Register Now
Why register?
 The leading web portal for pharmacy resources, news, education and careers October 24, 2017
Pharmacy Choice - Pharmaceutical News - Patent Issued for Dosage Form for Insertion into the Mouth (USPTO 9579295) - October 24, 2017

Pharmacy News Article

 3/17/17 - Patent Issued for Dosage Form for Insertion into the Mouth (USPTO 9579295)

By a News Reporter-Staff News Editor at Drug Week From Alexandria, Virginia, NewsRx journalists report that a patent by the inventors Ryoo, Je Phil (Princeton, NJ); Chu, Chun Kwong (Shatin, HK); Wang, Zheng (Bridgewater, NJ), filed on July 20, 2015, was published online on February 28, 2017 (see also NAL PHARMACEUTICAL GROUP LIMITED).

The patent's assignee for patent number 9579295 is NAL PHARMACEUTICAL GROUP LIMITED (Causeway Bay, HK).

News editors obtained the following quote from the background information supplied by the inventors: "Migraine is one of the most common neurological conditions. Migraine headaches affect a large portion of the U.S. population and are more prevalent than diabetes, epilepsy and asthma combined. Migraine is more than just a headache; it can be a debilitating condition which has a considerable impact on the quality of life of sufferers and their families. Attacks can be completely disabling, forcing the sufferer to abandon everyday activities. Even in symptom-free periods, sufferers may live in fear of the next attack. Migraine attacks normally last between 4 and 72 hours and sufferers are usually symptom free between attacks.

"Migraine is believed to be caused by the release of a chemical called serotonin or 5HT into the bloodstream. This causes the pain neurons in the blood vessel wall to become irritated. Exactly what causes the release of serotonin is still a subject for research and debate. However, certain factors have been identified which can trigger attacks in susceptible people. Some of these are stress or sometimes the relief of stress, lack of food or infrequent meals, foods containing ingredients such as mono-sodium glutamate, caffeine and chocolate, or alcohol (especially red wine), overtiredness (physical or mental), changes in sleep patterns (e.g., late nights or a weekend lie-in), or hormonal factors (e.g., monthly periods, the contraceptive pill or hormonal changes in males and females as they age).

"Migraines are more common than cluster headaches, and have been studied more extensively. In addition, a better and more effective set of drugs have been developed to treat migraines, than cluster headache. For those reasons, the discussion below focuses mainly on migraines, rather than cluster headaches.

"'Cluster headaches' were given that name because they tend to occur in episodic clusters, with a cluster cycle usually lasting 4 to 8 weeks. In some patients, a cluster occurs only once in a lifetime; in other patients, a cluster may occur roughly once a year, with periods of complete remission between attacks; and, in the roughly 10% of patients who are chronic sufferers, there are no significant periods of remission. As opposed to migraines (which occur in women at roughly 3 times the rates as in men), cluster headaches are more prevalent in men than in women, by a factor of about 5:1 or higher.

"Migraines and cluster headaches are both classified as 'recurrent primary headaches'. They are recurrent, since they recur with sufficient frequency to seriously interfere with the health and quality of life of a patient, to a point of requiring and demanding medical attention, as opposed to just taking aspirin or similar over-the-counter analgesics and lying down till it passes. They are also regarded as 'primary' headaches, since they usually arise as a primary adverse biologic condition, independently of other causative medical conditions such as tumors, sinus or other infections, bleeding problems, etc.

"Current methods for administering anti-migraine pharmaceuticals have major limitations. For example, due to degradation in the gastrointestinal track and low adsorption of the drug, oral ingestible dosage forms of anti-migraine medications have to be administered in large doses of about 20-100 mg. These high doses may causes nausea, vomiting and other unwanted adverse side effects. Many anti-migraine agents are subject to pre-systemic and first pass metabolism. Because of this, it is estimated that as little as 2-10% of the active unchanged drug actually reaches the blood stream. In fact this causes delay in the effectiveness of the drug as a treatment or prophylaxis of the disorder in the patient. Likewise, intranasal administration of anti-migraine agents is hampered with significant limitations due to reduced absorption and low bioavailability.

"Injectable and nasal spray forms of anti-migraine agents are also available for the treatment of migraines. Although parenteral administration of anti-migraine agents into the blood stream allows for a lower dose as compared to other non-injectable methods of administration, the inconvenience of an office visit for an injection or problems with the self-administration of injectables are self evident.

"In the past, migraine headaches have been treated by use of rizaptriptan, sumatriptan, zolmitriptan or other triptan drugs. These drugs have basically been administered using conventional dosage forms such as pills or capsules or for sumatriptan through injection and nasal spray. The problem with the gastrointestinal (GI) administered triptan anti-migraine pharmaceutical agents is that they have a low GI bioavailability of approximately 15% to 40% and cause GI irritations. In addition, it is important that these drugs be delivered rapidly to a patient to prevent or treat the onset of a migraine headache and give immediate relief. The delay in release of the drug from the dosage form into and the bioavailability of the drug after administration causes undue suffering in the patient which is especially acute with patients suffering from migraine headaches. Therefore, what is needed are formulations that are effective for treating migraines which allow rapid drug release and bioavailability while avoiding the GI irritations which occur with the known administration of anti-migraine medications.

"Triptans have been developed for the acute treatment of migraine. These medicines are available in the form of tablets for eletriptan, frovatriptan, sumatriptan, zolmitriptan, naratriptan, rizatriptan and almotriptan. These products are intended to be taken in amounts up to a maximum of 5 to 200 mg per day. Table A summarizes dosing regimens for triptan products.

"TABLE-US-00001 TABLE A Triptan Dosing Regimens Maximum 24 hour Generic Name Dose Brand Name Dose Almotriptan 12.5 mg Axert 12.5 mg Eletriptan 40 mg Relpax 80 mg Frovatriptan 2.5 mg Frova 7.5 mg Naratriptan 2.5 mg Amerge 5.0 mg Rizatriptan 10 mg Maxalt 30 mg Sumatriptan 100 mg Imitrex 200 mg Sumatriptan 6 mg Imitrex 6 mg injection Sumatriptan nasal 20 mg Imitrex 40 mg spray Zolmitriptan 2.5 mg Zomig 10 mg Zolmitriptan 5 mg Zomig ZMT 10 mg Zolmitriptan 5 mg Zomig ZMT 10 mg Oral form unless otherwise noted."

As a supplement to the background information on this patent, NewsRx correspondents also obtained the inventors' summary information for this patent: "We have discovered a water soluble matrix which can be incorporated into a solid, film or liquid oral dosage form for insertion into the mouth as a means for effectively delivering to, and transporting pharmaceutical active agents selectively through the oral mucosal tissue into the patient. This water soluble matrix system delivers the pharmaceutical active agent effectively and rapidly into the body through the mucous membranes in the mouth. While this system is effective for delivering pharmaceutically active agents, this system is ideally suited for delivering pharmaceutically active agents which treat or prevent migraine headaches, especially the triptans which include eletriptan, frovatriptan, sumatriptan, zolmitriptan, naratriptan, rizatriptan and almotriptan. Preferred triptans for selective oral mucosal delivery are rizaptriptan, sumatriptan and zolmitriptan.

"The oral dosage matrix of this invention transports these pharmaceutically active agents selectively through the mucous membrane in the mouth bypassing the GI system so as to avoid GI irritations and deactivation of the active agent in the GI track. Without GI inactivation, less active agent is needed to produce a therapeutic result. In addition, the oral dosage matrix of this invention rapidly releases the pharmaceutically active agent for transport quickly into the blood stream of the patient. Transport of the active agents selectively through the mucus membranes of the mouth is facilitated by incorporating one or more fatty acid esters of sucrose having a combined hydrophilic lipophilic balance (HLB) of about 8 to about 16 with the active agent to form the matrix. The fatty acid esters of sucrose are an effective absorption enhancer. The oral dosage matrix of this invention produces improved bioavailability and delivery of the pharmaceutical active agent with rapid onset of therapeutic effectiveness for the patient. Rapid release and rapid, efficient absorption is particularly important for patients suffering from migraine headaches.

"The oral dosage matrix, pharmaceutically active agent and fatty acid ester of sucrose, may be added to additional ingredients to produce dosage forms such as a film, a rapid releasing solid such as a powder or granule, a tablet, and also a liquid which contain an effective amount of the pharmaceutically active agent to relieve a migraine and related symptoms or act as a prophylactic disbursed therein. In accordance with this invention, this oral dosage matrix when incorporated into a tablet, film or other solid dosage form or solid dosage unit may further comprise a polymeric mixture of polyvinyl pyrrolidone and a polymeric alginate. This solid dosage form is of a size suitable for insertion into the mouth. In particular, this solid dosage form is particularly advantageous for administration of anti migraine agents which function, either or both, as a prophylactic and a treatment of migraine headaches."

For additional information on this patent, see: Ryoo, Je Phil; Chu, Chun Kwong; Wang, Zheng. Dosage Form for Insertion into the Mouth. U.S. Patent Number 9579295, filed July 20, 2015, and published online on February 28, 2017. Patent URL:

Keywords for this news article include: Pain, Antiinflammatory, Antimigraine Agents, Autacoids, Analgesics, Dosage Forms, Frovatriptan, Sulfonamides, Zomig Therapy, Imitrex Therapy, Cluster Headache, Gastroenterology, Biological Factors, Eletriptan Therapy, Headache Disorders, Almotriptan Therapy, Drugs and Therapies, Naratriptan Therapy, Rizatriptan Therapy.

Our reports deliver fact-based news of research and discoveries from around the world. Copyright 2017, NewsRx LLC

(c) 2017 NewsRx LLC

Pharmacy News Index
  Drug Delivery Systems
  FDA Final Approvals
  Front Page Healthcare News
  Generic Drugs
  Hospital Industry
  Internet Pharmacy
  IT in Healthcare
  Medicare & Medicaid
  Over-the-Counter Drugs
  Pharm Industry Trends and Policy
  Pharmaceutical Development
  Pharmaceutical Industry


Last Chance
Oct 24: Metabolic Syndrome: The Heart of Any Wellness Practice
Last Chance
Oct 25: Dispensing Controlled Substances in Today’s Pharmacy
Oct 26: Management of Schizophrenia & Acute Agitation
Oct 27: Influenza 2017-2018: An Update on Prevention and Treatment
Oct 30: Medication Safety & Drug Safety Alerts
Click for entire Webinar Calendar

Special Announcement

Free Membership
Enjoy Drug Search, industry newsletters and more...

Nursing Jobs
Are you a nurse looking for a job?

Check out the Nursing Job Source.

Your number one choice for nursing jobs.

Websites »
Copyright © 2017 Pharmacy Choice - All rights reserved.
Terms and Conditions | Privacy Statement