RespireRx Pharmaceuticals Inc. Announces Patent Filings Claiming Novel Lipid Based Formulations for Insoluble Compounds, Including Cannabinoids Such as Dronabinol
BY GlobeNewswire
— 8:00 AM ET 03/23/2022
Glen Rock, N.J., March 23, 2022 (GLOBE NEWSWIRE) -- RespireRx Pharmaceuticals Inc. ( RSPI) (“RespireRx” or the “Company”), a leader in the discovery and development of innovative and revolutionary treatments to combat diseases caused by disruption of neuronal signaling, in association with Jeffrey King Managing Attorney at Patent Networks Law Group, is pleased to announce that it has filed a provisional patent application describing novel lipid based formulation technology (LFT) that may be used to improve the solubility and bioavailability of poorly soluble drugs, particularly cannabinoids. Low aqueous solubility is a major problem encountered during the formulation development of drug molecules, with an estimated 70% of current drug research pipelines containing such molecules. Because of its recent use in the formulation of mRNA vaccines for COVID-19, LFT has become a focus for formulation research efforts.
ResolutionRx, our business unit focused on pharmaceutical cannabinoids, has been developing dronabinol (a synthetic form of ?9-tetrahydrocannabinol (“THC”)) that acts upon the nervous system’s endogenous cannabinoid receptors. Dronabinol was approved in 1985 by the FDA as Marinol® for the treatment of AIDS-related anorexia and later for the treatment of chemotherapy-induced nausea and vomiting. Using the commercial form of dronabinol, we have successfully completed two Phase 2 clinical trials demonstrating significant reductions in the major symptoms of obstructive sleep apnea (OSA). However, based on these results and those from pharmacokinetic studies, we have concluded that expansion of dronabinol’s use into OSA and other therapeutic indications will require new, improved formulations. As it is commercially sold, dronabinol is formulated as a sesame oil emulsion in a soft gelatin capsule that suffers from poor and highly variable absorption, low blood levels resulting from rapid and extensive (approximately 80%) first pass liver metabolism, as well as a relatively brief half-life (approximately 2 – 3 hours) requiring high doses in order to achieve sustained, therapeutic blood levels for 4 hours or longer.
In order to circumvent these problems, we have designated certain important properties around which we have created a number of lipid nanoparticle (LNP) formulations of dronabinol, three (3) of which (i) display appropriate water solubility and dissolution to improve absorption, (ii) nano-particle size and resistance to stomach acid conditions in order to reduce first pass liver metabolism and achieve higher and longer blood levels, as well as (iii) stability and ease of manufacturing to support commercial scale. Pending additional financing (availability of which cannot be assured), we plan to test these formulations in animal and human pharmacokinetic (PK) and pharmacodynamic (PD) studies. We believe that the development of a novel, proprietary formulation of dronabinol would not require significantly longer time to market entry compared to what would be required if we were to use the currently available soft gel capsule technology.
“We are very enthusiastic about our new LFT and its potential use in the development of formulations for a broad range of drugs, particularly our new dronabinol formulations. We believe that they may broaden the dronabinol market to include not only OSA but other indications, as well. For example, we believe that while dronabinol is approved for AIDS-related anorexia, its potential use in a broader form of the condition such as anorexia nervosa or avoidant restrictive food intake disorder (ARFID) would benefit from our improved formulations. Since dronabinol already has been approved for AIDS-related anorexia, we believe that a treatment specific formulation of dronabinol could be brought to market rapidly,” said Dr Arnold Lippa, Chief Scientific Officer, Interim President and Interim Chief Executive Officer and Executive Chairman of the Board. “The pharmaceutical use of cannabinoids is beginning to realize commercial expansion and we believe that our new technology can have significant impact.”
