Drug – bio-affecting and body treating compositions – Designated organic active ingredient containing – Having -c- – wherein x is chalcogen – bonded directly to...
Patent
1999-10-28
2000-12-05
Reamer, James H.
Drug, bio-affecting and body treating compositions
Designated organic active ingredient containing
Having -c-, wherein x is chalcogen, bonded directly to...
546 44, 546 46, A01N 4342
Patent
active
061567647
DESCRIPTION:
BRIEF SUMMARY
TECHNICAL FIELD OF THE INVENTION
The present invention relates to morphine and diamorphine salts of anionic non-narcotic analgesics belonging to the type of substituted carboxylic acids, preferably the morphine and diamorphine salts of diclofenac (Formula 1). The present invention further relates to processes for their production, the use of these salts in the treatment of diseases, as well as to pharmaceutical preparations comprising these salts.
BACKGROUND OF THE INVENTION
Pain is one of the most frequent signs of a disease or a damage. Though pain is to be understood as a warning and protective function of the organism, patients concerned generally call for pain-killing or at least pain-relieving substances. For this reason, one of the most important concerns in medicine is to provide such substances. The function of these substances, so-called analgesics, is to reduce or suppress the sensation of pain when given in therapeutic doses without having a general narcotic effect in these doses. Based on their potency, therapeutic mechanism and side effects one distinguishes between two groups of analgesics: very potent analgesics acting on the central nervous system and low to moderately potent ones primarily having a peripheral action. Active substances acting on the central nervous system frequently involve a habit-forming potential which might develop into addiction. Morphine (Formula 3a) is one example of an active substance acting on the central nervous system and having such a risk. In the form of its inorganic salts, for example its hydrochloride or sulfate, morphine is commercially available for parenteral or peroral application to control acute posttraumatic or postoperative pain, as well as chronic pain, for example, in the state of advanced cancer.
A derivative of morphine, diacetylmorphine (Formula 3b), also known as diamorphine or heroin, is dealt and consumed among drug addicts without any pharmacological, pharmaceutical, or pharmacokinetic control. Its qualified use in the treatment of drug addiction is a scientific and sociological problem that has not yet been solved.
In order to reduce the risk of morphine dependence in the clinical use of morphine preparations, other analgesics, preferably non-narcotic peripheral preparations, are administered at the same time or alternately. Owing to the great variety of peripherally effective analgesics, their different potency and thus their different dosage, there is a great uncertainty concerning the choice of preparations to be combined, resulting in patient discomfort because of the amount of drugs to be taken.
SUMMARY OF THE INVENTION
It is the object of the present invention to provide new analgesics having a maximum analgesic effect with minimum side effects.
This object is achieved by the new active substances characterized in the claims and by the pharmaceutical preparations comprising these active substances.
The active substances according to the present invention are the morphine and diamorphine salts of anionic non-narcotic analgesics of the type substituted carboxylic acids. Suitable anionic non-narcotic analgesics belonging to the type of substituted carboxylic acids include: diclofenac, indomethacin, sulindac, ketoprofen, or fenbufen.
The present invention preferably includes the salts morphine-diclofenate (Formula 1a) and diamorphine-diclofenate (Formula 1b) consisting of the anionic peripheral analgesic diclofenac ([2-[(2,6-dichlorophenyl)-amino]-phenyl]-acetic acid (Formula 2)) and the cationic analgesic morphine (Formula 3a) acting on the central nervous system or its derivative diacetylmorphine (Formula 3b), also referred to as diamorphine. In Formula 1, R may represent H or CH.sub.3 CO. If R stands for H, it is morphine-diclofenate (Formula 1a); if R stands for CH.sub.3 CO, it is diamorphine-diclofenate (Formula 1b). ##STR1##
The above-mentioned non-narcotic analgesics of the type substituted carboxylic acids and their salts are known. The sodium, potassium, diethylammonium salts of diclofenac (Formula 2) ([2-[2,6-dichloroph
REFERENCES:
patent: 4404209 (1983-09-01), Schmidt
Asmussen Bodo
Muller Walter
Riess Walter
Klaniecki James E.
LTS Lohmann Therapie-Systeme GmbH
Reamer James H.
Speckman Ann W.
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