Pharmaceutical P.I.N. Points Patent Innovation News

The purpose of this column is to highlight and summarize recent key patents in the pharmaceutical arena issued by the US Patent Office in November-December, 2019.

Full Spectrum Anti-Dengue Antibody;

R. Sasisekharan and K. Tharakaraman; Massachusetts Institute of Technology, US; U.S. Patent # 10,519,220; December 31, 2019.

Present invention discloses methods and compositions for the treatment and prevention of Dengue Virus (DV) infection. According to the description in this patent, over 3.6 billion people worldwide are at risk of being infected with DV and more than 200 million infections of DV are estimated to occur each year globally. Unfortunately, effective therapeutic regimens are not currently available and the most effective preventive measures are mosquito control. The compositions disclosed provide antibody agents to neutralize all four types of DV. These compositions comprise of the antibody in a pharmaceutically acceptable carrier.

Hydrophobic Modified Peptides and Their Use for Liver Specific Targeting;

W. Mier, S. Urban, S. Mehrle, and U. Haberkorn; Ruprecht-Karls-Heidelberg, Heidelberg, Germany; U.S. Patent # 10,513,539; December 24, 2019.

The liver plays a major role in metabolism and has a number of functions in the body, including glycogen storage, decomposition of red blood cells, synthesis of plasma proteins, and detoxification. Targeting any drug to a specific organ should allow exclusive transfer of the drug to the site of action, minimize effects on other tissues and organs and the carrier used should be inactive in nature. Present invention provides hydrophobic modified peptides conjugated to one or more drugs to create shorter peptides, which maintains liver specificity. Drugs conjugated to hydrophobic peptides are coupled to the N-terminal amino acid sequence of the peptide. Such coupling to the N-terminal site allows better delivery of drugs across the cell membrane and also allows to direct drugs directly to the site of action. It also contributes to the stability of the drug.

Peanut Formulations and Uses Thereof;

B. Walser and H.V. Raff ; Aimmune Therapeutics Inc., Brisbane, CA; U.S. Patent # 10,512,686; December 24, 2019.

Allergy to peanuts is among the most common food allergies. Peanuts are one of the food allergens most commonly associated with anaphylaxis, a sudden and potentially deadly condition that requires immediate attention and treatment. Currently, the only treatment for peanut allergy is a peanut-free diet and ready access to self-injectable epinephrine. The burden of avoidance and constant fear of accidental exposure negatively impacts the health-related quality of life for both subjects and their families. The present patent discloses compositions for oral immunotherapy of peanut allergies and methods for the preparation of the compositions for immunotherapy, and their use in immunotherapy. Present inventors disclosed a new formulation of peanut flour comprising peanut allergens and optionally gliders, lubricants, and diluents. Patent claims that new the formulation when administered to a patient according to a treatment regimen, provides oral immunotherapy (OIT) for subjects that are allergic to peanuts. Following treatment patients are partially or fully desensitized to peanuts.

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Combination of an Oxidant, a Photosensitizer and a Wound Healing Agent for Oral Disinfection and Treatment of Oral Disease;

R. Piergallini and N. Loupis; Klox Technologies, Inc., Laval, CA; U.S. Patent # 10,471,147; November 12, 2019.

This patent is for an antibacterial periodontal composition, method of full mouth disinfection and photodynamic assisted periodontal treatment. The formulation contains at least one oxidant, at least one photo-activator capable of activating the oxidant, and at least one healing factor chosen from hyaluronic acid, glucosamine and allantoin. To treat a red, swollen, or bleeding gum or to reduce bad breath, the formulation is applied to the affected area and the formulation is exposed to actinic light having an emission wavelength of about 400 nm and 700 nm for up to 5 minutes. An internally reinforced aerogel includes an  aerogel having a support at least partially penetrating the aerogel and having the aerogel penetrating the porous structure of the support.

Lozenge Dosage Form Having a Disintegrative Tablet Portion and a Candy Glass Shell Portion;

G.P. McNally, G. Koll, and O. Anderson; Johnson & Johnson Consumer, Inc., Skillman, NJ; U.S. Patent # 10,500,155; December 10, 2019.

Rapidly disintegrating tablets and lozenges are commonly used as individual dosage forms. This patent combines these two dosage forms in which the tablet dissolves quickly and the lozenge portion dissolves slowly. The rapidly disintegrating tablet is in the form of a plug, which is placed in the cavity in the center of the lozenge. The tablet plug may have two layers with separate drugs in each layer. One can add specialized excipients such as salivation inducing agents, sweeteners, colorants, etc. One can incorporate various kinds of active pharmaceutical ingredients in this dosage form.

Internally Reinforced Aerogel and Uses Thereof;

A. Sakaguchi, G. Poe, and M. Merwin; Blueshift Materials, Inc., Spencer, MA; U.S. Patent # 10,500,557; December 10, 2019.

A gel is a sponge like, three-dimensional solid network whose pores are filled with another non-gaseous substance, such as a liquid. The liquid of the gel is not able to diff use freely from the gel structure and remains in the pores. A Xerogel is obtained when the liquid phase of a gel is removed by evaporation. It may retain its original shape, but often cracks due to the extreme shrinkage that is experienced while being dried. An aerogel is obtained when the liquid phase of a gel is replaced by a gas in such a way that its solid network is retained, with only a slight or no shrinkage in the gel. Aerogels have high porosity (about 94-98%), and high specifi c surface area, which confer a number of useful properties to aerogel. However conventional aerogels lack mechanical durability. Present patent discloses an internally reinforced aerogel that provides improved durability while maintaining other beneficial characteristics of the aerogel. An internally reinforced aerogel includes an aerogel having a support at least partially penetrating the aerogel and having the aerogel penetrating the porous structure of the support.

Formulation for Effective Tocotrienol Delivery;

C.W. Fong, Y.W. Ung, and J.T. Petkov; KL-Kepong Oleomas SDN BHD, Selangor, MY; U.S. Patent # 10,478,417; November 19, 2019.

Tocotrienols are chemicals in the vitamin E family. The vitamin E family contains four isomers of tocopherol and four isomers of tocotrienols. Previously alpha-tocopherol was considered as the most active form, but now it is believed that tocotrienols have properties that are stronger and unique. The self-emulsifying formulation contains tocotrienol in an oil carrier and two nonionic emulsifiers—sorbitan monolaurate and polysorbate 80. The formulation can be filled in hard-shell and soft-shell gelatin capsule for oral delivery. Tocotrienol isomers are absorbed in vivo upon oral ingestion, which is independent of dietary fats.

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