Gatti Paolo,Colombo Italo,Gervasoni Dario,Pironti Vincenza,Alborghetti Lia,Fabiani Flavio,Boltri Luigi
申请号：
NZ71348711
公开号：
NZ713487A
申请日:
2011.12.22
申请国别(地区):
NZ
年份:
2017
代理人:
摘要：
Disclosed herein is a process for the preparation of a composite comprising at least one poorly soluble drug of Class II according to Biopharmaceutics Classification System (BCS) having low solubility and high gastrointestinal permeability, at least one polymeric carrier selected from the group consisting of cross-linked polyvinylpyrrolidone, crosslinked sodium carboxymethylcellulose, cross-linked cyclodextrins, cross-linked dextran, cross-linked starch, cross-linked methylcellulose and at least one not chemically cross-linked polymer, which is both soluble in water and organic solvent selected from the group consisting of hydroxypropylcellulose, hydroxyethylcellulose, hydroxypropylmethylcellulose, hydroxypropylmethycellulose acetate succinate, cellulose acetate trimellitate, acrylic and methacrylic polymers and their copolymers, methacrylic acid-methylmethacrylate copolymer, polyaminoalkyl methacrylate-methacrylic esters copolymer, dimethylaminoethyl methacrylate-butylmethacrylate-methylmethacrylate copolymer, vinylpyrrolidone-vinyl acetate copolymer, methylvinylether-maleic acid copolymer, polyethyleneglycol- caprolactame- vinylpyrrolidone copolymer, comprising the following steps: (1) Dissolving at least one poorly water soluble drug in a process solvent or process solvent mixture, wherein the solvent may is selected from methanol, ethanol, higher alcohols, acetone, chlorinated solvents, formamide, dimethylformamide, fluorinated hydrocarbons or mixture thereof (2) Dissolving at least one not cross-linked polymer, which is both water and organic solvent soluble, into the drug solution of step (1) (3) Swelling at least one polymeric carrier with the solution prepared in step (2), thus obtaining a swollen composite (4) Removing the process solvent from the swollen composite of step (3), wherein step (4) is carried out for a period of time which is equal or shorter than about 410 minutes and at a temperature from 35 to 60°C and wherein the process solvent is able to
