Formulation of biphasic release tablets containing slightly soluble drugs.
A new biphasic release system for slightly soluble drugs has been proposed. To enhance the dissolution rate, the drug was milled with a superdisintegrant. Then, double-layer tablets were prepared. One layer was formulated to release the drug in a very short time (fast-release). The other consisted of an extended-release hydroxypropylmethylcellulose (HPMC) matrix. Different HPMC concentrations (10, 16 and 22%) and viscosity grades (Methocel K4, K15 and K100M) were used to obtain different release rates of the drug from the extended-release layer, ketoprofen and praziquantel were used as slightly soluble model drugs. The in vitro dissolution tests of the prepared double-layer systems, showed the desired biphasic behaviour: the drug contained in the fast releasing layer dissolved within the first 15 min, while the drug contained in the prolonged-release layer was released at different times, depending on the formulation of the hydrophilic matrix. In particular, an increase in the percentage and viscosity grade of HPMC, in the extended release layer, leads to a decrease in the drug delivery rate and produces a wide range of different release rates from only a few hours up to 24 h.
Maggi
L
L
Dipartimento di Chimica Farmaceutica, University of Pavia, Pavia, Italy.
Machiste
E O
EO
Torre
M L
ML
Conte
U
U
D002626:Chemistry, Pharmaceutical; D003692:Delayed-Action Preparations; D005079:Excipients; D007660:Ketoprofen / Q000008:administration & dosage; D007700:Kinetics; D007785:Lactose / Q000031:analogs & derivatives; D008747:Methylcellulose / Q000031:analogs & derivatives; D010078:Oxazines; D010316:Particle Size; D004364:Pharmaceutical Preparations / Q000008:administration & dosage*; D011223:Praziquantel / Q000008:administration & dosage; D012995:Solubility; D013607:Tablets
D003692:Delayed-Action Preparations; D005079:Excipients; D010078:Oxazines; D004364:Pharmaceutical Preparations; D013607:Tablets; D011223:Praziquantel; D008747:Methylcellulose; D007660:Ketoprofen; C071191:MK 458; D007785:Lactose