Background: With its reported side effects Desvenlafaxine succinate (DSV) is a good candidate
to prepare prolonged release system. Such prolonged release could decrease the rapid DSV absorption
after oral administration and reduce its exaggerated side effects.
Methods: A prolonged release Desvenlafaxine succinate (DSV) multilayered system was prepared by
ionotropic gelation using sodium alginate (SA) and calcium chloride as a cross-linker. DSV was incorporated
simultaneously during the gelation stage and the formed beads were evaluated for shape and
particle size. Thirteen formulation variables including pH, DSV: polymer ratio, cross-linker concentration
and curing time were optimized for optimal drug entrapment. The optimized formula was evaluated
ex vivo using the everted sac technique to predict DSV absorption through intestinal mucosal cells, follow
the permeation and calculate its apparent permeability coefficient.
Results: The optimum formulation variables were: pH (8-9), DSV: SA ratio (2:1), cross-linker concentration
(5%w/v) and 30 min curing time. Multilayered beads coating using chitosan and SA was compared
with uncoated beads or the innovator for DSV release. Coating of the beads greatly retarded DSV
release with a release profile similar to that of the innovator. An optimized formula (T13) coated with
0.04% w/v of each of chitosan and SA was selected. The developed system gave rise to a prolonged release
pattern with high similarity factor with the innovator.
Conclusion: The results of the current work can be applied to prepare controlled release systems of
similar drugs that have intense side effects associated with their initial burst after oral administration.