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CLOSAPINE COMPOSITIONS WITH CONTROLLED RELEASE
专利权人:
АЛКЕРМЕС ФАРМА АЙЭЛЕНД ЛИМИТЕД (IE)
发明人:
РАДДИ Стефен Б. (US),МАКГУРК Саймон Л. (US),ПАТЕЛ Ракеш (US),БУЛЛОК Джон (US),КЕВАЛРАМАНИ Радж (US)
申请号:
RU2011145278/15
公开号:
RU2011145278A
申请日:
2010.04.08
申请国别(地区):
RU
年份:
2013
代理人:
摘要:
1. A composition comprising a semipermeable coating; clozapine particles having an effective average particle size of less than or about 2 microns and a surface stabilizer adsorbed on the surface of clozapine particles; and a solubilizing agent. 2. The composition of claim 1, wherein the semipermeable coating is a microporous coating with controlled porosity. The composition of claim 2, wherein the microporous coating with controlled porosity contains a polymer that is soluble in the environment of use and a pore-forming additive that is soluble in the environment of use. The composition of claim 3, wherein the polymer is selected from the group consisting of cellulose polymers, methacrylates and phthalates, where the pore forming additive is selected from the group consisting of HPMC, PVP, polyhydric alcohols and sugars. The composition according to claim 3, where the wt.% Pore forming additives in the microporous coating of adjustable porosity is selected from the group consisting of 0.5%, 1.0%, 1.5%, 2.0%, 2.5%, 3 , 0%, 3.5%, 4%, 4.5%, 5%, 6%, 7%, 8%, 9%, 10%, 12%, 13%, 15%, 17%, 19%, 21%, 22%, 24%, 26%, 28%, 30%, 32%, 34%, 36%, 38%, 41%, 43%, 45%, 47%, 49% and 50% .6. The composition of claim 1, wherein the effective average particle size is selected from the group consisting of less than or about 1900 nm, 1800 nm, 1700 nm, 1600 nm, 1500 nm, 1400 nm, 1300 nm, 1200 nm, 1100 nm, 1000 nm (1 μm), 900 nm, 800 nm, 700 nm, 600 nm, 500 nm, 400 nm, 300 nm, 200 nm, 150 nm, 100 nm, 75 nm and 50 nm. 7. The composition of claim 1, wherein the clozapine particles have D selected from the group consisting of less than or about 5000 nm, 4900 nm, 4800 nm, 4700 nm, 4600 nm, 4500 nm, 4400 nm, 4300 nm, 4200 nm, 4100 nm, 4000 nm, 3900 nm, 3800 nm, 3700 nm, 3600 nm, 3500 nm, 3400 nm, 3300 nm, 3200 nm, 3100 nm, 3000 nm, 2900 nm, 2800 nm, 2700 nm, 2600 nm, 2500 nm, 2400 nm, 2300 nm, 2200 nm, 2150 nm, 2100 nm, 2075 nm and 2000 nm. 8. The composition according to claim 1, where the surfa
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