The purpose of this column is to highlight and summarize recent key patents in the pharmaceutical arena issued by the US Patent Office in January 2019.
Stabilized Cabazitaxel Formulations; G. Malhotra, S. Singh, R.B. Vedamurthy, A.M. Th akur, and D. Abhyankar; Cipla Ltd., India; U.S. Patent # 10,188,626; January 29, 2019.
Present invention discloses an improved formulation of cabazitaxel. Cabazitaxel is a semi-synthetic anticancer compound and it is approved in combination with prednisone for the treatment of prostate cancer. Cabazitaxel is available in the market as an injection under the Jevtana® trade name. Jevtana contains 60 mg cabazitaxel in 1.5 mL sterile, non-pyrogenic, clear yellow to brownish-yellow viscous solution. It is diluted prior to administration in patients. The injectable formulations disclosed in the present invention claim to exhibit increased storage stability and they are ready-to-use and ready-to-dilute which improves handling and administration to patients. Cabazitaxel formulation includes combinations of albumin, solubilizers, surfactants, alcohols, acids and solvents to provide better stability to the formulation.
Lyophilized Therapeutic Peptibody Formulations; W.J. Callahan, R.L. Remmele, Jr., G. Ratnaswamy, R.F. Latypov, and D. Liu; Amgen, Inc., US; U.S. Patent # 10,166,189; January 1, 2019.
Peptibodies are formed when peptides are bound to antibodies. Through a peptibody, an activity of a peptide and the longer duration of activity of the antibody are combined. The present invention discloses methods of making lyophilized formulations of peptibodies which claims to result in a highly stable product. The ability to remain as a stable pharmaceutical composition is crucial when the composition contains active ingredients, such as antibodies, which tend to degrade faster upon storage. Present invention claims to solve this stability issue by providing methods of producing a lyophilized therapeutic peptibody. The composition of a lyophilized therapeutic peptibody comprises a buff er, a stabilizing agent, a surfactant and a bulking agent.
Transmucosal Ketamine Delivery Composition; J.A. McCarty; Pharmaceutical Productions, Inc., US; U.S. Patent # 10,172,810; January 8, 2019.
This patent provides the composition for transmucosal ketamine delivery wherein the therapeutically effective dose would be released and systemically administered to the patient within 5 to 15 minutes. The patent claims enhanced transmucosal delivery of the pharmaceutical formulation comprising an ionizable pharmaceutical agent, ketamine, and one or more oppositely charged lipophilic species. The interaction between ketamine and lipophilic species is disclosed here as lipophilic association (LA). LA shows high thermodynamic activity which helps the ketamine stay in solubilized form. This LA is then formulated into a low dielectric dosage form and on its hydration, ketamine is absorbed through mucosal tissue to systemic circulation. Formulation may further contain solvent, carrier and water-soluble excipient.
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Drug Delivery Implant Implanted into Bone; S.H. Kim, J.S. Heo, and E.C. Kim; University-Industry Cooperation Group of Kyung Hee University, Korea; U.S. Patent # 10,188,441; January 29, 2019.
Drug delivery system combines one or more traditional drug delivery methods with engineered technology. Such methods not only help minimize/eliminate side effects, helps bypass the body’s natural defenses but also control the rate at which a drug is released and the location in the body where it is released. This patent is particularly directed to drug delivery implants implanted into a bone of a designated region. The drug delivery implant has a hollow fixture region with an inlet at an upper end coupled with a drug supply cartridge which includes a cap. The cartridge has inner and outer membranes with first and second drug releasing holes. These holes selectively communicate with each other whenever external pressure is applied on cartridge. This drug delivery implant will not only help to continuously administer a drug into bone tissues but will also help in minimizing damage to the bone tissues due to the screw threads.
Silk-Based Capsules; T. Dyakonov, D. Bush, S.L. Gosangari, C.H. Yang, S. Majuru and A. Fatmi; Patheon Soft gels, Inc.; U.S. Patent #10,182,991; January 22, 2019.
Hard and soft capsules are preferred by patients as a dosage form where the drug-fill is contained within the capsule shell, resulting in a generally tasteless and odorless delivery system. This patent provides for a hard/soft capsule where the shell comprises a silk polymer and a film-forming polymer. The capsule shell essentially comprises of 0.28% silk fibroin, 41.8% gelatin, 9.5% glycerol, 11.4% sorbitol, and 37.0% water, by weight of the capsule shell. Such soft capsule shells provide extended release of a fill material at pH 7.2. The shell can further be comprised of a plasticizer, an enteric polymer, a gelling agent, a preservative, a colorant, a flavoring agent, a sugar, a pH-modifying agent, or a combination. The silk-based hard and soft capsules are more robust, exhibit better seams, and possess improved stability under storage, as compared to capsules prepared without the solubilized silk polymer.
Stents Having Protruding Drug-Delivery Features and Associated Systems and Methods; J. Fulkerson, I. Rizk, J.A. Mustapha, and T.S. Jimenez, Jr., Re Flow Medical, Inc., US; U.S. Patent # 10,172,729; January 8, 2019.
The present invention discloses different designs of expandable stents with projecting elements like spikes and flails. Figure 2A is the side view and Figure 2B shows the cross-section of one of the designs of the present invention. Figures 2A and 2B are taken from the patent. The inventors claim to overcome limitations of uniform drug delivery the desired treatment location and penetrating target tissue with already available drug eluting stents and balloons with this invention. Stents available in the market generally include drugs coated over the surface of stents. Stents disclosed here are delivered intravascularly at the treatment site where it delivers drug from the spikes or any other projecting element acting as a drug delivery feature. These projecting elements have different sizes, shapes and configurations.
Compositions and Methods for Administering Insulin or Insulin-Like Protein to the Brain; S. Jain, D. Genkin, and H.Hoppe; Xenetic Biosciences, Inc., U.S. Patent # 10,188,739; January 29, 2019.
Insulin is a naturally-occurring polypeptide hormone secreted by the pancreas and required by the cells of the body to regulate blood glucose levels. This patent invents a method of intranasal delivery of a pharmaceutical composition, comprising a polysaccharide derivative of insulin protein and pharmaceutically acceptable excipients, to a subject, where the insulin protein is delivered to the brain of the subject through the nasal mucosa. The method adopted here helps in administering a therapeutically effective amount of an insulin to the brain of an individual but not the serum of the individual.