Patent ID: 9283190
Filing Date: 2016-03-15
CPC Classification: A61K

Claim Text:
1. A method for preparing a high-efficacy, long-acting slow-release formulation of the poorly soluble drug, comprising the following steps: step 1. taking the poorly soluble drug 1 g, povidone K30 1-3 g, soybean lecithin 0.3-0.8 g and acrylic resin IV 0.2-0.5 g and injecting in absolute ethyl alcohol 20-40 ml (70° C. water-bath can be adopted to accelerate dissolution if necessary); after the said materials having dissolved, treating the solution with 60° C. water-bath; then rotarily evaporating the solution at 90 rpm, and then treating the substance with 70° C. water-bath till the solvent completely evaporates; putting the substance so obtained into a −20° C. freezer for 2 hours and then into a 60° C. drying oven for 12 hours; comminuting the substance and sieving it with 80 mesh; the solid dispersion of the poorly soluble drug is therefore obtained and ready for later use; step 2. taking cyclohexane 20-80 ml, nonyl phenol 10(NP-10) 4-8 ml and mixing them together; adding in-n-hexanol 1-3 ml, 25.6% ammonia water 1-3 ml and agitating for 1 hour at room temperature; slowly dropping in tetraethyl orthosilicate 3-5 ml and agitating for 24 hours at room temperature; adding in absolute ethyl alcohol 40-80 ml and-treating with ultrasound for 1 hour; and then centrifugally separating at 15000 rpm for 15 min and washing the precipitate with distilled water three times; adding water, freezing and drying the substance in succession, and silica nanoparticles 8 g-32 g are therefore obtained; taking the said silica nanoparticles 1 g, adding in 0.6 mol/L Na dissolving the poorly soluble drug 2 g in absolute ethyl alcohol 10-20 ml, soaking mesoporous silica nanoparticles 1 g in the solution for 24 hours, and then centrifugally separating at 15000 rpm for 15 min and washing the precipitate with absolute ethyl alcohol three times; adding in distilled water 10 ml, freezing and drying the substance in succession, and drug-loaded nanoparticles are therefore obtained; step 3. taking solid dispersion of the poorly soluble drug 1 g, mixing it with hypromellose K4M 0.2-0.3 g and L-HPC 0.1-0.2 g, sieving with 16 mesh and the wet granules so obtained are baked at 60° C. for 30 min, reshaping the granules with 16 mesh and the slow-release granules step 4. taking solid dispersion of the poorly soluble drug 1.8 g, mixing it with hypromellose K4M 0.1-0.2 g, L-HPC 0.2-0.3 g and drug-loaded silica nanoparticles 1.25-2.5 g; sieving with 16 mesh and the wet granules so obtained are baked at 60° C. for 30 min, reshaping the granules with 16-mesh and the slow-release granules step 5. mixing the slow-release granules