By a News Reporter-Staff News Editor at Drug Week A patent application by the inventors Lee, Catherine (West Linn, OR); Wang, Chien-Chiao (Taipei, TW), filed on November 14, 2016, was made available online on March 9, 2017, according to news reporting originating from Washington, D.C., by NewsRx correspondents (see also TAHO Pharmaceuticals Ltd.).
This patent application is assigned to TAHO Pharmaceuticals Ltd.
The following quote was obtained by the news editors from the background information supplied by the inventors: "There exist various ways of administering drugs. They include oral tablets, orally disintegrating tablets, oral solution and injectables. However, aside from injectable form, which is invasive, the other administration routes may not be suitable for those patients who have difficulty swallowing, such as children and the elderly as well as people with buccal conditions. Instead, a more appropriate administration route for patients who have difficulty swallowing may be orally disintegrating film (ODF), which has recently been developed for the pharmaceutical industry and can be adapted for a plethora of popular drugs such as ondansetron. Due to its ease of handling and storage as well as the fact that it does not require swallowing solids such as tablets, administration of drugs via ODF is beneficial, especially for those who have difficulty swallowing.
"An ODF typically has an established shelf-life of 2-3 years, depending on the active agent. However, it can be extremely sensitive to environmental moisture (Siddiqui et al., Advan. Biol. Res., 5(6): 291-303, 2011) as well as other environmental influences such as temperature and pH under various storage conditions. Therefore, functional excipients such as stabilizer (stabilizing agents), disintegrants, solubizer and filming-forming agents (in contrast to non-functional excipients such as sweetners, flavoring agents, etc. . . . ), have been described in other ODFs to enhance the ODF quality and performance properties.
"As an illustration, there are various patents that describe application of ODF technology to ondansetron with functional excipients as additives. For example, U.S. Pat. No. 8,580,830, to Leichs et al., discloses adding pH adjusting agents to enhance ondansetron stability and to stimulate saliva for dissolving the film.
"In addition, U.S. Pat. No. 8,663,687, to Myers et al. proposes preparing film compositions for delivery of drugs by including polyethylene oxide and saccharide-based polymer as a water soluble polymer composition in order to resolve any air trapping and void formation problems associated with conventional film forming process. The patent further claims incorporating active agents into nanoparticles or microparticles so as to ensure a non-self aggregating uniform heterogeneity.
"Further, U.S. Pat. No. 8,658,201, to Singh et al., discloses a rapidly dissolving film having significant drug loading capability while providing sustained and controlled release of an active agent. This film is made up of high molecular weight hydrophilic polymers in combination with a rapidly dissolving polymeric material including water soluble sugars, semi-synthetic and synthetic polymers, and commercially available disintegrants.
"Rather than using additives and complex formulations by the use of functional excipients as described in the patent listed above, there is a need for a fast acting ODF with a formulation that is easy to manufacture into a product and avoids a substantial number of additives that heretofore have been seen in many other ODF products while, at the same time, achieves desirable characteristics in an ODF product such as short buccal disintegration times, short dissolution times, strength for withstanding handling, minimum of gas bubbles, uniform distribution of API, smooth appearance appropriate for commercialization, etc. . . ."
In addition to the background information obtained for this patent application, NewsRx journalists also obtained the inventors' summary information for this patent application: "Accordingly, it is one objective of the present invention to provide a fast acting ODF for treatment of emesis.
"The present invention provides a fast acting disintegrating film which comprises ondansetron or a pharmaceutical acceptable salt thereof in an amount of 2 to 24 mg, at least a first hydrophilic film forming polymer in an amount of at least 8% by weight of the film, wherein the first hydrophilic film forming polymer is characterized by having a molecular weight of 5000 to 50000 Da and viscosity of 3 to 10 cps, and a water soluble excipient in an amount of 10 to 30% by weight of the film.
"The fast acting integrating film further comprises a second hydrophilic film forming polymer characterized by having a molecular weight of equal or greater than 50000 Da and viscosity equal or greater than 15 cps, wherein said first hydrophilic film forming polymer is mixed with said second hydrophilic film forming polymer in a ratio of at least about 0.1:1. In some embodiments, the mixture of said first hydrophilic film forming polymer to said second hydrophilic film forming polymer may be at a ratio of more than 0.5:1. And in other embodiments, the first hydrophilic film forming polymer may be in an amount of more than 20%, 50% or 65% by weight of the film.
"Another object of the present invention is to provide a method for preparing the ODF that remains stable over a period of time under a normal pharmacologically storage condition.
"Therefore, a method for preparing an orally administrable film dosage form is provided. The preparation method involves dissolving in water a pharmaceutically acceptable amount of active pharmaceutical ingredient, at least one hydrophilic film forming polymer in an amount of at least 8% by weight of the dosage form and is characterized by having a molecular weight of 5000 to 50000 Da and viscosity of 3 to 10 cps, and a water-soluble excipient in an amount of 10 to 30% by weight of the dosage form to form a viscous solution with a measured viscosity of about 2000 to 10000 cps. A layer of the viscous solution is then coated on a casting film and dried in an oven at about 80.degree. C. over a period of about 20 minutes so as to form the orally administrable film of desired thickness and size.
"In alternative embodiments, the method may further involves mixing another hydrophilic film forming polymer characterized by having a molecular weight of equal or greater than 50000 Da, wherein said at least one hydrophilic film forming polymer is mixed with said another hydrophilic film forming polymer in a ratio of at least about 0.1:1. And according to certain embodiments, said at least one hydrophilic film forming polymer may be mixed with said another hydrophilic film forming polymer at a ratio of more than 0.5:1.
"Still another object of the present invention is to provide an orally administered film that can disintegrate upon contact of saliva in the buccal cavity within about sixty seconds.
"The present invention provides an orally administered film characterized by having a pre-drying solution blend with a measured viscosity of about 2000 to 10000 cps. The orally administered film comprises ondansetron or pharmaceutical acceptable salt thereof in an amount of about 4 to 8 mg, at least one hydrophilic film forming polymer in an amount of at least 8% by weight of the film, wherein the at least one hydrophilic film forming polymer is characterized by having a molecular weight of 5000 to 50000 Da, and a water soluble excipient in an amount of 10 to 30% by weight of the film.
"Optionally, the orally administered film or fast acting orally disintegrating film may further include other ingredients such as one or more flavoring agent, sweetening agent and coloring agent to be dissolved or mixed with the pharmacologically active agent, hydrophilic film forming polymers and water soluble excipients in the method for preparing the film.
"Yet another object of the present invention is to provide a method for treating emesis using the ODF that mediates through antagonizing the action of 5-hydroxytryptamine (5HT or serotonin) at 5-HT3 receptors.
"The present invention also provides a method for treating or preventing nausea or vomiting or a treatment method mediated through antagonizing action of 5HT at 5-HT3 receptor by administering the above mentioned fast acting orally disintegrating film or orally administered film to a patient in need thereof."
URL and more information on this patent application, see: Lee, Catherine; Wang, Chien-Chiao. Fast Acting Orally Disintegrating Film. Filed November 14, 2016 and posted March 9, 2017. Patent URL: http://appft.uspto.gov/netacgi/nph-Parser?Sect1=PTO1&Sect2=HITOFF&d=PG01&p=1&u=%2Fnetahtml%2FPTO%2Fsrchnum.html&r=1&f=G&l=50&s1=%2220170056374%22.PGNR.&OS=DN/20170056374&RS=DN/20170056374
Keywords for this news article include: Antiemetic-Antivertigo Agents, TAHO Pharmaceuticals Ltd, Dosage Forms, Drugs and Therapies, Ondansetron Therapy, 5ht3 Receptor Antagonists, Central Nervous System Agents.
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