摘要
Solid lipid extrusion is a suitable technique to produce oral dosage forms with improved taste properties. The design of a lipid formulation for poorly water soluble drugs is a challenge because of the poor dissolution and potential bioavailability problems. In this study, solid lipid extrusion at room temperature was applied for the formulation development of the BCS Class II drug NXP 1210. Powdered hard fat (Witocan庐 42/44 mikrofein), glycerol distearate (Precirol庐 ato 5) and glycerol trimyristate (Dynasan庐 114) were investigated as lipid binders. Different amounts of polyvinylalcohol (PVA)-polyethyleneglycol (PEG)-graft copolymer (Kollicoat庐 IR) and crospovidone (Polyplasdone庐 Xl-10) were scrutinized as solubilizers. The dissolution profiles depicted a short lag time (about 2 min) and then fast and complete dissolution of NXP 1210 by increasing the amount of crospovidone. The initial release was more delayed with an increased amount of PVA-PEG-graft copolymer. Dissolution rate could also be influenced by changing the lipid binder from pure hard fat into a mixture of hard fat, glycerol distearate and glycerol trimyristate. The formulations are feasible for taste-masked granules or pellets containing poorly soluble drugs.