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, 2019.
Formulations and Methods for Vaginal Delivery of Antiprogestins;
J.S. Podolski and H. Kuang; Repros Therapeutics, Inc.; U.S. Patent #10,328,022; June 25, 2019.
Vaginal drug delivery refers to the delivery of drugs within or through the vaginal mucosa for local or systemic pharmacological action. The vaginal route offers many advantages due to its large permeation area, rich vascularization, avoidance of first pass effect and relatively low enzymatic activity. The present invention provides methods for the treatment of a variety of progesterone related conditions. Methods involve vaginal administration of a mucoadhesive capsule comprising pullulan; and active agents like antiprogestin along with one or more excipients. The patent claims that pullulan capsules provide a continuous release of the active agent. They are safe and effective.
Treatment Using Dantrolene;
D. Anderson, B.G. Cameransi, Jr., and V.M. Conklin; Lyotropic Therapeutics, Inc.; U.S. Patent #10,314,822; June 11, 2019.
Dantrolene is widely used as a muscle relaxant and for the treatment of malignant hyperthermia. Currently, marketed dantrolene formulations require excessive time and effort for reconstitution, which sometimes results in inaccurate dosing. The present invention discloses a new formulation of dantrolene and dantrolene salts that are safe for injection and requires only small liquid volume for administration. In an independent claim, the formulation is a stable colloidal suspension, containing a salt of dantrolene, PVP and water. In another independent claim, the lyophilized formulation is reconstituted to produce a colloidal suspension with average particle size of less than two microns.
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Composition for Inducing Proliferation or Accumulation of Regulatory T Cells;
K. Honda, K. Atarashi, K. Itoh, and T. Tanoue; Th e University of Tokyo, JP; U.S. Patent # 10,322,150; June 18, 2019.
Commensal means living in a relationship in which one organism derives food or other benefits from another organism without hurting or helping it. Commensal bacteria are part of the normal flora in the gastrointestinal tract. This invention uses two live commensal bacterial strains belonging to Clostridium clusters IV and/or XIVa, wherein the bacterial mixture induces proliferation and/or accumulation of regulatory T cells. These bacteria are in the form of spores and administered as a capsule. Individual commensal bacteria control differentiation of their specific immune cells in the mucosal immune system. For example, Bacteroides fragilis, which is a commensal bacterium in humans, specifically induces a systemic Th1 cell response and a mucosal IL-10-producing T cell response in mice and plays a role in protecting the host from colitis, which would otherwise be caused by a pathogen.
Drug Delivery Implant and a Method Using the Same;
G.A. Peyman; Sun City, AZ; U.S. Patent # 10,278,920; May 7, 2019.
This patent describes a method of drug delivery implant that is inserted into a cross-linked pocket formed in the cornea of the eye of the patient for the treatment of corneal scarring, which is the major cause of blindness. The process comprises of forming a pocket in the cornea of the eye to gain access to tissue and photo-sensitizing the inside of the pocket to facilitate cross-linking of the tissue. The method also describes irradiating the cornea to activate cross-linkers in the portion of the tissue surrounding the pocket and finally inserting a corneal drug delivery implant into the pocket, which is configured to release the medications into the eye of the patient.
Formulations of Water-Soluble Derivatives of Vitamin E and Soft Gel Compositions, Concentrates and Powders Containing Same;
P.J. Bromley; Virun, Inc.; U.S. Patent #10,285,971; May 14, 2019.
Non-polar ingredients such as vitamins and minerals are used in compositions for human ingestion in pharmaceuticals, nutraceuticals and dietary supplements. The major challenge is that they do not easily dissolve in aqueous solutions. This patent provides compositions that contain water soluble vitamin E derivative mixtures (compositions), such as tocopheryl polyethylene glycol succinate (TPGS), TPGS analogs, TPGS homologs and TPGS derivatives. The watersoluble vitamin E mixtures contain mixtures of dimers and monomers of the vitamin E derivative. It also provides methods for preparing products containing the water-soluble vitamin E derivative mixtures, including soft gel compositions, pre-gel concentrates, capsules and soft gel compositions that contain the pre-gel concentrates, and powders.
Pharmaceutical Suspensions Containing Drug Particles, Devices for Their Administration, and Methods of Their Use;
A. Heller; SynAgile Corporation; U.S. Patent # 10,300,033; May 28, 2019.
Pharmaceutical formulations containing drugs, which have a short physiological half-life and/or a narrow therapeutic window, possess several problems. This includes inconvenience in taking the drug multiple times during day and night. If the duration between subsequent dosing is not constant, it may result in a sub-optimal effect of the drug or increased side effects. The present invention aims to solve this problem. It discloses the composition of a pharmaceutical formulation in a delivery device, which continuously administers formulation for oral absorption. The pharmaceutical formulation disclosed in the invention contains drug particles, solid excipients, surfactant and water. The delivery device can be implanted in the oral cavity and it releases drug formulation continuously. Drug release can be stopped temporarily when the device is removed from mouth.
Hippocampal Drug Delivery Devices and Methods;
E. Leuthardt and P.J. Anand; Alcyone Lifescience, Inc.; U.S. Patent #10,300,251; May 28, 2019.
One of the major challenges of targeted drug delivery is to deliver drug into non-accessible locations in a minimally invasive manner. The present invention discloses methods and devices that deliver drug to certain non-accessible areas of the brain. It uses a device with a ventricular catheter from which the drug can diff use and flow into the hippocampus of the brain. The drug delivery method includes inserting a drug delivery device into the temporal horn, a part of the brain, of a patient. The delivery device can be configured to block a selective portion of the brain, which limits the flow of cerebrospinal fluid (CSF). This obstruction of CSF flow saturates the drug at the hippocampus and provides maximum effect without being diluted or carried away by CSF.