Drug – bio-affecting and body treating compositions – Antigen – epitope – or other immunospecific immunoeffector – Conjugate or complex
Patent
1996-01-29
1999-07-20
Witz, Jean C.
Drug, bio-affecting and body treating compositions
Antigen, epitope, or other immunospecific immunoeffector
Conjugate or complex
A61K 3578
Patent
active
059253550
DESCRIPTION:
BRIEF SUMMARY
Numerous clinical studies demonstrate that extracts from the leaves and flowers and/or fruits of Crataegus species are beneficial for the treatment of patients with decreasing cardiac performance. Therapeutic experience over many years also demonstrated the therapeutic efficacy of such extracts in case of unstable functional-vegetative stenocardias as well as in case of mild forms of bradycardic arrhythmia. These findings deutschen Bundesgesundheitsamt! to publish a monograph (see Official indications:
Decreasing cardiac performance corresponding to stages I to II according to NYHA; sensation of pressure and constriction in the cardiac region; senile heart not yet requiring digitalis therapy and mild forms of bradycardic arrhythmia.
Up to the present, the known therapeutic benefit as well as the pharmacodynamic spectrum of action of these Crataegus extracts are in general explained by the presence of flavonoids and oligomeric procyanidins in the Crataegus extracts. The pharmaceutical preparations are therefore standardized to these components. One of these known Crataegus extracts (WS 1442) contains approximately 18.5 to 19.5% oligomeric procyanidins.
The invention is based on unexpected findings obtained in animal tests using rats with experimentally induced ischemia. According to these findings, an extract from leaves with flowers of appropriate Crataegus species such as Crataegus monogyna JAQUIN emend. LINDMAN, Crataegus laevigata (POIRET) DE CANDOLLE syn. Crataegus oxyacantha L. p. p. et duct., Crataegus azarolus L., Crataegus nigra WALDSTEIN et KITAIBEL and Crataegus pentagyna WALDSTEIN et KITAIBEL ex WILLDENOW, obtained by extraction with a mixture of water and a water-miscible organic solvent such as ethanol life-threatening reperfusion-induced cardiovascular lesions present are not responsible for these effects.
These effects of the Crataegus extract--in the following also called fraction (a)--allow to deduce a therapeutic application of Crataegus extracts in the prevention and treatment of short periods of cardiac ischemia (circulatory disturbances of the heart), reperfusion-caused cardiac lesions and sudden death due to cardiac arrest as well as other life-threatening reperfusion-caused pathological conditions.
Extended tests with three new fractions of this Crataegus extract indicate that the particularly active component of the Crataegus extract has a molecular weight of more than 3000 Dalton. The structure of this component is not yet known.
Description of the tests
Fraction (a) Total extract from leaves with flowers of Crataegus monogyna, laevigata, azarolus, nigra and pentagyna, obtained by extraction with ethanol 45% by weight at 60.degree. C. with a content of 18.5 to 19.5% oligomeric procyanidins;
Fraction (b) Fraction of the compounds with molecular weights of more than 3000 Dalton, obtained by means of ultrafiltration of fraction (a) using a membrane filter with a cut-off limit of 3000 Dalton;
Fraction (c) obtained by means of liquid--liquid distribution (countercurrent extraction) of fraction (a) in butanol/water;
Fraction (d) obtained from fraction (a) from which the flavonoids and proanthocyanidins have been removed through adsorption using an adsorbent which binds these compounds, in particular hydroxypropylated polydextran, polyamides, aluminium oxide or activated charcoal. (1960), 398-407! applied in male Sprague-Dawley rats with a body weight between 250 and 350 g and anaesthetised with pentobarbital. Cardiac ischemia was provoked by ligature of the coronary artery and reperfusion initiated by reopening the ligature after a 7-minute ischemia. Blood pressure and heart rate of the animals were measured prior to and during the ischemia as well as after the reperfusion; we also determined the duration and type of cardiac arrhythmia during the reperfusion phase. Under such test conditions, approximately 50% of the control animals die within a reperfusion period of 15 minutes. Causes for such mortalities are the hypotensive crisis and ventricular fibrillation induced by and occurrin
REFERENCES:
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patent: 5064675 (1991-11-01), Jensen et al.
Li et al., J Tradit Chin Med 4(4): 289-292 (1984) (Abstract).
Li et al., J Tradit Chin Med 4(4): 283-288 (1984) (Abstract).
Fang et al., Zhongcaoyao 16(12): 548-51 (1985) (Abstract).
Chatterjee Shyam Sunder
Jaggy Hermann Ernst
Willmar Schwabe GmbH & Co.
Witz Jean C.
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