Drug – bio-affecting and body treating compositions – Plant material or plant extract of undetermined constitution... – Containing or obtained from cucumbrits
Reexamination Certificate
2001-10-26
2003-06-10
Prats, Francisco (Department: 1651)
Drug, bio-affecting and body treating compositions
Plant material or plant extract of undetermined constitution...
Containing or obtained from cucumbrits
C424S776000, C424S725000, C514S159000, C514S165000
Reexamination Certificate
active
06576274
ABSTRACT:
FIELD OF THE INVENTION
This invention relates to the preparation and use of biologically active celery seed extracts that alone and in combination with drugs and herbal medicines can be used to prevent and treat pain, inflammation and gastrointestinal irritation.
BACKGROUND OF THE INVENTION
The prevention or inhibition of inflammation and pain is of significant concern, particularly for those afflicted with arthritis and other musculoskeletal ailments, including sports-related injuries. Pain usually accompanies inflammation and vice versa.
Acute and chronic pain and inflammation are often treated with anti-inflammatory/analgesic compounds such as aspirin, ibuprofen and naproxen (K. D. Rainsford (1996) New Developments in Anti-Rheumatic Therapy. CRC Press Inc, Boca Raton). There are, however, appreciable risks from these drugs in particular gastro-intestinal ulceration and bleeding (Rainsford ibid). While another commonly-used pain-killing drug, acetaminophen does not have this side-effect, its benefits and range of uses is limited because it does not have anti-inflammatory activity. Acetaminophen is less effective in control of pain because it does not control the inflammatory reactions that often accompany pain, especially that from chronic conditions such as arthritis (Rainsford ibid). Furthermore, there is considerable concern about use of acetaminophen, especially at over-the-counter doses, because of the risks of severe and, rarely, irreversible liver damage that can lead to death (K. D. Rainsford and M. C. Powanda (1998) Safety and Efficacy of Non-prescription (OTC) Analgesics and NSAIDS, Kluwer Academic Publishers, Dordrecht; R. P. Rapp et al (1997) The Pill Book Guide to Over-the-Counter Medications. Bantam Books, New York).
Prostaglandins are a family of compounds that have been identified as playing a significant role in inflammation. Prostaglandins are produced throughout the body and are derived from enzymatic action on a common substrate, arachidonic acid. The first step in prostaglandin synthesis is the oxygenation of arachidonic acid by the enzyme cyclooxygenase. The oxygenated prostaglandin precursors are subject to further enzymatic processes which provide the various members of the prostaglandin family.
Recently, new anti-inflammatory/analgesic drugs have been developed that have been claimed to have lower propensity to cause gastro-intestinal ulcers and bleeding. These drugs have been designed to specifically inhibit the activity of cyclo-oxygenase-2 (COX-2). They do not, in contrast, affect the production of those prostaglandins that are derived from another enzyme, cyclo-oxygenase-1 (COX-1), which are important for protection of the gastro-intestinal tract against injury either from irritating substances or bacteria.
COX-1 is inhibited by aspirin and other older anti-inflammatory/analgesic drugs and this is a major factor underlying their ulcer-producing activity (Rainsford ibid). Some recent evidence suggests, however, that these new COX-2-selective drugs may not be without some gastro-intestinal irritancy, and may even have other adverse effects in the kidney in a similar manner to that from the older anti-inflammatory/analgesics. It is clear that there is a need for drugs that have anti-inflammatory and analgesic activity comparable with that of aspirin and related drugs but without the gastrointestinal ulcerogenic effects and bleeding that occurs with these drugs.
Relevant Literature
Wild celery is noted in the Ayurvedic pharmacopoeia for treatment for headaches and as a diuretic and spasmolytic (CRC Handbook of Ayurvedic Medicinal Plants, 1990, p 44, CRC Press Inc., Boca Raton). It is included in the 1983 British Herbal Pharmacopoeia as a treatment for arthritis and gout. The seed oil is used in perfumery, for flavoring food products and liqueurs, and also as a cercaricide. According to the Physician's Desk Reference for Herbal Medicines (1998, Medical Economics Company Inc, Montvale N.J.), “Preparations of celery are used as a diuretic, for blood purification, for regulating elimination of the bowels, for glandular stimulation, rheumatic complaints, gout, gall and kidney stones. Celery is also used for weight loss due to malnutrition, for loss of appetite, exhaustion and as a prophylactic for nervous unrest. The efficacy for the claimed applications is not documented.”
Lewis et al. (Int. J. Crude Drug Res., 1985;23:27-32) claimed anti-inflammatory compounds were present in aqueous extracts of the stem of cultivated celery. They could not identify the major active compounds, merely describing them as “unidentified polar substance(s)”.
Preclinical assessment of over the counter medications, including herbal medicines, available in Australia for the treatment of arthritis and rheumatism demonstrated that some, but clearly not all, celery seed extracts, have the capacity to treat and prevent inflammation (Whitehouse M W et al. Inflammopharmacology, 1999:7:89-105).
An International Patent Application, WO 95/00157 (Applicant: MOBIUS CONSULTANCY PTY. LTD.; Inventor: B. Daunter) makes claims for relief of inflammatory complaints based on plant extracts of the genus Umbelliferae, especially celery, parsley and dill, particularly citing alcohol-soluble purported constituents of the celery seed oil, namely phthalides, isobenzofurans, naphthoquinones, and some derivatives, e.g., isoindolones.
Indian process patent A.P.R. No. 445/1M/94 was issued in 1994 to Life Care Products Limited for a method of preparing pharmacologically active extracts from celery seed.
SUMMARY OF THE INVENTION
Compositions and methods are provided for the prevention and treatment of pain, inflammation and gastrointestinal irritation. The compositions comprise a purified, biologically active extract of celery seed, and may further be co-formulated with an additional analgesic or anti-inflammatory compound, e.g. non-steroidal anti-inflammatory drugs (NSAID), herbal medicines, etc. The compositions may be formulated for use in oral or topical preparations. Preparations of interest include pharmaceutical preparations, foods, lotions, and the like.
In a preferred embodiment, the biologically active extract of celery seed is prepared by supercritical fluid extraction. An alcoholic extract of fresh celery seed is mixed with a suitable adsorbant, and then subjected to supercritical fluid extraction. Optionally, the resulting product is further treated or fractionated. This product may be prepared in a pharmaceutical formulation for treatment of inflammation, pain, and/or gastrointestinal irritation.
In one embodiment of the invention, a biologically active formulation of celery seed extract is administered to provide a gastroprotective effect, or for the healing of gastrointestinal ulcers. In another embodiment of the invention, a combined formulation with an NSAID reduces or prevents gastrointestinal irritation associated with the NSAID activity. Such a combined formulation with an NSAID may also provide for a synergistic treatment of inflammation and pain.
DETAILED DESCRIPTION OF THE PREFERRED EMBODIMENTS
Purified extracts of celery seed are provided for use in pharmaceuticals to treat pain, inflammation and gastrointestinal irritation. These extracts may also be co-formulated with other analgesic or anti-inflammatory compounds, e.g. non-steroidal anti-inflammatory drugs (NSAID), herbal medicines, etc. In particular, the purified extracts are used in methods to relieve acute, as well as chronic pain and inflammation, and to provide gastroprotection, e.g. against drug-induced gastrotoxicity, ulcer healing, etc.
A preferred celery seed extract is produced by supercritical fluid extraction of the starting product. This supercritical fluid extract is characterized by a 5-10 fold increase in specific activity when tested in an experimental model of polyarthritis which was induced in rats by injecting a mycobacterial arthritogenic adjuvant, Whitehouse et al. (1997) Inflammopharmacology 5:237-246. This supercritical fluid extract also includes more highly purified fractions derived therefrom. In
Butters Desley Ethel
Davis Craig Kendall Charles
McGeary Ross Peter
Powanda Michael Christopher
Rainsford Kim Drummond
Bozicevic Field & Francis LLP
Coe Susan D.
International Celery Development Alliance Pty. LTD
Keddie James S.
Prats Francisco
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