COUGH-RELIEVING COMPOSITIONS

Abstract: Synergistic pharmaceutical compositions having cough-relieving effect and a method for relieving cough by the aid of the said compositions. The active ingredients of the composition are hog-fat, eucalyptus oil and optionally mustard.

Description: COUGH-RELIEVING COMPOSITIONS Field of the invention The present invention relates to physio- logically calmative and sedative cough-relieving com¬ positions 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 ormula ions (e.g. anisated expectorant li¬ quid, 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 com¬ positions 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/m 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 pro¬ longed 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 confort- ably and practically employable composition with pro¬ longed action which due to the prolonged release of the active ingredients has a continuous cough-re¬ lieving 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 op- tionally 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 : : o.l 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 composi¬ tions, 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 ingre¬ dient 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 com¬ ponents all have a very low effect per se, as it is widely known. These components synergistically en- hance each-others activity. The compositions exerts their effect partly transdermally, partly by the route of evap¬ oration inhalation. The temperature needed for the latter process is assured by the constant tempera- ture of the human body. If desired, the composition can be steri¬ lized, but the sufficient chemical and microbiologi¬ cal stability can also be assured by addition of an antioxidant. As antioxidant preferably butyl hydr- oxytoluene, 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 conven¬ tional 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 ab¬ sorbed by a suitable carrier, optionally covered by a removable protective layer and the carrier is pre¬ ferably supplied with means suitable for fixing the carrde r onto the skin. As suitable carrier gauze bandage, puri¬ fied 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 im- pregnated 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 prob¬ lem can also be solved by sticking a suitable in¬ sulating 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 prefer¬ ably be used. The active ingredients can also be in¬ corporated into creams, dressings, glycerogelatins, pastes and ointments. In this case vaseline or any other carrier commonly used in such types of pharma¬ ceutical 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 accord- xng 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/m , sticking the 2 poly- vinyl chloride or other foil to one of ita aides, placing thia side onto the 3 adhesive plaster and covering the other side which will be in contact with the skin with the k 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 inven¬ tion has no side-effect, it is not toxic. It exhi¬ bits its effect already within 10 to 15 minutes and this effect is exerted throughout 6 to 8 hours. There¬ after the treatment can be repeated without any harm- ful consequence. Its application is simple, it can be used disregard to the age of the patient and the sec¬ tion of the day. - - The invention is illustrated by the fol¬ lowing, non-limiting examples. Example 1 hog-fat 1000 g eucalyptua oil 3 g butyl hydroxytoluene 0.1 g These componenta are mixed, thereafter a piece of terry cloth (10x20 cm) ia 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 3 S butyl hydroxytoluene 3 S mustard 90 g The above components are mixed and a 20x20 cm piece of gauze ia aaturated with the mix- tι.re, One side of the gauze is impregnated with polyvinyl chloride and it ia fixed onto the cheat of the patient by the aid of two atripea of an adhesive plaster being on the oppos fc e sides of the carrier. Example 3 hog-fat 750 g eucalyptus oil 2.5 g mustard 75 S The above components are mixed, there¬ after the mixture is sterilized and cooled. A hydrophobia textile (10x15 cm) ia aaturated with thia mixture and a polyvinyl chloride foil of the same size is stic ed 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 adheaive plaater, thereafter that part of the carrier, which will contact the akin ia covered with a polyethylene foil. Example k 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 ptirified cotton ia 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 € > vaseline 1000 g The ingredients are thoroughly mixed. The effect of the composition according to the invention ia verified by the following teats: 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 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 k children suffering from double form of chronic bronchitis. The cough was significantly re¬ lieved 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 suπmarized in Table 1. Table 1 Age/Sex Diagnoais Comment 2/man Ac. viral pneumonia Other cough-re¬ lieving agents could be left /man Ac, tracheobronchitia The night cough discontinued 2/ oman Aatha bronchiale The application of (easential form) the composition essentially de¬ creased the in¬ tensity and period of caughing -fit/woman Trachβomalacia The number of the crisises essentially decreased and the intensify of the cough decreased 56/man Chronic bronchitis The cough de¬ in the acute period creased at night. The patient could sleep undisturbed¬ ly 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 compo¬ sition 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 (l 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 de¬ creased 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 eucalyptua 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 composi¬ tions 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 pharmaceu ical compositions which com¬ prises mixing hog- at, 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.

Inventors: LEOPOLD GASPAR, SZIKLAI ATTILA, LEOPOLD, GASPAR, SZIKLAI, ATTILA
Applicants: BEKE MGTSZ, "BEKE" MGTSZ
Application year: 1985
Main classification: A61K35
IPC codes: A61K9, A61K35, A61K36, A61L15