| 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’s disease, tremors, restless leg syndrome, sexual dysfunction and depressive disorders. |
