Classifications

• • A—HUMAN NECESSITIES
  • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
  • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
  • A61K31/00—Medicinal preparations containing organic active ingredients
  • A61K31/33—Heterocyclic compounds
  • A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
  • A61K31/495—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with two or more nitrogen atoms as the only ring heteroatoms, e.g. piperazine or tetrazines
  • A61K31/505—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim
  • A61K31/513—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim having oxo groups directly attached to the heterocyclic ring, e.g. cytosine
  • A61K31/515—Barbituric acids; Derivatives thereof, e.g. sodium pentobarbital
• • A—HUMAN NECESSITIES
  • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
  • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
  • A61K31/00—Medicinal preparations containing organic active ingredients
  • A61K31/60—Salicylic acid; Derivatives thereof

Definitions

• the present invention relates to a medicinal composition.
• compositions for the treatment of arthritis and associated rheumatic diseases are described as of proven benefit in the treatment of osteoarthrosis but may also be beneficial in cases of rheumatoid arthritis, ankylosing spondylitis, gout, Raynaud's diseas, Paget's disaese,
• Felty's syndrome systematic sclerosis, erato conjunctivitis, Still's disaese, chrondro-calcinosis and hydroxiapatite deposition.
• the present invention therefore includes the invention described and claimed in the said Application Serial No. 2062458 and extends the use of the composition to other disorders.
• the invention is first described in relation to the treatment of arthritis disorders.
• Rheumatoid arthritis is a very serious condition although it is seldom listed as the cause of death. Sufferers are known from statistics to have a low life expectancy and usually lead a uncomfortable existance from the onset of the disease until death. A major difficulty is that the drugs being administered often have only a transitory effect, so that greater and greater doses .are administered over long periods of time so that the side effects become pronounced. Drugs having serious side effects -could be tolerated in the treatment of arthritis if an immediate alleviation of a permanent nature could be ensured.
• the invention is based upon the original discovery that by combining two drugs having different effects, a permanent alleviation of quite serious conditions of arthritis can be effected.
• the two drugs involved are a short-acting soporific and an antipyretic which should not be of the hormone or steroid type. More specifically in accordance, with the invention there is provided a composition comprising in combination a short-acting barbiturate soporific and a non-hormone antipyretic agent having a specific activity greater than aspirin.
• the preferred barbiturate is sodium amytal (sometimes called amobarbitol, monosodium isoamyl ethyl barbiturate). This compound has the formula:
• Other pyrazolidine antipyretics as described in the said U.S . patent may be substituted, e. g. the ⁇ -cyclohexyl- derivative and the 4-n-propyl- and 4-isopropyl- derivatives of 1 :2-diphenyl- 3 :5-dioxo— pyrazolidine, and indeed more recently developed equivalent antipyretics notably of the pyrazolidine "type.
• the composition may also comprise a quantity of a soluble form of aspirin, and preferably also an ingestible form of ethyl alcohol. The aspirin is believed to agument the antipyretic effect and the alcohol accelerates the uptake of the drugs into the bloodstream. An equivalent dose of paracetamol may be substituted.
• the composition includes or is taken with a quantity of soda water.
• the composition may include a sweetening such as saccarin or a cy ⁇ lamate but should preferably not. contain any sugar. It may include ginger or other taste modifying agent.
• a preferred form of the composition may consist of:- phenylbutazone - 1 to 2 parts sodium amytal - 1 to 2 parts ingestible ethyl - 4000 to 6000 parts alcohol the balance including water together, optimally, with a non-sugar sweetening agent and/or taste modifying agent.
• the balance may include soda water and ginger.
• a suitable single dose would be 200 mg phenyl ⁇ butazone and 200 mg sodium amytal, together with 60 ml of a 65 or 70% proof spirit e.g. Scotch whisky or brandy diluted in an
• OMPI appropriate quantity e.g. 60 ml of soda water or diet giner ale.
• Such a dose suitably follows a dose of 900 mg soluble aspirin B.P.- or 650 mg paracetemol taken in •su ficient water to disolve the compound.
• composition may be sold in the form of a multiple dose elixir-.
• a suitable 10 dose elixir is as follows:—
• the aspirin may be combined in the elixir as follows:— Elixir_II (10 dose)
• some vitamin C may be incorporated.
• composition may alternatively be sold in the form of readily dissolving tablets containing citric or tartaric acid and sodium bicarbonate.
• Such tablets could readily include the aspirin component and could be dissolved in an appropriate amount of a proprietory alcoholic liquor, appropriately diluted with water or soda water or e.g., diet ginger ale.
• the effect of the composition is hereafter illustrated by reference to a clinical history.
• the patient at the periods in.question was an active man in his 60's who had been treated on a number of occasions for osteo arthrosis in one of the joints in the cervical region of the spine and also with a weak disc in the sacral bottom which had been relieved from time to time by treatment with phenylbutzone and distalgesic, together with soluble aspirin.
• the patient damaged his right knee by kicking a football. Within ten days of the incident the knee was swollen and painful and inflamed. About two months after the incident the patient visited his physician, at which time both the knee and lower leg were swollen and inflamed and resembled a thrombic condition the patient had had some years earlier. The physician arranged for examination by a vascular i expert who however diagnosed osteo arthrosis'in the knee which was confirmed by an X-ray. Examination by an arthritis specialist was delayed for six months.
• the final treatment attempted was to take 900 mg of soluble aspirin B.P. in sufficient water for dissolution and followed by 200 mg phenylbutazone and 200 mg sodium amytal taken with 60 ml of Scotch whisky and 60 ml of diet ginger ale as a stomachic medicine. Sugar was avoided to avoid increasing the output of uric acid.
• the patient immediately went to sleep and awoke 7 hours later feeling well. Upon examining his right leg he could see and feel and remarkable improvement. The swelling had subsided and the knee joint was freer and the cyst no longer pressed on the sciatic nerve, and the inflammation was generally reduced. .There was no constipation. The patient repeated the dose nightly for 7 further nights, after which all swelling had subsided and there was no more inflammation. The popliteal cyst was still evident but under no pressure .so that it was evident that excess fluid was no longer forming. In all, the
• the preferred composition as represented in the Example can lead to a complete recovery at least in certain cases of osteo arthritis. Since the treatment, if successful, is of short term, the danger from side effects is negligible and in any case the side effects from the preferred drugs are maxkedly less than those associated with e.g. steroids. Furthermore the long term effects of the drugs concerned are not a factor provided that the composition is used as advocated for a short treatment period.
• composition has been found useful in promoting growth of healthy tissue.
• the patient, after giving up the treatment is sufficiently active that recourse to surgery may be avoided.
• Example 2 Two patients contracted influenza from respective relatives who had been bed-ridden through the disease for some two weeks. A single dose of the composition as prescribed in Example 1 effectively controlled the disease to the extent that the patient was up within 72 hours. Temperaturesof over 10l°F (30.8 C) were bought down to normal within 36 hours.
• composition of the invention not only is effective in the control of arthritis but has an effect beyond this. It appears to act through the blood stream and repair damagedtissue through this process. Clearly if this ability can be brought out by further trials, it is likely to be useful in a wide range of medical disorders, notably in reversing the development of cancer if this is caught at a very early stage, through the process of repairing mutated cells in the blood stream before they reach a "rogue" condition. It has now become possible through the use of scanners to show cancerous conditions at a sufficiently early stage for this process to be applicable.
• composition acts by an accelerated healing process both within the bloodstream and by accelerated action upon the adjacent tissues as a result of the healing conditions brought about within the blood stream.
• This healing process is believed to be a syndrome of a number of factors, the two most notable being a catalytic effect upon the repair of damaged cells and the various bodily effects caused by a complete reduction of hypertension.
• the reduction of hypertension intimately associated with relief of inflammation at the wound location, with the possible addition of electrolytic catalysis of the repair mechanism are believed to be the critical contributory factors.
• composition of the invention acts by rectifying damage caused at an early stage within the bloodstream and by stimulating natural therapeutic factors.
• a blood plasma catalyst appears to be present which assists in bringing healing factors to target areas.
• the sodium ion is known to be a powerful blood catalyst and the sodium ion is a factor of importance within the composition of the invention, being present in one of the preferred compounds, sodium amytal and also in soluble aspirin.
• the choice of sodium amytal is also influenced by the knowledge that this short to medium acting soporific leads to residues (metabolised) which are easily excreted by the kidney.
• alcohol is selected from a study of the passage of drugs through cell membranes and the desirability of promoting active transport to accelerate the healing process. This can allow the drug to cross membranes even against concentration gradients.
• the concentration of sodium may require careful monitoring since it is known to be a natural constituent of full blood plasma and its addition can lead to undesirable ion gradients.
• aspirin a preferred ingredient
• the action of aspirin may be of importance in its effect in stimulating the lymph glands so speeding up the production of lymphacites and increasing the body's natural resistance towards pathogens.
• the increased ionic concentration may be an assisting factor in binding disrupted cells and other organic compounds essential to life, notably hormones and enzymes.
• Jhe sodium ion may also contribute by speeding up the oxygenation process and reducing the tendency to the formation of blood platelets, so smoothing and speeding the passage of the mixture through the blood to the target area.
• the sodium ion present in two possible ingredients may be of great catalytic importance, it is believed that the combination of the anti-inflammatory agent and soporific is critical.
• composition of the invention assists in the repair of elementary healthy building blocks within the bloodstream and in particular may assist in the healthy production of DNA and RNA which assists the body to build-up healthy tissue and destroy faulty cells.
• Speed of healing is a fundamental contributing factor since the treatment cannot be recommended over a long term, mainly due to the side effects of the prolonged usage of various of the ingredients. Nevertheless where the disease warrants - 12 -
• Example 1 a dose as prescribed in Example 1 could be used on alternative nights for sixty to ninety days with 5 extreme benefit to semi-crippled patients who would normally be housebound, enabling them to reach a sufficiently active stage to pursue a normal life.
• the invention provides a medical composition comprising in combination a short-acting barbiturate.
• Soporific e.g. sodium amytal
• a non-hormone antipyretic agent having a specific activity greater than aspirin, e.g. phenylbutazone.
• ⁇ here is also provided in accordance with the invention a process for the treatment of humans or animals which comprise the administration of one or more effective doses of the composition of the invention, for the purpose of correcting the disorders specified above.

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• Health & Medical Sciences (AREA)
• Chemical & Material Sciences (AREA)
• Medicinal Chemistry (AREA)
• Pharmacology & Pharmacy (AREA)
• Epidemiology (AREA)
• Life Sciences & Earth Sciences (AREA)
• Animal Behavior & Ethology (AREA)
• General Health & Medical Sciences (AREA)
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• Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)

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• 1981
  • 1981-05-21 AU AU71723/81A patent/AU7172381A/en not_active Abandoned
  • 1981-05-21 WO PCT/GB1981/000091 patent/WO1982003986A1/en unknown
  • 1981-05-21 EP EP19810901302 patent/EP0079329A1/de not_active Withdrawn

Non-Patent Citations (1)

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