FANG, LARRY YUN,HARRIS, DAVID,KRISHNA, GOPAL,PRESTIPINO, RUSSELL C,STEINMAN, MARC,WAN, JIANSHENG,WASKIN, HETTY ANNE,MOTON, ALLEN E
申请号：
NZ58846009
公开号：
NZ588460A
申请日:
2009.04.15
申请国别(地区):
NZ
年份:
2012
代理人:
摘要：
A composition comprising posaconazole dissolved or molecularly dispersed in a hydroxypropylmethyl-cellulose-derivative polymer is disclosed, wherein, when an amount of the composition comprising at least about 100 mg of posaconazole is administered orally to a human under fasted conditions, at least one of the following PK median parameters are observed: Cmax in at least about 300 ng/mL or an AUC(tf) of at least about 10,000 hr.ng/mL.Also disclosed is a process for preparing a composition comprising posaconazole and hydroxypropylmethylcellulose acetate succinate, the process comprises the steps of: (a) dry-blending HPMC-AS and posaconazole in a ratio of from about 1:1 (HPMC-AS:posaconazole) to about 4:1 (HPMC-AS:posaconazole) to form a homogeneous admixture (b) heating the admixture prepared in step "a" to a temperature below the glass transition temperature of the HPMC-AS present in the mixture and above the fluxing temperature of the mixture, thereby forming a melt, optionally while blending the admixture and (c) cooling the melt formed in Step "b", thereby providing a solid composition comprising posaconazole dissolved or molecularly dispersed in HPMC-AS.
