Drug – bio-affecting and body treating compositions – Antigen – epitope – or other immunospecific immunoeffector – Bacterium or component thereof or substance produced by said...
Patent
1981-07-22
1983-06-21
Friedman, Stanley J.
Drug, bio-affecting and body treating compositions
Antigen, epitope, or other immunospecific immunoeffector
Bacterium or component thereof or substance produced by said...
A61U 31485
Patent
active
043894046
DESCRIPTION:
BRIEF SUMMARY
FIELD OF THE INVENTION
The present invention relates to the art of medicine and, more specifically, to a pain-killing preparation featuring a long-lasting analgetic effect.
STATE OF THE ART
Pain-killers (analgetics) widely employed at the present time such as promedol, pontapone, and morphine provide but a short-time analgetic effect. After serious operations such as oncological ones a multiple administration of such preparations is necessary (4-5 times a day) which is associated with the risk of adaptation. A short-time effect of these analgetics provides a number of disadvantages during a long-time transportation of patients with pronounced pain syndroms, as well as complicated operation of the medical personnel in the case of pain-killing in incurable patients both at home and in stationaries. With all this in consideration, preparations with a long-time analgetic effect are of a great importance for medicine.
The duration of the analgetic effect during pain-killing procedures can be extended by introduction, into an aqueous solution of the analgetic, of a high-molecular compound such as poly-N-vinylpyrrolidone (PVP). A known pain-killer consists of poly-N-vinylpyrrolidone, morphine hydrochloride and water (Experimental Surgery and Anestesiology, No. 6, 1971, p. 70, "Meditsina" Publishing House /in Russian/). In this pain-killer use is made of said high-molecular compound with a molecular mass of from 40,000 to 80,000).
Administration of this pain-killing preparation provides a constant concentration of morphine hydrochloride in blood plasma for a long time period thus ensuring a long duration of the pain-killing effect (more than 24 hours in 34.5% of patients). As a result, it has become possible to effect a single intramuscular injection of the preparation instead of 4-6 usual injections of common analgetic. In contrast to pure morphine hydrochloride, the pain-killer does not cause inhibition of breathing and does not cause nausea and vomiting nausea, exerts a retarding effect on the intestinal perilstatics and does not affect the cardio-vascular system due to the fact that concentration of morphine hydrochloride in blood is insignificant.
However, this pain-killing preparation possesses a number of disadvantages. A high concentration of poly-N-vinylpyrrolidone with a molecular mass of from 40,000 to 80,000 (60%) in water is responsible for a high viscosity of the solution. This hinders its intramuscular injection and necessitates the use of special needles for administration of the preparation by means of a syrynge; a lasting infiltration of tissues at the site of administration of the pain-killer takes place.
Furthermore, in a polymer with the above-mentioned molecular mass up to 6% by weight of fractions are present which have a molecular mass of from 250,000 to 750,000. This is highly undesirable, since these high-molecular fractions are detailed in the organism.
DISCLOSURE OF THE INVENTION
The present invention is directed to a pain-killing preparation which possesses a more lasting pain-killing effect, contains no high-molecular fractions detailed in the organism and which, upon its administration, would not cause lasting infiltration of tissues.
This object is accomplished by a pain-killing composition consisting of poly-N-vinylpyrrolidone, morphine hydrochloride and water, wherein, according to the present invention poly-N-vinylpyrrolidone is used with a molecular mass of from 30,000 to 40,000 at the following concentrations of the components, g, per liter of water:
______________________________________ poly-N--vinylpyrrolidone
250 to 310
morphine hydrochloride 5 to 6.25
______________________________________
The pain-killing preparation according to the present invention comprises a low-viscosity transparent liquid of a yellowish color.
In comparison with the analgetics currently available in the medicinal practice, the pain-killer according to the present invention possesses a high analgetic activity, provides no irritating effect on tissues and its toxicity is not diff
REFERENCES:
patent: 4038397 (1977-07-01), Merz et al.
patent: 4083981 (1978-04-01), Yamamoto et al.
Experimental Surgery & Anesthesiology, No. 6, (1971) p. 70 ("Meditsina", Moscow).
Bairamov Jury J.
Karaputadze Temuri M.
Kirsh Jury E.
Shumsky Viktor I.
Zhorov Vladimor I.
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