Pisgah Labs’ Invention Improves Safety of Thyroid Hormones
PISGAH FOREST, NC, Aug. 17, 2010. Today, Pisgah Labs, Inc. (www.pisgahlabs.com) received a Notice of Allowance from the United States Patent and Trademark office (http://www.uspto.gov/) for an important new technology patent addressing global stability problems of thyroid hormone drugs. According to the FDA (http://www.fda.gov/): “Thyroid hormones effect protein, lipid, and carbohydrate metabolism, growth and development. Orally administered levothyroxine sodium is used as replacement therapy in conditions characterized by diminished or absent thyroid function, such as cretinism, myxedema, nontoxic goiter, or hypothyroidism. Levothyroxine sodium may be used to suppress the secretion of thyrotropin in the management of simple nonendemic goiter, chronic lymphocytic thyroiditis, and thyroid cancer.”
The shelf life of important treatments, particularly for prescription drugs is a factor that affects all patients. A medication past its expiry date has been shown to have decreased potency to the extent it may no longer exhibit therapeutic value. Drug product manufacturers in conjunction with the FDA routinely perform and monitor the stability of formulated drug products and of the active ingredients used to make those drug products. In the case of the thyroid hormones, the stability of the existing commercial drugs is inherently lacking and formulation techniques do little to correct the deficiency. Current manufacturers have responded to the FDA’s insistence for safe and efficacious medications, but breakthrough technology was, until now, unavailable.
Further, the criticality of drug product stability and associated shelf life is obviously very important and well exemplified when considering the low-dose requirements of the thyroid hormone drugs. During the past decade, the FDA implemented rigorous potency standards for thyroid related drug products such as Synthroid®, Unithroid®, Levothroid®, Levolet® and Levoxyl®. The very low dosage needed for therapeutic effect was susceptible to potency degradation during and after manufacturing, and the low dosage challenged manufacturing techniques for provision of a uniform tablet-to-tablet dosage. Endocrinologists know a patient being treated for hypothyroidism could experience the complete range of dosing—from an ineffective dose to an overdose—principally due to the instability of levothyroxine (T4) or liothyronine (T3).
In response to the potency variability, manufacturers employed various formulation techniques to improve the stability of these delicate and sensitive active ingredients. Regulatory mandates can typically only serve as patches to inherent problems when invention is required to completely resolve a serious problem. The FDA’s effort to narrow the release specification for these products defined an outcome, but not a means by which the desired result could be routinely obtained. Not surprisingly, the industry has remained handicapped with product quality often jeopardized. At the root of the stability and potency issue was a need to improve the inherent stability of the active ingredients prior to their formulation into dosage products.
Fortunately, Pisgah Labs has prepared thyroid hormone active ingredients in salt forms which exhibit unprecedented stability. Since the improved stability occurs at the active ingredient level, formulation demands are significantly lessened. With improved active ingredient stability, the formulation and manufacturing requirements are comparatively uncomplicated and can principally address the dosage and batch-to-batch uniformity.
Pisgah Labs is currently employing this and related technologies in drug product development activities which enhance the physical and chemical performance features of existing active ingredients and drug products. In a related area of intellectual property, Pisgah has identified a platform technology for imparting abuse deterrent features to the highly abuse opioid-base products such as hydrocodone, oxycodone, morphine, hydromorphone and oxymorphone. For those interested in additional information, please visit www.pisgahlabs.com.
Contact: Todd Stamps
803-212-8224 FOR IMMEDIATE RELEASE
Pisgah Labs, Inc. Announces Patent Issuance. Readies 11th Application Focused on ADD/ADHD Compositions of Abuse Deterrent Drugs
PISGAH FOREST, NC, June 28 PRNewswire/- Pisgah Labs, Inc. a drug product development company and an active pharmaceutical ingredient manufacturer is pleased to announce the May 18, 2010 issuance of US Patent 7,718,649. This patent culminates several years work and investment by Pisgah Labs, Inc. ( http://www.pisgahlabs.com) to demystify the physical states of Imipramine Pamoate drug substances. The patent also covers methods of manufacturing, purifying and use of the drug in pharmaceutical preparations, and marks the first allowance in a related series of applications pending before the UnitedStates Patent and Trademark Office (USPTO) (http://www.uspto.gov/main/patents.htm).
Further, Pisgah will soon file on its discoveries regarding abuse-deterrent formulations for the treatment of Attention Deficit Disorder (ADD)/Attention Deficit Hyperactivity Disorder (ADHD). In the past few years the Food and Drug Administration (FDA) ( http://www.fda.gov) has assertively engaged pharmaceutical companies to address America’s drug abuse epidemic as guided by the FDA’s Risk Evaluation and Mitigation Strategy (REMS) initiative. Pisgah’s patent filing regarding AD(H)D drugs is timely given the significant abuse of this disorder’s treatment medications. FDA has announced a 2-day public meeting to obtain input from stakeholders who have raised concerns about the impact of REMS on the healthcare system including prescribers, pharmacists and other affected stakeholders ( http://www.fda.gov/Drugs/NewsEvents/ucm210201.htm).
The industry’s challenge is to provide medically necessary products such as ADHD medications yet impede abuse. Pisgah’s technology enables the drug to perform properly when used for the intended medical purpose, yet perform poorly when abused or misused. In addition to basic abuse deterrent features, Pisgah has refined their technology to yield products which are unaffected by alcohol consumption. Pisgah’s technology is also applicable to a host of opioid controlled substances. Since the technology relies on salt formation, essentially any controlled substance containing a basic nitrogen will succumb to conversion to an abuse deterrent form. Therefore, a predictable product development cycle for abuse deterrent products is available to narcotics such as oxycodone, hydrocodone, morphine, oxymorphone, hydromorphone and methadone.
Law enforcement and supply chain security are also addressed within Pisgah’s technology. The platform affords a forensic methodology for addressing drug trafficking, diversion, counterfeiting and crime scene analysis by imparting a track-and-trace capability. This feature covers the actual active ingredient, and formulations can be adjusted to provide a chemical “fingerprint” for a specific manufacturer. A simple analysis will be sufficient for the DEA to determine if the drug was illegally diverted (and from where) or for Customs to determine if the drug is a counterfeit. It would appear Pisgah’s multi-level, abuse deterrent platform is a promising route to alleviating drug abuse which continues to increase at an alarming rate in America.
Pisgah’s technology is based on new salt forms of active ingredients exhibiting well-known patient safety and efficacy. However, the new salts demonstrate medicatious release when used as intended, but the salt lacks sufficient solubility in the mucosal membranes and won’t afford the “high” when abused. This feature also complicates the extraction of the active ingredient from the formulated dosage, and unlike other products on the market, crushing the tablet has no effect on releasing the controlled substance (for abuse).
Pisgah has advanced their technology platform to the final dose product development stage in preparation for FDA regulatory filings. Currently, Pisgah is seeking partnerships or licensing agreements to rapidly introduce these important products which will improve patient safety and health for all Americans.
Contact: Todd Stamps 803-212-8224 or tstamps@pisgahlabs.com
FOR IMMEDIATE RELEASE
Pisgah Labs Receives Notice of Patent Allowance
PISGAH FOREST, NC – March 26, 2010. Pisgah Labs, a drug product development company and an active pharmaceutical ingredient manufacturer (API) located in western North Carolina has received a patent allowance in a series of patent applications. The US Patent & Trademark Office (USPTO) has notified Pisgah Labs, Inc. (www.pisgahlabs.com) that a patent application related to a therapeutically significant family of pharmaceutical polymorphic compositions of imipramine pamoate has been allowed. The patent application also includes methods of manufacturing, purifying and use in pharmaceutical preparations.
Interestingly, imipramine is reported to exhibit therapeutic benefit besides the treatment of depression. Imipramine has been used in the treatment of fibromyalgia, childhood nocturnal enuresis and other types of urinary incontinence, trichotillomania, post-traumatic stress disorder, panic disorder and to provide analgesic-like relief for neuropathic pain. Researchers have reported a relationship between imipramine binding, serotonin uptake and the link between fibromyalgia and depression. Medical treatments for fibromyalgia are well documented on the University of Maryland Medical Center’s website:
http://www.umm.edu/patiented/articles/what_medical_treatments_fibromyalgia_000076_10.htm.
In regard to imipramine pamoate, used in the well known product, Tofranil PM®, some may say activity level required was disproportionate to the achievement. “Not so” says Pisgah’s president, Bill Bristol. “From what we learned while focused on this imipramine we have leveraged this knowledge into a new business opportunity for the Company. Our discoveries led to additional patent filings related to abuse-deterrent prescription drugs like oxycodone and hydrocodone. We realized we could apply our findings to pain products to achieve selective dissolution profiles. From our early work with imipramine, we’re now heavily engaged in developing abuse-deterrent forms of narcotics including hydrocodone—the most abused drug in America”.
Pisgah Labs’ intellectual property development has led to more than ten filed applications related to market and regulatory desirable performance features like ineffectiveness when snorted or injected; and grinding or chewing has no effect on accelerating active ingredient release. Extraction of the active, or to practice a dangerous abuse route called “dose dumping” is dramatically hindered. Observations so far indicate the chemistry is applicable to all of the potentially abused drugs. Pisgah is activelydeveloping a product stable of anti-abuse opioid products and breathing life into medically necessary, but often abused pain medications.
Pisgah anticipates additional patent allowances soon supporting its commercial (imipramine) efforts and the broader foray into abuse-deterrent products. To learn more about these opportunities and Pisgah’s technology licensing program, visit www.pisgahlabs.com
Contact:
Todd Stamps 803-212-8224 tstamps@pisgahlabs.com
Pisgah Labs, Inc. Tackles Prescription Drug Abuse As It Files Eighth Patent
PISGAH FOREST, N.C., Jan. 12, 2010 – According to the Office of National Drug Control Policy (http://www.whitehousedrugpolicy.gov/), prescription drug abuse is more prevalent than abuse of cocaine, heroin and methamphetamine. In fact, in the past year, prescription drug abuse ranked second only to marijuana use. In the face of this growing problem, Pisgah Labs, Inc. (http://www.pisgahlabs.com) has just filed its eighth patent application on a technology that promises to curb prescription drug abuse.
While large pharmaceutical companies have been unable to stop abuse of their prescription drugs -- particularly opiate-based drugs -- Pisgah Labs has been quietly working behind the scenes to create an anti-abuse chemical methodology that will work with the pain medications most often abused in the U.S. Now, with its eighth patent application filed on the technology, Pisgah Labs is working on receiving FDA approval to conduct clinical trials on the anti-abuse technology -- the company’s first offering in a lengthy product pipeline. The goal: to demonstrate the technology will interrupt and prevent drug abuse throughout the supply chain.
In developing its technology, Pisgah Labs focused on the six basic factors it says are necessary to reduce drug abuse. That focus paid off: The company’s research and development has yielded a tamper-proof technology capable of containing multiple mechanisms to inhibit abuse. With the technology, the active ingredient in a prescription drug cannot be easily or cheaply extracted. The anti-abuse properties are not defeated by chewing, grinding or otherwise physically manipulating the prescription drug. What’s more, when combined with Pisgah Labs’ anti-abuse technology, a drug’s active ingredient release rate is unaffected by alcohol consumption, rendering abusersunable to “dose dump” on demand by consuming alcohol in conjunction with the drug. The technology even has a built-in track-and-trace feature. But perhaps most importantly, while allowing a prescription drug to work as intended when taken as directed, Pisgah Labs’ anti-abuse technology causes the drug to not work at all when abused.
“In general, routes of abuse administration start with the ability to defeat the modified release properties the drug product contains or to circumvent the chemical and mechanical barriers intentionally designed into the product,” explained Bill Bristol, president and CEO of Pisgah Labs. “Pisgah’s platform technology addresses the drug abuse issue at the active ingredient level, which is then formulated into the actual dosage medication as a tablet or capsule. In this manner, the principle anti-abuse property starts at the molecular level with the active ingredient. Formulation can then provide additional defensive barriers to abuse.”
In other words, if Pisgah Labs has anything to say about it, it won’t be long before prescription drug abuse is on a steep decline. Though it still has to demonstrate clinical results to the FDA, the company is confident its patent-pending anti-abuse technology is up for the challenge. To learn more, visit http://www.pisgahlabs.com.
Dr. Cliff King Pisgah Labs, Inc. 828-884-2789 x223 crking@pisgahlabs.com