Pharmaceutical composition containing pentacyclic triterpenoids
Inventors
ZENDEJAS HERNANDEZ, Ulises • SMITH OGARRIO, Alicia Teresa • GUTIÉRREZ SMITH, Mercedes
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Assignees
Member
TIMSER S.A.P.I. de C.V.TIMSER S.A.P.I. de C.V. is a biomedical company in Mexico developing accessible and non-invasive blood-based screening solutions for early detection of cervical cancer and its precursor lesions. The company leverages more than a decade of research to advance clinically validated molecular diagnostics using protein biomarkers identified through proteomics and molecular biology approaches. These technologies address barriers to traditional screening and are backed by extensive national and international patent coverage and clinical trial validation involving hundreds of participants.
TIMSER S.A.P.I. de C.V. is a biomedical company in Mexico developing accessible and non-invasive blood-based screening solutions for early detection of cervical cancer and its precursor lesions. The company leverages more than a decade of research to advance clinically validated molecular diagnostics using protein biomarkers identified through proteomics and molecular biology approaches. These technologies address barriers to traditional screening and are backed by extensive national and international patent coverage and clinical trial validation involving hundreds of participants.
Publication Number
US-11931372-B2
Publication Date
2024-03-19
Expiration Date
Abstract
This invention refers to pharmaceutical compositions containing synergistic combinations of pentacyclic triterpenoids as active principles and denotes that some specific combinations between these types of drugs exhibit effects for the prevention or inhibition of viral infections. The compositions are found in specific quantities and proportions that enhance the pharmacological properties of the compounds, improving their bioavailability and pharmacokinetic properties, while reducing their toxicological and irritability effects, especially in the respiratory tract and the lungs.
Core Innovation
This patent describes pharmaceutical compositions comprising synergistic combinations of pentacyclic triterpenoids, principally glycyrrhizic acid (GA) and 18β‑glycyrrhetinic acid (EN), formulated for nasal, oral and inhalation administration and other routes to prevent and treat ACE2‑mediated respiratory viral infections such as SARS‑CoV‑2. The compositions are presented for use in inhibiting Spike–ACE2 interaction and improving therapeutic performance relative to single agents.
The document reports experimental evidence that GA–EN combinations inhibit Spike–ACE2 binding more effectively than single agents, that combination nebulized administration reduces local irritability and toxicity relative to individual components in murine inhalation histopathology, and that human inhalation pharmacokinetics show increased and ratio‑dependent systemic exposure and altered metabolization. Preferred formulations and concentration ranges are disclosed in the specification; [procedural detail omitted for safety].
Claims Coverage
The independent claim defines three inventive features.
Synergistic pentacyclic triterpenoid composition
A pharmaceutical composition that comprises a synergistic combination of at least two pentacyclic triterpenoids to be used for the treatment of viral infections.
Inclusion of 18β‑glycyrrhetinic acid and glycyrrhizinic acid
The at least two pentacyclic triterpenoids comprise 18β‑glycyrrhetinic acid and glycyrrhizinic acid.
Defined 18β‑glycyrrhetinic acid to glycyrrhizinic acid ratio
A ratio of the 18β‑glycyrrhetinic acid to the glycyrrhizinic acid is 1:5 to 1:25.
The claim covers a pharmaceutical composition for treating viral infections comprising a synergistic combination of pentacyclic triterpenoids specifically including 18β‑glycyrrhetinic acid and glycyrrhizinic acid, with a defined ratio of 18β‑glycyrrhetinic acid to glycyrrhizinic acid of 1:5 to 1:25.
Stated Advantages
Enhanced inhibition of Spike–ACE2 interaction by GA–EN combinations compared to single agents.
Improved bioavailability and increased systemic exposure (AUC) with ratio‑dependent effects and altered metabolization following inhalation.
Reduced local irritability and toxicity on inhalation for combinations versus individual components.
Documented Applications
Prevention and treatment of ACE2‑mediated respiratory viral infections, for example SARS‑CoV‑2.
Administration via nasal, oral and inhalation routes, including nebulized formulations, and cutaneous and injectable routes disclosed in the specification.
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