The purpose of this column is to highlight and summarize recent key patents in the pharmaceutical arena issued by the US Patent Offi ce in January-February, 2021.
Rutin Compositions
H. Kida, N. Yamaguchi, and M. Ono; Alps Pharmaceutical Ind. Co. Ltd., Japan; U.S. Patent # 10,918,654; February 16, 2021.
Rutin is a bioflavonoid or plant pigment that is found in certain vegetables and fruits. It exhibits a broad spectrum of biological activities like vasoprotective, cardioprotective, etc. However, rutin has low bioavailability due to poor absorption that limits its potential as a therapeutic agent. The present patent discloses a water-soluble composition containing rutin, L-arginine, and an alkali salt of ascorbic acid. In the composition, the molar ratio between the rutin, L-arginine, and the alkali salt of ascorbic acid is 1:1.6- 3.0:0.1-2.0.
Compositions and Methods for Non-Surgical Treatment of Ptosis
M. Silverberg; Voom LLC, USA; U.S. Patent # 10,912,765; February 9, 2021.
Ptosis involves drooping of the upper eyelid over the eye. It can limit or completely block normal vision. The cause can be damaged nerves, which control eye muscles or looseness of skin of upper eyelids. The patent proposed two compositions – 0.1% oxymetazoline and oxymetazoline with phenylephrine. Oxymetazoline does not cause pupillary dilation or mydriasis. The inventor showed that a single drop of 0.1% oxymetazoline solution was significantly more effective than the repeated administration of 0.025% oxymetazoline. The inventor also observed a synergistic effect of 0.1% oxymetazoline and 0.25% phenylephrine in lid elevation.
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Method to Evaluate the Stability of a Protein-Based Formulation
T. Chevolleau and J.B. Hamel; Becton Dickinson France, FR; U.S. Patent # 10,914,720; February 9, 2021.
Proteins can denature by interacting with surfaces resulting in a loss of activity. In prefilled syringes, tungsten residues, silicone-based lubricant and adhesives can cause incompatibility with the active molecules. This patent describes a method to evaluate the stability of a protein-based formulation in buff er and filled in a lubricated container. The method encompasses a) preparing a first solution comprising the buff er and the lubricant; b) evaluating a decrease over time of interfacial tension between the buffer and the lubricant in the first solution; c) preparing a second solution comprising the protein-based formulation and the lubricant; d) evaluating a decrease over time of interfacial tension between the protein-based formulation and the lubricant in the second solution; and e) identifying at least one component of the protein-based formulation exhibiting an interaction with the lubricant by comparing the decrease evaluated in step (d) with the decrease evaluated in step (b).
Composition for Food and Fat Absorption Inhibitor
Y. Oda and F. Ueda; Fujifi lm Corporation, Japan; U.S. Patent # 10,925,918; February 23, 2021.
A small amount of fat is an essential part of a healthy and balanced diet. But, in recent years, excessive fat ingestion is occurring due to a dietary life centered on high-fat food. For this reason, drugs or food materials that inhibit fat absorption have attracted attention. Inventors of the present patent found that intake of a composition or component having a fat absorption inhibitory effect as a food material deteriorates the intestinal environment. The present patent discloses the composition for food and a fat absorption inhibitor, each including a seaweed polyphenol and a tea extract. Disclosed compositions can effectively inhibit fat absorption without deteriorating the intestinal environment.
Disulfiram and Metal Salt Staggered Oral Dosing Regimen and Staggered-Release Oral Unit Dosage Forms
S. Marcus; Cantex Pharmaceuticals, Inc., USA; U.S. Patent # 10,905,661; February 2, 2021.
Disulfiram (DSF) is known to bind with bivalent metal ions. The chelation may enhance the transport of metals across the biological membranes. DSF/copper and DSF/ zinc have been shown to be effective in the treatment of cancers. However, DSF is incompatible with copper or zinc by simultaneous oral administration. Thus, in this patent, the inventors staggered the release of DSF and metal ions. Copper was formulated to be released one to three hours after the release of DSF. In a capsule, the inventor included a DSF minitablet, one copper minitablet and an effective amount of one anti-cancer compound. The copper minitablet is enteric coated and gets released at pH greater than 7.0 in the digestive system.
Opioid Formulations
F. Tiberg, I. Harwigsson, and M. Johnsson; Camurus AB, Sweden; U.S. Patent # 10,912,772; February 9, 2021.
The present invention relates to formulation precursors (pre-formulations) for the in-situ generation of controlled release opioid compositions, especially containing buprenorphine. Opioid formulations are hard to develop because of complicated requirements. They should provide a sufficient concentration within the therapeutic window for a sufficient length of time, and should not produce opioid dependence. The proposed formulation is administered subcutaneously once-weekly and comprises of 5% buprenorphine, ~ 10% ethanol, ~ 42% phosphatidylcholine and ~ 42% glycerol dioleate. The formulation forms a liquid crystalline phase structure upon exposure to aqueous phase. The formulation ensures the plasma buprenorphine concentration of 0.2 ng/ mL for at least one week.
Emulsions for Injectable Formulations
R. Ondei and E. Fernandes; Croda International PLC, USA; U.S. Patent # 10,888,614; January 12, 2021.
An emulsion is a mixture of two liquids that are immiscible. Water-in-oil (w/o) emulsions consists of an oil as a continuous phase and water as a discontinuous phase. The w/o emulsions are generally used in pharmaceutical formulations as a vehicle for delivery of active agents. In vaccinations, water-in-oil emulsions are commonly used as an adjuvant to stimulate the immune response against target antigens. Those based on mineral oils are known to be very efficient but can sometimes induce local reactions with reactive antigens. Non-mineral oil-based formulations are well tolerated, but less efficient with poor immunogens. There are certain inherent limitations of w/o emulsions, which make it difficult to obtain stable and fluid w/o emulsions, especially when based on metabolizable oils. The present invention relates to emulsifiers for injectable water-in-oil emulsions. The emulsifier is an alkoxylatedpolyol or polyamine, which is optionally acyl terminated. The emulsifiers described for emulsions may be required less than known emulsifiers and will also provide stable emulsions. The present invention also includes methods of preparing w/o formulations.