resumo
Simvastatin is a cholesterol-regulating drug of widespread use in the prevention of cardiovascular diseases associated with dyslipidaemia. Herein we report on the preparation of co-amorphous adducts of simvastatin with the solubilising agent beta-cyclodextrin by means of a solvent-free mechanochemical procedure and on the evaluation of their dissolution profiles. Production of co-milled adducts was carried out using a laboratory scale planetary ball mill. The resulting powders were characterised by X-ray powder diffraction, Fourier-transform infrared spectroscopy, differential scanning calorimetry and scanning electron microscopy. Dissolution of simvastatin from the co-milled powders into water was measured by ultra-violet/visible absorption spectroscopy (UV/Vis). Results show that co-amorphisation was obtained after 280 min of milling the two components, with formation of a solid that features a much more favourable dissolution profile and allows simvastatin concentration in aqueous solution to reach a value roughly to nine folds higher than the one obtained by dissolving the pure drug. In conclusion, co-grinding with beta-cyclodextrin is a simple and quick method to obtain simvastatin preparations with an improved dissolution profile.
palavras-chave
INCLUSION COMPLEXES; DISPERSIONS; SYSTEM; FTIR
categoria
Pharmacology & Pharmacy
autores
Braga, SS; El-Saleh, F; Oliveira, C; Barbosa, JS; Paz, FAA
nossos autores
Filipe Alexandre Almeida Paz
Investigador Principal
Jéssica Barbosa
Estudante de doutoramento
Susana Isabel Fonseca de Almeida Santos Braga
InvestigadorProjectos
Collaboratory for Emerging Technologies, CoLab (EMERGING TECHNOLOGIES)
CICECO - Aveiro Institute of Materials (UIDB/50011/2020)
CICECO - Aveiro Institute of Materials (UIDP/50011/2020)
Associated Laboratory CICECO-Aveiro Institute of Materials (LA/P/0006/2020)
agradecimentos
LAQV-REQUIMTE (Ref. UIDB/50006/2020) acknowledges financing by FCT/MCTES (Fundacao para a Ciencia e a Tecnologia, Ministerio da Ciencia, da Tecnologia e do Ensino Superior) through national founds (PIDDAC) and, where applicable, co -financed by the European Regional Development Fund (FEDER) , within the PT2020 Partnership Agreement. The work of CICECO authors was developed within the scope of the project CICECO - Aveiro Institute of Materials, UIDB/50011/2020, UIDP/50011/2020 & LA/P/0006/2020, financed by national funds through FCT/MCTES (PIDDAC) .