| 摘要 |
A dosing structure which is designed to provide a more prolonged release of the opiate when the dose is taken in the presence of alcohol, compared with taking the dose with water and no alcohol, is new. An oral dosing form (I) comprising an opiate has a dosing structure designed to provide prolonged release of the opiate in the presence of an aqueous medium containing alcohol in a concentration of ca. 20 vol.% or more. The ratio of the average maximum opiate concentration in the blood plasma from a single dose via an aqueous medium containing alcohol to the same average maximum opiate concentration from a single dose via an alcohol-free aqueous medium is less than or equal to ca. 1.8:1. Independent claims are also included for: (1) oral dosing form (II) as per (I), except that the ratio is less than or equal to ca. 5:1; (2) oral dosing form (III) comprising an opiate and a dosing structure designed to provide prolonged release of the opiate in the presence of an aqueous medium containing alcohol in a concentration of ca. 20 vol.% or more, such that the amount of opiate released into the medium over an extended period of ca. 2 h is ca. 80 wt.% or less of that released into an alcohol-free aqueous medium, as measured in vitro; (3) oral dosing form (IV) comprising an opiate and a dosing structure designed to provide prolonged release of the opiate in the presence of an aqueous solution containing alcohol in a concentration of ca. 20 vol.% or more, so that the ratio of the average time taken to reach the maximum concentration in blood plasma for a single dose via an aqueous medium containing alcohol to the same time for a single dose for an alcohol-free aqueous medium is ca. 0.5-1.0; and (4) use of (I)-(IV) for producing painkillers. |
