RICHARD BERGER,LEHUA CHANG,SCOTT D. EDMONDSON,STEPHEN D. GOBLE,SOOKHEE NICOLE HA,NAM FUNG KAR,IHOR E. KOPKA,BING LI,GREGORI J. MORRIELLO,CHRIS R. MOYES,DONG-MING SHEN,LIPING WANG,CHENG ZHU
申请号：
HRP20120129
公开号：
HRP20120129T2
申请日:
2012.02.07
申请国别(地区):
HR
年份:
2012
代理人:
摘要：
The invention relates to a sustained-release pharmaceutical composition comprising metoclopramide chlorhydrate in the form of tablets containing 30 mg of the active principle, intended for use in gastrointestinal disorders. The formulation mainly consists of a hydrophilic polymer, a hydrophobic polymer, a hydrophilic component and metoclopramide chlorhydrate. The hydrophilic polymer swells due to hydration upon contact with water, forming a layer of gel which controls the release of the active principle. The water inside the matrix dissolves the active principle which spreads towards the exterior through the layer of gel. The hydrophobic polymer displays deformation properties under compression, surrounding the particles of the active principle and reducing the quantity and dimensions of the pores in the matrix structure, thereby slowing the release of the active principle. The hydrophilic component forms part of the structure of the gel layer, supporting same. The active principle is metoclopramide chlorhydrate or a pharmaceutically acceptable salt thereof.Spoj formule I, ili njegova farmaceutski prihvatljiva sol, ili njegov stereoizmer, ili farmaceutski prihvatljiva sol njegovog stereoizomera: u kojemm je 0, 1,2,3 ili 4； n je 0, 1,2, 3, 4 ili 5, p je 0, 1 ili 2； q je 0,1, 2, 3 ili 4； t je 0, 1,2, 3, 4 ili 5； X je-CO-ili-SOL2-；Y je izabran iz grupe koju čine: (1) C1-C5 alkandiil, C2-C5 alkendiil i C2-C5 alkindiil, gdje je svaki od alkandiil, alkendiil i alkindiil izborno supstituiran sa jednom do tri grupe nezavisno izabrane od halogena, -ORa, -S(O)P-C1-C3 alkila； (2) -(CRaRa)j-Q-(CRaRa)k, gdje su j i k cijeli brojevi nezavisno izabrani od 0, 1 i 2, (3) veza, i (4) fenilen izborno supstituiran sa jednom do tri grupe nezavisno izabrane od R1； Z je izabran iz grupe koju čine: (1) fenil, (2) 5- ili 6-člani heterociklični prsten sa od 1 do 4 heteroatoma izabrana od kisika, sumpora i du®ika, (3) benzenov prsten fuzioniran za C5-C10 karbociklični prsten, (4) 5- ili 6-čla
