.

Pharmaceutical Business Intelligence

  • Anticipate P&T budget requirements
  • Evaluate market entry opportunities
  • Find generic sources and suppliers
  • Predict branded drug patent expiration

► Plans and Pricing

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

DrugPatentWatch Database Preview

Details for Patent: 9,446,001

« Back to Dashboard

Details for Patent: 9,446,001

Title:Increasing drug affinity for crystalline microparticle surfaces
Abstract: Methods are provided for promoting the adsorption of an active agent to microparticles by modifying the structural properties of the active agent in order to facilitate favorable association to the microparticle.
Inventor(s): Hokenson; Mark (Valencia, CA), Oberg; Keith A. (Valencia, CA)
Assignee: MannKind Corporation (Valencia, CA)
Filing Date:Jun 22, 2015
Application Number:14/746,656
Claims:1. A method of promoting binding of an active agent to a preformed crystalline diketopiperazine microparticle in suspension comprising the steps in the sequence set forth of: (i) modifying the chemical potential of a protein, polypeptide or peptide active agent wherein said modifying allows for an energetically favorable interaction between the active agent and the preformed crystalline diketopiperazine microparticle independent of removal of solvent; followed by (ii) allowing adsorption of the active agent onto the surface of the preformed crystalline diketopiperazine microparticle; wherein said modifying step causes said absorbing of said active agent onto a surface of said preformed crystalline diketopiperazine microparticle to provide a coating of said active agent on said preformed crystalline diketopiperazine microparticle; and wherein said preformed crystalline diketopiperazine microparticle does not comprise an active agent.

2. The method of claim 1, wherein modifying the chemical potential comprises modifying the structure, flexibility, rigidity, solubility or stability of the active agent.

3. The method of claim 2, wherein modifying the chemical potential of the active agent comprises altering solution conditions.

4. The method of claim 3, wherein said altering solution conditions comprises adding an active agent modifier to the solution and wherein said active agent modifier is selected from the group consisting of sodium chloride, hexylene-glycol (Hex-Gly), trehalose, glycine, polyethylene glycol, trimethylamine N-oxide, mannitol, proline, methanol, ethanol, trifluoroethanol, hexafluoroisopropanol, NaSCN, (CH.sub.3).sub.3N--HCl, Na.sub.2NO.sub.3, NaClO.sub.4, cesium chloride, sodium citrate, and sodium sulfate.

5. The method of claim 4, wherein said active agent modifier is sodium chloride.

6. The method of claim 1, wherein said modifying step comprises dissolving the active agent in a fluid phase of the suspension of preformed crystalline diketopiperazine microparticles and changing the pH of the fluid phase.

7. The method of claim 4, wherein the active agent modifier improves the structural stability or pharmacodynamics of the active agent.

8. The method of claim 1, wherein the active agent is selected from the group consisting of insulin, an insulin analog, ghrelin, growth hormone, and parathyroid hormone (PTH).

9. The method of claim 2, wherein modifying the chemical potential of the active agent comprises modulating one or more energetically favorable interactions with the crystalline diketopiperazine microparticle surface.

10. The method of claim 9, wherein the one or more energetically favorable interactions between the active agent and the crystalline diketopiperazine microparticle comprises an electrostatic interaction.

11. The method of claim 9, wherein the one or more energetically favorable interactions between the active agent and microparticle comprises a hydrophobic interaction.

12. The method of claim 9, wherein the one or more energetically favorable interactions between the active agent and microparticle comprises a hydrogen bonding interaction.

13. The method of claim 1, wherein the diketopiperazine is fumaryl diketopiperazine.

14. The method of claim 1, further comprising a step for removing the solvent after the allowing step.

15. The method of claim 1, wherein the active agent comprises human insulin.

16. The method of claim 1, wherein the active agent is insulin or an insulin analog and wherein the method comprises the steps of: (i) obtaining a crystalline diketopiperazine microparticle wherein the crystalline diketopiperazine microparticle comprises fumaryl diketopiperazine and does not comprise an active agent; (ii) forming a suspension comprising the crystalline diketopiperazine microparticle and an aqueous solvent; (iii) dissolving the insulin or insulin analog in the fluid phase of the suspension; (iv) changing the pH of the fluid phase from a low pH to about between 4.0 and 5.0; (v) absorbing of the insulin or insulin analog onto a surface of the diketopiperazine microparticle to provide a coating of the insulin or insulin analog on the crystalline diketopiperazine microparticle; (vi) removing or exchanging the solvent after step (v).
« Back to Dashboard

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

How are People Using DrugPatentWatch?

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.

`abc