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Formulation of a mixture of free-B-ring flavonoids and flavans as a therapeutic agent

A technology of mixtures and rings, applied in the field of mixture preparations of unsubstituted B-ring flavonoids and flavans as therapeutic agents, which can solve the problems of lack of cardiovascular side effects

Inactive Publication Date: 2008-05-07
UNIGEN
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

This reduced blood flow and limitation of nutrient and oxygen delivery may tip the balance in favor of AMI in sensitive patients (Bing and Lomnicka (2002) J. Am Coll. Cardiol 39:521)
[0014] In conclusion, recent evaluations of cyclooxygenase isoforms and their functions have demonstrated that the lack of appreciable COX-1 inhibition is a contrast to the observations observed with Vioxx (rofecoxib) and other highly selective COX-2 inhibitors. A plausible explanation for the associated increase in cardiovascular side effects

Method used

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  • Formulation of a mixture of free-B-ring flavonoids and flavans as a therapeutic agent
  • Formulation of a mixture of free-B-ring flavonoids and flavans as a therapeutic agent
  • Formulation of a mixture of free-B-ring flavonoids and flavans as a therapeutic agent

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0112] Example 1 describes a general method for preparing the extract. This extraction method yielded organic and aqueous extracts from each of the species studied. The extraction results of various species are listed in Table 2. In order to efficiently identify active compounds derived from plant extracts, a high-throughput fractionation method was used, as described in Example 2. Briefly, active organic and aqueous extracts were fractionated using two different methods, respectively. Fractions were collected on 96 deep well plates. Each fraction was then tested for biological activity.

Embodiment 3

[0113] Example 3 describes the isolation, purification and characterization of active Free-B-Ring flavonoids contained in organic extracts of Scutellaria orthocalyx. Referring to FIG. 1 , ten compounds are illustrated, in which baicalin was identified as the main active ingredient.

Embodiment 4

[0114] Example 4 and Table 3 list the content and amount of Free-B-Ring flavonoids in five active plant extracts from three different plant species. Free-B-Ring flavonoids are much more present in organic extracts than in aqueous extracts.

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PUM

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Abstract

The present invention provides a composition of matter comprised of a mixture of two specific classes of compounds --Free-B-Ring flavonoids and flavans- referred to herein as UP736 for use in the prevention and treatment of diseases and conditions related to platelet aggregation and platelet-induced thrombosis. The invention further provides a novel composition of matter comprised of UP736 in combination with injectable or oral anticoagulants, antiplatelet agents, non-steroidal anti-inflammatory drugs (NSAIDs) and COX-2 selective inhibitors and a method for using said composition in the prevention and treatment of diseases and conditions related to platelet aggregation and platelet-induced thrombosis. Finally, this invention provides a method for using UP736 in combination with anti-platelet, anti-coagulant, prophylaxis agents and NSAIDs as a means for reducing the dosage of these agents, decreasing the side effects associated with acute or chronic administration of these agents; counteracting or antagonizing the risks of acute or chronic administration of these agents and for achieving additional and / or multiple clinical benefits.

Description

field of invention [0001] The present invention relates to the prevention and treatment of diseases and conditions involving platelet aggregation and platelet-induced thrombosis. In particular, the present invention relates to a novel composition comprising a mixture of two special classes of compounds, Free-B-Ring flavonoids and flavans, also referred to in the present invention as UP736, for the prevention and treatment of Diseases and conditions mediated by platelet aggregation and platelet-induced thrombosis. The present invention also relates to the use of UP736 together with injectable or oral anticoagulants, antiplatelet agents, non-steroidal anti-inflammatory drugs (NSAIDs) and COX-2 selective inhibitors as an adjuvant and / or synergist, and / or synergists. Finally, the present invention relates to methods of using UP736 in combination with antiplatelet agents, anticoagulants, prophylactics and NSAIDs as a means of reducing the doses of these drugs, reducing side effec...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A01N43/04A01N43/16A61K31/35A61K31/70
CPCA61K31/353A61K36/48A61K36/54A61K31/405A61K36/53A61K31/365A61K36/185A61K31/415A61K45/06A61K31/727A61K31/366A61K36/15A61K36/60A61K31/192A61K36/906A61K36/47A61K36/28A61P29/00A61P43/00A61P7/02A61P9/00A61P9/10A61K31/70
Inventor 贾琦赵垣
Owner UNIGEN
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