FR2743721A1 - Association of magnesium, Crataegus and Eschscholzia extracts - Google Patents

Abstract

Composition with a mineral-plant association comprises at least one magnesium salt, an extract of Crataegus oxyacantha and an extract of Eschscholzia californica, in the form of tablets, for treating mild anxiety.

Description

 The invention relates to the treatment of minor anxiety and the symptoms which are generally associated with it such as mild sleep disturbances, anxiety, asthenia, etc.

Many herbal specialties prescribed for this indication are known, including Crataegus oxyacantha (hawthorn) and
Eschscholzia californica (California poppy), the sedative properties of which are well known and which have been used for a long time, alone or in combination, in particular for the symptomatic treatment of neurotonic conditions of adults and children, in particular in cases of minor sleep disorders.

 Plant extracts are sometimes used in combination with chemical active ingredients such as phenobarbital to enhance their action.

 However, these chemical active principles (active synthetic derivatives) all have more or less marked side effects which limit the possibilities of prescription: habituation, risks linked to overdose, enzymatic induction modifying the metabolism and risking in particular reducing the effectiveness of oral contraceptives, etc.

 The object of the invention is to propose a phytotherapeutic association with enhanced action, indicated in the treatment of mild anxiety, but which does not contain additional chemical active principles in the sense indicated above and which therefore overcomes the risks and disadvantages. associated with these.

 To this end, the invention proposes to combine with a specific phytotherapeutic association for the treatment of mild anxiety, such as a Crataegus and Eschscholzia association, a mineral therapy, also specific, by supplying magnesium to the body.

 We know that in the pathogenesis of stress, magnesium has "anti-stress" properties verified on multiple models of non-specific aggressions (see for example J. Durlach, Magnesium in Clinical Practice, John Libbey and Co. , London, 1988).

In particular, the magnesium deficit creates a state of hypersusceptibility to stress and, conversely, stress induces or worsens a magnesium deficit, so that a vicious pathogenic circle is realized. Magnesium, by its neuroregulatory role within the central nervous system, makes it possible to treat this situation (see for example
J. Lederer, Magnesium and realities, Ed. Molanes).

 Magnesium is also prescribed in other related indications such as for example the withdrawal of benzodiazepines (see a national pharmacoepidemiological study on 2316 subjects published in the Daily of the doctor no 5125, February 1993) and also in the treatment of spasmophilia .

 In this indication, magnesium must be prescribed in doses of the order of 300 mg of magnesium element per day, a value considered to be the typical operating dose necessary for magnesium to be able to develop the therapeutic effects sought in the abovementioned indication (J Lederer, supra).

 More specifically, the invention provides a mineralophytotherapeutic combination in unit dosage form of tablets which comprises as active principles associated with at least one magnesium salt, extract of Crataegus oxyacantha and extract of Eschscholzia californica, in an indication for the treatment of mild anxiety.

 The content of elemental magnesium is advantageously between 150 and 450, preferably about 300 mg per day, and the salt is preferably magnesium oxide.

 The respective proportions by weight of magnesium element: extract of Crataegus oxyacantha: extract of Eschscholzia californica are preferably around 75: 75: 20.

 The particular choice of oxide as the magnesium salt is due to the fact that the necessary daily intake, which is as indicated typically of 300 mg of magnesium element per day, is relatively large and that, on the other hand, in order to improve compliance, the final tablet should be as small as possible and the number of doses per day minimum (four tablets maximum in two doses).

 To meet these requirements, magnesium oxide proves to be particularly suitable, insofar as it is highly concentrated in elemental magnesium (60.32 ic) and has a completely satisfactory bioavailability and practically free of side effects.

 This choice is not, however, limiting, and one can envisage other magnesium salts, organic or inorganic. However, it should be noted that the organic magnesium salts (succinate, citrate, acetate, lactate or gluconate) cause an excess of alkalinity which must be eliminated by the kidneys which is a disadvantage when large doses are necessary, as in the case of the invention.

 As for the other soluble mineral salts (phosphate, sulphate) or insoluble (carbonate, hydroxide, which are soluble in the gastric liquid and turn into chloride before being absorbed), they can induce side effects in certain subjects for the required doses. , relatively high.

Unlike other salts, magnesium oxide has the advantage, in addition to its high concentration of elemental magnesium, of being able to be used without risk in magnesium supplementation by the oral route in doses of the order of 250 to 500 mg, with a bioavailability comparable to that of other salts (see in particular
J. Durlach, Magnesium in Health and Disease, John Libbey and Co.,
London, 1990).

 By the oral route, magnesium oxide is completely absorbed in the form of magnesium chloride by gastric transformation, so that magnesium oxide can be considered as a precursor of magnesium chloride, reputed to be very effective in the treatment of magnesium deficits (see in particular J. Durlach, cited above).

The solubility of magnesium oxide in the gastric medium, and therefore its transformation into magnesium chloride, being pH-dependent, it is advisable to take the tablets at the time when the gastric pH is the lowest, i.e. - say on an empty stomach.

By way of example, the combination according to the invention can be formulated into a tablet, the core of which has the following composition:
Dry extract of Crataegus oxyacantha 75 mg
Dry extract of Eschscholzia californica 20 mg
Magnesium oxide 124.35 mg
(quantity corresponding to Mg element 75 mg)
Microcrystalline cellulose 122 mg
Carboxymethyl starch 15 mg
Stearic acid 3.65 mg
To protect the extracts of Crataegus and Eschscholzia which are highly hygroscopic and to give the tablet a more attractive appearance and easier to administer, one can provide a coating whose formula can be for example
Shellac 1.65 mg
Polyvinylpyrrolidone 0.35 mg
Alcohol qs

 Demineralized water q. s.

Dye qs desired color
A tablet having a total mass of 375 mg is thus obtained. To meet the prescribed daily intake of 300 mg of elemental magnesium, the typical dosage will be four tablets per day (2 + 2).

 By thus supplementing phytotherapy with mineral therapy (magnesium at operative dose), the spectrum of action of the combination according to the invention is thus widened and the treatment of mild anxiety and the symptoms which are associated.

Claims (4)

 1. A mineral phyto-therapeutic association in unit dosage form of tablets, characterized in that it comprises as active principles associated with at least one magnesium salt, extract of Crataegus oxyacantha and Eschscholzia californica extract, in an indication for the treatment of mild anxiety.  2. The mineralo-phythotherapic combination of claim 1, wherein the content of elemental magnesium is between 150 and 450, preferably about 300 mg per day.  3. The mineralo-phythotherapic combination of claim 1, wherein the magnesium salt is magnesium oxide.  4. The mineralo-phythotherapic association of claim 1, in which the respective proportions by weight of magnesium element: extract of Crataegus oxyacantha: extract of Eschscholzia californica are approximately 75: 75: 20.