In-vitro and In-vivo Relationship of Gabapentin from Floating and Immediate Release Tablets
Article
| IMSEAR
| ID: sea-209974
ABSTRACT
Gabapentiniseffectiveagainst post-traumaticspinalinjury-inducedneuropathicpain.Itrequireshighdosageand frequency inthemanagementofneuropathicpain.Thepresentresearchworkwasanattempttoformulate andevaluategabapentingastro-retentivetabletstoprolonggastricresidenceandincreasedrug absorptionand furtherincreasebioavailability.Thefloatingtabletsofgabapentinwerepreparedintwodoses(300and600mg) byusingtwopolymers(hydroxylpropylmethylcelluloseandhydroxylpropylcellulose).Immediaterelease tabletsofgabapentincontaining thesamedoseswerepreparedandusedasreferenceformulations.The physicochemicalcharacteristicsofthepreparedtabletsweredetermined(drug content,weightvariation,friability, hardness,thicknessand diameter). Drugreleasefromthepreparedtabletswasfollowed and foundthatby increasingdrug concentrationinthetabletsreleaserateincreases.Floatingtabletsshowedprolongeddrugrelease (over96%)tomorethan15hrs.Immediatereleasetabletsshowedover97%drugreleasewithin48min.In-vivoresultsshowedthatplasmaexposuretogabapentininanimalsreceivingthedrug doesnotdose proportionalandtherefore maynotreachtherapeuticallyusefullevels.AUC0-24andCmaxincaseof300mgtabletsaremorethanthoseincaseof 600 mgtablets.Thein-vivo releaseofgabapentin doesnot correlatewiththein-vitroreleaseofthedrug.
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Index:
IMSEAR (South-East Asia)
Year:
2019
Type:
Article
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