Loading patent…
AssigneeSynthon BV
InventorsJacobus M. Lemmens, Dennie J. M. van den Heuvel, Johannes J. Platteeuw, Frans van Dalen
Estimating the term…
Hypnotic pharmaceutical compositions are made from pellets and exhibit a modified release. Zolpidem or a pharmaceutically acceptable salt thereof is a typical hypnotic. The pellets are preferably spherical and exhibit a dissolution profile that includes 60% of the hypnotic agent being release from the pellet not earlier than 5 minutes from the start of a specified in vitro dissolution test. Although the modified release profile can include 50% of the hypnotic agent being released not earlier than 15 minutes after the start of the dissolution test, the pellet preferably does not contain a release rate controlling excipient or coating. Instead, microcrystalline cellulose and the active constitute the majority of the pellet, e.g. 90% or more. Spherical pellets are also made by a convenient method that is applicable to any pharmaceutically active agent.
A pharmaceutical pellet comprising a substantially homogenous mixture of a rapidly-acting hypnotic agent or a pharmaceutically acceptable salt thereof and a pellet forming carrier of microcrystalline cellulose, wherein the amount of said hypnotic agent and said pellet forming carrier is at least 90% of the pellet weight, said pellet having a particle size within the range of 0.85 to 2.0 mm and wherein said pellet exhibits a dissolution profile under U.S. Pharmacopoeia XXIII, Dissolution method I, in a basket apparatus at temperature 37° C., in 0.01N HCl medium and at 100 r.p.m., such that at 5 minutes from the start of the test, less than 60% of the hypnotic agent has been released from the pellet.
A pharmaceutically acceptable monolithic spherical pellet comprising microcrystalline cellulose and zolpidem or a pharmaceutically acceptable salt thereof, wherein said pellet does not contain a release rate controlling excipient or coating, does not contain a surface coating, and exhibits a dissolution profile under US Pharmacopoeia XXIII, Dissolution method I, in a basket apparatus at temperature 37° C., in 0.01N HCl medium and at 100 r.p.m., such that at 15 minutes from the start of the test, less than 70% of the zolpidem has been released from the pellet.
Dependencies are inferred from the claim text.