The influence of agitation sequence and ionic strength on in vitro drug release from hypromellose (E4M and K4M) ER matrices--the use of the USP III apparatus.

2.50
Hdl Handle:
http://hdl.handle.net/2436/575956
Title:
The influence of agitation sequence and ionic strength on in vitro drug release from hypromellose (E4M and K4M) ER matrices--the use of the USP III apparatus.
Authors:
Asare-Addo, Kofi; Kaialy, Waseem; Levina, Marina; Rajabi-Siahboomi, Ali; Ghori, Mohammed U; Supuk, Enes; Laity, Peter R; Conway, Barbara R; Nokhodchi, Ali
Abstract:
Theophylline extended release (ER) matrices containing hypromellose (hydroxypropyl methylcellulose (HPMC) E4M and K4M were evaluated in media with a pH range of 1.2-7.5, using an automated USP type III, Bio-Dis dissolution apparatus. The objectives of this study were to evaluate the effects of systematic agitation, ionic strength and pH on the release of theophylline from the gel forming hydrophilic polymeric matrices with different methoxyl substitution levels. Tribo-electric charging of hypromellose, theophylline and their formulated blends containing E4M and K4M grades has been characterised, along with quantitative observations of flow, compression behaviour and particle morphology. Agitations were studied at 5, 10, 15, 20, 25, 30 dips per minute (dpm) and also in the ascending and descending order in the dissolution vials. The ionic concentration strength of the media was also varied over a range of 0-0.4M to simulate the gastrointestinal fed and fasted states and various physiological pH conditions. To study the effect of ionic strength on the hydrophilic matrices, agitation was set at 20 dpm. The charge results on individual components imply that the positively charged particles have coupled with the negatively charged particles to form a stable ordered mixture which is believed to result in a more homogeneous and stable system. The particle shape analysis showed the HPMC K4M polymer to have a more irregular morphology and a rougher surface texture in comparison to the HPMC E4M polymer, possibly a contributory factor to the gelation process. The results showed gelation occurred quicker for the K4M tablet matrices. Drug release increased with increased agitation. This was more pronounced for the E4M tablet matrices. The ionic strength also had more of an effect on the drug release from the E4M matrices. The experiments highlighted the resilience of the K4M matrices in comparison with the E4M matrices. The results thus show that despite similar viscosities of E4M and K4M, the methoxyl substitution makes a difference to their control of drug release and as such care and consideration should be given to the choice of polymer used for extended release. The use of systematic change of agitation method and ionic strength may indicate potential fed and fasted effects on drug release from hydrophilic matrices.
Citation:
The influence of agitation sequence and ionic strength on in vitro drug release from hypromellose (E4M and K4M) ER matrices--the use of the USP III apparatus. 2013, 104:54-60 Colloids Surf B Biointerfaces
Publisher:
Elsevier
Journal:
Colloids and surfaces. B, Biointerfaces
Issue Date:
1-Apr-2013
URI:
http://hdl.handle.net/2436/575956
DOI:
10.1016/j.colsurfb.2012.11.020
PubMed ID:
23298588
Type:
Article
Language:
en
ISSN:
1873-4367
Appears in Collections:
Pharmacy and Natural Products Research Group

Full metadata record

DC FieldValue Language
dc.contributor.authorAsare-Addo, Kofien
dc.contributor.authorKaialy, Waseemen
dc.contributor.authorLevina, Marinaen
dc.contributor.authorRajabi-Siahboomi, Alien
dc.contributor.authorGhori, Mohammed Uen
dc.contributor.authorSupuk, Enesen
dc.contributor.authorLaity, Peter Ren
dc.contributor.authorConway, Barbara Ren
dc.contributor.authorNokhodchi, Alien
dc.date.accessioned2015-08-25T14:00:22Zen
dc.date.available2015-08-25T14:00:22Zen
dc.date.issued2013-04-01en
dc.identifier.citationThe influence of agitation sequence and ionic strength on in vitro drug release from hypromellose (E4M and K4M) ER matrices--the use of the USP III apparatus. 2013, 104:54-60 Colloids Surf B Biointerfacesen
dc.identifier.issn1873-4367en
dc.identifier.pmid23298588en
dc.identifier.doi10.1016/j.colsurfb.2012.11.020en
dc.identifier.urihttp://hdl.handle.net/2436/575956en
dc.description.abstractTheophylline extended release (ER) matrices containing hypromellose (hydroxypropyl methylcellulose (HPMC) E4M and K4M were evaluated in media with a pH range of 1.2-7.5, using an automated USP type III, Bio-Dis dissolution apparatus. The objectives of this study were to evaluate the effects of systematic agitation, ionic strength and pH on the release of theophylline from the gel forming hydrophilic polymeric matrices with different methoxyl substitution levels. Tribo-electric charging of hypromellose, theophylline and their formulated blends containing E4M and K4M grades has been characterised, along with quantitative observations of flow, compression behaviour and particle morphology. Agitations were studied at 5, 10, 15, 20, 25, 30 dips per minute (dpm) and also in the ascending and descending order in the dissolution vials. The ionic concentration strength of the media was also varied over a range of 0-0.4M to simulate the gastrointestinal fed and fasted states and various physiological pH conditions. To study the effect of ionic strength on the hydrophilic matrices, agitation was set at 20 dpm. The charge results on individual components imply that the positively charged particles have coupled with the negatively charged particles to form a stable ordered mixture which is believed to result in a more homogeneous and stable system. The particle shape analysis showed the HPMC K4M polymer to have a more irregular morphology and a rougher surface texture in comparison to the HPMC E4M polymer, possibly a contributory factor to the gelation process. The results showed gelation occurred quicker for the K4M tablet matrices. Drug release increased with increased agitation. This was more pronounced for the E4M tablet matrices. The ionic strength also had more of an effect on the drug release from the E4M matrices. The experiments highlighted the resilience of the K4M matrices in comparison with the E4M matrices. The results thus show that despite similar viscosities of E4M and K4M, the methoxyl substitution makes a difference to their control of drug release and as such care and consideration should be given to the choice of polymer used for extended release. The use of systematic change of agitation method and ionic strength may indicate potential fed and fasted effects on drug release from hydrophilic matrices.en
dc.language.isoenen
dc.publisherElsevieren
dc.rightsArchived with thanks to Colloids and surfaces. B, Biointerfacesen
dc.subjectAgitationen
dc.subjectIonic concentration strengthen
dc.subjectHPMCen
dc.subjectSimilarity factoren
dc.subjectKinetics of drug releaseen
dc.subjectDSCen
dc.subjectParticle sizeen
dc.subjectTriboelectrificationen
dc.subjectTheophyllineen
dc.subjectUSP IIIen
dc.subject.meshChemistry, Pharmaceuticalen
dc.subject.meshHydrogen-Ion Concentrationen
dc.subject.meshHypromellose Derivativesen
dc.subject.meshMethylcelluloseen
dc.subject.meshOsmolar Concentrationen
dc.subject.meshParticle Sizeen
dc.subject.meshPolymersen
dc.subject.meshSolubilityen
dc.subject.meshStatic Electricityen
dc.subject.meshSurface Propertiesen
dc.subject.meshTabletsen
dc.subject.meshTheophyllineen
dc.titleThe influence of agitation sequence and ionic strength on in vitro drug release from hypromellose (E4M and K4M) ER matrices--the use of the USP III apparatus.en
dc.typeArticleen
dc.identifier.journalColloids and surfaces. B, Biointerfacesen

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