The purpose of this column is to highlight and summarize recent key patents in the pharmaceutical arena issued by the US Patent Office in September-October 2019.
Ionic Liquids for Transdermal Drug Delivery; M. Zakrewsky, S. Mitragotri, D.T. Fox, A. Koppisch, R. Del Sesto and K. Lovejoy; University of California, Triad National Security and Northern Arizona University; U.S. Patent # 10,449,254; October 22, 2019.
Skin is a great barrier for entry of chemicals and microbes which protects our body. In transdermal drug delivery systems, penetration enhancers are often used which many times cause skin irritation. The current invention provides a composition improving transport of therapeutic, prophylactic and diagnostic agents. A eutectic solvent, which is a mixture of a cationic and anionic component, is used in this drug delivery system. Based on the composition of ionic liquid, the transport across skin is increased or the drug is delivered in the skin layer for a local action. These ionic liquids were also shown to cross biofilms and are effective against pseudomonas and salmonella. In one of the embodiments, the anionic component is geranate and the cationic component is a choline cation.
Implantable Solid Dosage Form; D.F.H. Chowdhury; NDM Technologies Ltd; U.S. Patent # 10,434,060; October 8, 2019.
Present invention relates to the transdermal delivery of drugs to a patient. It discloses a method of manufacturing and delivering a solid dosage form, transdermally to a human or animal. Syringes and needles have been widely used to deliver drugs but it requires skilled personnel to deliver the drug and the syringe stay inserted in the skin as long as needed to deliver the drug. Present invention describes a carrier with a hollow core through which the carrier pierces the skin and delivers drug. The solid dose is manufactured by wet casting, direct compression molding or extrusion techniques. To deliver active drugs, the carrier and solid dose is pressed and then pushed into the skin to a desired depth. The carrier is then lifted to leave the solid dose in the skin.
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Method of Determining Consumption of Decayed Drug Through Drug Taggants; D.R. Hall, D. Allen, C. Rosenbrock, D. Hendricks, A. Nguyen, S.J.M. Butala, T. Niederhauser, T. Pearman, and J. Fox; U.S. Patent # 10, 408,849; September 10, 2019
Radio-Frequency identification (RFID) uses electromagnetic fields to automatically identify and track tags attached to objects. A taggant is a radio frequency microchip used in automated identification and data capture. A taggant is also a chemical or physical marker added to materials to allow various forms of testing. Drugs lose their efficacy due to light, temperature, oxygen and age. This patent describes a method of tagging a drug composition to detect decay of an active ingredient in the drug composition. The first taggant is photosensitive. The second taggant is heat sensitive and resistant to light. The taggants may be detected in biological samples, including urine and feces. Taggants may be sprayed on pills, included as a powder or liquid ingredient in a pill or capsule or dispersed or dissolved in a liquid medication.
Drug Delivery Systems and Methods for Treatment of Prostate; D. Giesing; Taris Biomedical LLC; U.S. Patent #10,406,335; September 10, 2019.
In the present invention, the drug used in the treatment of prostate cancer is delivered locally into the bladder of a patient. This provides sufficient concentration of drug in urine in the bladder, which then goes to prostate glands. It also describes the use of an intravesicle drug delivery device, which can be inserted directly to the bladder and it produces an extended release of drug. This extended release may last from hours to days. The drug used to treat prostate cancer herein is gemcitabine. The device can be configured to continuously deliver gemcitabine from 1 mg/day to 300 mg/day up to 14 days. Traditional therapies of prostate cancer require drug administration by intravenous, intramuscular, oral, transdermal or intranasal route. If drug is delivered locally, its exposure to nearby tissues and unwanted harmful effects of the drug can be avoided or reduced.
Microneedles Made from Polycarbonate-Polycarbonate/Polysiloxane Copolymer Compositions; M.D. Martinez Canovas, M.A.J. Van Der Mee, R.D. Van De Grampel, and J. De Brouwer; Sabic Global Technologies, NL; U.S. Patent # 10,449,344; October 22, 2019.
Microneedles are attractive for delivery as they typically only penetrate the outermost layer of skin and do not reach nerves. There are significant challenges in mass producing microneedles at lower cost and in a short time. The microneedles must release smoothly from molds and yet must have high strength to prevent breaking during usage. A microneedle comprises a shaft having a proximal end, a distal end and a capillary space within said shaft. The microneedle composition contains optionally polycarbonate, polycarbonate-polysiloxane copolymer, and mold release agent. The mold release agent comprises one or more of pentaerythritol stearate, glycerol monostearate, a wax, polyethylene or a poly alpha olefi n. Polycarbonate is flexible in molding conditions, easily formable and has acceptable mechanical properties for the application in microneedles.
Vaccines Comprising Cholesterol and CpG as Sole Adjuvant-Carrier Molecules; H.L. Davis, R. Weeratna, and P.J. Dominowski; Zoetis, Belgium; U.S. Patent # 10,456,463; October 29, 2019.
Vaccines typically comprise an antigen (the target for the immune response) and an adjuvant (coadministered compound meant to promote the immune response to the antigen). The adjuvant is the part of the reconstituted formulation that is administered. Compounds that are given separately and/or at a different time point are called immunomodulators like CpG. Immunomodulators pre condition the immune system. The CpG sites or CG sites are regions of DNA where a cytosine nucleotide is followed by a guanine nucleotide in the linear sequence of bases along its 5’ 3’ direction. In mammals, 70% to 80% of CpG cytosines are methylated. Unmethylated cytosine–guanine dinucleotide (CpG) motifs are potent stimulators of the host immune response. The present patent describes vaccines comprising one or more antigens and cholesterol, and vaccines comprising one or more antigens, one or more immune modulatory molecules and cholesterol. It has been discovered that cholesterol can potentiate the activity of immune modulatory molecules and therefore the combination of cholesterol and immune modulatory molecules can be used in the treatment and/or prevention of human and animal disorders.
Dry Powder Vancomycin Compositions and Associated Methods; J. Lord, J.T. Jouhikainen, H.E. Snyder, P. Soni, and M.C. Kuo; Savara, Inc.; U.S. Patent # 10,420,722; September 24, 2019.
Vancomycin is a glycopeptide antibiotic. It is bactericidal. It acts by inhibiting proper cell wall synthesis in Gram-positive bacteria. The present patent discloses dry powder Vancomycin compositions. The composition comprises vancomycin or a pharmaceutically acceptable salt (~75% to 95%) and leucine (5% to 20%), wherein the composition is a dry powder. It may also contain less than 10% of a bulking agent. It discloses methods for administering such compositions to subject’s lungs. Vancomycin can be used for inhalation via a nebulizer to treat infections of the lower and upper respiratory tract, and in cystic fibrosis patients. Currently, there are no known commercially available dry powder inhalable forms of vancomycin. Dry powder inhalers are easier to use and cause fewer irritant effects.