FR283F - Drug based on sarcosyluric acid. - Google Patents

Description

FRENCH REPUBLIC JHE ADDITION

ministry ATJ PATENT OF INVENTION

OF INDUSTRIAL DEVELOPMENT DB-CmVLMI. W VC.HA1VW AND SCIENTIFIC

No. 6.142 M

of the Industrial Property P-V. ii ° 143.311 N ° 283 CAM

International classification: A 61 k // C 07 d

Drug based on sarcosyluric acid. 13ibIlOth Gôk.

Mr. Francis, Aliîeiit KIRSCH residing in France (Paris). BtlT Illd E / i ^ eilcLom

(Main patent issued March 20, 1967.) ^

Requested on March 12, 1968, at 13.50m, in Paris.

Issued by decree of September 22, 1969.

(Official Bulletin of Industrial Property [B.S.M.], No. 44 of November 3, 1969.)

The main patent describes a medicament which can be used, in particular, for the treatment of disturbances in the metabolism of uric acid and nucleoproteins, lymphoid leukemias and neoplasias, as well as for the inhibition of immune hyperactivity.

This medication comprises, as active principle, sarcosyluric acid.

The main patent had already mentioned the reductions in the level of urea in the blood observed in patients treated with the drug according to the invention.

The aim of the present addition is to clarify these properties to clearly show that the drug can also be used to fight against neoglucogenesis, hyperureogenesis, hyperuremia of nephritis (with the possibility of increasing the protein ration), osteoporosis and to inhibit exaggerated protein catabolism, any conditions which increase the level of urea in the blood.

To this end, the results of pharmacological tests carried out on the drug of the invention will be given above.

I. Experimental protocol.

Two control female rabbits with an average weight of 3 kg received 10 ml / kg of a 10% aqueous solution of arginine hydrochloride (ie 1 g / kg of arginine hydrochloride) via the veins. Blood samples were taken: five minutes before the arginine injection, then one hour, two hours, three hours, four hours, six hours, eight hours and twenty-four hours after the injection. The serum urea assay was carried out in each of the samples by a specific micromethod, involving urease.

A batch of 8 female rabbits with an average weight of 2.5 kg orally received 100 mg / kg of sarcosyluric acid in 1.5% solution in water

0 210 030 7

distilled: 1 g / kg of arginine hydrochloride was then injected by the venous route;

To 3 rabbits thirty minutes after the administration of sarcosyluric acid;

To 3 rabbits one hour after the administration of sarcosyluric acid;

To 2 rabbits twenty-four hours after administration of sarcosyluric acid.

Blood samples were taken: five minutes before the arginine injection, then one hour, two hours, three hours, four hours, eight hours, twenty-four hours and 30 hours after these. The serum urea assay was performed in each sample.

II. Results.

The figures obtained are reported in the Table below.

(See table on next page)

In the accompanying drawing, the single figure illustrates these results by a graph giving the percentage increase in the urea rate as a function of time. Curve A relates to the control animals which received only 1 g / kg (i.v.) of arginine. ; curve B to those who received 100 mg / kg oral sarcosyluric acid thirty minutes before the administration of arginine, curve C to those who received 100 mg / kg orally one hour before the administration of arginine; and curve D to those who received 100 mg / kg orally twenty-four hours before the administration of arginine.

It emerges from the above tests that sarcosyluric acid opposes ureogenesis and that it is capable either of reducing hyperureogenesis or of inhibiting exaggerated catabolisms.

It may also oppose gluconeogenesis in diabetics in whom there is a hyperglycaemic arrow after an injection

[283 CAM / 6.142 M]

- 3

Percentage increase in serum urea level relative to urea level before arginine injection

Treated with sarcosyluric acid

Witnesses

100 mg / kg

Time after arginine i.v.

(arginine

30 minutes

1 hour

24 hours

only)

before before before

arginine arginine arginine

1 hour

24

25.8

18.4

29.1

2 hours

35

41.3

24.5

42.5

3 hours

78.5

43.2

33.4

41.2

4 hours

75

43.7

34.7

41.2

6 hours

74.5

39.7

21.5

28.4

8 hours

65

50.1

11.4

38.5

24 hours

9

- 2

-35.8

2.5

30 hours

-20

-5

72 hours

- 7

arginine.

This action would be obtained by inhibiting deaminations, a mechanism which seems to intervene against the neoformation of glucose, especially when the organism is fasting or diabetic.

ABSTRACT

The object of the addition is the application of the drug of the type described in the main patent, to fight against gluconeogenesis, hyperureogenesis, hyperuremia of nephritis (with the possibility of increasing the protein ration), esteoporosis and to inhibit exaggerated protein catabolism.

Francis, Albert KIRSCH

Vicarious :

Cabinet Lavoix

DOCUMENTARY NOTICE ON THE NEW FEATURE

Documents likely to affect the novelty of the medicinal product:

- French patent (B.S.M.) n ° 6.Î42 M.

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