Drug – bio-affecting and body treating compositions – Preparations characterized by special physical form – Tablets – lozenges – or pills
Reexamination Certificate
2001-03-16
2002-11-05
Page, Thurman K. (Department: 1615)
Drug, bio-affecting and body treating compositions
Preparations characterized by special physical form
Tablets, lozenges, or pills
C424S451000, C514S023000, C514S024000, C514S025000, C514S054000
Reexamination Certificate
active
06475520
ABSTRACT:
FIELD OF THE INVENTION
The present invention relates to the pharmaceutical composition with low toxicity for anti-inflammation and anti-exudation. Particularly, this pharmaceutical compositon contains as active components escin compounds of general formula I and general formula II obtained from the ESCIN as well as a pharmaceutical carrier and excipient .
BACKGROUND
The ESCIN is an active component for anti-inflammation and anti-exudation, which is obtained by extraction from dry and ripen seed of the plant of Aesculus (buckeye). Recently the injection of ESCIN is wildly applied in clinic for the treatment of cerebral edema complicating dysfunction of brain, burn, scald, chronic incompetence of vein, wound, fracture, edema and hematoma after the operation. Even so, because of higher toxicity and side effects of ESCIN (LD
50
is 3.99 mg/kg only) with its stronger stimulation after administrating, this drug is restricted during the clinical use. The Japanese Laid Open Hei 10-17591 disclosed some anti-inflammatory agents containing the compounds of formula IA, IB or the mixture of them.
Therefore, it is still necessary to develop some pharmaceutical compositions with low toxicity and low side effects for anti-inflammation and anti-exudation.
OBJECT OF THE INVENTION
The object of the present invention is searching for and developing some pharmaceutical compositions with low toxicity and low side effects for anti-inflammation and anti-exudation.
SUMMARY OF THE INVENTION
The inventors have made wide and deep study and discovered that the compositions containing escin having the general formula I and II maintain the ESCIN having activity of anti-inflammation and anti-exudation by the ESCIN, and the toxic action and side effects are lowered simultaneously. The present invention is accomplished thereby. Consequently the present invention relates to a new pharmaceutical composition including escin compounds with formula I and II as well as a pharmaceutical carrier or excipient. Such composition retaining the activity of ESCIN simultaneously can greatly lower the toxicity and side effect of ESCIN.
According to the present invention, the term “escin with general formula I” used in the present application refers to such a stereoisomer which is consisted of 21-position (Z) (cis-form) and (E) (trans-form) of general formula I.
According to the present invention, the term “escin with general formula II” used in the present application refers to such a stereoisomer which is consisted of 21-position (Z) (cis-form) and (E) (trans-form) of general formula II.
REFERENCES:
patent: 10017591 (1998-01-01), None
patent: 10-017591 (1998-01-01), None
Matsuda et al. Bio L. Pharm. Bull. 1997, 20(10), 1092-1095.*
Matsuda et al. 1997, 7(13), 1611-1616.*
Biol. Pharm. Bull. (1997), 20 (10), 1092-1095.
Bioorg. Med. Chem. Lett (1997), 7 (13), 1611-1616.
J. Smooth, Muscle. Res. (1996), 32 (5), 219-228.
Chem. Pharm. Bull. (1998), 46 (11), 1764-1769.
Li Shixu
Liu Shuyan
Liu Wanhui
Su Kajia
Zhang Qingchun
Burns Doane Swecker & Mathis L.L.P.
Channavajjala Lakshmi
Page Thurman K.
Shandong Luye Pharmaceutical Co., Ltd.
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