.

Deeper Knowledge, Faster

  • Plan your formulary budget
  • Identify first generic entrants
  • Drug patents in 130+ countries

► See Plans & Pricing

Upgrade to enjoy subscriber-only features like email alerts and data export. See the Plans and Pricing

Serving 500+ biopharmaceutical companies globally:

Farmers Insurance
Medtronic
Argus Health
Express Scripts
Harvard Business School
Deloitte
Johnson and Johnson
US Department of Justice
McKesson
Cerilliant

Generated: June 26, 2017

DrugPatentWatch Database Preview

Claims for Patent: 8,133,514

« Back to Dashboard

Claims for Patent: 8,133,514

Title:Carbon-substituted diketopiperazine delivery systems
Abstract: Compositions useful in the delivery of active agents are provided. These delivery compositions include (a) an active agent; and (b) a carrier of at least one mono-C-substituted or di-C-substituted diketopiperazine. Methods for preparing these compositions and administering these compositions are also provided.
Inventor(s): Milstein; Samuel J. (Larchmont, NY)
Assignee: MannKind Corporation (Valencia, CA)
Application Number:12/473,192
Patent Claims: 1. A delivery composition comprising: (a) an active agent; and (b) at least one di-C-substituted diketopiperazine of formula I: ##STR00005## wherein R and R.sup.1 are each C.sub.2-C.sub.24 alkenyl and have at least one functional group selected from the group consisting of O and carboxyl group, and at least one of R and R.sup.1 contain a carboxyl group; and wherein R and R.sup.1 are optionally interrupted by O or N, or a combination thereof.

2. A delivery composition as defined in claim 1, comprising a microsphere.

3. A delivery composition as defined in claim 2, wherein said microsphere comprises a microcapsule.

4. A delivery composition as defined in claim 2, wherein said microsphere has a diameter of less than about 10 .mu.m.

5. A delivery composition as defined in claim 1, wherein said active agent comprises a fragrance.

6. A delivery composition as defined in claim 1, wherein said active agent comprises a biologically active agent.

7. A delivery composition as defined in claim 6, wherein said biologically active agent is selected from the group consisting of a peptide, a mucopolysaccharide, a carbohydrate, a lipid, a pesticide, or any combination thereof.

8. The delivery composition as defined in claim 7, wherein said biologically-active agent is selected from the group consisting of human growth hormone, bovine growth hormone, growth hormone-releasing hormone, an interferon, interleukin-II, insulin, heparin, calcitonin, erythropoietin, atrial naturetic factor, an antigen, a monoclonal antibody, somatostatin, adrenocorticotropin, gonadotropin releasing hormone, oxytocin, vasopressin, vancomycin, desferrioxamine (DFO), or any combination of any of the foregoing.

9. A delivery composition as defined in claim 6, wherein said biologically-active agent is selected from the group consisting of an interferon, interleukin-II, insulin, heparin, calcitonin, oxytocin, vasopressin, cromolyn sodium, vancomycin, DFO, or any combination of any of the foregoing.

10. A delivery composition as defined in claim 1, wherein said diketopiperazine is derived from two .alpha.-amino acids.

11. A delivery composition as defined in claim 10, wherein said two .alpha.-amino acids from which said diketopiperazine is derived are independently selected from the group consisting of glutamic acid, aspartic acid, tyrosine, phenylalanine, and optical isomers thereof.

12. A delivery composition as defined in claim 10, wherein said two .alpha.-amino acids from which said diketopiperazine is derived are the same.

13. A delivery composition as defined in claim 10, wherein said diketopiperazine is prepared by the thermal condensation of said two .alpha.-amino acids from which said diketopiperazine is derived.

14. A delivery composition as defined in claim 1, further comprising (c) at least one enzyme inhibitor.

15. A dosage unit form comprising: (A) a delivery composition as defined in claim 1; and (B) (a) an excipient, (b) a diluent, (c) a disintegrant, (d) a lubricant, (e) a plasticizer, (f) a colorant, (g) a dosing vehicle, or (h) any combination thereof.

16. A dosage unit form as defined in claim 15, comprising an oral dosage unit form.

17. A method for preparing microspheres containing an active agent, said method comprising: (A) solubilizing, in a solvent, at least one di-C-substituted diketopiperazine according to claim 1; and (B) contacting said diketopiperazine solution with said active agent and a precipitator solution in which said diketopiperazine is insoluble.

18. A method as defined in claim 17, wherein said diketopiperazine solution has a pH within a first range and said precipitator solution has a pH within a second range, said first range being different than said second range.
« Back to Dashboard

For more information try a trial or see the database preview and plans and pricing

Serving 500+ biopharmaceutical companies globally:

Merck
Cipla
Argus Health
Accenture
Novartis
Healthtrust
Cantor Fitzgerald
Julphar
Chinese Patent Office
McKinsey

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.

Copyright 2002-2017 thinkBiotech LLC
ISSN: 2162-2639

Secure SSL Encrypted

Follow DrugPatentWatch:



Google
Twitter
Google Plus
botpot