DE2722113A1 - Hypolipaemic combination preparations - contg. a nicotinic acid salt of a hypoglycaemic biguanide and the magnesium salt of clofibric acid - Google Patents

Abstract

New therapeutic agents contain (a) nicotinates of biguanides of formula R1R2N-C(=NH)-NH-C(=NH2 (I) (where R1 is 1-5C alkyl or beta-phenethyl in which the aromatic residue may be substd. by a lower alkyl gp. or a halogen atom, and R2 is H or lower alkyl), in combination with (b) the magnesium salt of clofibric acid. The agents ae hypolipaemic agents. Use of nicotinic acid in the form of its salts with (I) gives improved glucose tolerance. The hypolipaemic activity of the nicotinic acid salt is potentiated by the magnesium salt of clofibric acid. and the Mg ions promote fibrinolysis and exert central sedative and smooth muscle relaxant effects. The nicotinic acid content is reduced, thus avoiding the flushing which could otherwise occur. In an example, tablets for oral admin. contain 40 mg phenformin mononicotinate and 450 mg (b).

Description

'Therapeutic Agent'

(Addition to the patent ........... (Patent application P11 The main application relates to a therapeutic agent, the nicotinate of biguanides of the general formula in which R1 is either an alkyl radical with 1 to 5 carbon atoms or a ß-phenethyl radical, the aromatic part of which can be substituted by a low molecular weight alkyl radical or by a halogen atom, and R2 is either a hydrogen atom or a low molecular weight alkyl radical, in combination with nicotinic acid or inorganic Contains salts of nicotinic acid.

The subject of claim 2 of the main patent is a therapeutic one Means containing magnesium nicotinate.

The agent according to the main patent has the advantage of improving glucose tolerance to the use of nicotinic acid and enhancing the lipid-lowering effect. Surprisingly, it has also been shown that the combination does not result in a type change, ie, no increase in LDL into the pathological range. The use of the easily soluble magnesium salt of nicotinic acid has the advantage that fibrinolysis is promoted and also has a pronounced central sedative effect and a relaxing effect on the smooth muscles. The invention relates to a further embodiment of claim 2 of the main patent and consists in a therapeutic agent containing biguanide nicotinates of the general formula in which R1 is either an alkyl radical with 1 to 5 carbon atoms or a β-phenethyl radical, the aromatic part of which can be substituted by a low molecular weight alkyl radical or by a halogen atom, and R2 is either a hydrogen atom or a low molecular weight alkyl radical in combination with the magnesium salt of clofibric acid . In the therapeutic agent according to the invention, this salt takes the place of the magnesium nicotinate of claim 2 of the main patent.

The therapeutic agent of the present invention is concerned with the same Task like the therapeutic agent according to claim 2 of the main patent and has also basically the same effects but with the advantage that the salary of nicotinic acid can be lowered, which may reduce nicotinic acid conditional flush phenomena can be avoided.

Example: A compilation is given as a drug specialty, without thereby limiting the use of biguanide nicotinates. For oral use, e.g. in tablets with an active ingredient content of 40 mg phenformin mononicotinate 450 mg of the magnesium salt of clofibric acid.

The compression into tablets is carried out with the usual auxiliaries.

Claims (1)

Claims Therapeutic agent containing biguanide nicotinates of the general formula in which R1 is either an alkyl radical with 1 to 5 carbon atoms or a ß-phenethyl radical, the aromatic part of which can be substituted by a low molecular weight alkyl radical or by a halogen atom, and R2 is either a hydrogen atom or a low molecular weight alkyl radical in combination with magnesium nicotinate according to claim 2 of the Main patent ........... (patent application ............) characterized in that the magnesium salt of clofibric acid takes the place of magnesium nicotinate.