MOUTH-SOLUBLE PHARMACEUTICAL COMPOSITIONS CONTAINING ACETYLCYSTEINE

Abstract: Mouth-soluble pharmaceutical compositions comprising acetylcysteine, alkaline bicarbonates, carbohydrates and fruit flavouring, produced in the form of tablets for treating affections of the oral cavity.

Description: Field of the invention This invention relates to mouth-soluble pharmaceutical compositions containing acetylcysteine for treating affections of the oral cavity. Known art It is known to use acetylcysteine as a mucolytic and expectorant for the purpose of fluidizing the dense viscous secretions of the respiratory system in bronchitis, bronchial catarrh, emphysema, mucoviscidosis etc. Known compositions are available for systemic treatment of respiratory diseases or for aerosol treatment. They are prepared in granular or tablet form to be dissolved in water and immediately swallowed, in capsule form for oral use, or in aerosol vials. Tablets to be dissolved in water, of the effervescent type are disclosed by GB 2.192.790. Compositions containing acetylcysteine for dissolving in the mouth are not known, although such compositions would be of use in treating affections of the oral cavity. This limitation is due to the fact that acetylcysteine is a substance with high acidity (pKa = 3.24) and its continued presence in the mouth causes severe aggression of the mucous membrane of the tongue and oral cavity. In addition, acetylcysteine has an extremely unpleasant taste and this characteristic is a further contraindication with regard to its dissolving in the mouth. Summary of the invention The aim of the present invention is to provide pharmaceutical compositions containing acetylcysteine for dissolving in the mouth, which obviate the drawbacks of the known art and in particular the mucous membrane aggression and unpleasant taste. Said compositions are characterised by comprising acetylcysteine, alkaline bicarbonates, carbohydrates and fruit flavouring. Detailed description of the invention The characteristics and advantages of the pharmaceutical compositions according to the invention will be apparent from the detailed description given hereinafter by way of non-limiting example. Said pharmaceutical compositions comprise acetylcysteine, alkaline bicarbonates, suitably chosen carbohydrates and small quantities of fruit flavouring. The alkaline bicarbonates used are sodium bicarbonate and potassium bicarbonate in a NaHCO₃/KHCO₃ weight ratio of between 93:7 and 97:3. The weight ratio of the bicarbonate mixture to the acetylcysteine is between 45:100 and 55:100. Neither saccharose nor glucose can be chosen as carbohydrates because of their diabetogenic and cariogenic nature, in consideration of the long period for which they remain in the mouth. In addition, experimental tests carried out on compositions containing lysine or arginine or arginine/sorbitol or lysine/sorbitol or citrates have not satisfactorily solved the problem of poor taste. However a satisfactory solution to the taste problem has been surprisingly found by using sorbitol/fructose, sorbitol/xylitol and xylitol/fructose with the two carbohydrates in a weight ratio of between 0.8:1.2 and 1.2:0.8. The weight ratio of carbohydrates to the acetylcysteine is between 20:1 and 50:1. The flavouring is preferably chosen from orange, lemon, grapefruit, peach and apricot. They are contained in small quantity in the compositions. The compositions of the invention are produced preferably in the form of tablets with an acetylcysteine content of between 50 and 300 mg per dose. Said compositions are suitable to be dissolved in the mouth. They are not aggressive in any way to the mucous membrane and are of pleasant taste. This form of administration allows the acetylcysteine to be distributed at the oropharyngeal level followed by ingestion and gastric absorption. In this manner the compositions according to the invention find useful application in oral cavity affections of inflammatory origin such as glossitis, gingivitis, stomatitis, leukoplakia etc., in affections caused by abnormal secretion of mucus such as mucocele, oral manifestations of the Siogren syndrome etc., and in halitosis. Finally, said compositions produce that pleasant effect of freshness particularly desirable in the case of inflamed mucous membranes. In addition the presence of small quantities of fruit flavouring further improves their taste.

Claims: Claims for the following Contracting States : AT, BE, CH, DE, FR, GB, IT, LI, LU, NL, SE A mouth-soluble pharmaceutical tablet composition which is slowly dissolvable in the oral cavity, comprising: acetylcysteine; a mixture of sodium bicarbonate and potassium bicarbonate wherein the weight ratio NaHCO₃/KHCO₃ is between 93:7 and 97:3, and wherein said mixture is present in an amount of 45-55 parts by weight based on 100 parts by weight of acetylcysteine; a mixture of two carbohydrates selected from the group consisting of sorbitol, xylitol and fructose, wherein the weight ratio between said two carbohydrates is from 0.8 to 1.2 and 1.2 to 0.8, and wherein said carbohydrate mixture is present in an amount of 20-50 parts by weight based on 1 part by weight of acetylcysteine; and a fruit flavoring. The composition according to claim 1 wherein said fruit flavoring is chosen from orange, lemon,grapefruit, peach and apricot flavoring. The composition according to claim 1 having an acetylcysteine content of between 50 and 300 mg per dose. Claims for the following Contracting States : GR, ES Process for the production of a mouth-soluble pharmaceutical tablet composition which is slowly dissolvable in the oral cavity, comprising the mixing of: acetylcysteine; a mixture of sodium bicarbonate and potassium bicarbonate wherein the weight ratio NaHCO₃/KHCO₃ is between 93:7 and 97:3, and wherein said mixture is present in an amount of 45-55 parts by weight based on 100 parts by weight of acetylcysteine; a mixture of two carbohydrates selected from the group consisting of sorbitol, xylitol and fructose, wherein the weight ratio between said two carbohydrates is from 0.8 to 1.2 and 1.2 to 0.8, and wherein said carbohydrate mixture is present in an amount of 20-50 parts by weight based on 1 part by weight of acetylcysteine; and a fruit flavoring. The process according to claim 1 wherein said fruit flavoring is chosen from orange, lemon, grapefruit, peach and apricot flavoring. The process according to claim 1 wherein said composition has an acetylcysteine content of between 50 and 300 mg per dose.

Inventors: LUALDI, PAOLO, ZIGGIOTTI, ANTONIO
Applicants: ALTERGON S.A.
Application year: 1989
Main classification: A61K9
IPC codes: A61K9, A61K31