The Role of Excipients in the Control of Dehydroepiandrosterone Inclusion Complex Delivery

The Role of Excipients in the Control of Dehydroepiandrosterone Inclusion Complex Delivery
Bergamante, Valentina; Gian Carlo Ceschel; Simone Lombardi Borgia; Ronchi, Celestino; Fini, Adamo
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Aim: The aim of this study was to develop systems containing dehydroepiandrosterone (DHEA), in the form of an inclusion complex with a-cyclodestrin (c-DHEA), which are able to change the release profile of the hormone according to time and excipient composition.
Method: Twenty-five formulations were prepared containing DHEA (prasterone) in the chemical form of an inclusion complex with a-cyclodextrin (57.3% w/w). The drug was mixed with three different excipient systems: the first `fast' one was a mixture of two disintegrants (microcrystalline cellulose and sodium carboxymethyl starch at prefixed 4.15 weight ratio); the second `gelling' excipient contained two gel-forming agents (high viscosity hydroxypropyl methylcellulose and cross-linked polyvinyl pyrrolidone) at three weight ratios: 0.31, 1.00, and 2.45; and the third type of `binary' mixture was prepared by combining `fast' and `gelling' systems at three weight ratios: 1?:?2, 1?:?1, and 2?:?1. Tablets were prepared by direct compression or after wet granulation of these formulations.
Results: `Fast' tablets induced a rapid release of the drug while `gelling' tablets were found to modify the release, according to composition. A profile, characterized by an initial phase of rapid drug release, followed by a period of slower release is achieved with series 1?:?1 tablets. Series 1?:?2 tablets provide linear release of the drug; while an undifferentiated profile was found for series 2?:?1 tablets.
Conclusion: Different release mechanisms and the control of drug release were obtained by using DHEA in its inclusion complex and varying the weight ratios of the excipients.
Document Type: Research article
Affiliations: 1: 1 Department of Pharmaceutical Science, University of Bologna, Bologna, Italy 2: 2 MonteResearch S.r.l., Bollate, Milan, Italy 3: 3 Department of Metal Science, Electrochemistry and Chemical Techniques, University of Bologna, Bologna, Italy
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