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 July- August 2019.

Bacterially-Derived, Intact Minicells that Encompass Plasmid-Free Functional Nucleic Acid for in vivo Delivery to Mammalian Cells; H. Brahmbhatt, J. MacDiarmid and T. Hulf; EnGeneIC Molecular Delivery; U.S. Patent # 10,383,827; August 20, 2019.

Present invention discloses an effi cacious methodology for delivering functional nucleic acids, such as regulatory RNAs, to target cells. Inventors of bacterially-derived, intact minicells disclose a composition of plasmid free-nucleic acid in a minicell and a carrier. Examples of these functional nucleic acids include single, double or multi-stranded DNAs and RNAs. The functional nucleic acid packaged in a minicell may target the transcription of a protein responsible for drug resistance, to apoptosis resistance in a cancer tumor, or even growth of a cancer tumor. This phenomenon is also claimed to be used in delivery of drugs to mammalian cells.

Cyclodextrin and Antibody-Drug Conjugate Formulations; H. Li, S. Jiang, M. Wallace, and D. Meyer; Seattle Genetics, Inc., U.S. Patent 10,391,181; August 27, 2019.

The present invention addresses an effective means of delivering an Antibody-Drug Conjugate (ADC) to a targeted site in a tissue or organism. Delivering drugs to a target such as a tumor by the antibody minimizes exposure of non-target tissues to toxic drugs and limits adverse effects associated with the toxicity of the same. The invention also addresses the need of removal of high potency drug related impurities, such as benzodiazepines, from an ADC prior to administration to the human body. The disclosed method for removing benzodiazepine drug-related impurities is by tangential flow filtration with cyclodextrin. Cyclodextrin in the purification process is added in sufficient amounts to maintain the solubility of the components in the ADC mixture and prevent aggregation.

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Syringe Systems and Methods for Multi-Stage Fluid Delivery; M. Hopkins; True Concepts Medical Technologies, U.S. Patent #10,369,285; August 6, 2019.

Present patent discloses syringe systems and methods for multi-stage fluid delivery. Adenosine and numerous other medications are given as rapid bolus with saline flush immediately after the drug injection. Adenosine has an extremely short plasma half-life, due to its rapid transport into tissues. Current system to administer adenosine utilize a stopcock. A stopcock is attached to a capped I.V. line where adenosine is hooked up to one port and a saline flush is hooked up to the other. After the adenosine is pushed, the swivel is switched, and the saline flush quickly follows. Such systems have their own limitations. Present patent discloses multi-stage fluid delivery. This syringe-based delivery device has a distal reservoir for a medicament and a proximal reservoir for a flush fluid. First the drug solution in the distal reservoir is injected. With further pressure, saline in the proximal reservoir gets injected through a port in the center.

Prodrugs Activated by Caspase; S.Y. Kim, Y. Byun, and S.W. Chung; Pharosgen Co. Ltd. South Korea; U.S. Patent # 10,357,572; July 23, 2019.

A prodrug is a biologically inactive compound, which can be metabolized in the body to produce a drug. Present patent describes prodrug conjugates capable of releasing a drug upon activation by caspase, related methods of inducing apoptosis, amplifying apoptosis, and treating cancer. Caspases are a family of protease enzymes playing essential roles in programmed cell death (including apoptosis, pyroptosis and necroptosis) and inflammation. Prodrug conjugates comprises of (i) a functional moiety, (ii) a caspase-cleavable peptide linker, and (iii) a chemotherapeutic agent. Functional moiety helps in localizing and binding to target cell and chemotherapeutic agent induces apoptosis of tumor cell.

Fecal Oxygenation; R. M. Dayton; U.S. Patent # 10,342,828; July 9, 2019.

Clostridium difficile is a Gram-positive, spore-forming bacterium infecting the colon of patients following antibiotic treatment. Microbiomes in the gut usually prevent C. difficile colonization. Antibiotic treatment alter microbiomes and allows growth of C. difficile. C. difficile does not survive in the presence of oxygen. Oxygen can be introduced to the infected C. difficile region, such as in the large intestine and colon, optionally using a catheter type arrangement where oxygen is pumped. The claimed device in this patent contains multiple oxygen packets with at least 40% oxygen. The outer coating protects the oxygen packets from the materials in the patient’s digestive tract. The oxygen is released at a desired time based on the properties of outer coating and in a desired region in the GI tract where there is a C. difficile infection.

Use of Lactulose in the Treatment of Autism; J.M. Fallon and R. Feltenstein; Curemark LLC; U.S. Patent # 10,350,229; July 16, 2019.

Lactulose is a synthetic sugar used to treat constipation. Its degradation pull water into colon. It also reduces the amount of ammonia in the blood of patients with liver disease. It is available as a solution – 10 g/15 mL. Certain drugs such as augmentin (amoxicillin + clavulanate potassium) have been known to leave an ammonia residue in the gastrointestinal tract. The increased levels of ear infections in children with autism and the use of Augmentin to treat these and other infections makes the child vulnerable to the potential buildup of ammonia in the digestive system as well as the blood, thus leading to a potential neurotoxic state. By giving lactulose immediately following the administration of Augmentin or other ammonia producing substances, the potential for a neurotoxic disease is reduced. In one embodiment of the present invention, the treatment has a formulation of 0.4 g/kg lactulose and 0.1 g/kg mannitol. In another embodiment, the treatment has a formulation of 0.3 g/kg lactulose. In either embodiment, the treatment is administered two to five times per day.

Dosage Forms with Desired Release Profiles and Methods of Designing and Making Thereof; F. Deng, X. Li, and S. Cheng; Tirastek, Inc., China; U.S. Patent # 10,350,822; July 16, 2019.

Efficacy and toxicity of a drug or a combination of drugs both in timing and location require complex administration schemes and resulting release profiles. This can be achieved by computer-generated 3-D dosage forms. Multi-layered structures with a plurality of layers containing drug(s), erodible materials, insulating materials with various mass fractions were utilized. Materials used in the formulations were chosen based on their desired properties. The desired drug release profile was divided into a plurality of time intervals, each time interval corresponded to a layer in a multi-layered structure. This methodology was essentially applicable to oral drug dosage forms.

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