The purpose of this column is to highlight and summarize recent key patents in the pharmaceutical arena issued by the US Patent Office in December 2023.
Eutectic Formulations of Cyclobenzaprine Hydrochloride and Amitriptyline Hydrochloride;
M. Nebuloni and P. Colombo; Tonix Pharma Holdings, Dublin, IE; U.S. Patent # 11,839,594; December 12, 2023.
The invention describes an eutectic of cyclobenzaprine HCl and mannitol or Amitriptyline HCl and mannitol. Cyclobenzaprine is a muscle relaxer used to treat muscle spasms. Amitryptyline is a tricyclic antidepressant used to treat major depressive disorder, and a variety of pain syndromes such as neuropathic pain fibromyalgia, and migraine. A eutectic system is a mixture of chemical compounds that has a single chemical composition that melts at a lower temperature than any other composition made up of the same ingredients. These two actives have slow absorption when administered orally. Also, these are unstable in basic pH. Both problems could be solved by making eutectic mixtures (75:25) with mannitol.
Combination Therapies for Treatment of BCMA-Related Cancers and Autoimmune Disorders;
S.R. Riddell, D. Green, and T. Hill; Fred Hutchinson Cancer Center, U.S.A; U.S. Patent # 11,845,803; December 19, 2023.
B lymphocytes or B cells produce antibodies, which mediate the destruction of pathogens. B cells may contain molecules on their surface such as B Cell Maturation Antigen (BCMA). BCMA binds to B cell activation factor and a proliferation-inducing ligand, which leads to NF-Kappa B activation. Uncontrolled proliferation of B cells may result in cancer, autoimmune disease, and inflammatory disease. BCMA-specific chimeric antigen receptor (CAR) modified T cells etc. can be used to treat B cell malignancies. The CAR comprises a hydrophobic portion disposed between an extracellular component and an intracellular component. The extracellular component comprises a BCMA-specific binding domain and a therapeutically effective amount of secretase inhibitor.
Compositions for Fecal Floral Transplantation and Methods for Making and Using Them and Devices for Delivering Them;
T. J. Borody; Finch Therapeutics Holding, USA; U.S. Patent # 11,850,269; December 26, 2023.
Human flora, rather than just being waste material resulting from the digestion of food, is an important virtual organ containing large numbers of living microorganisms. Bacteria make up 60% of the dry masses of the feces. Infection of the bowel flora can impact the health of the individual. The invention provides compositions, e.g., formulations or preparations, devices, used for the transplantation of a treated or isolated fecal flora, and methods for making and using them. Devices and methods of the invention can be used for any gastric, gastrointestinal, and or colonic treatment or lavage. It can also be used for the amelioration, stabilization, treatment, and/or prevention of a disease or a condition such as constipation, Crohn’s Disease, exposure to a poison or a toxin, or an infection.
Nanoparticles with pH-Triggered Drug Release;
S. Chopra, R. Karnik, A. Wang, O.C. Farokhzad, and X.Q. Zhang; The Brigham and Women’s Hospital, and Massachusetts Institute of Technology, U.S.A.; U.S. Patent # 11,833,255; December 5, 2023
Some pharmaceuticals are sensitive to conditions found in the gastrointestinal tract such as wide fluctuations in pH and enzyme activity. For example, therapeutic biologics include large protein molecules such as insulin, calcitonin, etc. Their large size, and sensitivity to the complex gastrointestinal environment with of a wide range of pH and enzyme activity, make it challenging to deliver these biologics orally. Rapid release of the payload is one way of addressing the problem of delivering sensitive drugs to the body. The present disclosure provides pH-responsive nanoparticles (NPs) and methods of making them. The invention ensured a small NP diameter and satisfactory drug loading. The drug and the NP survive the changes in pH in the complex environment of the gastrointestinal tract, and it also triggers a quick release of a majority of the drug before the NP is excreted from the body.
Lower Dosage Strength Imiquimod Formulations and Short Dosing Regimens for Treating Genital and Perianal Warts;
M.T. Nordsiek, and J. J. Gregory; Medicis Pharma, USA; U.S. Patent # 11,850,245; December 26, 2023.
This patent describes pharmaceutical formulations and methods for the topical or transdermal delivery of 1-isobutyl-1H-imidazo[4,5-c]- quinoline-4-amine or 1-(2-methylpropyl)-1H-imidazo[4,5c]quinoline-4-amine], i.e., imiquimod, to treat genital/perianal warts with shorter durations of therapy. Current FDA-approved Aldara® 5% imiquimod cream for EGWs (external genital and perianal warts/ condyloma acuminate) has limitations like unsimplified (once a day, 3 times per week) and lengthy dosing regimen (Median time = 10 weeks). If applied too thickly or generously, Aldara® 5% imiquimod cream can cause site or local skin reactions. Other symptoms, such as perianal itching or systemic effects such as fl u[1]like symptoms, may also occur. The present invention provides novel and improved imiquimod treatment regimens of short duration (for up to 8 weeks), lower dosage strength (between 1% and 4.25%), and simplified dosing regimens to treat EGWs. (1 application daily).
Use of Sublingual Dexmedetomidine for the Treatment of Agitation;
K. Nandbalan, F. Yocca, S. Sharma, H. Negi, and D. Saini; Bioxcel Therapeutics, U.S.A.; U.S. Patent # 11,839,604; December 12, 2023.
Agitation is a term that can refer to many behavioral disorders and can be associated with neurodegenerative and neuropsychiatric disorders such as dementia and schizophrenia. The treatments for agitation in patients with such conditions are still limited. The present invention provides a method of treating agitation or the signs of agitation in a subject comprising sublingual administration of an effective amount of dexmedetomidine or a pharmaceutically acceptable salt thereof without causing significant sedation.
Composition and Methods for Stimulating Clearance of Amyloid-Beta Protein;
K. Pahan, and A. Ghosh; Rush University Medical Center, U.S.A.; U.S. Patent # 11,844,767; December 19, 2023.
Astrocytes are the principal cells responsible for maintaining the brain homeostasis. Additionally, these glial cells are also involved in homo-cellular and hetero-cellular signaling and metabolism. This invention describes compositions and methods for stimulating astroglial uptake and degradation of amyloid-beta protein aggregates. They used a combination of vitamin A and an agonist of proliferator-activated receptor alpha (PPAR alpha). The inventor used gemfibrozil as the PPAR alpha. The combination can be used to treat Alzheimer’s disease or Parkinson’s’ disease.
Author Details
Neelam Sharma, MS, Lakshmi Lavanya Kundurthy, BE and Hemant N. Joshi, Ph.D., MBA* - Tara Innovations, LLC; www.tara innovations.com;*[email protected]
Publication Details
This article appeared in American Pharmaceutical Review:Vol. 27, No. 2March 2024Pages: 56-57
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