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Development of mucoadhesive patches for buccal drug delivery

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Resumo(s)

Clonazepam is a benzodiazepine used for the treatment of epilepsy and panic disorders. Its poor water solubility compromises its bioavailability, making it necessary to develop strategies that bypass this problem. A very promising one is the complexation with cyclodextrins, which has been widely used in the pharmaceutical field. Antiepileptic drug are usually given orally, but to avoid certain drawbacks like the first pass metabolism, other routes are being considered, such as the transmucosal systems. The objective of this study was to develop a mucoadhesive buccal patch for systemic CLZ delivery. The effect of complexation with β-CD and Met-β-CD in the in vitro release of CLZ was analyzed, as well as the influence of the preparation method of the complexes. To attempt unidirectional release, different backing layers were tested. The complexes were prepared by physical mixing and co-grinding and the patches were covered on one side with impermeable backing layers. The release tests were performed with Sartorius and analyzed in HPLC. The complexation resulted in an improved solubility and consequently release of CLZ from the patches. Among all the formulations, the one with the binary system Me-β-CD-CLZ prepared by co-grinding showed the highest improvement in the release profile. The layer which better provided a unidirectional release was the Kollicoat® layer.

Descrição

Trabalho Final de Mestrado Integrado, Ciências Farmacêuticas, Universidade de Lisboa, Faculdade de Farmácia, 2014

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Clonazepam Unidirectional release Buccal delivery Cyclodextrin’s complexation Transmucosal systems Mucoadhesive patch Mestrado Integrado - 2014

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