Drug – bio-affecting and body treating compositions – Designated organic active ingredient containing – Heterocyclic carbon compounds containing a hetero ring...
Reexamination Certificate
1999-07-02
2001-01-16
Krass, Frederick (Department: 1614)
Drug, bio-affecting and body treating compositions
Designated organic active ingredient containing
Heterocyclic carbon compounds containing a hetero ring...
C518S721000, C518S721000, C518S721000, C518S721000
Reexamination Certificate
active
06174876
ABSTRACT:
BACKGROUND OF THE INVENTION
The present invention relates to the use of pure boswellic acid, a physiologically acceptable salt, a derivative, a salt of said derivative or a vegetable preparation containing boswellic acid for the production of a pharmaceutical composition for the treatment of brain tumours.
The present invention also relates to the use of pure boswellic acid, a physiologically acceptable salt, a derivative, a salt of said derivative or a vegetable preparation containing boswellic acid for the treatment of brain tumours.
The possibilities known to date for the therapeutical treatment of brain tumours are unsatisfactory:
So far, the possibilities for a treatment of malignant brain tumours are insufficient. Neurosurgical removal of the brain tumours represents severe surgery and, depending on type, size and position of the brain tumours, in many cases does not lead to the complete removal of the malignant tumours. For these reasons, the average survival of the patients suffering from malignant brain tumours is only about 9 months even after a combined treatment including surgery and radiotherapy. An additional chemotherapy using the cytostatics known so far is able to achieve a prolongation of the survival of only about 10% (Lesser, G. J., Grossman S., The chemotherapy of high-grade astrocytomas, Seminars in Oncology, 1994, 21:220-235).
Glucocorticosteroids have been used for the symptomatic treatment which, however. are not able to effectively reduce the peritumoural brain oedemas so that their use does achieve the desired success.
Therefore, it is an object of the present invention to provide the use of preparations useful for the treatment of brain tumours, the inhibition of the peritumoural brain oedema as well as the growth of tumour cells, and for the destruction of the tumour cells. In particular. there is provided a preparation which, without exhibiting the side effects and the reduced efficiency accompanying the use of the cytostatics employed to date for the therapy of tumours, allow a significantly more efficient treatment of brain tumours. The pharmaceutical composition or preparation, respectively, provided according to the invention is intended to show a lower toxicity and, therefore, to be well tolerated by the patients. Much research has been carried out to provide a pharmaceutical composition of that type (De Vita, D., Helman, S., Rosenberg, S. A. (eds.), Cancer—Principles and Practice of Oncology, 4th edition, 1993, J. B. Lippincott Company, Philadelphia; Lesser, G. J., Grossman, S., The chemotherapy of high-grade astrocytomas, Seminars in Oncology, 1994, 21:220-235), documenting the high demand for the creation of such a pharmaceutical composition.
Now, it has been surprisingly found that boswellic acid, a physiologically acceptable salt, a derivative, a salt of said derivative or a vegetable preparation containing boswellic acid is effective for the treatment of brain tumours.
India's ayurvedic medicine uses pharmaceutical compositions containing preparations from the plant
Boswellia serrata
for the treatment of inflammation but also of rheumatism. However, there are no publications containing evidence as to the treatment of brain tumours using these pharmaceutical compositions. Due to the efficacy of preparations from the plant
Boswellia serrata
in the treatment of inflammable diseases this gum has already been examined with respect to its components. Thus, Pardhy & Bhattacharyya report (Ind. J. Chem., 16B:176-178, 1978) that
Boswellia serrata
contains essentially the following components:
&bgr;boswellic acid, acetyl-&bgr;-boswellic acid, acetyl-11-keto-&bgr;-boswellic acid, 11-keto-&bgr;-boswellic acid.
SUMMARY OF THE INVENTION
So far, no research is known concerning the efficacy of these compounds for the treatment of brain tumours.
In the following, the structural formulas of boswellic acid and some of its derivatives are shown:
As boswellic acid, there is preferably used &bgr;-boswellic acid which according to references has been isolated from
Boswellia serrata
or other known plants containing boswellic acid. The &bgr;-boswellic acid may contain, in minor amounts &agr;- or &bgr;-boswellic acid. As physiologically acceptable salts of boswellic acid, there may be used the sodium, potassium, ammonium, calcium salts. As derivatives of boswellic acid, there may be used lower alkyl esters obtained by esterification of the carboxyl group with an C
1
-C
6
alcohol, preferably the methyl ester, or esters obtained by esterification of the hydroxyl group with a physiologically acceptable carboxylic acid. Preferred derivatives are &bgr;-boswellic acetate, &bgr;-boswellic formate, &bgr;-boswellic acid methyl ester, acetyl-&bgr;-boswellic acid, acetyl-11-keto-&bgr;-boswellic acid, and 11-keto-&bgr;-boswellic acid.
DETAILED DESCRIPTION OF THE INVENTION
Further, according to the invention it is possible to use a vegetable preparation containing boswellic acid. According to the invention, there are used preparations obtained from the gum of Boswellia species (olibanum, incense).
Plants containing boswellic acid (syn.: boswellinic acid) are:
Boswellia
(
serrata, papyrifera, frereana, carteri, thurifera, glabra, bhaw
-
dajiana, oblongata, socotrana
and other members of this family).
An ethanolic extract from the gum of
Boswellia serrata
containing the above mentioned boswellic acids proves to be especially efficient: the application of this preparation—in the following referred to as phytopharmacon H 15 (produced and sold by the company Ayurmedica, Pöcking)—allows within a treatment period of seven days to achieve a reduction of the peritumoural brain oedema of 22 to 48%. A histopathological examination of the tumour tissue of the patients treated shows to be necrotic as far as possible, a fact that is extraordinarily exceptional. The vitality of the explanted cells is extraordinarily low and is about 3.5 to 4.5% in cell cultures. Usually, the vitality of such cells is about 80%. In contrast to the cells of untreated patients, the cells of the treated tumour tissue show no tendency to proliferate within two weeks.
These experiments show that H 15 inhibits the peritumoural brain oedema as well as tumour growth and leads to the death of the tumour cells.
Further, according to the invention there is the possibility that the use is carried out together with other chemically pure pharmaceutical agents and/or other vegetable drugs. Examples for such other chemically pure pharmaceutical agents are the following:
Cytostatics, e.g. nimustine, carmustine, lomustine, methyl lomustine, semustine, methotrexate, teniposide, dacarbacine, procarbacine, temozolamide, topotecane, paclitaxel. streptococine, cisplatin, 5-fluoro uracil; glucocorticosteroids, such as dexamethasone, prednisolone, methyl prednisolone, prednisone, hydrocortisol, cloprednole, betamethasone.
An example for such a vegetable drug is vincristine.
According to the invention, the boswellic acid is administered as required. Since it has a low toxicity, the dosage is not critical and can be easily varied by the physician depending on the severity of the disease, the weight of the patient to be treated and the duration of the treatment.
For example, unit dosages may be administered once to four times per day. The exact dose depends on the route of administration and the condition to be treated. Naturally, it can be required to carry out routine variations of the dose depending on the age and weight of the patient as well as the severity of the disease state.
The preparations used according to the invention can be formulated in a manner known per se using one or more of pharmaceutically acceptable carriers or diluents. The preparations can be formulated for oral, parenteral, rectal, intracranial or intrathecal administration. Preparations of the compounds for oral administration are preferred.
The pharmaceutical preparations for oral administration may be in the form of tablets or capsules prepared according to procedures known per se together with pharmaceutically acceptable diluents, such
Ammon Hermann P. T.
Simmet Thomas
Akin, Bump, Strauss, Hauer & Feld, L.L.P.
Krass Frederick
Thomas Simmet
LandOfFree
Use of boswellic acid for treating brain tumors does not yet have a rating. At this time, there are no reviews or comments for this patent.
If you have personal experience with Use of boswellic acid for treating brain tumors, we encourage you to share that experience with our LandOfFree.com community. Your opinion is very important and Use of boswellic acid for treating brain tumors will most certainly appreciate the feedback.
Profile ID: LFUS-PAI-O-2461449