Drug – bio-affecting and body treating compositions – Extract – body fluid – or cellular material of undetermined... – Derived from mollusk
Reexamination Certificate
2000-07-05
2002-02-12
Lankford, Jr., Leon B. (Department: 1651)
Drug, bio-affecting and body treating compositions
Extract, body fluid, or cellular material of undetermined...
Derived from mollusk
C424S520000, C424S522000, C424S523000
Reexamination Certificate
active
06346278
ABSTRACT:
FIELD OF THE INVENTION
This invention relates in general to a preparation having anti-inflammatory, and particularly anti-arthritic, activity which is a lipid extract of mussels, including the New Zealand green lipped mussel,
Perna canaliculus
, and the blue mussel
Mytilus edulis.
BACKGROUND OF THE INVENTION
There is at the present time a significant medical need for new anti-inflammatory and anti-arthritic drugs with reduced side effects and prolonged in vivo activity and in particular for compounds which will moderate the progress of the arthropathies. Plants and other living cells offer a vast reservoir of compounds which have pharmacological effects on humans. Natural products have frequently been the source of effective drugs and lately there has been an increased interest in the analysis of these natural products, especially where a clinical benefit is claimed. Marine organisms contain metabolites that can act as pharmacological agents and aid in the treatment of inflammation.
An anti-inflammatory activity of
Perna canaliculus
(New Zealand Green Lipped Mussel) was first implicated as part of a pharmacological study on leukaemia. Initial assessment of the anti-inflammatory activity of
Perna canaliculus
was first attempted using a polyarthritis model in rats
1
. These studies however failed to show the presence of any significant anti-inflammatory activity in the mussel preparation. In contrast, Miller and Ormrod
2
using a carrageenin-induced paw oedema assay
3
, were able to show that mussel preparations, when administered intraperitoneally, gave a significant reduction in the swelling of a carrageenin-induced rat paw oedema. Subsequently, they fractionated a non-dialysable, water-soluble fraction from the mussel preparation that possessed anti-inflammatory activity. The aqueous extract showed a dose-ependent anti-inflammatory activity when administered intraperitoneally and could not be detected upon oral administration of the mussel powder. It was suggested that the water-soluble fraction therefore contained an irritant component possessing apparent anti-inflammatory activity.
Rainsford and Whitehouse
4
also reported that freeze-dried powdered preparations of the whole mussel given orally to rats showed some modest anti-inflammatory activity in the carrageenin-induced paw oedema assay, and that this material strikingly reduced the gastric ulcerogenicity of several non-steroidal anti-inflammatory drugs in rats and pigs.
Use of the whole mussel extract in the treatment of both rheumatoid arthritis and osteoarthritis in human patients has also been reported
5
.
Initial work leading to the present invention based on lipid extracts from
Perna canaliculus
powder prepared using solvent extraction techniques (in contrast to earlier work on aqueous fractions), established that the lipid fractions show a measure of anti-inflammatory activity when tested in appropriate model systems. A reliable source of lipid extract of
Perna canaliculus
and
Mytilus edulis
has subsequently become available through the procedure of supercritical fluid extraction (SFE). The lipid extract is obtained as a dark yellow-brown viscous oil exhibiting strong ultraviolet absorbing character which is consistent in physical data to lipid extracts obtained from earlier solvent extraction procedures.
SUMMARY OF THE INVENTION
Accordingly to one aspect, the present invention provides a method of anti-inflammatory treatment of a human or animal patient, which comprises administration to the patient of an effective amount of a lipid extract of
Perna canaliculus
or
Mytilus edulis.
In another aspect, the present invention provides an anti-inflammatory composition comprising a lipid extract of
Perna canaliculus
or
Mytilus edulis
as an active component thereof, together with one or more pharmaceutically acceptable carriers and/or diluents.
In yet another aspect, the invention extends to the use of a lipid extract of
Perna canaliculus
or
Mytilus edulis
in the preparation of a composition for anti-inflammatory treatment of a human or animal patient.
DETAILED DESCRIPTION OF THE INVENTION
The terms “anti-inflammatory treatment” and “anti-inflammatory composition” as used herein, relate to treatment of, or compositions for treatment of inflammatory conditions in general, including arthritic conditions such as osteoarthritis and rheumatoid arthritis, as well as in treatment of multiple sclerosis and various viral infections. Activity of a compound for use in such treatment may be demonstrated using standard assays, for example using a carrageenin-induced paw oedema assay or by the ability to beneficially limit the onset or progression of an experimental polyarthritis, as described in detail herein.
Preferably, the lipid extract which is used in the treatment or composition of the present invention is an extract prepared by supercritical fluid extraction (SFE) of freeze-dried powdered mussel using a cryogenic fluid (such as cryogenic fluid CO
2
) as the extracting medium. In comparison to solvent extraction techniques, supercritical fluid extraction using cryogenic fluid CO
2
produces a lipid extract rich in non-polar lipids, particularly in free fatty acids. While the exact composition of the lipid extract has not yet been established, it is known to contain not only free fatty acids (including unsaturated fatty acids), but also triglycerides and cholesterol esters.
A variety of administration routines are available. The particular mode selected will depend, of course, upon the particular condition being treated and the dosage required for therapeutic efficacy. The methods of this invention, generally speaking, may be practised using any mode of administration that is medically acceptable, meaning any mode that produces therapeutic levels of the active component of the invention without causing clinically unacceptable adverse effects. Such modes of administration include oral, rectal, topical, nasal, transdermal or parenteral (e.g. subcutaneous, intramuscular and intravenous) routes. In particular, the lipid extract of the present invention has been found to be active when administered orally, subcutaneously and transdermally.
Transdermal administration of the lipid extract is a particularly preferred administration mode, as the lipid extract has been found to have surprising anti-inflammatory activity when administered transdermally.
The compositions of this invention may conveniently be presented in unit dosage form and may be prepared by any of the methods well known in the art of pharmacy. Such methods include the step of bringing the active component into association with a carrier which constitutes one or more accessory ingredients. In general, the compositions are prepared by uniformly and intimately bringing the active component into association with a liquid carrier, a finely divided solid carrier, or both, and then, if necessary, shaping the product.
Compositions of the present invention suitable for oral administration may be presented as discrete units such as capsules, cachets, tablets or lozenges, each containing a predetermined amount of the active component, in liposomes or as a suspension in an aqueous liquid or non-liquid such as a syrup, an elixir, or an emulsion.
Compositions suitable for parenteral administration conveniently comprise a sterile aqueous preparation of the active component which is preferably isotonic with the blood of the recipient. This aqueous preparation may be formulated according to known methods using those suitable dispersing or wetting agents and suspending agents. A sterile injectable preparation may be formulated as a sterile injectable solution or suspension in a nontoxic parenterally-acceptable diluent or solvent, for example as a solution in polyethylene glycol and lactic acid. Among the acceptable vehicles and solvents that may be employed are water, Ringer's solution and isotonic sodium chloride solution. In addition, sterile, fixed oils are conventionally employed as a solvent or suspending medium. For this purpose, any bland fixed oil ma
Kalafatis Nicolette
Macrides Theodore
Lankford , Jr. Leon B.
Pharmalink International Limited
Pillsbury & Winthrop LLP
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