Twenty-five formulations were prepared containing dehydroepiandrosterone (prasterone, DHEA) in the chemical form of inclusion complex with α-cyclodextrin (c-DHEA, 57.30% w/w). The drug was mixed with three different excipient systems: the first “fast” one was a mixture of two disintegrants (Avicel PH 101 and Explotab, at prefixed 4.15 weight ratio); the second “gelling” excipient contained two gel-forming agents (Kollidon PK30 and Methocel K4M) at three weight ratios: 0.31 (A) - 1.00 (B) - 2.45 (C). The third type of “binary” mixture was prepared by combining “fast” and “gelling” systems at three weight ratios: 1:2 – 1:1 – 2:1. Tablets were prepared by direct compression or after wet granulation of these formulations and identified by the same symbols. “Fast” tablets induced a rapid release of the drug while “gelling” tablets were found to modify the release, according to composition. A release profile, characterized by an initial phase of rapid drug release, followed by a period of slower release is achieved with “binary” 1:1 tablets. Series 1:2 tablets provide linear release of the drug; while an undifferentiated release profile was found for series 2:1 tablets. Different release mechanisms and control of drug release are thus obtained by using DHEA as inclusion complex and varying the weight ratios between the different compounds forming the excipients.
The Role of Excipients in the Control of Dehydroepiandrosterone Inclusion Complex Delivery
BERGAMANTE, VALENTINA;FINI, ADAMO
2006
Abstract
Twenty-five formulations were prepared containing dehydroepiandrosterone (prasterone, DHEA) in the chemical form of inclusion complex with α-cyclodextrin (c-DHEA, 57.30% w/w). The drug was mixed with three different excipient systems: the first “fast” one was a mixture of two disintegrants (Avicel PH 101 and Explotab, at prefixed 4.15 weight ratio); the second “gelling” excipient contained two gel-forming agents (Kollidon PK30 and Methocel K4M) at three weight ratios: 0.31 (A) - 1.00 (B) - 2.45 (C). The third type of “binary” mixture was prepared by combining “fast” and “gelling” systems at three weight ratios: 1:2 – 1:1 – 2:1. Tablets were prepared by direct compression or after wet granulation of these formulations and identified by the same symbols. “Fast” tablets induced a rapid release of the drug while “gelling” tablets were found to modify the release, according to composition. A release profile, characterized by an initial phase of rapid drug release, followed by a period of slower release is achieved with “binary” 1:1 tablets. Series 1:2 tablets provide linear release of the drug; while an undifferentiated release profile was found for series 2:1 tablets. Different release mechanisms and control of drug release are thus obtained by using DHEA as inclusion complex and varying the weight ratios between the different compounds forming the excipients.I documenti in IRIS sono protetti da copyright e tutti i diritti sono riservati, salvo diversa indicazione.
