Formulation of venlafaxine for once daily administration using polymeric material hybrids

Objective: Controlled release venlafaxine for once daily administration. Methods: Drug resin complexation followed by polymer encapsulation. A 4 1 .2 1 factorial design was used to study the effect of polymer type and core: coat ratio on the release profile and kinetics. Polymer combinations were tr...

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Bibliographic Details
Published in:Journal of microencapsulation 2016-06, Vol.33 (4), p.299-306
Main Authors: Ibrahim, Howida Kamal, Salah, Salwa
Format: Article
Language:English
Subjects:
Animals
Delayed-Action Preparations - chemistry
Delayed-Action Preparations - pharmacokinetics
drug resinate
Male
mathematical modelling
microcapsules
Once daily dosing
Polyesters - chemistry
Polyesters - pharmacokinetics
Polyesters - pharmacology
Polyglactin 910 - chemistry
Polyglactin 910 - pharmacokinetics
Polyglactin 910 - pharmacology
Rabbits
venlafaxine HCL
Venlafaxine Hydrochloride - chemistry
Venlafaxine Hydrochloride - pharmacokinetics
Venlafaxine Hydrochloride - pharmacology
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Summary:Objective: Controlled release venlafaxine for once daily administration. Methods: Drug resin complexation followed by polymer encapsulation. A 4 1 .2 1 factorial design was used to study the effect of polymer type and core: coat ratio on the release profile and kinetics. Polymer combinations were tried for optimisation adapting the desIMNCility function. The optimised formula was tested in rabbits against commercial extended release capsules. Results: Poly-epsilon-caprolactone, poly(d, l-lactide-co-glycolide) ester and poly(d, l-lactide) ester polymers were more efficient in lowering the release rate and the initial burst release than Eudragit ® RS100. Encapsulation at 1:1 ratio ensured complete coats and drug release sustainment. Formula prepared using 50:50 PLA/Eudragit at 1:1 ratio sustained the drug release up to 24 h with low burst release. This formula had higher venlafaxine absorption in rabbits compared to the commercial capsules. Conclusions: The optimised formula is superior to the available once-daily trials regarding enhanced bioavailability, dosage form versatility and ease of scaling up.
ISSN:0265-2048
1464-5246
DOI:10.1080/02652048.2016.1178351