EP0363355A1 - Medicament contenant des anesthesiques locaux et des nucleosides, ainsi que son emploi pour traiter des lesions musculaires - Google Patents

Medicament contenant des anesthesiques locaux et des nucleosides, ainsi que son emploi pour traiter des lesions musculaires

Info

Publication number
EP0363355A1
EP0363355A1 EP19880901040 EP88901040A EP0363355A1 EP 0363355 A1 EP0363355 A1 EP 0363355A1 EP 19880901040 EP19880901040 EP 19880901040 EP 88901040 A EP88901040 A EP 88901040A EP 0363355 A1 EP0363355 A1 EP 0363355A1
Authority
EP
European Patent Office
Prior art keywords
adenosine
muscle
medicament according
guanosine
nucleosides
Prior art date
Legal status (The legal status is an assumption and is not a legal conclusion. Google has not performed a legal analysis and makes no representation as to the accuracy of the status listed.)
Pending
Application number
EP19880901040
Other languages
German (de)
English (en)
Inventor
Wolfgang Frankhof
Klaus Thiemer
Current Assignee (The listed assignees may be inaccurate. Google has not performed a legal analysis and makes no representation or warranty as to the accuracy of the list.)
Individual
Original Assignee
Individual
Priority date (The priority date is an assumption and is not a legal conclusion. Google has not performed a legal analysis and makes no representation as to the accuracy of the date listed.)
Filing date
Publication date
Application filed by Individual filed Critical Individual
Publication of EP0363355A1 publication Critical patent/EP0363355A1/fr
Pending legal-status Critical Current

Links

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
    • A61K31/70—Carbohydrates; Sugars; Derivatives thereof

Definitions

  • the invention relates to a medicament which contains local anesthetics and one or more nucleosides or their phosphoric acid esters.
  • the invention also relates to the use of such medicaments for the treatment of muscle injuries.
  • such injuries can best be cured by immobilizing the affected muscle area over a long period of time or at least only exerting a slight load. This is associated with a longer break in work or even incapacity to work.
  • aqueous medicaments which contain certain local anesthetics and one or more nucleosides together with conventional carriers and auxiliaries meet all the requirements with regard to universal applicability, freedom from side effects and freedom from recurrence and are nevertheless highly effective.
  • the invention relates to medicaments containing in the aqueous phase 1 to 100 g / 1 of a local anesthetic, 1 to 100 g / 1 of one or more nucleosides from the group adenosine, guanosine, inosine, uridine and their water-soluble mono-, di- and triphosphate ester salts, and one or more physiologically acceptable preservatives which are compatible with the active ingredients, and, if appropriate, customary carriers and auxiliaries.
  • the invention also relates to the use of such medicaments for the local infiltration treatment of muscle injuries.
  • a large number of local anesthetics which are effective internally are suitable for the medicaments according to the invention.
  • these are local anesthetics from the group of basic acid anilides and their HCl adducts, such as, for example, l-methylpiperidine-2-carboxylic acid N- (2 '.6 r -dimethylphenyl-) amide (mepivacaine) or its hydrochloride .
  • other local anesthetics are suitable instead or together with them if they can be administered via injections.
  • the local anesthetics mentioned or related to the mentioned are used in concentrations of 1 to
  • 100 g / 1 aqueous phase preferably 10 to 30 g / 1 aqueous phase, are used in the medicament according to the invention.
  • 0.5 to 2% strength solutions of the respective local anesthetic are particularly preferably used in amounts between 1 and 20 ml per dose of the drug administered, preferably in amounts of 5 to 10 ml per dose of the drug.
  • the solutions mentioned, for example 1% solutions, of such local anesthetics are largely commercially available, for example under the names Meaverin or Scandicaine.
  • the medicaments according to the invention contain one or more nucleosides from the group adenosine, guanosine, inosine, uridine and their water-soluble mono-, di- and triphosphate ester salts as further components.
  • Certain of the nucleosides mentioned can be contained in the medicinal products. However, a mixture of all four of the nucleosides mentioned and one or more of their phosphate salts is preferred.
  • Sodium salts, acidic sodium salts and the respective nucleoside monophosphoric acids, diphosphoric acids and triphosphoric acids are preferably used.
  • adenosine, guanosine, inosine and uridine and disodium dihydrogen adenosine triphosphate, adenosine diphosphoric acid, adenosine monophosphoric acid and guanosine monophosphoric acid are used.
  • the mixing ratios of the individual nucleosides or their phosphate salts can vary within wide limits.
  • Adenosine, guanosine, inosine and uridine in a weight ratio of 5: 1: 5: 1 and also disodium dihydrogen adenosine triphosphate, adenosine diphosphoric acid, adenosine monophosphoric acid and guanosine monophosphoric acid in a weight ratio are preferred
  • the nucleosides or their mixtures can be mixed as such and in the process or thereafter dissolved in physiologically acceptable media such as water or physiological common salt solution. However, preference is given to commercially available mixtures of the nucleosides or their salts in the media mentioned, for example laevadosin 2.
  • the total concentration of the nucleoside components mentioned in the medicaments according to the invention is in the range from 1 to 100 g / l of aqueous phase, preferably in the range from 10 to 30 g / 1 aqueous phase.
  • the medicament according to the invention also contains one or more preservatives which must be compatible with the above-mentioned active ingredients.
  • preservatives which must be compatible with the above-mentioned active ingredients.
  • chlorocresol and related compounds to call are present, for example, in an amount of 0.1 to 1000 mg / l in the medicaments according to the invention.
  • the medicaments according to the invention can also contain other carriers and auxiliaries which are customary for such agents.
  • Liquids which allow administration via infiltration or injection, such as water or physiological saline, are to be regarded as such.
  • the medicinal products containing the described components can, as has surprisingly been found, be used with great success for the treatment of muscle injuries.
  • the use extends in particular to the treatment of muscle strains, muscle tears, muscle tears and muscle contusions.
  • the medicaments according to the invention are used in that they are infiltrated into the traumatized muscle area as soon as possible after the injury has occurred. This is independent of the severity and type of muscle injury, so that a differentiated diagnosis of the injury, which sometimes intervenes in the injured muscle area, can be omitted. This is advantageous because even doctors with little experience in sports medicine can use the medicines according to the invention safely and with a safe onset of action.
  • the frequency of the use of the medicaments according to the invention by infiltration fluctuates depending on the objective severity of the injury and on the subjective condition.
  • a Single use leads to freedom from pain and full functionality of the diseased muscles.
  • the frequency of application can be increased without hesitation up to one or more daily applications if the severity of the injury so requires.
  • the one-off treatment usually results in a significant reduction in complaints.
  • no relapses were observed in the muscle areas treated with the medicaments according to the invention.
  • local or systemic side effects never occurred.
  • a further advantage of the use of the medicaments according to the invention is to be seen in the fact that the slight local pain reaction which occurs shortly after the infiltration provides information about the severity of the injury and the correct application of the medicaments. This represents a further diagnostic aid since the infiltration of the medicaments according to the invention into healthy muscle tissue does not cause a pain reaction.
  • a single infiltration of 10 ml of a drug (volume mixture 1: 1 of a solution with 10 mg / ml mepivacaine HCl and a solution containing (per ml) 6 mg disodium dihydrogen adenosine triphosphate, 2 mg adenoindine diphosphoric acid, 2 mg adenosine monophosphoric acid , 4 mg guanosine monophosphoric acid, 10 mg adenosine, 2 mg guanosine, 10 mg inosine, 2 mg uridine and 2 mg chlorocresol) in the painful muscle area gave almost complete freedom from pain and full functionality after only two days, so that after four Days of training could be resumed.
  • the athlete received the usual physical treatment. Since the end of the treatment there have been no complaints in the area of the right thigh muscles.
  • Example 3 In the course of five to six years, this patient could not be used repeatedly in games because of painful muscle hardening in both thighs. The patient was treated a total of three times with 10 ml of the drug mentioned in Example 1 in each of the two thighs (infiltration into the hamstring muscles). After a four-day break from training there was complete freedom from pain. Myogeloses were no longer palpable. Subsequently, there were no recurrences in the muscle groups mentioned. Example 3
  • the patient was washed twice with 7 ml of a medicinal product in the thigh muscle palpable scar on the right in Ober ⁇ ⁇ interval of 10 days, treatment, 5 ml of an aqueous solution containing 10 mg / ml mepivacaine. HC1 and 2 ml of an aqueous nucleic acid solution, which was composed as in Example 1. Significant pain relief already occurred after the first infiltration. Four days after the second infiltration, the treated muscle groups were completely free of pain and functional. Since then there have been no complaints from the patient.
  • the patient had muscle tensions that were relatively resistant to therapy for three weeks, sometimes with considerable pain-related impairment of performance, particularly when playing the head ball.
  • the patient was diagnosed with several very painful myogeloses in the extensor muscles of the back with a minor S-shaped scoliosis of the thoracic spine.
  • the patient was given five infiltrations into the affected myogeloses on five consecutive days, 2 ml each of an aqueous medicinal solution solution composed according to Example 1. During a follow-up examination after five days, no muscle hard to be felt more. No physical therapy was given after the infiltration treatment.
  • a fresh muscle fiber tear in the area of the right hamstring muscles was diagnosed in the patient.
  • Four days after the injury occurred 10 ml of the aqueous medicinal solution composed according to Example 1 were infiltrated into the affected muscle area.
  • Example 9 Every three days, 2 ml of an aqueous pharmaceutical solution composed according to Example 3 were infiltrated twice. After four days, the patient was completely free of pain. To date, no recurrence has been demonstrated.
  • Example 9

Landscapes

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

Abstract

Le médicament décrit contient dans sa phase aqueuse (1) 1 à 100 g/l d'un anesthésique local, 1 à 100 g/l d'un ou plusieurs nucléosides du groupe constitué par l'adénosine, la guanosine, l'inosine, l'uridine et leurs sels hydrosolubles de mono-, di- et triphosphate, et un ou plusieurs conservateurs physiologiquement neutres et compatibles avec les principes actifs, et éventuellement des excipients et adjuvants usuels. Est également décrit l'emploi de ce médicament pour le traitement par infiltration locale de lésions musculaires.
EP19880901040 1987-01-20 1988-01-16 Medicament contenant des anesthesiques locaux et des nucleosides, ainsi que son emploi pour traiter des lesions musculaires Pending EP0363355A1 (fr)

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
DE3701497 1987-01-20
DE19873701497 DE3701497A1 (de) 1987-01-20 1987-01-20 Arzneimittel, enthaltend lokalanaesthetika und nukleoside sowie dessen verwendung zur behandlung von muskelverletzungen

Publications (1)

Publication Number Publication Date
EP0363355A1 true EP0363355A1 (fr) 1990-04-18

Family

ID=6319130

Family Applications (2)

Application Number Title Priority Date Filing Date
EP19880901040 Pending EP0363355A1 (fr) 1987-01-20 1988-01-16 Medicament contenant des anesthesiques locaux et des nucleosides, ainsi que son emploi pour traiter des lesions musculaires
EP19880200123 Withdrawn EP0297630A1 (fr) 1987-01-20 1988-01-16 Médicament contenant des anesthésiques locaux et des nucléosides

Family Applications After (1)

Application Number Title Priority Date Filing Date
EP19880200123 Withdrawn EP0297630A1 (fr) 1987-01-20 1988-01-16 Médicament contenant des anesthésiques locaux et des nucléosides

Country Status (4)

Country Link
EP (2) EP0363355A1 (fr)
AU (1) AU1150888A (fr)
DE (1) DE3701497A1 (fr)
WO (1) WO1988005299A1 (fr)

Families Citing this family (5)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
FR2692784B1 (fr) * 1992-06-24 1995-06-30 Pf Medicament Utilisation de la guanosine, de ses precurseurs et ses derives pour la fabrication de medicaments destines a traiter les deficits fonctionnels cerebraux.
FR2782270B1 (fr) * 1998-08-12 2001-06-22 Michel Seman Adenosine et nucleotides adenyliques par voie orale pour l'amelioration du travail musculaire
WO2007112986A1 (fr) * 2006-03-31 2007-10-11 Adenobio N.V. Compositions, procédés, et trousses utilisant l'adénosine et l'inosine combinées pour un diagnostic et un traitement
HU227743B1 (en) 2011-07-22 2012-02-28 Debreceni Egyetem Eardrop composition and process for producing this
CN114469981A (zh) * 2021-12-16 2022-05-13 中国科学院动物研究所 尿苷在促进组织器官再生或治疗和/或预防和/或缓解和/或改善组织器官损伤中的应用

Non-Patent Citations (1)

* Cited by examiner, † Cited by third party
Title
See references of WO8805299A1 *

Also Published As

Publication number Publication date
AU1150888A (en) 1988-08-10
WO1988005299A1 (fr) 1988-07-28
DE3701497A1 (de) 1988-07-28
EP0297630A1 (fr) 1989-01-04

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