ml). The pharmacokinetics of Ganershu normal pellets (GNPs) and GSP was studied in beagle dogs after oral administration. The naringenin as an index, the area under the curve0-∞ of naringenin in GSP was 1.38 times greater than that of GNP. Meanwhile,
This study can clearly indicate that we enhanced the oral bioavailability of Ganershu by preparing the GSP, which had the sustained dissolution and improved the potential of it for clinical application.
Url:
DOI: 10.4103/0973-1296.137360
PubMed: 25210307
PubMed Central: 4159913
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<record><TEI><teiHeader><fileDesc><titleStmt><title xml:lang="en">Preparation and pharmacokinetics in beagle dogs of ganershu sustained-release pellets</title><author><name sortKey="Pan, Jin Huo" sort="Pan, Jin Huo" uniqKey="Pan J" first="Jin-Huo" last="Pan">Jin-Huo Pan</name><affiliation><nlm:aff id="aff1"><italic>College of Pharmacy, Nanjing University of Chinese Medicine, Nanjing 210023, China</italic></nlm:aff></affiliation><affiliation><nlm:aff id="aff2"><italic>Department of Pharmacy Office, Traditional Chinese Medicine Hospital of Zhang-jia-gang, Zhangjiagang 215600, China</italic></nlm:aff></affiliation></author><author><name sortKey="Wang, Jian Chun" sort="Wang, Jian Chun" uniqKey="Wang J" first="Jian-Chun" last="Wang">Jian-Chun Wang</name><affiliation><nlm:aff id="aff2"><italic>Department of Pharmacy Office, Traditional Chinese Medicine Hospital of Zhang-jia-gang, Zhangjiagang 215600, China</italic></nlm:aff></affiliation></author><author><name sortKey="Jiang, Zhi Tao" sort="Jiang, Zhi Tao" uniqKey="Jiang Z" first="Zhi-Tao" last="Jiang">Zhi-Tao Jiang</name><affiliation><nlm:aff id="aff2"><italic>Department of Pharmacy Office, Traditional Chinese Medicine Hospital of Zhang-jia-gang, Zhangjiagang 215600, China</italic></nlm:aff></affiliation></author><author><name sortKey="Zhang, Ting" sort="Zhang, Ting" uniqKey="Zhang T" first="Ting" last="Zhang">Ting Zhang</name><affiliation><nlm:aff id="aff1"><italic>College of Pharmacy, Nanjing University of Chinese Medicine, Nanjing 210023, China</italic></nlm:aff></affiliation></author><author><name sortKey="Ge, Shao Bo" sort="Ge, Shao Bo" uniqKey="Ge S" first="Shao-Bo" last="Ge">Shao-Bo Ge</name><affiliation><nlm:aff id="aff1"><italic>College of Pharmacy, Nanjing University of Chinese Medicine, Nanjing 210023, China</italic></nlm:aff></affiliation></author><author><name sortKey="Zhang, Ye Xia" sort="Zhang, Ye Xia" uniqKey="Zhang Y" first="Ye-Xia" last="Zhang">Ye-Xia Zhang</name><affiliation><nlm:aff id="aff1"><italic>College of Pharmacy, Nanjing University of Chinese Medicine, Nanjing 210023, China</italic></nlm:aff></affiliation></author><author><name sortKey="Jin, Xin" sort="Jin, Xin" uniqKey="Jin X" first="Xin" last="Jin">Xin Jin</name><affiliation><nlm:aff id="aff3"><italic>Department of Pharmacy Office, The First People's Hospital of Suqian, Suqian 223800, China</italic></nlm:aff></affiliation></author><author><name sortKey="Yan, Guo Jun" sort="Yan, Guo Jun" uniqKey="Yan G" first="Guo-Jun" last="Yan">Guo-Jun Yan</name><affiliation><nlm:aff id="aff1"><italic>College of Pharmacy, Nanjing University of Chinese Medicine, Nanjing 210023, China</italic></nlm:aff></affiliation></author></titleStmt><publicationStmt><idno type="wicri:source">PMC</idno><idno type="pmid">25210307</idno><idno type="pmc">4159913</idno><idno type="url">http://www.ncbi.nlm.nih.gov/pmc/articles/PMC4159913</idno><idno type="RBID">PMC:4159913</idno><idno type="doi">10.4103/0973-1296.137360</idno><date when="2014">2014</date><idno type="wicri:Area/Pmc/Corpus">000052</idno><idno type="wicri:explorRef" wicri:stream="Pmc" wicri:step="Corpus" wicri:corpus="PMC">000052</idno><idno type="wicri:Area/Pmc/Curation">000052</idno><idno type="wicri:explorRef" wicri:stream="Pmc" wicri:step="Curation">000052</idno><idno type="wicri:Area/Pmc/Checkpoint">000010</idno><idno type="wicri:explorRef" wicri:stream="Pmc" wicri:step="Checkpoint">000010</idno><idno type="wicri:Area/Ncbi/Merge">000599</idno><idno type="wicri:Area/Ncbi/Curation">000599</idno><idno type="wicri:Area/Ncbi/Checkpoint">000599</idno><idno type="wicri:doubleKey">0973-1296:2014:Pan J:preparation:and:pharmacokinetics</idno><idno type="wicri:Area/Main/Merge">000168</idno></publicationStmt><sourceDesc><biblStruct><analytic><title xml:lang="en" level="a" type="main">Preparation and pharmacokinetics in beagle dogs of ganershu sustained-release pellets</title><author><name sortKey="Pan, Jin Huo" sort="Pan, Jin Huo" uniqKey="Pan J" first="Jin-Huo" last="Pan">Jin-Huo Pan</name><affiliation><nlm:aff id="aff1"><italic>College of Pharmacy, Nanjing University of Chinese Medicine, Nanjing 210023, China</italic></nlm:aff></affiliation><affiliation><nlm:aff id="aff2"><italic>Department of Pharmacy Office, Traditional Chinese Medicine Hospital of Zhang-jia-gang, Zhangjiagang 215600, China</italic></nlm:aff></affiliation></author><author><name sortKey="Wang, Jian Chun" sort="Wang, Jian Chun" uniqKey="Wang J" first="Jian-Chun" last="Wang">Jian-Chun Wang</name><affiliation><nlm:aff id="aff2"><italic>Department of Pharmacy Office, Traditional Chinese Medicine Hospital of Zhang-jia-gang, Zhangjiagang 215600, China</italic></nlm:aff></affiliation></author><author><name sortKey="Jiang, Zhi Tao" sort="Jiang, Zhi Tao" uniqKey="Jiang Z" first="Zhi-Tao" last="Jiang">Zhi-Tao Jiang</name><affiliation><nlm:aff id="aff2"><italic>Department of Pharmacy Office, Traditional Chinese Medicine Hospital of Zhang-jia-gang, Zhangjiagang 215600, China</italic></nlm:aff></affiliation></author><author><name sortKey="Zhang, Ting" sort="Zhang, Ting" uniqKey="Zhang T" first="Ting" last="Zhang">Ting Zhang</name><affiliation><nlm:aff id="aff1"><italic>College of Pharmacy, Nanjing University of Chinese Medicine, Nanjing 210023, China</italic></nlm:aff></affiliation></author><author><name sortKey="Ge, Shao Bo" sort="Ge, Shao Bo" uniqKey="Ge S" first="Shao-Bo" last="Ge">Shao-Bo Ge</name><affiliation><nlm:aff id="aff1"><italic>College of Pharmacy, Nanjing University of Chinese Medicine, Nanjing 210023, China</italic></nlm:aff></affiliation></author><author><name sortKey="Zhang, Ye Xia" sort="Zhang, Ye Xia" uniqKey="Zhang Y" first="Ye-Xia" last="Zhang">Ye-Xia Zhang</name><affiliation><nlm:aff id="aff1"><italic>College of Pharmacy, Nanjing University of Chinese Medicine, Nanjing 210023, China</italic></nlm:aff></affiliation></author><author><name sortKey="Jin, Xin" sort="Jin, Xin" uniqKey="Jin X" first="Xin" last="Jin">Xin Jin</name><affiliation><nlm:aff id="aff3"><italic>Department of Pharmacy Office, The First People's Hospital of Suqian, Suqian 223800, China</italic></nlm:aff></affiliation></author><author><name sortKey="Yan, Guo Jun" sort="Yan, Guo Jun" uniqKey="Yan G" first="Guo-Jun" last="Yan">Guo-Jun Yan</name><affiliation><nlm:aff id="aff1"><italic>College of Pharmacy, Nanjing University of Chinese Medicine, Nanjing 210023, China</italic></nlm:aff></affiliation></author></analytic><series><title level="j">Pharmacognosy Magazine</title><idno type="ISSN">0973-1296</idno><idno type="eISSN">0976-4062</idno><imprint><date when="2014">2014</date></imprint></series></biblStruct></sourceDesc></fileDesc><profileDesc><textClass></textClass></profileDesc></teiHeader><front><div type="abstract" xml:lang="en"><sec id="st1"><title>Background:</title><p>The active ingredients of Ganershu compound recipe, which are effective for hepatitis treatment in liver protection and transaminase reduction. However, the active ingredients of Ganershu compound recipe are poor absorption, which conduct it has a low oral bioavailability.</p></sec><sec id="st2"><title>Objective:</title><p>We prepared Ganershu sustained-release pellets (GSPs) by fluidized-bed on central composite design-response surface methodology and increase its bioavailability in beagle dogs.</p></sec><sec id="st3"><title>Materials and Methods:</title><p>In this study, GSPs were successfully prepared. The Drug-loaded pellets and sustained-release coated were carried out in fluidized-bed machine. GSP was optimized for fitting release, roundness, and the overall desirability by central composite design-response surface methodology.</p></sec><sec id="st4"><title>Results:</title><p>To optimize cumulative release profile, the outermost ethyl cellulose coating layer and the hydroxypropyl methyl cellulose (HPMC) swelling layer were employed, which were respectively given coating levels in terms of weight gain of 22% and 6%, the concentration of HPMC is 4.5% (g/ml). The pharmacokinetics of Ganershu normal pellets (GNPs) and GSP was studied in beagle dogs after oral administration. The naringenin as an index, the area under the curve<sub>0-∞</sub> of naringenin in GSP was 1.38 times greater than that of GNP. Meanwhile, <italic>T</italic>max of GSP was prolonged for about 74%.</p></sec><sec id="st5"><title>Conclusion:</title><p>This study can clearly indicate that we enhanced the oral bioavailability of Ganershu by preparing the GSP, which had the sustained dissolution and improved the potential of it for clinical application.</p></sec></div></front><back><div1 type="bibliography"><listBibl><biblStruct><analytic><author><name sortKey="Fung, J" uniqKey="Fung J">J Fung</name></author><author><name sortKey="Yuen, Mf" uniqKey="Yuen M">MF Yuen</name></author></analytic></biblStruct><biblStruct><analytic><author><name sortKey="Hou, Zs" uniqKey="Hou Z">ZS Hou</name></author><author><name sortKey="Cai, Ll" uniqKey="Cai L">LL Cai</name></author><author><name sortKey="Pan, Jh" uniqKey="Pan J">JH Pan</name></author></analytic></biblStruct><biblStruct><analytic><author><name sortKey="Zhang, T" uniqKey="Zhang T">T Zhang</name></author><author><name sortKey="Yan, Gj" uniqKey="Yan G">GJ 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Y">Y Zou</name></author><author><name sortKey="Bai, S" uniqKey="Bai S">S Bai</name></author></analytic></biblStruct><biblStruct><analytic><author><name sortKey="Haddish Berhane, N" uniqKey="Haddish Berhane N">N Haddish-Berhane</name></author><author><name sortKey="Jeong, Sh" uniqKey="Jeong S">SH Jeong</name></author><author><name sortKey="Haghighi, K" uniqKey="Haghighi K">K Haghighi</name></author><author><name sortKey="Park, K" uniqKey="Park K">K Park</name></author></analytic></biblStruct><biblStruct><analytic><author><name sortKey="Bechgaard, H" uniqKey="Bechgaard H">H Bechgaard</name></author><author><name sortKey="Nielsen, Gh" uniqKey="Nielsen G">GH Nielsen</name></author></analytic></biblStruct></listBibl></div1></back></TEI></record>Pour manipuler ce document sous Unix (Dilib)
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