|
|
Post by mango on Jun 1, 2021 16:48:17 GMT -5
Number 1 seems handy dandy. Good timing. The present invention to provide improved methods for coating crystalline particles such as fumaryl diketopiperazine (FDKP) microparticles with active agents, such as proteins, using electrostatically, hydrophobically, or hydrogen-bond driven associations. In the present invention, liquid can optionally be removed (for recovery of active agent coated microparticles) by filtration or drying, or replaced by exchanging for a different solution medium. In any case, removal of the liquid medium is not an obligatory step in formation of the active agent-microparticle complex. This invention discloses a method for microparticle coating based on changing the surface properties of the crystalline microparticles to achieve adsorption of active agent to the microparticle.In particular embodiments of the present invention, there is provided a method of coating a preformed crystalline microparticle in suspension with an active agent comprising; i) adjusting the energetic interaction between the active agent and the crystalline microparticle independent of solvent removal; and ii) allowing time for the active agent to adsorb onto the surface of the microparticle. In some embodiments, the method of coating a preformed crystalline microparticle in suspension with an active agent can further comprise a step of removing or exchanging the solvent without substantial effect on the interaction between active agent and microparticle. In other particular embodiments of the present invention, the method of coating the microparticle with active agent is accomplished by modifying the surface properties of the microparticle. Modification of the surface properties of the microparticle is achieved by altering solution conditions. These conditions, in a non-limiting manner, comprise changing the pH. In other embodiments of the invention, the surface properties of the microparticle are modified by: 1) altering the polarity of the solution; 2) the addition of monovalent or multivalent ions; and 3) chemical derivatization of the microparticle. In yet another embodiment, the present invention further comprises a step of dissolving the active agent in the fluid phase of the suspension of microparticles and subsequently changing the pH. In the claims of same patent: 10. The composition of claim 1, wherein the active agent is selected from the group consisting of insulin or an analog thereof, growth hormone, parathyroid hormone (PTH), ghrelin, granulocyte macrophage colony stimulating factor (GM-CSF), glucagon-like peptide 1 (GLP-1), antibodies and fragments thereof, and cyclosporins. 18. The pharmaceutical composition of claim 12, wherein the active agent is selected from the group consisting of vasoactive agents, neuroactive agents, hormones, anticoagulants, immunomodulating agents, cytotoxic agents, antibiotics, antiviral agents, antigens, antibodies, insulin and analogs thereof, growth hormone, parathyroid hormone (PTH), ghrelin, granulocyte macrophage colony stimulating factor (GM-CSF), glucagon-like peptide 1 (GLP-1), cyclosporins, clopiogrel and PPACK (D-phenylalanyl-L-prolyl-L-arginine chloromethyl ketone), antibodies and fragments thereof, humanized or chimeric antibodies; F(ab), F(ab)2, or single-chain antibody alone or fused to other polypeptides; therapeutic or diagnostic monoclonal antibodies to cancer antigens, cytokines, infectious agents, inflammatory mediators, hormones, and cell surface antigens, anti-SSX-241-49 (synovial sarcoma, X breakpoint 2), anti-NY-ESO-1 (esophageal tumor associated antigen), anti-PRAME (preferentially expressed antigen of melanoma), anti-PSMA (prostate-specific membrane antigen), anti-Melan-A (melanoma tumor associated antigen), anti-tyrosinase (melanoma tumor associated antigen), and anti-MOPC-21 (myeloma plasma-cell protein). 19. The pharmaceutical composition of claim 12, wherein the active agent is a vasoactive agent or a neuroactive agent. |
|
|
|
Post by peppy on Jun 1, 2021 17:27:39 GMT -5
Number 1 seems handy dandy. Good timing. The present invention to provide improved methods for coating crystalline particles such as fumaryl diketopiperazine (FDKP) microparticles with active agents, such as proteins, using electrostatically, hydrophobically, or hydrogen-bond driven associations. In the present invention, liquid can optionally be removed (for recovery of active agent coated microparticles) by filtration or drying, or replaced by exchanging for a different solution medium. In any case, removal of the liquid medium is not an obligatory step in formation of the active agent-microparticle complex. This invention discloses a method for microparticle coating based on changing the surface properties of the crystalline microparticles to achieve adsorption of active agent to the microparticle.In particular embodiments of the present invention, there is provided a method of coating a preformed crystalline microparticle in suspension with an active agent comprising; i) adjusting the energetic interaction between the active agent and the crystalline microparticle independent of solvent removal; and ii) allowing time for the active agent to adsorb onto the surface of the microparticle. In some embodiments, the method of coating a preformed crystalline microparticle in suspension with an active agent can further comprise a step of removing or exchanging the solvent without substantial effect on the interaction between active agent and microparticle. In other particular embodiments of the present invention, the method of coating the microparticle with active agent is accomplished by modifying the surface properties of the microparticle. Modification of the surface properties of the microparticle is achieved by altering solution conditions. These conditions, in a non-limiting manner, comprise changing the pH. In other embodiments of the invention, the surface properties of the microparticle are modified by: 1) altering the polarity of the solution; 2) the addition of monovalent or multivalent ions; and 3) chemical derivatization of the microparticle. In yet another embodiment, the present invention further comprises a step of dissolving the active agent in the fluid phase of the suspension of microparticles and subsequently changing the pH. In the claims of same patent: 10. The composition of claim 1, wherein the active agent is selected from the group consisting of insulin or an analog thereof, growth hormone, parathyroid hormone (PTH), ghrelin, granulocyte macrophage colony stimulating factor (GM-CSF), glucagon-like peptide 1 (GLP-1), antibodies and fragments thereof, and cyclosporins. 18. The pharmaceutical composition of claim 12, wherein the active agent is selected from the group consisting of vasoactive agents, neuroactive agents, hormones, anticoagulants, immunomodulating agents, cytotoxic agents, antibiotics, antiviral agents, antigens, antibodies, insulin and analogs thereof, growth hormone, parathyroid hormone (PTH), ghrelin, granulocyte macrophage colony stimulating factor (GM-CSF), glucagon-like peptide 1 (GLP-1), cyclosporins, clopiogrel and PPACK (D-phenylalanyl-L-prolyl-L-arginine chloromethyl ketone), antibodies and fragments thereof, humanized or chimeric antibodies; F(ab), F(ab)2, or single-chain antibody alone or fused to other polypeptides; therapeutic or diagnostic monoclonal antibodies to cancer antigens, cytokines, infectious agents, inflammatory mediators, hormones, and cell surface antigens, anti-SSX-241-49 (synovial sarcoma, X breakpoint 2), anti-NY-ESO-1 (esophageal tumor associated antigen), anti-PRAME (preferentially expressed antigen of melanoma), anti-PSMA (prostate-specific membrane antigen), anti-Melan-A (melanoma tumor associated antigen), anti-tyrosinase (melanoma tumor associated antigen), and anti-MOPC-21 (myeloma plasma-cell protein). 19. The pharmaceutical composition of claim 12, wherein the active agent is a vasoactive agent or a neuroactive agent. Mango, help me out here, why couldn't MNKD put vaccines on technosphere? What did MNKD sell? Anyway, the monoclonals, that is the ticket. |
|
|
|
Post by mango on Jul 7, 2021 5:48:26 GMT -5
|
|
|
|
Post by prcgorman2 on Jul 7, 2021 6:24:54 GMT -5
Not sure how long international patents take to get awarded, but USPO awards can often take 2 to 3 years or even more. Also, I’ve seen where new patents are issued associated with older inventions but which cover newer claims. Just observing that we’re seeing the results of work of Mannkind inventors from a few years ago and that Mannkind inventors are both creative and ensuring their work is protected with US and international Intellectual Property Rights (IPR). Smart, but not necessarily cheap. The cost of filing patents is not inconsiderable, and international IPR can require additional filing costs over time to keep the patent current (I think).
The fact that MNKD is filing those patents is some indication of their faith in commercial viability. Insulin for DM. Treprostinil for PAH and PAH-ILD. Clofizamine for DR-TB. CBD for health and recreation. Another compound for migraines. I look at the pipeline as the foundation on which the house of Afrezza will eventually be built. Thanks to Sanofi, it’s crawl, walk, run. Thanks to current MNKD management and the BOD, we’re still here to keep moving.
|
|
|
|
Post by parrerob on Aug 27, 2021 6:09:15 GMT -5
|
|
|
|
Post by mango on Aug 30, 2021 11:54:36 GMT -5
|
|
|
|
Post by bones1026 on Aug 30, 2021 20:51:47 GMT -5
Little surprising to see David Kendall’s name on that one.. |
|
|
|
Post by mannmade on Aug 31, 2021 16:04:37 GMT -5
Little surprising to see David Kendall’s name on that one.. Not if you consider that obesity is the main driver for adult onset and type 2 diabetes later in life and also with peds. |
|
|
|
Post by mango on Sept 8, 2021 16:42:58 GMT -5
I’ve missed some patents recently but here are 3 very recent patents published. Things are looking very good, folks. FDA approval of Tyvaso DPI next month BTW. 1. Method of drug formulation based on increasing the affinity of active agents for crystalline microparticle surfacespatents.justia.com/patent/111034592. Reactor for producing pharmaceutical particles in a precipitation processpatents.justia.com/patent/111038473. Composition and method for reducing hypoglycemia events in diabetes treatmentpatents.justia.com/patent/11110151 |
|
|
|
Post by sayhey24 on Sept 8, 2021 16:57:48 GMT -5
Patenting afrezza for reducing hypoglycemic events by using it in place of RAAs is a new twist I had not thought of. If they get the patent maybe it could help with their argument to get changes to the SoC but I am not holding my breath. Having a patent pending technique to reduce hypo's is a good marketing ploy.
|
|
|
|
Post by prcgorman2 on Sept 9, 2021 7:00:22 GMT -5
Patenting afrezza for reducing hypoglycemic events by using it in place of RAAs is a new twist I had not thought of. If they get the patent maybe it could help with their argument to get changes to the SoC but I am not holding my breath. Having a patent pending technique to reduce hypo's is a good marketing ploy. It 100% underscores the “NARRATIVE” that Afrezza’s SAFETY is quite literally second to none. I’m convinced safety is the single most important point to marketing Afrezza. Kudos to the tireless Mannkind inventors and their efforts to protect valuable intellectual property with patents. |
|
|
|
Post by mango on Sept 9, 2021 9:27:09 GMT -5
Patenting afrezza for reducing hypoglycemic events by using it in place of RAAs is a new twist I had not thought of. If they get the patent maybe it could help with their argument to get changes to the SoC but I am not holding my breath. Having a patent pending technique to reduce hypo's is a good marketing ploy. It 100% underscores the “NARRATIVE” that Afrezza’s SAFETY is quite literally second to none. I’m convinced safety is the single most important point to marketing Afrezza. Kudos to the tireless Mannkind inventors and their efforts to protect valuable intellectual property with patents. Afrezza has proven to be the safest insulin ever. Let’s hope big diabetes influencers like Ginger Vieira, who has recently become a convert, highlights Afrezza’s remarkable safety profile. In essence, Afrezza’s remarkable safety characteristics is simply a consequence of the extraordinary PK/PD profiles, revolutionary dry powder formulation, and expertly designed inhaler. Without those three critical components, Afrezza would not have level of life-changing safety it does. |
|
|
|
Post by longliner on Sept 9, 2021 9:29:49 GMT -5
It 100% underscores the “NARRATIVE” that Afrezza’s SAFETY is quite literally second to none. I’m convinced safety is the single most important point to marketing Afrezza. Kudos to the tireless Mannkind inventors and their efforts to protect valuable intellectual property with patents. Let’s hope big diabetes influencers like Ginger Vieira, who has recently become a convert, highlights Afrezza’s remarkable safety profile. In essence, Afrezza’s remarkable safety characteristics is simply a consequence of the extraordinary PK/PD profiles, revolutionary dry powder formulation, and expertly designed inhaler. Without those three critical components, Afrezza would not have level of life-changing safety it does. The conversation needs to pivot from it's not safe, (ie. black box), to accurately describe it as the safest insulin ever. |
|
|
|
Post by mango on Nov 30, 2021 13:02:04 GMT -5
|
|
|
|
Post by mango on Nov 30, 2021 13:32:00 GMT -5
|
|
