Pharmaceutical composition for improving or preventing progression of chronic kidney disease
Inventors
SINGH, Ankit Shyam • MISHRA, Vedprakash • TONGRA, Neelima
Assignees
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Publication Number
US-10973782-B2
Publication Date
2021-04-13
Expiration Date
Abstract
The present application relates to a pharmaceutical composition/formulation for improving or preventing progression of chronic kidney disease (CKD) caused due to inflammation and/or Klotho under expression. More particularly, the invention relates to a composition/formulation comprising a synergistic combination of Palmitoylethanolamide (PEA), Cholecalciferol and one or more natural ingredients. The invention also provides various formulations and methods of preparing the same.
Core Innovation
The patent describes a CKD disease-modifying pharmaceutical composition intended to improve or prevent progression of chronic kidney disease driven by inflammation and/or Klotho under-expression. The composition centers on a synergistic combination that includes palmitoylethanolamide (PEA), one or more naturally occurring Fatty Acid Amine Hydrolase (FAAH) inhibitor(s), and cholecalciferol (vitamin D3).
The natural FAAH inhibitors are described as selectable exemplars including quercetin, myricetin, isorhamnetin, kaempferol, pristimerin, biochanin A, genistein, daidzein, and combinations thereof. The document also provides extensive ingredient ranges for component amounts and formulation/dosage-form options, together with optional natural antioxidants, vitamins, and co-enzymes.
The document reports preclinical testing in a 5/6 nephrectomy rat model, including reductions in serum creatinine, blood urea nitrogen (BUN), and interleukin-6 (IL-6), and increases in glomerular filtration rate (GFR/eGFR) for combinations of PEA plus a natural FAAH inhibitor plus cholecalciferol versus individual components. It also reports safety/no mortality and histopathology/necroscopy observations.
Claims Coverage
The partial content identifies one independent claim, directed to a pharmaceutical composition defined by three components with specific weight-percent ranges for PEA and cholecalciferol, and related refinements add further component selections and formulation limits.
Weight-percent combination of PEA, natural FAAH inhibitors, and cholecalciferol
A pharmaceutical composition comprising 30 to 65% by wt. Palmitoylethanolamide (PEA), one or more naturally occurring Fatty Acid Amine Hydrolase (FAAH) Inhibitors, and 0.11 to 10% by wt. Cholecalciferol.
Selectable naturally occurring FAAH inhibitors
A pharmaceutical composition in which the naturally occurring FAAH inhibitor is selected from Quercetin, Myricetin, Isorhamnetin, Kaempferol, Pristimerin, Biochanin A, Genistein, Daidzein, or combinations thereof.
Quantified FAAH inhibitor weight-percent range
A pharmaceutical composition that includes a naturally occurring FAAH inhibitor in an amount ranging from 0.5 to 60% by weight of the composition.
Quantified natural antioxidant amount
The pharmaceutical composition includes a natural antioxidant amount that is within 0.04 to 50% by weight of the composition.
Specified pharmaceutically acceptable excipients
A pharmaceutical composition in which pharmaceutically acceptable excipients are chosen from specified excipient types or combinations thereof, including diluent, disintegrant, binder, lubricant, glidant, solubilizing agent, solvent, and combinations thereof.
Oral dosage-form formulation categories
A pharmaceutical composition formulated into oral dosage forms including tablet, capsule, pill, hard capsule filled with liquid or solid, soft capsule, sachet, powder, granule, suspension, solution, or modified release formulation.
Coverage centers on a pharmaceutical composition combining PEA with one or more naturally occurring FAAH inhibitors and cholecalciferol, with refinements specifying particular FAAH inhibitor selections, quantitative weight-percent ranges, optional natural antioxidant content, allowable excipients, and oral dosage-form categories.
Stated Advantages
Improves or prevents progression of chronic kidney disease driven by inflammation and/or Klotho under-expression.
Reduces serum creatinine and blood urea nitrogen (BUN) and reduces interleukin-6 (IL-6) in the reported 5/6 nephrectomy rat study.
Increases glomerular filtration rate (GFR/eGFR) in the reported 5/6 nephrectomy rat study for the combination versus individual components.
Reports safety/no mortality in the reported preclinical study and includes histopathology/necropsy observations consistent with improved kidney function.
Documented Applications
Use in a CKD disease-modifying pharmaceutical composition intended to improve or prevent progression of chronic kidney disease driven by inflammation and/or Klotho under-expression.
Preclinical evaluation in a 5/6 nephrectomy induced CKD rat model with group comparisons for combinations versus individual components.
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