Bilayer composition for the sustained release of acetaminophen and tramadol

摘要

The invention relates to a bilayer composition for the delivery of acetaminophen and tramadol over at least a twelve hour period following initial administration. A single administration of the bilayer composition can provide analgesia starting in less than half an hour to about one hour after initial administration with a duration of at least twelve hours after initial administration.

主权项

1. A bilayer composition for the delivery of tramadol and acetaminophen, the bilayer composition comprising:
a. a first layer defining a rapid release portion of the composition and comprising a first amount of acetaminophen; and b. a second layer defining a sustained release portion of the composition comprising a second amount of acetaminophen, tramadol, and a controlled release excipient selected from the group consisting of cross-linked high amylose starch, and hydroxypropylmethylcellulose, and a mixture thereof,wherein, when tested in a U.S.P. Type III Apparatus at 20 dips per minute at 37° C. in 250 mL of a solution of potassium phosphate monobasic pH 6.8 for one hour, after which the solution is removed and replaced with a fresh 250 mL of potassium phosphate monobasic pH 6.8 for eleven hours, the acetaminophen and tramadol are released with the following kineticsTimeAcetaminophenTramadol(hours)% release (by weight)% release (by weight)130-60≦35460-9045-65880-90≦9012≧90 ≧90,and wherein a single bolus administration of the bilayer composition to a subject achieves (i) an effective plasma concentration of acetaminophen within about half an hour after initial administration, and (ii) effective plasma concentrations of acetaminophen and tramadol over a twelve hour period following initial administration.