DK9300080U4 - Suction or chewable tablet containing ubiqinone - Google Patents

Description

The invention relates to a suction / chewable tablet for use in the controlled release of ubiqinone for i. oral mucosa.

Ubiqinone is coenzyme Q10 (CoQ10), also called vitamin Q, and the ischemic name is 2,3-dimethoxy-5-methyl-6-decaprenyl-1,4-benzoquinone. Ubiqinone is an important part of the so-called electron transport chain imitochondria membrane. which binds the energy of the nutrients iadenosine triphosphate (ATP), the cell's energy store. Specifically, ubiqinone is part of the enzyme succinate dehydrogenase co-Q10, see Flytlie, K. T. and Dhalvad, T.: Q10 - Your body's fuel. Published New Science, 1991, 96 pp. And Hessel, L.: The secret of Q10., Lademann's health series. Det Ny Lademann A / S, 1992, 64 pp., Is hereby incorporated in its entirety as references.

By the addition of ubiqinone to suction or chewable tablets, the release of the substance is achieved during the period in which the tablet is sucked or chewed.

It is known to administer pharmacologically / biologically active substances by release from lozenges or bolches. For the treatment of oral cavities and pharynx, lozenges are often used, eg Hexokain® lozenges from DAK-Laboratoriet A / S, Copenhagen, containing the active substances benzocaine and chlorhexidine hydrochloride. Furthermore, it is known to produce caches containing cough suppressants. medicaments.

However, these known lozenges or bolches do not contain ubiquinone, and it is desired to provide a suction or tablet tablet with improved effect on oral cavity disorders, including periodontosis. At the same time, a number of other beneficial effects are obtained which are not limited to the oral cavity, as the released ubiqinone co-injected will pass through the esophagus and stomach and be absorbed into the digestive tract. Ubiqinon's beneficial effects include both prevention and treatment of a variety of disorders such as angina pectoris, hypertension, muscular dystrophy and periodontal disease, Greenberg: J. Clin. Pharmacol. 1990, 30: 596-608. Ubiqinone significance for weight regulation has also been studied, see VanGaal, L., DeLeeuw, J., Vadhsnsvikit, S. et Folkers, K.: Biomed. andcl in. aspects of Q10; 4: 369-373, (1984).

What is new in the manufacture consists in the formulation of a sugary chewable tablet comprising a preventative and / or therapeutic amount of ubiqinone.

By sucking or chewing said new tablet, an extended or controlled release of ubiqinone to the oral mucosa and, secondarily, to the gastrointestinal tract is achieved. This ensures a direct effect of ubiqinone in the prevention and treatment of diseases of the oral cavity, preferably periodontosis.

For the preparation of ubiquinone lozenges, a hard tablet form is preferred which is slowly dissolved or disintegrated in the oral cavity during the release of ubiqinone. Suction tablets are made by casting and cutting or by compression. In casting, the ingredients are mixed as powder or in liquid form with the tablet base, usually sucrose, acacia or tragacanth, to produce a paste cut into uniform pieces which are dried in a heat chamber. Flavoring and coloring can be added. Suction tablets prepared by compression are prepared as usual tablets using conventional tablet aids such as 1 actose, dextrose, starch, sodium chloride and acacia, in dry or moist granulation but where higher compression pressures are used.

For the preparation of ubiquinone chewable tablets, a softer tablet, preferably a gelatin, starch or pectin tablet, in which ubiqinone is distributed, is preferred, preferably as a dispersed powder.

In a preferred embodiment of the preparation, an amount of from 1 mg to 200 mg, preferably from 10-30 mg, from 50-75 mg or from 100-150 mg of ubiqinone, and preferably in microcapsulated form, is added to the one suction or chewable tablet of 1 g. oxidation protection and slow release during suction / chewing are obtained. Preferably, the microcapsules have a diameter of less than 100 µm.

Since ubiqinone is lipid soluble, an oil solution, such as soya oil solution, is added to a natural emulsifier such as lecithin, preferably soya lecithin or a suspension or emulsion in soya lecithin to ensure absorption into the aqueous environment of the oral cavity and gastrointestinal tract. Hiro et. eel. (Biomedical and clinical aspects of coenzyme Q, Volume 4, Elsevier, (1984)) have shown that atubiqinone is best absorbed as lipid solution. In addition, additional additives may be used that increase the uptake of ubiqinone alone or in conjunction with lecithin.

The ubiquinone solution, suspension or emulsion may be microencapsulated in a colloid matrix such as gelatin, gum arabic, starch etc. or in sugar.

Ubiqinone can also be added directly to the suction / chewable tablet in solid form e.g. as a granule or powder form in admixture with soy lecithin preferably in a 1: 1 ratio.

The daily dose should be at least from approx. 30 mg to approx. 100 mgubiqinone declared almost without side effects, see Langsjoen, P.H. et Folkers, K.: Am. J. Cardiol .: 65: 7: 521-3 (1990). Therefore, it is recommended to suck or chew at least 1 tablet of 30 mg microencapsulated ubiqinone for at least 10 minutes daily.

The tablet also preferably comprises flavors such as peppermint oil and fruit flavors and sweeteners such as sugar, including sucrose, 1 actose, fructose and glucose, or sugar alcohols, preferably sorbitol or xylitol.

Ubiqinon has no particular taste and can therefore be mixed with the most common sugary or chewable tablet recipes without the addition of additional flavor or sweeteners.

The preparation preferably comprises a lozenge of from 10 to 100 mg, preferably from 30 to 70 mg of a mixture of ubiquinone and lecithin in a ratio of 1: 0.5 to 0.5: 1.

The production is further described in the following examples.

Example 1

Suction tablets of 1 g per gram are known in the known manner. PCS. with the following content in mg: sucrose 300 mg 1 actose 639 mg flavors 1 mg ubiqinone / lecithin mixture 1: 1 60 mg

The tablets should be packed in light-tight packaging as ubiqinon is degraded by sunlight.

Example 2

Suction tablets of 1 g per gram are known in the known manner. PCS. with the following content in mg: licorice extract 70 mg anis oil 5 mg menthol 5 mg saccharin sodium 300 mg magnesium stearate 600 mg ubiqinone / lecithin mixture 1: 1 20 mg

Example 3

Suction tablets of 1 g per gram are known in the known manner. PCS. with the following content in mg: acacia rubber 35 mg tragacanth 10 mg eucalyptus oil 5 mg sorbitol 150 mg magnesium stearate 700 mg ubiqinone / lecithin bl breath 1: 1 100 mg

Claims (9)

1. Suction or chewable tablet containing ubiqinone. 2. Suction or chewable tablet containing ubiqinone in a preventive and / or therapeutic amount. The tablet of claim 1 or 2 containing from 10 to 30 mg of ubiquinone per day. PCS. The tablet of claim 1 or 2 containing from 50 to 75 mg of ubiqinone per day. PCS. The tablet of claim 1 or 2 containing from 100 to 150 mgubinquinone per day. PCS. Tablet according to any one of the preceding claims, characterized in that the ubiquinone is microencapsulated. Tablet according to any one of the preceding claims, characterized in that it comprises from 1 to 10% of a single mixture of ubiquinone and lecithin in a ratio of 1: 0.5 to 0.5: 1. A tablet according to any one of the preceding claims for the prevention and / or treatment of periodontosis. A tablet according to any one of the preceding claims prevention and / or treatment of overweight.