The purpose of this column is to highlight and summarize recent key patents in the pharmaceutical arena issued by the US Patent Office in November-December, 2020.
Systems and Methods for Long-Term Transdermal Administration;
E.S. Lee, A.K. Jain, and P. Singh; Corium Inc., CA; US Patent # 10,835,499; November 17, 2020.
Transdermal drug delivery systems have several advantages over oral and injectable formulations. However, they have their own set of difficulties, especially if one desires to deliver a drug over a long time, such as seven days. Some of the issues are – patch not sticking fully, patch curling/wrinkling, suitable breathability (normally higher breathability reduced drug flux) etc. This patent claims a transdermal patch, comprising: (a) a first backing layer comprised of an elastic material; (b) an interfacing adhesive layer; (c) a composite layer comprising a plurality of segments that are at least partially separated, the composite layer comprised of: (i) a second backing layer, and (ii) an adhesive active agent layer; (d) a contact adhesive layer; and (e) a release liner, wherein the contact adhesive layer is positioned between the adhesive active agent layer of the composite layer and the release liner.
Biodegradable Polymer Microsphere Compositions for Parenteral Administration;
N. Dormer and C. Berkland; Adare Pharmaceuticals USA, Inc., NJ; US Patent # 10,874,612; December 29, 2020.
The patent describes an injectable formulation containing an active drug, a mixture of biodegradable polymer and an ethyl cellulose derivative. The drug content is high in the granules and the cellulose-based polymer helps to harden the microspheres, maintain a spherical shape and narrow the dispersity of the microspheres. Ethyl cellulose improves the drug entrapment and being hydrophobic, it prevents escaping of the drug. It was observed to improve microsphere stability in terms of dissolution behavior and thermal resistance. The drug release rate can be easily adjusted to the desired value in the presence of ethyl cellulose derivatives.
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Bupropion as a Modulator of Drug Activity;
H. Tabuteau; Antecip Bioventures II LLC, NY; US Patent # 10,864,209; December 15, 2020.
Bupropion, sold under the brand names Wellbutrin and Zyban, is a medication primarily used as an antidepressant and to support smoking cessation. The patent claims a combination drug therapy of bupropion and dextromethorphan to treat resistant depression. Dextromethorphan is commonly used as a cough suppressant to provide temporary relief from coughing. Bupropion reduces the metabolism of dextromethorphan thereby increasing its plasma level and also, its elimination half-life. This effect is most prominent in a person who metabolizes dextromethorphan very quickly. Here, the dextromethorphan is formulated for immediate release and the bupropion is formulated for sustained release.
Gastro-Retentive Dosage Forms for Sustained Drug Delivery;
K. Meghpara, J. Vaghashiya, N.H. Shah, D. Desai, W. Phuapradit, H.K. Sandhu, S.R.K Vaka, N.B. Shelke, and A. Chatterji; Kashiv Biosciences LLC, NJ; US Patent # 10,857,098; December 8, 2020.
The present patent relates to floating gastro-retentive oral dosage forms for modified release of active pharmaceutical agents. Gastro-retentive oral dosage forms are particularly beneficial for drugs having a narrow absorption window (NAW) in the upper gastrointestinal (GI) tract. Weakly basic drugs that have high pH-dependent solubility, drugs that act locally in the upper GI tract, drugs that degrade in the colon, or drugs that disturb normal colonic microbes are good candidates for such a technology. The rapidly expanding floating gastro-retentive dosage forms feature a matrix core. This sustained release swellable matrix core comprises an active agent, a super-disintegrant, a water-soluble polymer, an acid, and a gasgenerating agent; and a membrane that is a water-insoluble, permeable, elastic, and self-adjusting comprising a plasticizer and at least one copolymer. The membrane surrounds the matrix core. The floating gastroretentive dosage form provides sustained release of the active agent in a patient’s stomach and swells to approximately 200% in gastric fluid in about 30 minutes. The patent also provides rapidly expanding sustained release or combined immediate release and sustained release formulations that require targeted release in the proximal gastro-intestinal tract.
Devices and Methods for Controlling Tremor;
K.H. Rosenluth, S.L. Delp, J. Paderi, V. Rajasekhar, and T. Altman; Cala Health, Inc., CA; US Patent # 10,850,090; December 1, 2020.
A tremor is a rhythmic shaking movement in one or more parts of your body. It is involuntary. There are various types of tremors like Essential Tremor (ET), Parkinsonian Tremor and Dystonic Tremors. ET is the most common type. It usually affects your hands, but it can also affect your head, voice, tongue, legs, and trunk. There is no cure for most forms of tremor, but there are treatments available like drugs and brain surgery to help manage symptoms. But there is a great need for alternative treatments for ET patients that reduce tremors without the side effects of drugs and without the risks of brain surgery. Present patent relates to system, devices, and methods for treating tremor by stimulation of a peripheral nerve. A peripheral nerve stimulator can be used to stimulate a peripheral nerve to treat ET, Parkinson Tremor, and other forms of tremor. The peripheral nerve stimulator can be either a non-invasive surface stimulator or an implanted stimulator. Stimulation can be electrical, mechanical, or chemical. Stimulation can be delivered using either an open loop system or a closed loop system with feedback.
Methods and Devices for Delivery of Pharmaceutical Agents Within Orifices of the Body;
N. Barak; RDD Pharma Ltd, Tel Aviv, Israel; US Patent # 10,821,274; November 3, 2020.
Oral dosage forms may suffer from several drawbacks such as poor bioavailability, too slow or too fast drug delivery, first-pass metabolism, etc. Orifices such as the nose, ear, rectum, and vagina off er the possibility of delivering medicines. Different dosage forms such as suppositories, tampons, vaginal implants, sprays, drops etc. can be used. The patent claims a drug delivery device comprising an active agent and a carrier, wherein the carrier has a melting point of 23°C to 37.5°C and the carrier may be PEG. The device has a shell elastically stressed by the pharmaceutical composition and the shell is configured for the respective orifice of the body.
Ophthalmic Drug Delivery;
B.L. Ballou, Jr., M. Packer, R.J. Mumper, and T. Ianchulev; Evenovia, Inc., NY; US Patent # 10,839,960; November 17, 2020.
Despite traditional eye drops being convenient and simple to use, they are not very effi cient. Only a small amount of the dose is eff ectively delivered and retained to its intended target, most is lost due to clearance mechanisms. The present patent includes and provides a method of delivering a medicament to an eye. The method includes: (a) providing droplets containing the medicament with a specifi ed average size and average initial ejecting velocity; and (b) delivering the medicament to the eye, where the droplets deliver a percentage of the ejected mass of the droplets to the eye. Percentage can vary between 80 to 100% of the ejected mass.