FR2690344A1 - Compsns. for treatment of psoriasis - contain distilled aq. extracts of plantain, rose, and orange with mercury salt - Google Patents

Abstract

Compsns. contain distilled aq. extracts of (a) leaves and ears of plantain (Plantago major L.), (b) petals of wild rose (Rosa canina L.), (c) flowers of bitter orange (Citrus aurantium L.), and (d) an organic or inorganic mercury salt. The pref. compsns. pref. contain 45-60 vol.% plantain water, 20-35 vol.% rose water, 10-20 vol.% organge water, and 1-2.5% weight/vol. of mercury salt. The mixt. is then partially distilled to eliminate 5-20 vol.% of the original mixt.. The pref. mercury salt is ethyl mercury thiosalicylate. USE/ADVANTAGE - Topical treatment of psoriasis. The treatment is effective, simple to carry out, non-toxic, reduces the risk of a relapse, and is easily adapted for commerical prodn..

Description

COXPOSI TIO1iS TOPICAL DOSING DA & LE
EFFECTIVE TREATMENT OF PSORIASIS
Technical area
The present invention relates to therapeutic compositions for topical use in the treatment of psoriasis based on the combination of aqueous extracts of plants and mercury salts and their process for obtaining.

State of the art
Psoriasis is a frequent, chronic and recurrent disease, characterized by the formation on defined surfaces of the epidermis of silvery, dry and well delimited papules and desquamative plaques, of different sizes. This disease characteristically affects the scalp, the extended surface of the extremities, in particular the elbows and knees, the back and buttocks, as well as the nails, eyebrows, armpits, navel and anogenital region. Occasionally, the disease becomes generalized.

 Its causes are unknown and, therefore, current methods of treatment are symptomatic. Therefore, we consider as effective treatment that by which we obtain a high percentage of remission of lesions for a relatively long time without these lesions reappearing.

 There are different drugs for the treatment of psoriasis, which in general have problems and complications. For example, methotrexate and etretinate are too toxic to allow continuous preventive treatment. Salicylic acid only is effective only in mild cases. Coal tar, which is generally used in combination with zinc oxide, has problems with patient acceptance because of its bad smell and the difficulty in applying it. The ditranol, despite its effectiveness, irritates the epidermis and produces stains on clothing, nails and skin. Corticosteroids for topical use have the disadvantage of tachyfilaxis and, moreover, when treatment is stopped, there is a sudden recurrence of symptoms. Finally, treatment with ultraviolet radiation is problematic because of its long-term effects, as well as premature aging of the skin, and increased risk of skin cancer.

 We also know the use of extracts of natural origin in the topical treatment of the disease. For example, published PCT patent application No. 89/05651 proposes the use of oily extracts from a group of plants such as garlic, common nettle, speedwell, etc.

The published European patent application No. 367103 describes the use of jojoba and beeswax or whale white ointments. Finally, the published Spanish patent No. 2,006,474 describes the use of plant extracts from the zygophilaceae family with an aqueous solution of a halide of a non-alkali metal.

 Mercury and arsenic salts were once used in the topical treatment of psoriasis in the form of ointments and ointments, but they are hardly used anymore.

 As can be seen, there are many treatment methods but none have sufficient efficacy and safety, due to the need for an effective treatment for psoriasis which does not involve residual toxic effects or the rapid onset of relapses, which at the same time is easily acceptable to patients so as not to be unpleasant.

 The present invention solves these problems by the fact that it offers aqueous compositions for topical use which are highly effective and with a prolonged effect which, moreover, are of pleasant application for the patient.

 Surprisingly, compositions have been discovered which contain mercury salts, due to the action of the plant extracts which they contain, and which exhibit low toxicity and high efficiency.

Subject of the invention
The main object of the present invention is to produce aqueous compositions of plant extracts and mercury salts capable of allowing effective topical treatment against psoriasis, without toxic effects and which minimizes the appearance of relapses.

 Another object of the present invention lies in a process for obtaining the cited compositions, simple and easy to adapt to industrial needs.

Description of the invention
The compositions for the topical treatment of psoriasis which are the subject of the present invention essentially consist of the combination of aqueous extracts distilled from the leaves and ears of large plantain (Plantago major L.), wild rose petals (Rosa canina
L.), and bitter orange flowers (Citrus aurantium L.), with an organic or inorganic mercury salt.

 These extracts, generally known as plantain water, rose water and orange water, are obtained separately by aqueous maceration of the parts of the plants indicated and subsequent distillation of the extract, preserving the distillate as material useful for the effects of this. invention.

 Plantain, rose and orange water can be prepared "in situ" or can be purchased commercially.

 The mercury salts used can be organic or inorganic. Among the organics, mention may be made, as preferred for the effects of the present invention, of ethylmercury thiosalicylate, known as thiomersel.

Among the inorganic salts, mention may be made of mercuric chloride.

 In order to achieve the objective of highlighting the excellent therapeutic qualities against psoriasis described above, it is absolutely essential that the compositions which are the subject of the present invention contain the three types of plant extracts: plantain water, water rose and orange water, and at least one mercury salt.

 Once the mixing of the components has been carried out, it is preferable to remove, by distillation, approximately between 5 and 20% of the total volume of liquid.

 Consequently, the process for obtaining consists in mixing the three distilled aqueous extracts of plantain, rose and orange tree, in adding the mercury salt, in carrying out an elimination between 5 and 20% of the volume, by distillation at atmospheric pressure, and to carry out a filtration until the desired composition is obtained.

Good therapeutic results are obtained when the essential components are found in the following proportions
Plantain water: 45-60% (V / V)
Rose water: 20-35% (V / V)
Orange water: 10-20% (V / V)
Mercury salt: 1- 2.5% (W / V) relative to the total volume of the mixture before proceeding with the volume reduction by distillation, considering that (V / V) indicates the proportion by volume and (W / V ) indicates the proportion of weight by volume expressed as equivalent by weight of mercury.

The best therapeutic results in relation to its effectiveness are obtained when the proportion between plantain water, expressed in volume as indicated above, is greater than 50%, that of rose water is less than 30% and that orange water is more than 12%
From the point of view of the tolerance of the patients to the treatment, that is to say, of the low toxicity, the best results have been obtained with the use of thiomersel as mercury salt, consequently the use of this product. is highly preferred.

 It has been verified by clinical experiments that the application of the compositions which are the object of this invention to the psoriatic plaques of different types of patients produces their detachment since the cell renewal cycle of the skin is normalized which recovers its natural elasticity .

 It has also been verified that relapses decrease considerably, with much less pronounced symptoms, and that prolonged treatment leads to complete recovery.

 On the other hand, the compositions, objects of the present invention, have a harmless appearance, a pleasant odor of rose and are not irritating and that they are therefore very well accepted by patients.

 In order to better understand the description of the present invention, without this being considered as a limitation, examples of embodiments are given below.

Examples Example 1
Plantain, rose, and orange water are obtained by maceration of a powder of the plant, at room temperature for 10-24 hours, with a volume of distilled water equivalent to 600-800 ml of water per each 100 g of plant powder. The maceration is subjected to simple distillation until a distilled equivalent to 60% of the initial volume is obtained.

In a suitable container, the aqueous distilled extracts obtained are mixed in the following amounts
Plantain water: 1.620 ml
Rose water: 810 ml
Orange water: 450 ml
Then 120 g of ethylmercury thiosalicylate are added and, once they are dissolved, the volume is made up with distilled water until three liters are reached.

 The solution thus obtained is distilled at 100 ° C. for 15 minutes, leaving a residual volume of approximately 2.7 liters. It is allowed to cool and then filtered.

 The solution is allowed to stand for 24 hours and is refiltered, after which it is ready for use.

Example 2
In a suitable container, the distilled aqueous extracts obtained according to what was described in Example 1 are mixed in the following amounts
Plantain water: 1.620 ml
Rose water: 810 ml
Orange water: 450 ml
Then 75 g of mercuric chloride and 45 g of sodium chloride are added and, once they are dissolved, the volume is made up with distilled water until three liters are reached.

 The solution thus obtained is distilled at 100 ° C. for 15 minutes, leaving a residual volume of approximately 2.7 liters. It is allowed to cool and filtered.

 The solution is left to stand for 24 hours and is refiltered: the solution is then ready for use.

Example 3
In a suitable container, the distilled aqueous extracts, obtained according to what was described in Example 1, are mixed in the following amounts
Plantain water: 1,350 ml
Rose water: 960 ml
Orange water: 450 ml
Then 60 g of ethyl mercury thiosalicylate are added and, once they are dissolved, the volume is made up with distilled water until three liters are reached.

 The solution thus obtained is distilled at 100 ° C. for 15 minutes, leaving a residual volume of approximately 2.7 liters. It is allowed to cool and filtered.

 The solution is allowed to stand for 24 hours and is refiltered, after which it is ready for use.

Example 4
In a suitable container, the distilled aqueous extracts obtained according to what was described in Example 1 are mixed in the following amounts
Plantain water: 1,500 ml
Rose water: 1.050 ml
Orange water: 360 ml
Then 56 g of mercuric chloride and 34 g of sodium chloride are added and, once they are dissolved, the volume is made up with distilled water until three liters are reached.

 The solution thus obtained is distilled at 100 ° C. for 15 minutes, leaving a residual volume of approximately 2.7 liters. It is allowed to cool and filtered.

 The solution is allowed to stand for 24 hours and is refiltered, after which it is ready for use.

Example 5
Clinical trials were carried out with the compositions obtained in the previous examples.

Treatment is carried out in 75 patients with different types of psoriasis, varying them according to the types mentioned in accordance with the following parameters
vulgar psoriasis. Applications every day, preferably at night. After 20 days of treatment, the product can be applied twice a day, for 5-6 days, only on desquamative surfaces. We continue with the application every day until total whitening.

 Psoriasis of the soles of the feet. The product is applied every 48 hours, for a total of 10 applications and, subsequently, it can be applied every day, preferably at night.

 Psoriasis guttata. The product is applied every 48 hours, for a total of 5 applications and, subsequently, applications will be made every 24 hours, only on the points where there are plaques or scales, until the external signs disappear. .

If the disease resists in any area, apply the product twice a day for 6-8 days and continue afterwards with daily applications.

 Pustular psoriasis. The product is applied every 48 hours, for a total of 6 applications and subsequently, the applications are made every day.

If the disease resists any area, the product can be applied twice a day for 6-8 days, and continued afterwards with daily applications.

 The results obtained are reproduced in Table 1.

Table 1
Composition Efficiency Tolerance
Example 1
Example 2 ++++ ++
Example 3 ++
Example 4 ++ ++
The evaluation is represented by crosses depending on the effects observed.

 All the compositions have been found to be effective and with good tolerance, but, as can be observed in the table, the behavior of the composition of Example 1 stands out, both in effectiveness and in tolerance.

 In Table 2, the results obtained with a composition similar to that of Example 1 are set out.

Table 2
Type Number Duration% zone Psoriasis time affected psoriasis patients Whitening
(years) (months)
Vulnerable 58 0.3-51 2-80 1-6
Plantar palm 4 2 -18 5 2-4
Guttata 8 1.5-24 10-99 2-4
Pustulosa 5 9 -50 15-95 3-7
Total rank 75 0.3-51 2-99 1-7
The tests carried out on the patients show that after an initial whitening, 2 to 4 relapses can be observed in a maximum period of two years, these being very reduced in surface and becoming lighter and punctual, until that there is a complete disappearance of symptoms.

 Once the first two years have passed, and even after an average of three years after the end of treatment, the disease no longer manifests.

Claims (7)

1. Therapeutic compositions for its use in the treatment of psoriasis, characterized in that they consist essentially in the combination of aqueous extracts distilled from leaves and ears of great plantain (Plantago major L.), of wild rose petals ( Rosa Canina L.) and bitter orange flowers (Citrus aurantium L.,), with an organic or inorganic mercury salt. 2. Therapeutic compositions according to claim 1, characterized in that they are prepared by mixing the components in the following -proportions  Plantain water: 45-60% (V / V)  Rose water: 20-35% (V / V)  Orange water: 10-20% (V / V)  Mercury salt: 1-2.5% (W / V) relative to the total volume of the mixture, (V / V) indicating the proportion by volume and (W / V) indicating the proportion of weight by volume expressed as equivalent in weight of mercury and then removing, by distillation, a volume corresponding to 5-20% of the initial volume of the mixture. 3. Therapeutic compositions according to one of claims 1 or 2, characterized in that the mercury salt is ethylmercury thiosalycilate. 4. Therapeutic compositions according to claim 2, characterized in that in the initial mixture the proportion of the volume of plantain water is greater than 50% 5. Method for obtaining compositions for therapeutic use in the treatment of psoriasis, characterized in that it comprises the following steps a. - mix plantain water, rose water and orange water and dissolve in this mixture a mercury salt, organic or inorganic. b. - Distill the resulting dissolution until its volume is reduced between 5% and 20% c. - Remove the distillate and collect the active product which is the distillation residue. 6. Method according to claim 5, characterized in that the proportions of the essential components are  Plantain water: 45-60% (V / V)  Rose water: 20-35% (V / V)  Orange water: 10-20% (V / V)  Mercury salt: 1-2.5% (W / V) relative to the total volume of the mixture, considering that (V / V) indicates the proportion by volume and (W / V) indicates the proportion of weight by volume expressed as equivalent by weight of mercury. 7. Method according to one of claims 5 or 6, characterized in that the mercury salt is ethyl mercury thiosalycilate.