EP0198003A1

EP0198003A1 - Cough-relieving compositions

Info

Publication number: EP0198003A1
Application number: EP85905100A
Authority: EP
Inventors: Gáspár LEOPOLD; Attila Sziklai
Original assignee: BEKE MGTSZ
Current assignee: BEKE MGTSZ
Priority date: 1984-10-12
Filing date: 1985-10-11
Publication date: 1986-10-22
Also published as: WO1986002270A1; DK277486A; DK277486D0; HU187414B; DD243642A5

Abstract

Des compositions pharmaceutiques synergétiques ont un effet calmant sur la toux, et un procédé permet de calmer la toux à l'aide de ces compositions. Les ingrédients actifs de la composition sont la graisse de porc, l'huile d'eucalyptus et facultativement de la moutarde.Synergistic pharmaceutical compositions have a calming effect on coughing, and a method allows calming cough using these compositions. The active ingredients of the composition are pork fat, eucalyptus oil and optionally mustard.

Description

COUGH-RELIEVING COMPOSITIONS

Field of the invention

The present invention relates to physiologically calmative and sedative cough-relieving compositions and a method for relieving cough by the aid of the said compositions.

Background art It is known that synthetic medicaments

[e.g. Codein (morphine monomethyl ether)] and other galenic formulations (e.g. anisated expectorant liquid, elixir comprising eucalyptus oil or thimal) are used for cough relieving. Hog-fat is used for the easing of cough in the traditional popular therapy.

The great disadvantage of the synthetic medicaments is that they comprise smaller or higher amount of exciting alkaloids, therefore certain compositions are considered as doping (stimulating) agents. The alkaloids can also have an undesired side-effect to the heart. The drawback of the galenic formulations is that their effect is relatively weak. According to French Patent Specification

No. 71,37158 into a square shawl having a cut in the middle for the head 1 to 10 g/m² of a volatile oil, e.g. menthol, thimol, eucalyptus oil, camphor or a mixture thereof is absorbed and this shawl is used tightly wound around the neck against bronchitis and cold. No reference is made in the specification to any cough-relieving effect of the shawl or to its prolonged action or to any other pharmaceutical action. The practiαal use of this shawl is quite complicated and the effect of the volatile oils is rather low. Efforts were made to work out a confortably and practically employable composition with prolonged action which due to the prolonged release of the active ingredients has a continuous cough-relieving effect, has no or only local side-effect and does not comprise any toxic component.

SUMMARY OF THE INVENTION

The compositions according to the present invention comprise hog-fat, eucalyptus oil and optionally mustard in a weight ratio of 700 to 1200 : : 2.5 to 50 : 70 to 160 as active ingredients.

If the composition is not sterilized, it should also comprise an antioxidant. The weight ratio of hog-fat to the antioxydant should be 700 to 1200 : : 0.1 to 5.

DETAILED DESCRIPTION OF THE INVENTION

The effect of the compositions according to the invention is assured by hog-fat, eucalyptus oil and mustard, latter being optionally present. Mustard is not an essential element of the compositions, however, its addition enhances the activity of the compositions.

The active ingredient of the hog-fat is mainly prostaglandine but also the volatile fatty acids ( triglycerides) have a favourable effect on the inner cilia of the bronchi. The active ingredient of cough-relieving and expectorant effect of mustard is mustard oil. The cough-relieving effect of eucalyptus oil is known, but in our case it is also useful for the perfuming of the composition. The effect of the compositions of the invention is different from the additive effect of hog-fat, eucalyptus oil and mustard which components all have a very low effect per se, as it is widely known. These components synergistically enhance each-others activity.

The compositions exerts their effect partly transdermally, partly by the route of evaporation inhalation. The temperature needed for the latter process is assured by the constant temperature of the human body.

If desired, the composition can be sterilized, but the sufficient chemical and microbiological stability can also be assured by addition of an antioxidant. As antioxidant preferably butyl hydroxytoluene, commonly used for protecting hog-fat from growing rancid, can be used.

The active agents of the invention can be applied onto the skin by any means that produces contact of the active agent with the agent's site of action. They can be administered by any conventional means available for use. They can be applied alone, but are generally applied with a pharmaceutical carrier.

When the composition is formulated as a plaster the active ingredients are preferably absorbed by a suitable carrier, optionally covered by a removable protective layer and the carrier is preferably supplied with means suitable for fixing the carrier onto the skin.

As suitable carrier gauze bandage, purified cotton, absorbent gauze, terry cloth or any other hydrophobic, soft, non-irritating material can be mentioned.

In order to prevent the drying or the seeping of the active ingredients through the back side of the carrier, the carrier is preferably impregnated on the back side by e.g. a polymer such as polyvinyl chloride, or such a carrier is used of which the back side is of close texture. This problem can also be solved by sticking a suitable insulating material, e.g. aluminium or polymer foil onto the back side of the carrier.

The mixture of the active ingredients can be applied onto the chest of the patient confined to bed per se, or absorbed by a suitable carrier, the carrier is preferably fixed onto the skin of the patient. The fixing can be carried out by sticking the carrier saturated by the active ingredients on its two or four edges onto the skin by the aid of adhesive plaster stripes, but the carrier can also be put onto a piece of an adhesive plaster being bigger in size than the carrier itself and the parts of the plaster overlaping the carrier fasten the carrier to the akin.

The adhesive tape can be of the surgical type with an adhesive being neutral from the point of view of skin allergy. Preferably the tape can be a rubber based one or can have an acrylate coating attached. The adhesive tape can be woven or nonwoven fabric.

That side of the carrier saturated with the active ingredients which will contact the skin is preferably covered by a protective layer which can be removed before use. As protective layer polyvinyl chloride, polyethylene or aluminium foil can preferably be used.

The active ingredients can also be incorporated into creams, dressings, glycerogelatins, pastes and ointments. In this case vaseline or any other carrier commonly used in such types of pharmaceutical formulations can be employed as carrier. The plaster according to the invention suitable for external application contains from about 1 g to 100 g of active ingredients per unit. In the pharmaceutical compositions the active ingredients will ordinarily be present in an amount of about 5 to 100 % by weight based on the total weight of the compositions.

As preferred embodiment of the invention is illustrated by Figure 1. The composition according to Figure 1 is prepared by saturating the 1 terry cloth piece with the mixture of the active ingredients in an amount of 250 to 2500 g/m², sticking the 2 polyvinyl chloride or other foil to one of ita aides, placing this side onto the 3 adhesive plaster and covering the other side which will be in contact with the skin with the 4 polyvinyl or polyethylene foil which can be removed before use. The preferred form of the preparation according to the invention is a square or rectangle with 10 to 20 cm sides. The preparation according to the invention has no side-effect, it is not toxic. It exhibits its effect already within 10 to 15 minutes and this effect is exerted throughout 6 to 8 hours. Thereafter the treatment can be repeated without any harmful consequence. Its application is simple, it can be used disregard to the age of the patient and the section of the day. The invention is illustrated by the following, non-limiting examples.

Example 1 hog-fat 1000 g eucalyptus oil 3 g butyl hydroxytoluene 0.1 g

These components are mixed, thereafter a piece of terry cloth (10x20 cm) is aaturated with the mixture. That side of the terry cloth which will not contact the skin is of close structure in order to prevent the evaporation of the volatile oil and the penetration of hog-fat. The carrier saturated like this is applied onto a 13x13 cm piece of an adhesive plaster and that side of the terry cloth which will contact the skin is covered by a polyvinyl chloride foil,

Example 2 hog-fat 1200 g eucalyptus oil 43 g butyl hydroxytoluene 3 g mustard 90 g The above components are mixed and a

20x20 cm piece of gauze is aaturated with the mixture, One side of the gauze is impregnated with polyvinyl chloride and it is fixed onto the cheat of the patient by the aid of two atripes of an adhesive plaster being on the opposite sides of the carrier.

Example 3 hog-fat 750 g eucalyptus oil 2.5 g mustard 75 S

The above components are mixed, thereafter the mixture is sterilized and cooled. A hydrophobic textile (10x15 cm) is saturated with this mixture and a polyvinyl chloride foil of the same size is sticked onto that aide of the material which will not contact the akin. The carrier is applied onto a 12 x 17 cm piece of an adhesive plaster, thereafter that part of the carrier, which will contact the akin is covered with a polyethylene foil.

Example 4 hog-fat 1200 g muatard 160 g eucalyptus oil 18 g butyl hydroxytoluene 3 S

The above components are mixed and a 20x20 cm piece of purified cotton is saturated with thxs mixture. The saturated cotton can be applied onto the chest of a child suffering from bronchitis. Example 5 - Ointment hog-fat 700 g eucalyptus oil 5 g mustard 70 g butyl hydroxytoluene 5 g vaseline 1000 g

The ingredients are thoroughly mixed.

The effect of the composition according to the invention is verified by the following tests: The composition according to Example 2 was applied. a) The composition was applied onto the cheat of 17 patients suffering from asthma or bronchitis. The cough completely ceased in the case of 8 patients, it was relieved in great extent in 5 cases and in less extent in 4 cases. The composition was applied for night. No disadvantageous or harmful side-effect could be observed. b) The composition was applied onto the chest of 4 children suffering from double form of chronic bronchitis. The cough was significantly relieved even due to only one treatment and the stethoscopic diagnosis improved as well in all the four cases, c) The composition was applied onto the chest of 10 patients. The results are summarized in Table 1. Table 1

Age/Sex Diagnoais Comment 42/man Ac. viral pneumonia Other cough-relieving agents could be left

39/man Ac, tracheobronchitis The night cough discontinued

42/woman Aatha bronchiale The application of (easential form) the composition essentially decreased the intensity and period of caughing 44 /woman Tracheomalacia The number of the crisises essentially decreased and the intensity of the cough decreased 56/man Chronic bronchitis The cough dein the acute period creased at night. The patient could sleep undisturbedly 36/woman Acute viral infection The cough ceased of the upper respiratory 20 minutes after tracts the application of Table 1 ( cont , )

Age/Sex Diagnosis Comment the composition

4 patients Pleuritis of post- The cough practical-thoracitomic origin ly ceased

d) The composition was applied onto the chest of 10 1 to 4 years old and 10, 5 to 14 years old patients suffering from obstructive bronchitis, asthma bronchiale or bronchopneumonia. The composition was applied at night, before going to bed for the younger children, while it was used at night and day too, for the elder children, in both cases as a supplement of the basic medicines. The younger children (1 to 4 years old) became aubatantially tranquil, they could better sleep, while they auffered from air-thrist before the application of the composition. The effect of the composition decreased after about 2 hours.

The elder children reported on that their air-thrist and feeling of suffocation decreased, their general condition and spirit improved. The only side-effect of the composition was that the adheaive plaater irritated the skin of the children. e) The plaster was proved on 17 patienta auffering from asthma or bronchitis. Due to the plaster applied at night the cough ceased in 8 cases, was relieved in 5 cases and no effect could be observed in 4 cases.

f) Comparative test f) 6 patients suffering from asthma were treated with hog-fat poultice at night. In the case of 2 patienta the intenaity of the attacks of coughing somewhat decreased, in four cases the poultice was completely ineffective.

The chest of the same 6 patients was smeared with eucalyptus oil. No effect could be observed in any one of the cases.

A carrier was saturated with mustard and this waa applied to the chest of the same 6 patients. No effect could be observed in any one of the cases.

Claims

Patent Claims

1. Synergistic pharmaceutical compositions which comprise hog-fat, eucalyptus oil and optionally mustard.

2. The compositions according to Claim 1 which comprise the active ingredients in a weight ratio of 700 to 1200 : 2. 5 to 50 : 70 to l6θ,

3. The compositions according to Claim 1 which comprise an antioxidant.

4. The compositions according to Claim 1 wherein butyl hydroxytoluene is used as antioxidant,

5. The compositions according to Claim 3 or 4 wherein the weight ratio of hog-fat and the antioxydant is 700 to 1200 : 0.1 to 5.

6. The compositions according to Claim 1 in the form of a plaster, ointment, dressing, paste, cream or glycerogelatine.

7. The compositions according to Claim 1 which comprise a pharmaceutically acceptable carrier and if desired means suitable for fixing the carrier onto the skin.

8. The compositions according to Claim 7 wherein the carrier is selected from the group of absorbent gauze, bandage, terry cloth, purified cotton or any other hydrophobic textile,

9. The compositions according to Claim 7 wherein the means suitable for fixing the carrier onto the skin are adhesive plasters.

10, Method for the releiving of cough which comprises applying a composition according to any of Claima 1 to 9 to the chest of the patient.

11, Process for the preparation of synergistic pharmaceutical compositions which comprises mixing hog-fat, eucalyptus oil and optionally mustard.

12. The process according to Claim 11 which comprises mixing the active ingredients in a weight ratio of 700 to 1200 : 2.5 to 50 : 70 to 160.

13. The process according to Claim 11 which comprises adding an antioxidant to the active ingredients.

14. The process according to Claim 11 wherein butyl hydroxytoluene is used as antioxidant.

15. The process according to Claim 13 or 14 which comprises mixing hog-fat and the antioxydant in a weight ratio of 700 to 1200 : 0.1 to 5.

16. The process according to Claim 10 which comprises formulating the composition in the form of a plaster, ointment, dressing, paste, cream or glycerogelatine.

17. The process according to Claim 11 which comprises saturating a suitable carrier with the mixture of the active ingredients and optionally the antioxydant and supplying the carrier with means suitable for fixing the carrier onto the skin.

18. The process according to Claim 17 which comprises using a carrier selected from the group of absorbent gauze, bandage, terry cloth, purified cotton or any other hydrophobic textile.

19. The process according to Claim 17 which comprises using adhesive plaster aa means suitable for fixing the carrier onto the skin.