BRYSON NATHAN JOHN,GIOVINAZZO ANTHONY JOHN,BARNHART SCOTT DAVID,KOONS MICHAEL CLINTON
申请号：
NZ61268611
公开号：
NZ612686A
申请日:
2011.12.16
申请国别(地区):
NZ
年份:
2015
代理人:
摘要：
Provided are sublingual film pharmaceutical compositions comprising dopamine agonists. Preferred dopamine agonists are apomorphine or ropinerol (ropinirole). In one embodiment the composition is in a unit dosage form formulated for sublingual administration, wherein said unit dosage form is a film comprising: (A) a first layer comprising: (i) from 10 to 75% (w/w) apomorphine hydrochloride； (ii) from 0.5 to 10% (w/w) a low molecular weight polymer having a weight average molecular weight of from 5 KDa to 50 KDa selected from hydroxypropyl cellulose, hydroxypropyl methyl cellulose, hydroxyethyl cellulose, carboxymethyl cellulose, and methyl cellulose； and (iii) from 4 to 35% (w/w) a high molecular weight polymer having a weight average molecular 15 weight of greater than 60 KDa selected from hydroxypropyl cellulose, hydroxypropyl methyl cellulose, hydroxyethyl cellulose, carboxymethyl cellulose, and methyl cellulose； and (B) a second layer comprising: (iv) from 6 to 65% (w/w) a pH neutralizing agent that is an organic base having a pKa of 5 ± 2, and (v) from 15 to 50% (w/w) of a high molecular weight polymer having a weight average molecular weight of greater than 60 KDa selected from hydroxypropyl cellulose, hydroxypropyl methyl cellulose, hydroxyethyl cellulose, carboxymethyl cellulose, and methyl cellulose, wherein said first layer comprises from 2 to 60 mg of apomorphine hydrochloride. In another embodiment the composition is in unit dosage form formulated for sublingual administration, wherein said unit dosage form is a film comprising a first layer and a second layer, wherein the first layer comprises from 2 to 60 mg of apomorphine hydrochloride and wherein the second layer comprises a pH neutralizing agent that is an organic base having a pKa of 5 ± 2, wherein said organic base is selected from the group consisting of pyridoxine, citrate, and histidine. The formulations are useful in the treatment of Parkinson&rsquo；s disease, tremors, restless leg syndrome, se
