Controlled release preparation
First Claim
1. An oral controlled release pharmaceutical preparation in the form of a multiple unit hard gelatin capsule enclosing particles containing a therapeutically effective amount of a salt of morphine for administration once daily characterized in that it consists of at least 50 particles with a size in the range of 0.2 to 3 mm, each having a core containing a salt of morphine coated with a barrier layer containing at least one water insoluble component selected from the group consisting of ethyl cellulose, copolymers synthesized from acrylic acid esters and methacrylic acid esters, natural waxes, and synthetic waxes, providing a virtually pH-independent drug release within the pH range of 1.0 to 7.0 and in that the serum concentration of morphine obtained is at least 50% of the maximum serum concentration during at least 12 hours after the administration of a single dose of said preparation and providing at least about 80% of the bioavailability of said preparation.
3 Assignments
0 Petitions
Accused Products
Abstract
An oral controlled release pharmaceutical preparation in the form of a tablet, capsule or sachet containing a plurality of coated particles comprising a therapeutically effective amount of a salt of morphine coated with a barrier membrane providing a controlled, preferably pH-independent, release of morphine in that the serum concentration of morphine obtained is at least 50% of the maximum serum concentration during at least 12 hours after administration of a single dose, and providing a significantly reduced plasma concentration fluctuation compared to known morphine preparations. A method for the manufacture of such a preparation and the use of such preparations for the manufacture of an analgesic useful in the treatment of severe chronicle pain are also provided.
145 Citations
13 Claims
- 1. An oral controlled release pharmaceutical preparation in the form of a multiple unit hard gelatin capsule enclosing particles containing a therapeutically effective amount of a salt of morphine for administration once daily characterized in that it consists of at least 50 particles with a size in the range of 0.2 to 3 mm, each having a core containing a salt of morphine coated with a barrier layer containing at least one water insoluble component selected from the group consisting of ethyl cellulose, copolymers synthesized from acrylic acid esters and methacrylic acid esters, natural waxes, and synthetic waxes, providing a virtually pH-independent drug release within the pH range of 1.0 to 7.0 and in that the serum concentration of morphine obtained is at least 50% of the maximum serum concentration during at least 12 hours after the administration of a single dose of said preparation and providing at least about 80% of the bioavailability of said preparation.
Specification