The purpose of this column is to highlight and summarize recent key patents in the pharmaceutical arena issued by the US Patent Office in March 2020.
Pharmaceutical Formulation for Use in Spinal Fusion; J. Schense, S. Mark, M. Alvisi, V. Martinez, and A. Maria; Kuros Biosurgery, Zurich, CH; US Patent # 10, 589,001; March 17, 2020.
A pharmaceutical formulation of a bioactive factor with two matrix precursor components for use in a spinal fusion method has been disclosed in the present invention. Spinal fusion is also known as spondylodesis or spondylosyndesis. It is a surgical treatment method used for the treatment of degenerative disc disease, spondylolisthesis (slippage of a vertebra), spinal stenosis, scoliosis, fracture, infection, or tumor. The pharmaceutical formulation comprises two matrix material precursor components. Precursor components are capable of forming a matrix by cross-linking under appropriate conditions. The composition also contains a bioactive factor. The bioactive factor is a biologically active agent, which stimulates bone formation between two vertebrae, to support spinal fusion. Parathyroid hormone (PTH) containing peptides have been disclosed to be used as bioactive factors in this invention.
Pharmaceutical Compositions for Colon-Specific Delivery; L. Li; Gateway Pharmaceuticals, Chesterfield, MO, US. Patent # 10,588,864; March 17, 2020.
Pharmaceutical treatment of colon diseases, such as C. difficile infection, ulcerative colitis, and Crohn’s disease, requires the drug to reach the colon in an effective form. Present patent discloses oral compositions that can be used to target drugs to the colon and methods of administering these compositions. The pharmaceutical composition comprises particulates comprising: a) a core comprising an active pharmaceutical compound or salt, b) an inner coating surrounding the core, and c) an outer coating which surrounds the inner coating. The inner coating comprises of a pharmaceutically acceptable polysaccharide that is susceptible to enzymatic digestion by one or more enzymes present in colonic microflora and the outer coating comprises a polymer, which is stable at upper gastrointestinal pH but can dissolve at pH >6. The core of a particulate can comprise an excipient such as a diluent, a binder, a disintegrant, a lubricant, a glidant or a combination.
High Concentration Formulation; L.M. Longo; Cassiopea, S.P.A., Lainate, Italy; US Patent # 10,603,327; March 31, 2020.
Alopecia is a group of disorders that causes hair loss from the body. The most common form is androgenetic alopecia. Present invention discloses high concentration formulations of cortexolone-17α-propionate. It also discloses a method of treating androgenetic alopecia by topically administering a pharmaceutical formulation of 5 to 15 weight percent cortexolone-17α-propionate with inactive ingredients such as alcohol, a polyol ether and water. Cortexolone-17α-propionate is fully solubilized in the formulation. Cortexolone-17α-propionate is a known topical antiandrogen that is suitable for treating acne, alopecia, and other diseases of skin and cutaneous appendages. Present invention addresses the problem of inherent solubility limitations of the active ingredient.
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Stable, Highly Pure L-Cysteine Compositions for Injection and Methods of Use; J. Maloney, A. Koganti, and P. Koneru; Exela Pharma Sciences, Lenoir, NC; US Patent # 10,583,155; March 10, 2020.
L-cysteine is an amino acid that is important for human life. While healthy adults can naturally synthesize small amounts, high-risk patients such as preterm and/or low birth weight infants and patients with severe liver disease require L-cysteine supplementation by parenteral administration (i.e., injection or intravenous infusion). L-cysteine is administered as a component of a nutritional supplement regimen referred to as “total parenteral nutrition” (TPN). One significant drawback of such L-cysteine products is that they are known to contain high amounts of aluminum. Present patent discloses compositions for parenteral administration comprising L-cysteine that are stable and have desirable safety attributes for extended periods of time. Also described are compositions for a total parenteral nutrition regimen and methods for their use.
Pharmaceutical Suspensions Containing Drug Particles, Devices for Their Administration, and Methods of Their Use; A. Heller, and J. Spiridigliozzi; SynAgile Corp., Wilson, WY; US Patent # 10,588,882; March 17, 2020.
The invention features a pharmaceutical suspension in a drug delivery device for continuous administration of the drug in the mouth cavity. The device is placed in the mouth, which can release the formulation continuously or at intermittent administrations for up to 4 hours. The flow rate of drug release is between 0.001 mL/hour to 1.25 mL/hour. Such a system can be used for drugs with narrow therapeutic index and short half-lives. The invention features a device that can be removed after inserted in a patient’s mouth. The device has a first chamber containing drug-including fluid, a second chamber containing a propellant, and a flexible and/or deformable diaphragm separating first and second chambers. The device may also contain an electrical pump system.
Affinity Based Drug Release Formulations; R. Wylie, and V. Huynh; McMaster University, Hamilton, CA; US Patent # 10,576,061; March 3, 2020.
This is a unique affinity-based drug delivery system. In step 1, drug is bound to a first member of an affinity binding pair. In step 2, a second member of the affinity binding pair is introduced, wherein the drug conjugate reversibly binds to the second member of the affinity binding pair thereby releasing the drug. As an example, streptavidin is conjugated with a drug. Agarose gel is modified with desthiobiotin. Streptavidindrug conjugate is introduced to the gel and it gets immobilized due to the high but reversible affinity of streptavidin and desthiobiotin. A sparingly soluble biotin derivative is then introduced in the system, which binds with streptavidin due to its higher affinity to streptavidin. This allows the drug to be released from the streptavidin-drug conjugate, allowing the drug to be released from the gel.
Compositions Containing Cyclodextrin-Based Metal Organic Frameworks; B.N. Limketkai, and Y.Y. Botros; PanaceaNano, Laguna Niguel, CA; US. Patent # 10,583,147; March 10, 2020.
Cyclodextrins have been widely used in drug delivery systems. The current invention describes a formulation containing at least one active agent, at least one cyclodextrin-based metal organic framework (CD-MOF) and excipients. CD-MOFs have emerged as a new class of multifunctional materials based on a porous framework with an extended structure displaying robust crystallinity, permanent porosity, and biocompatibility. The family of CD-MOFs has been enlarged by a growing collection of metal nodes involving alkali metal cations (Li+, Na+, K+, Rb+, Cs+). The composition in this patent comprises: 0.2 to 0.75 mg drug per mg of CD-MOF, and a carrier that is a mixture of oil and water. At least 50% of the active is released in the first hour.