FR4727M - Hydroxyproline and its drug combinations in the treatment of rheumatic diseases. - Google Patents

Description

FRENCH REPUBLIC

MINISTRY OF INDUSTRY

INDUSTRIAL PROPERTY SERVICE

SPECIAL MEDICINAL PATENT

P.V. n ° 37.265 International Classification

N ° 4.727 M A 61k

The 1. hydroxyproline and its drug combinations in the etraWëHfôifif of rheumatic diseases. (Invention: J.-C. Denis and J. Rambaud.) HGINDCV;

14 »m h h oh h

! I I I chaoh-c — c — c — c-cho I I I! oh oh h nh2

cehiaosn = 179.17

The formula of l.hydroxyproline:

ho

\

hc h2c

-ch2

I

ch

\not

COO-

c5h903n = 131.13

Pharmacodynamic properties. - Glucosamine hydrochloride and l.hydroxyproline were administered to animals, respectively at a dose of 150 and 15 mg / kg, in the various tests usually used to measure the analgesic action and the anti-inflammatory action of drugs. These include, but are not limited to, torsion syndrome caused in mice by phenyl-benzoquinone, inhibition of pain caused by experimental inflammation of the rat paw, inflammation caused by cotton pellets or turpentine gasoline injection.

Glucosamine hydrochloride and l.hydroxyproline have also been administered to animals in combination with known anti-rheumatic drugs including:

Acetylsalicylic acid and salicylates;

Acetyl p.aminophenol;

Phenyl - 1 - dimethyl - 2 - 3 - isopyrazolone (antipyrine);

7 210551 7 • +. price of the booklet

Company known as: TECPAN S. A. residing in Mexico.

Requested on November 4, 1965, at 3 p.m. 3m, at the aris.

Issued by decree of January 2, 1967. [

{Official Bulletin of Industrial Property [5.5.M.], No. 6 of February 6, 1967.)

The present invention consists of the use of l.hydroxyproline in combination:

- With glucosamine (or one of its salts as hydrochloride);

Or with an antirhumastimal drug;

Or with glucosamine and an anti-rheumatic drug.

Glucosamine has the following formula:

3.5 - dioxo -

Phenyl - 1 - dimethyl ^ '2 * ^ "3' - 4-dimethylamino-pyrazolone (amidopyrine);

Dioxy - 3,5 diphenyl - 1,2 n - butyl - 4 - pyrazo-lidine (phenylbutazone);

1 - phenyl - 2 (p.hydroxyphenyl)

4 - n - butyl - pyrazolidine;

Griseofulvin;

Hydroxychloroquine ;

Extract of articular cartilage and bone marrow.

Pharmacodynamic tests revealed:

1 ° The advantage of simultaneously using glucosamine with l.hydroxyproline to obtain an anti-inflammatory effect;

2 ° The advantage of adding to l.hydroxyproline or to the glucosamine - l.hydroxyproline combination, an antirheumatic drug, such as those mentioned above, if one wishes to obtain a faster and more important effect.

Indeed, l.hydroxyproline and even more the glucosamine-hydroxyproline combination not only potentiate the effects of anti-rheumatic drugs but also prolong their action over time and allow them to be used, for the same effectiveness, at lower doses and therefore less toxic.

Therapeutic applications. - l.hydroxyproline and the glucosamine - l.hydroxyproline combination can be used successfully in various rheumatic conditions, either alone or simultaneously with other known medications, according to the examples below:

Chl. glucosamine, g 0.200

1.hydroxyproline, g, 0.020

Excipient q.s. for one tablet.

4 to 6 tablets per day as a background for rheumatic affections;

treatment of b. Acetyl p. aminophenol, g 0.400

l. hydroxyproline, g 0.010

2 francs

[4.727 M]

4 to 6 tablets per day, in rheumatic pain;

vs. Acetylsalicylic acid, g 0.250

Chl. glucosamine, g 0.150

1.hydroxyproline, g 0.015

Excipient q.s. for one tablet.

6 tablets per day, for all rheumatic pain;

■ d. Dioxy-, 3,5 -diphenyl-1,2 -re-butyl-4- 0.100 pyrazolidine, g.

Chl. glucosamine, g 0.100

1.hydroxyproline, g 0.010

Excipient q.s. for one tablet.

1 to 2 tablets per day in cases of rheumatic fever, rheumatoid arthritis, arthritis, periarthritis, phlebitis.

Pharmaceutical forms. - Glucosamine, or one of its salts such as glucosamine hydrochloride, and l.hydroxyproline can be used:

Either in solution in a pharma-ceutically acceptable presentation such as injectable or drinkable ampoules, syrups, solutions;

Either in the powder form in a pharmaceutically acceptable presentation which may be that of tablets, capsules, sachets, granules, suppositories, alone or in combination with other drugs or pharmaceutically acceptable compounds.

ABSTRACT

1 ° The present invention relates to the use of l.hydroxyproline in combination with glucosamine (or one of its salts such as hydrochloride), or with an antirheumatic drug, or with glucosamine and an antirheumatic drug, in the treatment rheumatic diseases.

2 ° The addition of l.hydroxyproline and even more of the l.hydroxyproline-chl association. of glucosamine to an antirheumatic drug results in greater, longer lasting and less toxic therapeutic activity than that which would have been obtained with the antirheumatic drug administered alone.

Company known as: TECPAN S. A.

Vicarious :

Blétry

DOCUMENTARY NOTICE ON THE NEW FEATURE

Documents likely to affect the novelty of the medicinal product: none.

Documents illustrating the state of the art in this area: none.

For the sale of booklets, contact the Imprimerie Nationale, 27, rue de la Convention, Paris (15th).