The purpose of this column is to highlight and summarize recent key patents in the pharmaceutical arena issued by the US Patent Office in December, 2016.
Orally Disintegrating Tablet J.C. Chen, K. Day, and C.E. Szymczak; Johnson & Johnson Consumer, Inc.; U.S. Patent # 9,511,028, December 6, 2016.
The present invention relates to pharmaceutical orally disintegrating tablets (“ODTs”) having properties of rapid oral disintegration, low density, and improved robustness. The improved robustness to handling (e.g., lower friability) is also enabled by the selection of specific materials to form a low-density tablet with a more resilient structure that is less susceptible to friability. The patent claims an ODT comprising primarily of maltodextrin (15-45% by weight), and sugar or sugar alcohol (20-64% by weight). The combined weight of maltodextrin and sugar/sugar alcohol should be at least 60% by weight, of the tablet; The tablet should have a friability of less than about 5%, a density less than about 0.8 g/cc and it disintegrates in the mouth when placed on the tongue in less than about 30 seconds. It also claims that the tablet comprises less than 5% by weight of a polyethylene glycol.
Crystal Encapsulated Nanoparticles Methods and Compositions D.A. Reese, S.F. Son, and A.H. Yan; Purdue Research Foundation; U.S. Patent # 9,517,361; December 13, 2016.
Nanoparticles provide opportunities for technological advancement in various fields. However, their use in industries have been limited to date due to significant challenges in areas such as handling, dispersion, safety, and ultimate strength. The possible biological impacts of the use of nanoparticles have become a growing cause for possible concern. Due to their extremely small size, the possible interaction between such particles and cell functioning can be of concern, as such interaction may interrupt vital processes. The present invention can advantageously serve to mitigate various concerns regarding the use of nanoparticles in propellant compositions by containing the nanometric material inside of appropriate micron-size particles. The patent claims a method for making a composite of nanometric particles encapsulated by crystals where said method comprising: crystallizing a solution comprising nanometric particles, a micelle-forming material, a nonpolar dispersant for the micelle-forming material and a crystalforming material to form crystal-encapsulated nanometric particles.
Combination of Effective Substances Causing Synergistic Effects of Multiple Targeting and Use Thereof D.H. Lee and S. Cho; Vivozon, Inc., Korea; U.S. Patent # 9,526,718; December 27, 2016.
Various diseases have been treated and prevented by using a “single target-single disease” approach to control a specific hormone or to target a single receptor. However, such an approach has not been sufficient to treat and prevent many diseases and may cause unexpected side effects. The present patent provides the combination of active components inducing synergistic effects of multi-targeting and a use thereof. It disclosed a method comprising functional food composition, a cosmetic composition, a pain-suppressive composition, and a composition for treatment or prevention of pruritus or atopic dermatitis. The composition further comprise as active components, two or more components selected from a group consisting of (a) a 5-hydroxytryptamine subtype 2 (5-HT2) receptor antagonist; (b) a P2X receptor antagonist; and (c) any one of a glycine receptor agonist, a glycine transporter (GlyT) antagonist, a gamma-aminobutyric acid (GABA) receptor agonist, and a GABA transporter 1 (GAT1) antagonist.
Synergistic Combinations of OX40L Antibodies for the Treatment of GVHD P. Bland-Ward, M. Kosmac, S. Holmes, I. Kirby, and J. Campbell; Kymab Ltd., U.S. Patent # 9,512,229; December 6, 2016.
OX40 ligand (OX40L) is a TNF (Tumor Necrosis Factor) family member; a 34 kDa type II transmembrane protein. Graft versus host disease (GvHD) is a major cause of mortality following allogeneic bone marrow treatment. This invention claims a method of treating or preventing GvHD by administering a therapeutically or prophylactically effective amount of anti-OX40L antibody or its fragment that antagonizes specific binding of OX40 to OX40L along with a therapeutically or prophylactically effective amount of a second agent selected from the group consisting of rapamycin, tacrolimus, cyclosporine, a corticosteroid or methylprednisolone. It also consists of anti-IL2R antibodies which helps in achieving synergistic effect between anti-OX40L and the second agent. The whole treatment is supposed to be administered at least one time before and one time after the transplant.
Dry Powder Inhaler and System for Drug Delivery C.C. Smutney, P.S. Kinsey, C.R. Sahi, B. Adamo, J.M. Polidoro, S. McLean, D. Overfield, A. Bryant, T. He, and A. Mann; MannKind Corp.; U.S. Patent # 9,511,198; December 6, 2016.
Drugs delivered by inhalation are typically delivered using positive pressure relative to atmospheric pressure in air with propellants. Drug delivery to lung tissue has been achieved with dry powder inhalers. Dry powder inhalers can be breathactivated and can deliver drugs by converting drug particles in a carrier into a fine dry powder, which is entrained into an air flow and inhaled by the patient. Various factors such as particle size, moisture content etc. affect the dose and dose reproducibility. This dry powder inhaler is compact; can be provided in various shapes and sizes, colors, and comprises a housing, a mouthpiece, a cartridge placement area, and a mechanism for opening and closing the medicament cartridge. The device is easy to manufacture, provides a pre-metered single unit dose, it is relatively easy to use, and can be reusable or disposable.
Pharmaceutical Combination S. Caltabiano, E. Ohlstein, and S. McCallum; Velicept Therapeutics, Inc., U.S. Patent # 9,522,129, December 20, 2016.
Over-active bladder is associated with involuntary contraction of bladder, and shows symptoms of a complex of urgency, with or without urge incontinence, accompanied by frequency and nocturia. Antimuscarinics are believed to reduce bladder overactivity by inhibiting bladder smooth muscle contractility. The treatment combination according to the invention comprises a beta- 3 adrenergic receptor agonist and a muscarinic receptor antagonist. Beta-adrenergic receptors have been subdivided into three types: beta1-, beta2- and beta3-adrenergic receptors. Beta1-adrenergic receptors are predominant in the heart, beta2-adrenergic receptors-in the respiratory system, and beta3-adrenergic receptors-in the adipose tissues, gall bladder and urinary bladder. In the urinary bladder beta- 3 receptor agonists are thought to cause relaxation of the bladder and prevention of urination. The beta-3 adrenergic receptor agonist can comprise a compound selected from the group consisting of solabegron, CL-316,243, and mirabegron. The muscarinic receptor antagonist can comprise a compound selected from the group consisting of oxybutynin, tolterodine, and solifenacin.
Delivery of Agents Using Interfering Nanoparticles T.M. Rana; Sanford-Burnham Medical Research Institute; U.S. Patent # 9,526,693; December 27, 2016.
RNA silencing or RNA interference refers to a family of gene silencing effects by which gene expression is negatively regulated by non-coding RNAs such as microRNAs. MicroRNAs (miRNAs) are small, endogenous, non-coding RNAs that post-transcriptionally regulate gene expression by binding with imperfect complementarity in 3’ untranslated regions (3’-UTR) of their target messenger RNAs (mRNAs). The nanotransporters of the present invention are referred to as interfering nanoparticles (iNOP) and may be functionalized to provide functionalized iNOP derivatives allowing target delivery of agents. Nanotransporters can be used for delivery of therapeutic agents, such as RNA silencing agents to cells. The core of the nanotransporter is a nanoparticle such as a dendrimer with one or more surface functional group. The functional surface groups are chosen for their ability to increase the functionality of the nanotransporter, for example, to increase cell targeting specificity, to increase delivery of the nanotransporter to the target cell, and/or to impart a precise biological function.