Pharmaceutical P.I.N. Points Patent Innovation News

Easily Dosable Solid Preparation; Mochida Pharmaceutical Co. Ltd.; Y. Kudou, K. Warabino, and H. Ito; US patent # 9,789,068; October 17, 2017.

When high-dose solid preparations are prepared as a single unit tablet, they are large in size and if prepared as a powder or a granule, they becomes bulky due to low density, making it difficult for children and aged people to swallow. The present invention provides a method to develop an easily producible coated preparation having the effect of masking an unpleasant taste, good swallowability and improved dissolution. The surface layer of a tablet rapidly turns into a gel in the presence of a small amount of water or saliva. It uses a metal crosslinked thickener to increase viscosity, such as carboxy-vinyl polymer and/ or sodium alginate, which is crosslinked by polyvalent metal ions generated from a polyvalent metal compound. As a result, a relatively hard jelly-like composition is formed that helps the tablet to slip on the mucosa improving its swallowability. The gelatinous coating film suppresses short-term drug dissolution before the swallowing of the tablet, thus masking its unpleasant taste. It disintegrates rapidly and thus, does not affect the dissolution of a drug.

Endoluminal Drug Delivery Device; Cook Medical Technologies LLC; S. Aggerholm, C. Rauff Hansen and S.D. Chambers; U.S. Patent # 9,795,772; October 24, 2017.

Various technologies have been developed to deliver bioactive agents to a vessel wall for treating a variety of medical indications. One example involves the use of a drug coated medical balloon technology. A problem with such medical balloons is that they choke off blood supply from organs downstream of the balloon, and as a result any procedure involving such balloons is time limited. Attempts have been made to overcome the limitations of such balloons, by developing balloons having an internal lumen, which allows continued passage of blood through the balloon. The present invention provides an improved endoluminal drug delivery device for delivering one or more bioactive agents into a vessel of a patient. Patent claims the vascular device wherein the bioactive materials are paclitaxel and sirolimus.

Low Molecular Weight Polyethylene Glycol Drug Conjugates Having Improved Drug Biological Activity; Jenkem Technology Co. Ltd., L. Xu, X. Zhao, Z. Feng, J. Wang, and Z. Wang; US patent # 9,789,198; October 17, 2017.

Polyethylene glycol (PEG) has attracted a lot of attention in recent years. In this patent, drugs (2 to 4) were conjugated with the PEG molecule via a spacer molecule. After combining with the polyethylene glycol, the pharmacokinetics of the drug change and thereby the pharmacodynamics change so that the drug in vivo activity is improved. The capability of a drug penetrating the blood-brain barrier is usually related to relative molecular mass, fat solubility, charge property of the drug itself and its bonding capability with plasma protein and a special carrier or receptor transport system. Sometimes, the drugs permeation is too much in the brain and sometimes, it is not enough. Properties of drugs can be modified by conjugating them with PEG, especially, if we can combine more than one drug to the same PEG molecule.

Coating Formulations for Scoring or Cutting Balloon Catheters; AngioScore, Inc.; U. Speck and M.C. Berg; US patent # 9,770,536; September 26, 2017.

During an angioplasty, the concern is the transfer of drug loosely adhering to the surface of the balloon catheter. The problem is solved by a scoring or cutting the balloon catheter carrying on a portion of its surface at least one drug and at least one lipophilic antioxidant at a ratio of 3-100% by weight of at least one lipophilic antioxidant in relation to 100% by weight of the drug. During testing, it was discovered that certain lipophilic antioxidants added to even more lipophilic and less water soluble drugs in a defined mass ratio significantly increase the adherence of the drug to scoring and cutting balloons during handling and on the way to the target lesion even if the target lesion is located far away from the site where the device first enters a blood-filled introductory sheath, guiding catheter or vessel containing rapidly flowing blood.

Solid Solution Compositions and Use in Chronic Inflammation; Infirst Healthcare Ltd.; R.M. Bannister, J. Brew, R.R. Reiley III, and W. Caparros Wanderley; US patent # 9,775,820; October 3, 2017.

Acute inflammation is often treated using NSAID’s. But attempts to treat chronic inflammation have a very limited success. The patent discloses solid solution pharmaceutical compositions, which are formulated to be a lipid-adjuvant delivery system. This system enables a therapeutic compound having anti-inflammatory activity to be delivered in a manner, that effectively inhibits a pro-inflammatory response. The solid solution pharmaceutical composition comprises of one or more room temperature solid and liquid lipids, a stabilizing agent and a neutralizing agent. The present invention discloses four general types of solid solution compositions, namely lipid-soluble drug formulations, free acid/free base drug formulations, salt drug formulations, and combination drug formulations.

Intranasal Methods of Treating Women for Anorgasmia with 0.6% and 0.72% Testosterone Gels; Acerus Pharmaceutials SRL; W. Kreppner, S. Fogarty, W. Oberegger, and P. Maes; US patent 9,757,388, September 12, 2017.

Testosterone has historically been thought of as a male hormone, but it is also synthesized in women in small amounts, primarily by the ovaries and adrenal glands. Generally, women with testosterone deficiency have total testosterone levels of less than about 20-25 ng/ dL. Hypoactive sexual desire disorder (HSDD) and Anorgasmia, are the most frequently reported women’s sexual problems. The present invention relates to lower dosage strength pernasal testosterone gel formulations for intranasal administration and treatment methods for using the lower dosage strength pernasal testosterone gel formulations for treating a female subject with anorgasmia and/ or hypoactive sexual desire disorder. The patent claims a method to administering testosterone gel, which comprises about 0.6% testosterone wherein the testosterone has a particle size of greater than 10 microns to prevent the testosterone particles from entering the respiratory tract following said intranasal administration.

Lysine Delivery Systems for Blood Coagulation; Park City Bio LLC; J.M. Benns and M.C. Lawyer; US patent 9,757,547; September 12, 2017.

Coagulation is an important part of hemostasis, which is the cessation of blood loss from a damaged vessel, wherein a damaged blood vessel wall is covered by a platelet and fibrin-containing clot to stop bleeding and begin repair of the damaged vessel. Disorders of coagulation can lead to an increased risk of bleeding (hemorrhage) or obstructive clotting (thrombosis). The present invention provides a hemostatic composition for coagulating blood including a lysine or its derivative in an amount sufficient to coagulate blood, in a nasal passageway, wound, surgical site, or vagina. The patent also claims a device where the body comprises of a cylindrical or conical member with a first end having the hemostatic lysine composition, configured for insertion into a nasal passageway or vagina. The hemostatic lysine composition is associated with the blood-absorptive portion.

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