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 2021 – January 2022.
Neelam Sharma, MS, Lavanya Kundurthy, BE and Hemant N. Joshi, Ph.D., MBA*
Tara Innovations, LLC, www.tarainovations.com and www.tara-marketing.com
*[email protected]
Pharmaceutical Formulations Containing Cannabidiol and Nicotine for Treating Smokeless Tobacco Addiction; J.R. Williams; CV Sciences, Inc., US; U.S. Patent # 11,191,736; December 7, 2021.
The amount of nicotine absorption from a typical smokeless tobacco product can be four times or more than the amount absorbed from smoking a cigarette. Existing nicotine replacement therapy (NRT) products have been largely unsuccessful in the treatment of smokeless tobacco addiction. Present patent discloses the pharmaceutical formulations containing cannabidiol and nicotine for treating smokeless tobacco addiction. Patent also describes combination of cannabidiol and nicotine, in certain dosage forms provide a synergistic activity that is particularly efficacious for the treatment of smokeless tobacco addiction. Composition can be administered by transmucosal delivery, transdermal delivery or can be a tablet or capsule.
Inner Ear Plug; K.J.M. Verhoeven, D. Smyth, M. Andersson, C.G. Treaba, and F. Dadd; Cochlear Ltd., US; U.S. Patent # 11,213,430; January 4, 2022.
Hearing loss can be due to problems at two levels – Conductive (outer and middle ear) and sensori-neural (nerves from inner ear to brain). This application for a securable inner drug delivery plug includes a body with an elongate frustoconical shape and screw threads into an opening in an inner ear of the recipient, and secured within, an opening of the inner ear of a recipient. Drug delivery plug comprises a membrane, which is configured to seal the reservoir during insertion of the body into the opening and deliver drugs directly into the inner ear. The inner ear opening is sealed to prevent egress of inner ear fluid through the inner ear opening past the screw threads.
Lacrimal Drug Delivery Device; A. Schieber, L. Thai, and M. Kahook; The Regents of the University of Colorado, US; U.S. Patent # 11,207, 211; December 28, 2021.
A lacrimal drug delivery device includes a reservoir configured to hold a drug. The reservoir moveable between a relaxed state and an expanded state. A connector fluidly coupled to the reservoir, the connector configured such that drug flows from the reservoir to a delivery site through the first lumen and a delivery guide is removably received within the second lumen during use. A hydrogel within the relaxed state configured to absorb drug from the reservoir and to control the rate of flow of drug to the delivery guide during the use. A delivery guide within the second lumen and configured to transfer the reservoir between the relaxed state to the expanded state, the delivery guide detachably coupled to the reservoir to position the reservoir in a lacrimal sac of a patient.
Polypeptide Eye Absorption Enhancer and Use Thereof; G. Wei, K. Jiang, W. Lu, C. Liu, L. Tai, and X. Gao; Fudan University, China; U.S. Patent # 11,213,591; January 4, 2022.
Various intra-ocular and fundus drug delivery methods are available to clinically treat ocular diseases. Out of all, eye drops are the most ideal ophthalmic dosage forms. Introducing absorption enhancers into the formulation of eye drops improve the efficiency of intraocular drug delivery. Small molecule absorption enhancers are irritating to the eye and also not easily metabolized, making them unsuitable for ocular applications. A naturally occurring polypeptide - penetratin is known. Penetratin derivatives have a strong ability to penetrate ocular tissues, and do not cause ocular cytotoxicity. The purpose of the present invention is to overcome the shortcomings of the existing absorption enhancer for ocular application. The patent also provides a class of artificially modified CPPs (Cell Penetrating peptides), which are used as an ocular absorption enhancer. Structurally modified penetratin derivatives could be administered by eye drops through a non-traumatic route to deliver covalently or non-covalently linked drugs into the eye.
Antiviral Supplement Formulations; K.E. Phillips and C.A. Winning; Vymedic LLC, US; U.S. Patent # 11,224,606; January 18, 2022.
The patent provides an oral antiviral supplement composition comprising lysine, an ascorbic compound, a flavonoid glycoside, threonine, and pyridoxine. It is mainly useful to treat cells infected with influenza virus. In the United States, there are two classes of drugs approved by the FDA for treating or preventing influenza virus infection: the M2-ion channel blockers and the neuraminidase inhibitors (NAIs). Cases developing cross-resistance have been reported. Not every patient gets access to anti-viral treatments for several reasons. To examine the activity of the proposed agents, the inventors conducted several in vitro assays such as – Influenza A mRNA activity, Amplex Red Neuroaminidase assay, Metaloproteinase 9 (MMP 9) inhibition, and MMP 2 inhibition. A small clinical study (14 patients) was also conducted during Influenza outbreak.
Extended-Release Compositions Comprising Pyridostigmine; S.R.K. Vaka, N.B. Shelke, D. Desai, W. Phupradit, and N.H. Shah; Kashiv Biosciences LLC, US; U.S. Patent # 11,229,606; January 25, 2022.
Pyridostigmine is a medication used to treat myasthenia gravis and underactive bladder. It is important to minimize initial burst/release and maintain stable plasma concentration. The patent describes matrix tablets, gastro-retentive tablets and pellets with extended release of drug. A gastro-retentive dosage form comprising an immediate release portion and an extended-release portion. The extended-release portion comprises a core, and a permeable elastic membrane comprising at least one orifice. The dosage form also contains an acid, a gas-generating agent, and a swellable water-soluble hydrophilic elastic polymer. The composition provides an extended release of pyridostigmine for at least about 14 hours. The composition releases less than about 35% of drug within two hours of dissolution of the composition in 900 ml of dissolution medium comprising pH 5 buffer and 150 mM NaCl, measuring using USP Apparatus I, at 100 rpm and 37°C.
Silica Nanoparticle with An Insoluble Drug; P. Tiet and J. Berlin; City of Hope, CA, US; U.S. Patent # 11,191,745; December 7, 2021.
Many drugs have very poor aqueous solubility. Nano-suspensions of such drugs in a pure crystalline form do not require toxic, harmful excipients. However, many of these suspensions result in fusion and aggregation of nanocrystals over time. This problem was solved using the following procedure - (a) mixing an insoluble drug and an amphiphilic polymer in an organic solvent; (b) removing the organic solvent, adding a solvent (e.g., water or aqueous solution), and sonicating the mixture to form nano-crystals; and (c) mixing tetraethyl orthosilicate (TEOS, colorless liquid that degrades in water producing silicone dioxide), phenyltrimethoxysilane (PTMS), and hydrolyzed aminopropyltriethoxy silane (APTES) with the nano-crystal to form a nanoparticle. Thus, these nano-particles include the insoluble drug, a polymer and silica.
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