Deep knowledge on
small-molecule drugs and
the 110,000 global patents
Anticipate generic drug launch
Manage your formulary budget
Find generic entry opportunities
Proactively manage your pharmacy inventory
Drug patents …
… from Kazakhstan to Kalamazoo
Flat-rate pricing for predictable budgeting
Short-term plans for project- or client-based billing
Upgrade to enjoy subscriber-only features like email alerts and data export. See the Plans and Pricing
|Title:||Formulations of pharmacological agents, methods for the preparation thereof and methods for the use thereof|
|Abstract:||In accordance with the present invention, there are provided compositions and methods useful for the in vivo delivery of substantially water insoluble pharmacologically active agents (such as the anticancer drug paclitaxel) in which the pharmacologically active agent is delivered in the form of suspended particles coated with protein (which acts as a stabilizing agent). In particular, protein and pharmacologically active agent in a biocompatible dispersing medium are subjected to high shear, in the absence of any conventional surfactants, and also in the absence of any polymeric core material for the particles. The procedure yields particles with a diameter of less than about 1 micron. The use of specific composition and preparation conditions (e.g., addition of a polar solvent to the organic phase), and careful selection of the proper organic phase and phase fraction, enables the reproducible production of unusually small nanoparticles of less than 200 nm diameter, which can be sterile-filtered. The particulate system produced according to the invention can be converted into a redispersible dry powder comprising nanoparticles of water-insoluble drug coated with a protein, and free protein to which molecules of the pharmacological agent are bound. This results in a unique delivery system, in which part of the pharmacologically active agent is readily bioavailable (in the form of molecules bound to the protein), and part of the agent is present within particles without any polymeric matrix therein.|
|Inventor(s):||Desai; Neil P. (Los Angeles, CA), Tao; Chunlin (Los Angeles, CA), Yang; Andrew (Rosemead, CA), Louie; Leslie (Montabello, CA), Soon-Shiong; Patrick (Los Angeles, CA)|
|Assignee:||Abraxis Bioscience, LLC (Los Angeles, CA)|
|Filing Date:||Sep 12, 2006|
|Claims:||1. An emulsion comprising paclitaxel, the emulsion comprising a first phase comprising nanodroplets comprising paclitaxel dissolved in chloroform and a water miscible alcohol solvent for paclitaxel, wherein the concentration of the water miscible alcohol solvent in the first phase is about 5-25% (v/v), and a second phase comprising water and albumin, wherein the emulsion is free of surfactants. |
2. The emulsion of claim 1, wherein the water miscible alcohol solvent for paclitaxel is ethanol.
3. The emulsion of claim 1, wherein the albumin concentration in the emulsion is about 0.05% to 25% (w/v).
4. The emulsion of claim 3, wherein the albumin concentration in the emulsion is about 0.5% to 5%.
5. The emulsion of claim 2, wherein the chloroform to ethanol ratio in the emulsion is 9:1.
6. The emulsion of claim 1, wherein the phase fraction of the first phase in the emulsion is between about 0.5% and 15%.
7. The emulsion of claim 6, wherein the phase fraction of the first phase in the emulsion is between 1% and 8%.
8. The emulsion of claim 1, wherein the albumin is human albumin.
9. The emulsion of claim 2, wherein the albumin is human albumin.
10. The emulsion of claim 3, wherein the albumin is human albumin.
11. The emulsion of claim 4, wherein the albumin is human albumin.
12. The emulsion of claim 5, wherein the albumin is human albumin.
13. The emulsion of claim 6, wherein the albumin is human albumin.
14. The emulsion of claim 7, wherein the albumin is human albumin.
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.