Sustained release solid formulations and methods of manufacturing the same

摘要

Disclosed are a sustained release solid formulation comprising a drug, for example, oxycodone or its pharmaceutically acceptable salt, in a water-insoluble matrix, which comprises a wax type excipient and copovidone, and thus, has increased compressibility and fluidity and reduced adhesiveness, and a method of preparing the same.

主权项

1. A sustained release solid oral formulation comprising oxycodone or oxycodone hydrochloride that is first coated with a liquid or semisolid hydrophobic carrier selected from the group consisting of vegetable oil, mineral oil, synthetic oil, amphoteric surfactant having an HLB (hydrophilic-lipophilic balance) value less than 6, phospholipid lecithin and a mixture thereof, and is then adsorbed with an adsorbent selected from the group consisting of colloidal silicon dioxide, talc and a mixture thereof, in a water-insoluble matrix, wherein the water-insoluble matrix comprises copovidone as a binder and a wax type excipient selected from the group consisting of glyceryl fatty acid ester and hydrogenated oil, wherein the matrix has a void and/or surface, the void being filled or the surface being coated with the wax type excipient and the copovidone which have been melted, cooled and solidified, wherein the sustained release solid oral formulation achieves a linear release rate of oxycodone or oxycodone hydrochloride for a period of at least 12 hours.