A sustained-release formulation for an acetylcholinesterase inhibitor, comprising an acetylcholinesterase inhibitor and at least two gel-forming polymers, and methods of manufacture thereof. The acetylcholinesterase inhibitor preferably comprises donepezil.
대표청구항▼
1. A sustained-release formulation comprising an acetylcholinesterase inhibitor, wherein the acetylcholinesterase inhibitor is donepezil or a pharmaceutically acceptable salt thereof, wherein the release rate of the acetylcholinesterase inhibitor is controlled by two non-ionic gel-forming polymers w
1. A sustained-release formulation comprising an acetylcholinesterase inhibitor, wherein the acetylcholinesterase inhibitor is donepezil or a pharmaceutically acceptable salt thereof, wherein the release rate of the acetylcholinesterase inhibitor is controlled by two non-ionic gel-forming polymers which are a combination of a low viscosity grade hydroxypropyl methylcellulose polymer (low viscosity grade HPMC polymer) and a high viscosity grade hydroxypropyl methylcellulose polymer (high viscosity grade HPMC polymer), the formulation comprising: (a) donepezil or a pharmaceutically acceptable salt thereof in a concentration of about 10% (w/w) of the total formulation;(b) the low viscosity grade HPMC polymer in a concentration in the range of from about 11% to about 19% (w/w) of the total formulation;(c) the high viscosity grade HPMC polymer in a concentration in the range of from about 3% to about 5% (w/w) of the total formulation; and(d) at least one excipient selected from the group consisting of a filler, a binder, a disintegrant, and a glidant. 2. The formulation of claim 1, wherein the pharmaceutically acceptable salt of donepezil is donepezil hydrochloride. 3. The formulation of claim 1, wherein the filler is selected from the group consisting of lactose, glucose, fructose, sucrose, dicalcium phosphate, a sugar alcohol, corn starch, potato starch, sodium carboxymethylcellulose, ethylcellulose, cellulose acetate, hydroxypropyl methylcellulose acetate succinate, cellulose acetate phthalate, hydroxypropyl methyl cellulose phthalate, polyvinyl acetate phthalate, poly(methacrylic acid, methyl methacrylate) 1:1, poly(methacrylic acid, ethyl acrylate) 1:1, alginic acid, sodium alginate, and a mixture thereof. 4. The formulation of claim 1, wherein the binder is selected from the group consisting of polyvinyl pyrrolidone, a copolymer of polyvinyl pyrrolidone and polyvinyl acetate, low molecular weight hydroxypropyl cellulose, low molecular weight carboxy methyl cellulose, ethylcellulose, gelatin, polyethylene oxide, acacia, dextrin, magnesium aluminum silicate, starch, polymethacrylate, hydroxvpropyl methylcellulose acetate succinate, cellulose acetate phthalate, hydroxypropyl methyl cellulose phthalate, polyvinyl acetate phthalate, poly(methacrylic acid, methyl methacrylate) 1:1, poly(methacrylic acid, ethyl acrylate) 1:1, alginic acid, sodium alginate, and a mixture thereof. 5. The formulation of claim 1, wherein the disintegrant is selected from the group consisting of low-substituted carboxymethyl cellulose sodium, crospovidone, sodium carboxymethyl starch, cross-linked sodium carboxymethyl cellulose, pregelatinized starch, microcrystalline cellulose, water insoluble starch, calcium carboxymethyl cellulose, low substituted hydroxypropyl cellulose, magnesium silicate, aluminum silicate, and a mixture thereof. 6. The formulation of claim 1, wherein the glidant comprises at least one of silicone dioxide and magnesium stearate. 7. The formulation of claim 1, wherein the low viscosity grade HPMC polymer is HPMC K100 and the high viscosity grade HPMC polymer is HPMC K100M. 8. The formulation of claim 1, wherein the low viscosity grade HPMC polymer is HPMC K100 and the high viscosity grade HPMC polymer is HPMC K15M.
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