Drug – bio-affecting and body treating compositions – Designated organic active ingredient containing – Cyclopentanohydrophenanthrene ring system doai
Reexamination Certificate
1999-09-02
2002-06-18
Jarvis, William R. A. (Department: 1614)
Drug, bio-affecting and body treating compositions
Designated organic active ingredient containing
Cyclopentanohydrophenanthrene ring system doai
C514S863000
Reexamination Certificate
active
06407085
ABSTRACT:
This application is 391 of PCT/EP98/00227 filed Jan. 16, 1998.
The object of the invention is a medicament which contains betasitosterol—phytoserol mixtures and/or betasitosterol and its physiological metabolites. Processes for dissolving betasitosterol, which in itself is difficult to dissolve, in various oils, paraffins, and glycerins were discovered which open new indications for the use of these substances. In addition, the esterification of betasitosterol with carboxylic acids opens up therapeutic possibilities for asthma, enflamed intestinal diseases, arterial hypertension, autoimmnune diseases of the skin, and for relieving pain which extend far beyond the currently known range for the use of betasitosterol and/or phytosterol/betasitosterol mixtures.
Naturally occurring phytosterols are usually a mixture of various sterols (e.g., campesterol, stigmasterol, among others), the most important component of which is the betasitosterol. For example, it can be derived as an extract from plants, including soy beans or saw palmetto berries by known methods. For decades it has been used in medicine with two indications:
1. As a medication for benign prostatic hyperplasia.
2. As a cholesterol resorption inhibitor.
The substance is practically nontoxic and interferes with the release of eicosanoic acid from biomembranes, as a result of which inflammation processes are retarded. A drawback is its insolubility; accordingly it attains a resorption quotient of only around 5% in healthy subjects. A further drawback is that at elevated doses, as it is used for lowering lipids, the resorption quotient and thus the systemic bioavailability drops drastically, i.e., almost no resorption takes place (saturation kinetic).
The use of betasitosterol is extremely low in side effects. Even in the case of oral administration of up to 24 g per day, a blood count of only 10 mg is reached due to the low resorption quotient. In the organism, it is 60% to 75% glucoronidated and around 20% is metabolized into cholic acid (C
23
H
36
(OH)
3
COOH) and chenodesoxycholic acid (C
23
H
37
(OH)
2
COOH). Cholic acid is further reduced by intestinal bacteria into desoxycholic acid.
The percutaneous use of betasitosterol and/or its physiologic metabolites in diseases of the skin and the subcutaneous tissue is unknown. In like manner, no areas of application are known for betasitosterol/phytosterol mixtures in oral administration other than the indications “benign prostatic hyperplasia” and “cholesterol resorption inhibition.”
It is known that the resorption quotient, distributability, and excretion quotient, in short the pharmacokinetics of a preparation, are very strongly dependent not only on its chemical partners, but also on its physical solubility in various media.
REFERENCES:
patent: 4260603 (1981-04-01), Pegel et al.
patent: 5487900 (1996-01-01), Itoh et al.
patent: 5574063 (1996-11-01), Perricone
patent: 5709868 (1998-01-01), Perricone
patent: 5965618 (1999-10-01), Perricone
patent: 35 46 360 (1987-06-01), None
patent: 0 358 970 (1990-03-01), None
patent: 0 509 656 (1992-10-01), None
patent: 0 514 328 (1992-11-01), None
patent: 645167 (1995-03-01), None
patent: 0 203 277 (1996-12-01), None
patent: 938 937 (1963-10-01), None
patent: 2 238 476 (1991-06-01), None
patent: 63 156 727 (1988-06-01), None
patent: 02 025 425 (1990-01-01), None
patent: 07 277 986 (1995-10-01), None
patent: 07 304 684 (1995-11-01), None
patent: 08 081 352 (1996-03-01), None
patent: 08 104 632 (1996-04-01), None
patent: 09 169 659 (1997-06-01), None
patent: 2 069 557 (1996-11-01), None
patent: 1 138 162 (1985-02-01), None
Antan et al., Spectrophotometric . . . , Khim.-Farm Zh., vol. 29/6, pp. 57-61, 1995.*
Marteau et al, Action of cholic and chenodeoxycholic . . . , Can. J. Physio. Pharmacol. vol. 58/9, pp. 1058-1062, 1980.*
Marugo et al., Effects of ursodeoxycholic acid . . . , IRCS Medical Science, vol. 7/10, pp. 531, 1979.*
Deschner et al, The influence of dietary . . . , Precancerous lesions Gastrointest. Tract.-1983, pp. 219-221, 1981.
Banner & Witcoff , Ltd.
Jarvis William R. A.
Kim Vickie
LandOfFree
Medicament containing betasitosterol and/or... does not yet have a rating. At this time, there are no reviews or comments for this patent.
If you have personal experience with Medicament containing betasitosterol and/or..., we encourage you to share that experience with our LandOfFree.com community. Your opinion is very important and Medicament containing betasitosterol and/or... will most certainly appreciate the feedback.
Profile ID: LFUS-PAI-O-2900914