Bend Research Inc. a leading independent drug-formulation development and manufacturing company, announced that it has received a new US patent covering the use of polymer additives to improve and sustain the bio-availability of low-solubility drugs in the human body.
The patent protects formulations that enhance the absorption of low-solubility drugs by blending the drug with an additive, resulting in improved bio-availability. There is a growing need for this technology, since it is estimated that more than 40% of drugs in development have low aqueous solubility. Use of these polymer additives means lower drug doses can be used to achieve better therapies for these drugs.
The technology works by sustaining high concentrations of drug in the gastrointestinal tract. “This technology is on target with our mission of advancing our clients’ best new medicines,” said Bend Research president and CEO Rod Ray. “It provides one more way we can help our customers provide novel therapies to treat illnesses that desperately need new approaches.” “Pharmaceutical industry leaders acknowledge that discovering and bringing these new compounds forward is very complicated,” Ray observed, “and Bend Research scientists and engineers are well known for providing key assistance to leading pharmaceutical companies facing this challenge.”
The patent covers blending solubility-improved drug forms with solubility-enhancing polymer additives. Drug forms covered by the patent are nano-particles, absorbed drugs, drugs in nano-suspensions, supercooled drug melts, cyclodextrin/drug forms, gelatin dosage forms, and soft-gel dosage forms. Often, such drug forms dissolve rapidly in the GI tract and then precipitate to low-solubility forms before they can be absorbed.
Blending these drug forms with a solubility-enhancing polymer provides a simple way to keep the compounds in solution so they can be absorbed. Solubility-enhancing polymers sustain high concentrations of drug in the GI tract by inhibiting crystallization or precipitation of the drug to a lower-solubility drug form.
The patent is one in a growing number of formulation- and process-related patents associated with Bend Research’s solubility-enhancing drug-formulation technologies. These solubilization technologies enhance the concentration of drug in patients’ bloodstreams and enable faster drug dissolution than is possible with crystalline drug forms. The patent, which is titled “Pharmaceutical Compositions Comprising Drug and Concentration-Enhancing Polymers,” was assigned Patent No. 7,887,840 by the US Patent and Trademark Office.
The inventors are Dwayne Friesen, Bend Research vice president of Research, and former Pfizer employee William Curatolo. The patent is assigned to Bend Research Inc. This patent complements a number of patents that use spray-drying to create amorphous dispersions. The technology covered by this patent does not require spray-drying or Hot-Melt Extrusion (HME) formulation to improve bio-availability, but rather involves conventional blending of the drug form with a polymer additive.
Bend Research technologies have successfully enabled the advancement of hundreds of compounds from preclinical studies to several large Phase 3 clinical trials.
Bend Research provides formulation and dosage-form support, assists in process development and optimization, manufactures clinical-trial quantities of drug candidates in its cGMP facility, and advances promising drug candidates from conception through commercialization.