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Development and characterization of clonazepam-cyclodextrins binary systems
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Resumo(s)
Clonazepam, a benzodiazepine used to treat convulsive disorders and panic attacks, is commonly given orally, in a dose divided per three times a day, for long periods. The aim of the main work was to develop a formulation of a mucoadhesive buccal patch for controlled release of the drug in order to decrease the number of administrations per day and increase the safety and the compliance of the patient.
Concerning to the present paper, the purpose was to prepare and characterize binary systems of clonazepam with a variety of cyclodextrins, in order to choose the suitable ones to proceed with the main research. It was the lipophilic nature of the drug that lead to the use of these carriers that provided the needed increasing of solubility, allowing the development of the proposed pharmaceutical dosage form.
Considering previous results from other studies, several cyclodextrins were used in our assessment.
Phase solubility studies were done and classified, and used to obtain the stability constants of each cyclodextrins. The binary systems were prepared using four different techniques: physical mixture, co-grinding, kneading and Coevaporation; and then characterized in solid state by differential scanning calorimetry, fourier transform infrared and x-ray powder diffraction; and in solution, by dissolution rate studies.
The best binary systems suitable to proceed with the main purpose was obtained with Randomly Methylated β-Cyclodextrin, Sulfobutyl Ether β-Cyclodextrin and β-Cyclodextrin-epichlorohydrin polymer, showing the best increase in solubility.
Descrição
Trabalho Final de Mestrado Integrado, Ciências Farmacêuticas, Universidade de Lisboa, Faculdade de Farmácia, 2014
Palavras-chave
Cyclodextrins (CD) Clonazepam (CLZ) Binary systems Solubility Mestrado Integrado - 2014