Development of a sustained-release matrix tablet formulation of DHEA as ternary complex with α-cyclodextrin and glycine

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Sustained-release matrix-tablets of dehydroepiandrosterone (DHEA) as ternary complex with α-cyclodextrin and glycine (c-DHEA) were prepared by direct compression with suitable excipients. The influence of the swelling properties of hydroxypropylmethylcellulose (HPMC) and the disintegrating power of Explotab® used in combination, as well as the effect of the presence, type and amount of suitable channelling agents (Emcocel® and spray-dried lactose, alone or in combination) on drug release behaviour from matrix-tablets has been evaluated.

The best performances in terms of drug release was obtained from formulations containing a 75:25 w/w spray-dried lactose:Emcocel® combination in the presence of HPMC as matrix-forming polymer, leading to a more than 65% DHEA released at the end of the test, a value which was, respectively, 1.9 and 2.7 times higher than those achieved with the corresponding formulations containing spray-dried lactose or Emcocel® alone. The drug release profile from the most effective matrix-tablet formulation of c-DHEA allowed achievement of a more than 6-fold increase in the drug amount released within 24 h in comparison with the same formulation containing the simple physical mixtures of DHEA, α-cyclodextrin and glycine. Therefore the advantage of using DHEA as ternary complex, prepared by mechano-chemical treatment, was clearly demonstrated, thus allowing the development of an effective sustained-release formulation of the drug.