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WO1996041641A1 - Pharmaceutical compositions with analgesic activity - Google Patents

Pharmaceutical compositions with analgesic activity Download PDF

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Publication number
WO1996041641A1
WO1996041641A1 PCT/EP1996/002472 EP9602472W WO9641641A1 WO 1996041641 A1 WO1996041641 A1 WO 1996041641A1 EP 9602472 W EP9602472 W EP 9602472W WO 9641641 A1 WO9641641 A1 WO 9641641A1
Authority
WO
WIPO (PCT)
Prior art keywords
analgesic activity
pharmaceutical compositions
perchloric acid
extracting
liver
Prior art date
Application number
PCT/EP1996/002472
Other languages
French (fr)
Inventor
Alberto Bartorelli
Original Assignee
Zetesis S.P.A.
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 Zetesis S.P.A. filed Critical Zetesis S.P.A.
Priority to AU62234/96A priority Critical patent/AU6223496A/en
Publication of WO1996041641A1 publication Critical patent/WO1996041641A1/en

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Classifications

    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K38/00Medicinal preparations containing peptides
    • A61K38/16Peptides having more than 20 amino acids; Gastrins; Somatostatins; Melanotropins; Derivatives thereof
    • A61K38/17Peptides having more than 20 amino acids; Gastrins; Somatostatins; Melanotropins; Derivatives thereof from animals; from humans
    • A61K38/1703Peptides having more than 20 amino acids; Gastrins; Somatostatins; Melanotropins; Derivatives thereof from animals; from humans from vertebrates
    • A61K38/1709Peptides having more than 20 amino acids; Gastrins; Somatostatins; Melanotropins; Derivatives thereof from animals; from humans from vertebrates from mammals

Definitions

  • the present invention relates to pharmaceutical formulations with analgesic activity containing as active ingredient polypeptides obtainable by extraction of mammal liver, particularly goat liver, with perchloric acid.
  • polypeptides which can be used according to the invention are disclosed in EP 574 394 as potent antineoplastic agents.
  • EP 574 394 the effectiveness of said polypeptides in controlling tumor-related pain is described.
  • compositions of the invention will preferably contain the goat liver extract defined in EP 574 394 with the abbreviation L6E, essentially consisting of three main protein components with molecular weights of 50,000, 14,000 and 10,000 daltons in SDS-PA6E, or the single protein components with molecular weights of 50,000 and/or 14,000 and/or 10,000.
  • compositions will be preferably administered by the parenteral route, for example intramuscularly or subcutaneously, in the form of sterile solutions or suspensions.
  • parenteral route for example intramuscularly or subcutaneously
  • examples of said formulations comprise vials or ampoules containing the freeze-dried ingredient to be dissolved before use with physiological sterile solutions, solutions or suspensions in sterile aqueous or oily solvents suitable to the in vivo administration.
  • the daily dosage, related to the LGE extract will typically range from 0.1 to 20 mg of extract (or the equivalent of the components thereof) .
  • the central analgesic activity is particularly fast and it is not accompanied by tolerance and/or addiction phenomena.
  • Analgesic thresholds were evaluated using the hot plate test (56*C). LGE was administered subcutaneously to normal Sprague Dawley rats (Charles River, Calco, CO) at the doses reported in the table.
  • the hot plate test evidences a "central" analgesic effect.

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  • Health & Medical Sciences (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Immunology (AREA)
  • Medicinal Chemistry (AREA)
  • Gastroenterology & Hepatology (AREA)
  • Chemical & Material Sciences (AREA)
  • Engineering & Computer Science (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Marine Sciences & Fisheries (AREA)
  • Zoology (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Proteomics, Peptides & Aminoacids (AREA)
  • Epidemiology (AREA)
  • Animal Behavior & Ethology (AREA)
  • General Health & Medical Sciences (AREA)
  • Public Health (AREA)
  • Veterinary Medicine (AREA)
  • Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)

Abstract

Pharmaceutical compositions with analgesic activity, containing as the active ingredient polypeptides obtainable by extracting mammal liver with perchloric acid.

Description

PHARMACEUTICAL COMPOSITIONS WITH ANALGESIC ACTIVITY
The present invention relates to pharmaceutical formulations with analgesic activity containing as active ingredient polypeptides obtainable by extraction of mammal liver, particularly goat liver, with perchloric acid.
The polypeptides which can be used according to the invention are disclosed in EP 574 394 as potent antineoplastic agents. In the same Patent EP 574 394, the effectiveness of said polypeptides in controlling tumor-related pain is described.
Now it has been found that said polypeptides have a potent central analgesic activity and are therefore capable of controlling pain of various etiology and not only that tumour-related. The compositions of the invention will preferably contain the goat liver extract defined in EP 574 394 with the abbreviation L6E, essentially consisting of three main protein components with molecular weights of 50,000, 14,000 and 10,000 daltons in SDS-PA6E, or the single protein components with molecular weights of 50,000 and/or 14,000 and/or 10,000.
The compositions will be preferably administered by the parenteral route, for example intramuscularly or subcutaneously, in the form of sterile solutions or suspensions. Examples of said formulations comprise vials or ampoules containing the freeze-dried ingredient to be dissolved before use with physiological sterile solutions, solutions or suspensions in sterile aqueous or oily solvents suitable to the in vivo administration. The daily dosage, related to the LGE extract, will typically range from 0.1 to 20 mg of extract (or the equivalent of the components thereof) .
The central analgesic activity, evidenced on the basis of the pharmacological tests reported hereinbelow, is particularly fast and it is not accompanied by tolerance and/or addiction phenomena.
EXAMPLE
Analgesic thresholds were evaluated using the hot plate test (56*C). LGE was administered subcutaneously to normal Sprague Dawley rats (Charles River, Calco, CO) at the doses reported in the table.
Statistical analysis was carried out by means of the variance analysis, followed by the Dunnet's test for multiple comparisons.
Figure imgf000005_0001
Treatment Basal 30 min. 60 min. 120 min. 240 min. 24 hours
Controls 9.3 ± 0.4* 9.6 ± 0.5 9.6 ± 0.4 9.0 ± 0.4 9.3 ± 0.4 10 ± 0.6 (physiologi¬ cal solution)
LGE20 9.2 ± 0.4 11.1 ± 0.6 10.9 1 0.8 10.2 1 0.4 9.0 ± 0.6 10.7 1 0.5 μg/rat >
LGE40 9.8 ± 0.3 11.3 ± 0.4 12 ± 0.6 9.7 ± 0.4 9.5 ± 0.5 10.9 ± 0.7 μg/rat
LGE80 9.3 ± 0.4 11.1 ± 0.8 11 ± 0.5 9.9 ± 0.4 10.3 ± 0.5 10.6 ± 0.6 μg/rat
LGE160 9.8 ± 0.4 12.7 ± 0.5 12.9 ± 0.5 10.7 ± 0.4 10.7 ± 0.3 10.2 ± 0.6 μg/rat
* = mean ± standard error of 8 animals
A significant increase in the analgesia threshold is observed compared with the basal values at times 30 and 60 minutes for higher dosages, with a dose/response effect not elucidated.
The hot plate test evidences a "central" analgesic effect.

Claims

1. Pharmaceutical compositions with analgesic activity containing as the active ingredient one or more of the polypeptides obtainable by extracting mammal liver with perchloric acid.
2. Compositions according to claim 1, containing as the active ingredient one or more of the polypeptides obtainable by extracting goat liver with perchloric acid.
3. The use of the polypeptides obtainable by extracting goat liver with perchloric acid, for the preparation of a medicament with analgesic activity.
PCT/EP1996/002472 1995-06-13 1996-06-07 Pharmaceutical compositions with analgesic activity WO1996041641A1 (en)

Priority Applications (1)

Application Number Priority Date Filing Date Title
AU62234/96A AU6223496A (en) 1995-06-13 1996-06-07 Pharmaceutical compositions with analgesic activity

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
IT95MI001253A IT1276707B1 (en) 1995-06-13 1995-06-13 PHARMACEUTICAL COMPOSITIONS WITH ANALGESIC ACTIVITY
ITMI95A001253 1995-06-13

Publications (1)

Publication Number Publication Date
WO1996041641A1 true WO1996041641A1 (en) 1996-12-27

Family

ID=11371805

Family Applications (1)

Application Number Title Priority Date Filing Date
PCT/EP1996/002472 WO1996041641A1 (en) 1995-06-13 1996-06-07 Pharmaceutical compositions with analgesic activity

Country Status (4)

Country Link
AU (1) AU6223496A (en)
IT (1) IT1276707B1 (en)
WO (1) WO1996041641A1 (en)
ZA (1) ZA964954B (en)

Citations (2)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO1992010197A1 (en) * 1990-12-11 1992-06-25 Zetesis S.P.A. Substances of polypeptide nature useful in human therapy
WO1996002567A1 (en) * 1994-07-14 1996-02-01 Zetesis S.P.A. Proteins from mammalian liver and their use in oncology

Patent Citations (2)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO1992010197A1 (en) * 1990-12-11 1992-06-25 Zetesis S.P.A. Substances of polypeptide nature useful in human therapy
WO1996002567A1 (en) * 1994-07-14 1996-02-01 Zetesis S.P.A. Proteins from mammalian liver and their use in oncology

Also Published As

Publication number Publication date
IT1276707B1 (en) 1997-11-03
ITMI951253A0 (en) 1995-06-13
ZA964954B (en) 1997-01-23
AU6223496A (en) 1997-01-09
ITMI951253A1 (en) 1996-12-13

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