TY - JOUR
T1 - Tablet formulation for the fast and sustained-release of flavonoids
T2 - Naringin and naringenin
AU - Lauro, M. R.
AU - Torre, M. L.
AU - Maggi, L.
AU - De Simone, F.
AU - Conte, U.
AU - Aquino, R. P.
PY - 2001
Y1 - 2001
N2 - Naringin and its metabolite naringenin are flavonoids, naturally occurring plant products, possessing a variety of biological effects in mammalian cell systems, used in medicine and characterised by a low water solubility. In vivo, they show slow and irregular absorption and low bioavailability when administered as solid oral dosage forms. Their poor and pH-dependent solubility is likely to give a low dissolution rate of the drugs from the solid form, which could be the limiting or rate-controlling step for bioabsorption. In this work, pharmaceutical dosage forms were set up and optimised to enhance the therapeutic potential of these flavonoids after oral administration. In order to improve their dissolution rate, naringin and naringenin were loaded by co-mixing on sodium carboxymethylcellulose as a superdisintegrant and dissolution rate enhancer. These drug/polymer systems were used for the preparation of both quick release tablets and slow release matrices, the last one formulated with HPMC of different viscosity grade. The results of the dissolution tests show that an extended release of the drugs for times ranging from 6 to 24 h can be obtained depending on the type and viscosity of the HPMC used. In the case of the formulations containing HPMC of higher viscosity, improved and considerably constant drug release rates were achieved.
AB - Naringin and its metabolite naringenin are flavonoids, naturally occurring plant products, possessing a variety of biological effects in mammalian cell systems, used in medicine and characterised by a low water solubility. In vivo, they show slow and irregular absorption and low bioavailability when administered as solid oral dosage forms. Their poor and pH-dependent solubility is likely to give a low dissolution rate of the drugs from the solid form, which could be the limiting or rate-controlling step for bioabsorption. In this work, pharmaceutical dosage forms were set up and optimised to enhance the therapeutic potential of these flavonoids after oral administration. In order to improve their dissolution rate, naringin and naringenin were loaded by co-mixing on sodium carboxymethylcellulose as a superdisintegrant and dissolution rate enhancer. These drug/polymer systems were used for the preparation of both quick release tablets and slow release matrices, the last one formulated with HPMC of different viscosity grade. The results of the dissolution tests show that an extended release of the drugs for times ranging from 6 to 24 h can be obtained depending on the type and viscosity of the HPMC used. In the case of the formulations containing HPMC of higher viscosity, improved and considerably constant drug release rates were achieved.
KW - Dissolution rate enhancers
KW - Fast release tablets
KW - Flavonoids
KW - Hydrophilic matrices
KW - Naringenin
KW - Naringin
KW - Sustained release formulations.
UR - http://www.scopus.com/inward/record.url?scp=0034829792&partnerID=8YFLogxK
M3 - Article
SN - 1157-1489
VL - 11
SP - 265
EP - 269
JO - S.T.P. Pharma Sciences
JF - S.T.P. Pharma Sciences
IS - 4
ER -