The purpose of this column is to highlight and summarize recent key patents in the pharmaceutical arena issued by the US Patent Office in July-August 2018.
pH-Sensitive Peptides and their Nanoparticles for Drug Delivery; The Trustees of the Univ. of Pennsylvania; I-Wei, Chen, H, Choi, and R., Zhou; U.S. Patent # 10,058,622, August 28, 2018.
The present invention provides a novel molecular formulation for pH-sensitive de-novo peptides that form robust nanoparticle carriers for gene and drug delivery for tumor-treating applications. They have many advantages in drug uptake, potency, non-toxicity and low manufacturing costs. They may further set a new stage for implementing advanced molecular/gene therapy strategies. The composition comprises one or more peptide sub-blocks and each peptide sub-blocks comprises an amino acid sequence and a linker. The amino acid sequence comprises one or more histidine molecules and one or more non-polar amino acids. The amino acid sequence in each subblock contains 2-7 amino acids, 1-5 histidine molecules, and 1-5 nonpolar amino acids. The peptide is sensitive to changes in pH. The peptide may be soluble in an aqueous solution at pH below 7.0.
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Device for Coating a Stent and Associated Coating Method and Stent Produced According to the Method; Cortronik GMBH; K. Sternberg, H.K. Kroemer, K.P. Schmitz, W. Weitschies, N. Grabow, C. Harder, P. Littwin, and D. Bajer; U.S. Patent # 10,016,775; July 10, 2018.
This invention discusses a method and a device for coating implants such as stents; a temporary hollow support placed inside a blood vessel or an organ to relieve obstruction. The invention uses a holder for the stent, a spraying unit and an air-nozzle to coat stents with a suitable coating material. When a section of a blocked blood vessel is dilated with the stent and subsequently becomes constricted again this is known as in-stent restenosis. This invention may help meet the challenge of in-stent restenosis associated with most commonly used bare metal stents. Local drug delivery of an active ingredient is achieved when an active ingredient is coated on a stent. Here, the active ingredient prevents restenosis and supports the treatment of vascular diseases.
Swallowable Drug Delivery Device and Method of Delivery; Rani Therapeutics, LLC; M. Imran; U.S. Patent 10,039,908; August 7, 2018.
This patent invention provides for swallowable devices, its preparation and methods for delivering drugs and therapeutic agents within the GI tract. This is useful for the delivery of drugs, which are poorly absorbed, tolerated and/or chemically degraded in the GI tract. This device features a capsule sized to be swallowed that passes through the intestinal tract. The capsule can include a guide tube, one or more tissue penetrating members in the guide tube, a delivery member, an actuating mechanism and a release element. The release element degrades on exposure to varying conditions in the intestine to release and enable the actuating mechanism.
Use of Arsenic Compounds for Treatment of Pain and Inflammation; Panaphix, Inc.; M. Hwang and Y.J. Yang; U.S. Patent # 10,058,570; August 28, 2018.
The present patent describes the methods and compositions for treating pain and inflammation, as well as treating autoimmune and immunological disorders using arsenic compounds such as sodium meta arsenite, arsenic trioxide, and/or arsenic hexoxid or salts thereof. The patent claims the method of treating noncancer-associated inflammation in a mammal is accomplished by using a therapeutically effective amount of a composition comprising sodium meta arsenite, wherein the non-cancerassociated inflammation is associated with a condition selected from the group consisting of lupus, asthma, pulmonary disease, autoimmune disease, immunological disorders, arthritis, multiple sclerosis, Crohn’s disease, ulcerative colitis, stomach disorder, Herpes neuralgia and diabetes type I.
Lyophilized Liposomal Formulations with Two or More Encapsulated Drugs are Disclosed. These formulations display superior drug retention profiles and also maintain size distribution following lyophilization and reconstitution; Celator Pharm. Inc.; D. Cabral-Lilly, L. Mayer, P. Tardi, D. Watkins, and Y. Zeng; U.S. Patent # 10,028,912; July 24, 2018.
Liposomes are closed vesicles having at least one lipid bilayer surrounding an aqueous core, which contains the drugs. The drug delivery system is expected to be physically and chemically stable. The lyophilization process is known to stabilize many drug formulations. During lyophilization, the ice crystals can rupture the liposomes and may cause aggregation and fusion of liposomes. After reconstitution, lyophilized liposomal formulations may show accelerated drug leakage. Liposomes in a gel phase were found to be more stable during the lyophilization process. The formulation also contained cryoprotectants such as saccharides. These lyophilized liposomes provided satisfactory properties.
Composition for On-Demand Ultrasound-Triggered Drug Delivery; Columbia University, MIT, and Children’s Medical Center Corporation; U.S. Patent # 10,010,709; July 3, 2018.
This patent provides for an on-demand drug delivery triggered by ultrasound. The on-demand drug delivery systems contain a drug depot and a drug encapsulated in an encapsulating material, where the encapsulating material is diff erent from the depot. The depot contains micro-bubbles that encapsulate one or more gases. The micro-bubbles enhance the drug release when ultrasound is applied compared to the same system in the absence of microbubbles. In the above patent the drug delivery system is an injectable, multi-component system consisting of encapsulating material, preferably liposomes, drug to be delivered, microbubbles and more than two hydrogel-forming precursor components. The patient can control the time, location and dosage released by administering ultrasound following an injection or implantation.
Child Resistant Blister Package; WestRock MWV, LLC; G. O’Dwyer and S.P. Jones; U.S. Patent # 10,058,479, August 28, 2018.
The present invention provides an inexpensive and easy to manufacture child resistant packaging to items like pharmaceutical tablets and capsules dispensed in suitable packaging systems such as blister packs. It achieves increased safety to the dispensed item by using a blister pack and a tab strip sandwiched between two panels. It also includes a pull tab for safe and convenient removal of the dispensed item from blister pack. When this pull tab is pulled, it removes a tab strip from between the panels and exposes the item to be dispensed. The dispensed item is then taken out from the blister pack by applying pressure.