2.3.
De (oorspronkelijke) Engelse tekst van de conclusies van EP 868 luidt als volgt:
1. The use of synthetic piperine or an extract containing piperine for the manufacture of a composition for increasing gastrointestinal nutrient absorption in a subject at a dose of no more than 0.15 mg/kg of body weight of said subject.
2. The use according to claim 1, wherein said dose is 0.0004 to 0.15 mg/kg of body weight for oral administration.
3. The use according to claim 1, wherein said dose is 0.00004 to 0.015 mg/kg of body weight for topical or parenteral administration.
4. The use of synthetic piperine or an extract containing piperine for the manufacture of a composition for increasing lean body mass in a subject.
5. The use according to anyone of the previous claims, wherein said extract containing piperine comprises at least
one member selected from the group consisting of an extract from black pepper and an extract from long pepper.
6. The use according to anyone of the previous claims, wherein said subject is a human.
7. The use according to anyone of the previous claims, wherein said composition comprises at least one additional
material selected from the group consisting of herbal extracts, water-soluble vitamins, fat-soluble vitamins, amino
acids, minerals and antioxidants.
8. The use according to claim 7, wherein said herbal extracts are selected from the group consisting of an extract
from roots of zingiber officinale, ginseng extract, curcumin, boswellin, ashwagandha, ginkgo biloba, capsaicin and
aconitine, said water-soluble vitamins are selected from the group consisting of vitamin B1, vitamin B2, niacinamide, vitamin B6, vitamin B12, folic acid and vitamin C, said fat-soluble vitamins are selected from the group
consisting of vitamin A, vitamin 0, vitamin E and vitamin K, said antioxidants are selected from the group consisting
of vitamin A, vitamin C, vitamin E, alpha-carotene, trans-beta-carotene, beta-cryptoxanthin, Iycopene, lutein/ze-axanthin, pine bark bioflavonals complex, germanium, selenium and zinc, said amino acids are selected from the
group consisting of lysine, isoleucine, leucine, threonine, valine, tryptophan, phenylalanine, methionine and L-selenomethionine, and said minerals are selected from the group consisting of calcium, iron, zinc, vanadium, selenium, chromium, iodine, potassium, manganese, copper and magnesium.
2.5.
In de beschrijving van het octrooi is onder meer het volgende opgenomen:
[0027] Subject matter of the present invention is the use of synthetic piperine or an extract containing piperine for
the manufacture of a composition for increasing gastrointestinal nutrient absorption according to claim 1, and for in-
creasing lean body mass, according to claim 4. Dependent claims 2, 3 and 5 to 8 relate to preferred embodiments
thereof.
[0028] The preparations manufactured according to the use of the present invention improve the bioavailability of
nutritional compounds. The compositions manufactured according to the use of the present invention increase gastrointestinal absorption, improve crossing over through certain biological barriers such as respiratory lining, urinary lining, blood brain barrier and skin, and systemic utilization of certain nutrients and biological compounds.
[0029] The compositions manufactured according to the use of the present invention contain, as an essential ingredient, piperine. This compound may be obtained as an extract from the fruit of piper nigrum comprising at least 98% piperine. Alternatively, the compositions may be prepared from an extract of the fruit of piper Iongum. Piperine made synthetically may also be used in the present invention. Compositions used according to the present invention may also contain extract from roots of zingiber officinale, with the active ingredients 6-gingerol and 6-shogoal. The compositions may be formulated with the extract from fruit of piper nigrum, extract from fruit of piper longum, and extract from fruits of zingiber officinale combined in any weight ratio. Preferred weight ratios include 2:2:1, 1:1:1,2:1:1, and 1 :2:1.
[0030] As a daily supplement taken with a nutrient or nutrients by an average healthy adult, piperine is effective and safe in a broad dose range. A preferred effective dose range of piperine for oral use to enhance gastrointestinal nutrient absorption is 0.0004-0.15 mg/kg/day. The recommended dose of piperine for a healthy individual for oral use is approximately 5 mg/person/day. The recommended dose in cases of clinically diagnosed nutritional deficiencies is up to 15 mg/person/day in divided doses, i.e., 5 mg every six hours (in the morning, at noon, and in the evening). When used as a preparation for topical or parenteral use to improve crossing over through a biological barrier, the compositions manufactured according to the use of the present invention contain, as an essential ingredient, 0.00004-0.015 mg/kg of body weight of piperine. The nutritional materials are used in nutritionally effective amounts.
[0031] Black pepper contains approximately 5-9% piperine and is listed by the FDA as an herb which is generally
recognized as safe (GRAS) for its intended use as spice, seasoning, or flavoring. The bioenhancing dose of piperine as used in the present invention is a maximum of approximately 15 mg/person/day, or no more than 20 mg/day in divided doses, which corresponds to from several thousands to up to 40,000 times less than the LD50 dose of piperine, as established in various experiments on rodents.
[0032] The active ingredient of the present invention may be prepared by a process which produces piperine of a purity greater than 98%.
(…)
Description of the Preferred Embodiments
[0052] Many of the nutrients, biological compounds and nutritional supplements which may be included in the compositions manufactured according to the use of the present invention are available commercially. Particularly, vitamin, mineral, amino acid and antioxidants are available commercially. The herbal compounds are generally used in powder form which is a dried ethanol extract of a particular plant. For example, Boswellic acid is from an ethanol extract of Boswellia serrata roots. Ginsenosides are from an ethanol extract of Ginseng roots. Withanaloids are from an ethanol extract of Whitania somnifera plant. Gingko flavinoids are from an ethanol extract of Gingko biloba plant. Curcuminoids are from ethanol extract of Cucuma longa plant. Pycnogenol is from an ethanol extract of Pinus pinaseter bark. Proanthocyanidins are from an ethanol extract of pine bark. Some of the herbal compounds are also available commercially from a variety of sources. The piperine in the invention may be produced by the new method of isolation of piperine shown in Example 14, below. The compound obtained in this manner has the trademark name of Bioperine® . Alternatively, piperine may be provided by the prior art methods or made synthetically.
[0084] A preparation obtained in a unique manufacturing process.
[0085] Commercially available Black pepper oleoresin or Long pepper oleoresin is used as the source of piperine. Ground up Black pepper or Long pepper can also be used.
[0086] To a mixture of butanol and hexane (35 liters), 35 kg Black pepper oleoresin is added and heated to 40°C.
The mixture is then cooled and filtered.
[0087] The precipitate is washed with Butanol/hexane mixture to obtain crude piperine.
[0088] The crude piperine is dissolved in methanol at 60°C and treated with alumina and charcoal by stirring. It is then filtered and concentrated under vacuum to obtain a powder.
[0089] Bioperine®
[0090] Material thus prepared has the following specifications: Color: Pale yellow crystalline powder
[0091] Melting range: 128 degrees - 131 degrees Celsius
[0092] Assay: min. 98% pure piperine (by HPLC)