Manage your formulary budget
Anticipate generic drug launch
Drug patents …
… from Kazakhstan to Kalamazoo
Find generic entry opportunities
Proactively manage your pharmacy inventory
Deep knowledge on
small-molecule drugs and
the 110,000 global patents
Upgrade to enjoy subscriber-only features like email alerts and data export. See the Plans and Pricing
|Title:||Process for the preparation of polymer-based sustained release compositions|
|Abstract:||The invention relates to a sustained release composition and methods of forming and using said composition for the sustained release of biologically active agent. The sustained release compositions of the invention comprise a biocompatible polymer and a biologically active agent characterized by a porous center and a less porous outer layer wherein the center and outer layer consist of essentially the same materials. The sustained release compositions can be prepared by annealing at least a substantial portion of the exterior surface of a polymer/active agent matrix. The compositions which have been annealed exhibit a decrease in the release of agent over the first 24 hours following administration (i.e., reduced burst) and as a result can show an increase in the duration of sustained release thereby providing increased therapeutic benefits.|
|Inventor(s):||Jaworowicz; Warren E. (Boxboro, MA), Wright; James I. (Lexington, MA)|
|Assignee:||Alkermes Controlled Therapeutics, Inc. (Cambridge, MA)|
|Filing Date:||Aug 10, 2000|
|Claims:||1. A method for preparing a composition for the sustained release of a biologically active agent, comprising the steps of: |
a) forming a mixture comprising a biologically active agent, a biocompatible polymer, and a polymer solvent;
b) removing the polymer solvent thereby forming a solid polymer/active agent matrix; and
c) annealing at least a substantial portion of the exterior surface of the polymer/active agent matrix by the application of an annealing solvent.
2. The method of claim 1 wherein annealing is accomplished by the application of an annealing solvent to the polymer/active agent matrix in a fluidized bed system.
3. The method of claim 2 wherein the fluidized bed system is a bottom spray system.
4. The method of claim 1 wherein the annealing solvent is selected from the group consisting of: methylene chloride, chloroform, acetone, ethyl acetate, anisole, methyl acetate, hexafluoroisopropanol, tetrahydrofuran, dimethylsulfoxide and any combination thereof.
5. The method of claim 1 wherein the temperature of the fluidized bed is below the flashpoint and above the freezing point of the annealing solvent.
6. The method of claim 1 wherein the polymer/active agent matrix is in the form of microparticles.
7. The method of claim 1 wherein about 25% or more of the exterior surface is annealed.
8. The method of claim 1 wherein about 40% or more of the exterior surface is annealed.
9. The method of claim 1 wherein between about 50% and about 100% of the exterior surface is annealed.
10. The method of claim 1 further comprising the steps of: forming droplets of the polymer/active agent mixture and freezing the droplets of the polymer/active agent mixture, wherein said forming and freezing steps are performed prior to removing the polymer solvent.
11. The method of claim 10 wherein the droplets are microdroplets.
12. The method of claim 1 wherein the biocompatible polymer is biodegradable.
13. The method of claim 12 wherein the biodegradable polymer is selected from the group consisting of poly(lactide)s, poly(glycolide)s, poly(lactide-coglycolide)s, poly(lactic acid)s, poly(glycolic acid)s, poly(lactic acid-co-glycolic acid)s, poly(caprolactone), polycarbonates, polyesteramides, polyanhydrides, poly(amino acid)s, poly(ortho ester)s, polycyanoacrylates, polyamides, polyacetals, poly(ether ester)s, copolymers of poly(ethylene glycol) and poly(ortho ester)s, poly(dioxanone)s, poly(alkylene alkylate)s, biodegradable polyurethanes, blends and copolymers thereof.
14. The method of claim 13 wherein said polymer is poly(lactide-co-glycolide).
15. The method of claim 1 wherein the biocompatible polymer is non-biodegradable.
16. The method of claim 1 wherein the polymer solvent is methylene chloride, chloroform, acetone, ethyl acetate, anisole, methyl acetate, dimethylsulfoxide, hexafluoroisopropanol or any combinations thereof.
17. The method of claim 1 wherein the biologically active agent is a protein, peptide or nucleic acid.
Drugs may be covered by multiple patents or regulatory protections. All trademarks and applicant names are the property of their respective owners or licensors. Although great care is taken in the proper and correct provision of this service, thinkBiotech LLC does not accept any responsibility for possible consequences of errors or omissions in the provided data. The data presented herein is for information purposes only. There is no warranty that the data contained herein is error free. thinkBiotech performs no independent verifification of facts as provided by public sources nor are attempts made to provide legal or investing advice. Any reliance on data provided herein is done solely at the discretion of the user. Users of this service are advised to seek professional advice and independent confirmation before considering acting on any of the provided information. thinkBiotech LLC reserves the right to amend, extend or withdraw any part or all of the offered service without notice.