The purpose of this column is to highlight and summarize recent key patents in the pharmaceutical arena issued by the US Patent Office in April-June, 2017.
Multilayered Dosage Form; M.K. Bhavarisetti, K. Vivek, S. Narravula and R.B. Singh; Sun Pharmaceutical Industries Ltd.; U.S. Patent # 9,622,979, April 18, 2017.
The present invention claims a novel multilayered coated tablet comprising a minimum of three layers, where the first and third layers contains one active pharmaceutical ingredient, which can be the same or different. The second layer is either a placebo or an immediate-release drug layer. This tablet further comprises a delayed-release coating which may contain one or more poreforming agents and/or have orifices on one or both sides. The orifice or pore-forming agents present in the coating lead to an initial hydration and slow-release of the drug until the time it reaches the intestine. After reaching the intestine, the delayedrelease coating and the second placebo or drug layer dissolve or erode separating the first and third drug layers. The first and third drug layers of the dosage form can be two extendedrelease layers or one immediate-release and another extendedrelease layer. The present dosage form can be formulated for two incompatible drugs into a single tablet, wherein the second layer prevents the two drugs from coming in contact with each other.
Gastric Reflux Resistant Dosage Forms N. Chidambaram; Banner Life Sciences LLC; U.S. Patent # 9,693,966; July 4, 2017.
The objective of the invention was to provide a gastric resistant capsule shell, which can encapsulate a liquid, semi-solid, or solid fill made of a gastric resistant filmforming composition comprising a gastric resistant natural polymer at relatively low concentrations. Gastric resistant film-forming compositions are comprised of a gastric resistant natural polymer, a film-forming natural polymer, and optionally a gelling agent. Suitable gastric resistant natural polymers (concentration less than about 5% by weight) include polysaccharides such as pectin and pectin-like polymers. Suitable film-forming natural polymers (concentration about 20 - 40% by weight) include gelatin and gelatin-like polymers. Suitable gelling agents (concentration less than about 2% by weight) include divalent cations such as Ca+2 and Mg+2. The composition can further comprise one or more plasticizers to facilitate the film-forming process.
Swallowable Medication Capsule; H. Zou and J. Shimizu; Medimetrics Personalized Drug Delivery; U.S. Patent # 9,687,638; June 27, 2017.
The patent is for a swallowable electronic capsule. The purpose is to release the medication from a capsule dosage form at a particular site in the gastro-intestinal tract using external activation. The capsule can mainly deliver a liquid or a gel. The capsule has a medication compartment, an actuator compartment, a displaceable surface driven by the displacement actuator, an exit hole and a vent hole. The patent did not disclose a practical example of the application of their capsule, manufacturing aspects of the capsule or the size of the capsule.
Theranostic Nanoparticle and Methods for Making and Using the Nanoparticle; M. Zhang and C. Fang; University of Washington; U.S. Patent # 9,687,569; June 27, 2017.
Theranostics is a new field of medicine which combines specific targeted therapy based on specific targeted diagnostic tests (diagnostics+therapy). This patent provides satisfactory concentration of chemotherapeutic agents inside the cancer cells. The efficacy of chemotherapy is impaired by the development of the multidrug resistance (MDR) phenotype by cancer cells. MDR is characterized by the overexpression of ATP-binding cassette (ABC) transporters which increase the efflux of chemotherapeutic drugs out of cancer cells. Nanoparticle-based therapeutics offers a new approach to circumvent MDR by improving the intracellular accumulation of chemotherapy drugs. Despite the promise of these theranostic nanoparticles, fabrication of reproducible and consistent formulations with controlled drug loading and release profiles remains a significant challenge and a major barrier to their clinical application.
Graphene Based Theranostics for Tumor Targeted Drug/Gene Delivery and Imaging; S. Mohapatra and C. Wang; University of South Florida; U.S. Patent # 9,675,714; June 13, 2017.
The present invention discloses the theranostic nanoparticles configured for simultaneous delivery of a diagnostic moiety, drug moiety, and a gene therapy moiety. The patent claims a nanoparticle comprising: a chemically reduced graphene sheet; wherein the chitosan, magnetic resonance imaging (MRI) contrast agent, chemotherapeutic agent, and a DNA plasmid are loaded onto the chemically reduced graphene sheet. Patent also claims a super paramagnetic agent and radio contrast agent as MRI contrast agent.
Self-Preserved Oil Dispersions Comprising Boric Acid; J. S. Garrigue, F. Lallemand, and B. Philips; Santen SAS;
U.S. Patent # 9,682,147; June 20, 2017. The invention summarizes an ophthalmic, sterile oil dispersion formulation containing an oil phase, an aqueous phase, at least one cationic surfactant, and boric acid or a salt of boric acid in the amount ranging from 0.005% to 0.075%. Boric acid has mild antibiotic properties against fungal or bacterial infections. Boric acid ophthalmic dosage for is used as an eye wash to cleanse or irrigate the eyes. Boric acid provides soothing relief from eye irritation, and helps to remove pollutants from the eye such as smog, chlorine, or other chemicals. It is clear that boric acid itself has pharmacological properties and also acts as a preservative for the multi-dose ophthalmic dosage form. One can add other medications such as betamethasone, latanoprost etc in this oil-dispersion system containing boric acid.
Delivery Device for Implantable Monitor; S. C. Christian; Given Imaging Ltd.; U.S. Patent # 9,675,285; June 13, 2017.
Gastroesophageal reflux disease (GERD) is a clinical condition in which the reflux of stomach acid into the esophagus is frequent enough and severe enough to impact a patient’s normal functioning or to cause damage to the esophagus. Accurate diagnosis of GERD is difficult but important. Acid reflux also leads to esophageal inflammation, which causes symptoms such as painful and difficulty swallowing. The present invention describes techniques for placing an implantable capsule used for sensing one or more parameters within a body lumen of a patient. The patent claims a delivery device that may be configured to anchor the capsule to tissue at a specific site within the body lumen during a first motion of an actuator and release the capsule from the delivery device during a second motion of the actuator. In this manner, a user may place the capsule by interacting with a single actuator.