Cigarette filter for the administration of taurine by inhalation.

(12) PATENT

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NORWAY (19) NO (11) 307451 (13) B1 (51) Int Cl⁷ A 61 M 15/06, A 24 D 3/00, A 61 K 31/165,

A61 K 31/185

NIPO

<td>(21) Application no (22) Starting day (24) Running day (41) Alm. avail. (45) Date announced</td><td>19933483 (86) Int. Entering day and 1993.09.29 application number 1993.09.29 (85) Continuation Day 1994.04.05 (30) Priority 1992.09.30, FR, 9211645 2000.04.10</td>

<td>(71) Patent holder (72) Inventor (74) Agent</td><td>Jesus Covarrubias, 2 Cerrada de San Jeronimo 110, Mexico 20 - DF, MX Applicant Bryn &amp; Aarflot AS, 0104 Oslo</td>

<td>(54) Designation</td><td>Device for administration of taurine by inhalation</td>

<td>(56) Cited publications</td><td>Am. Fox. Resp. Dis., Vol. 131, n 4 Suppl., 1985, Abstract A 179, Gordon et al: Taurine Prevention Nitrogen Dioxide Disruption of Bronciolar Epithelial Barrier Function EP 3064</td>

<td>(57) Summary</td><td>Apparatus for administering taurine to smokers, by inhalation, comprising a cigarette filter (1) comprising: a filtering material (4) for filtering the smoke from burning tobacco (3) passing through said filtering material (4), and means for including taurine (5) in said filtration material (4) and introducing it into the smoke as it passes through said filtration material (4). The device is useful for preventing diseases of the respiratory tract of smokers.</td>

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The present invention relates to a device for the oral delivery of medical or nutritional substances, and more particularly to a device for administering a pharmacologically active substance, such as taurine, to a smoker's lungs, by inhalation, par ticularly in a preventive treatment of diseases of the airways.

Several devices are known in which active or aromatic substances are added to a cigarette to modify the taste or to confer similar properties. For example, U.S. Pat. The smoker can gain moisture by squeezing the filter to cause the capsule to burst, or may leave the capsule unbroken to inhale dry smoke. For example, the liquid incorporated in the capsules may contain flavoring agents or a synthetic saliva solution.

It is also known to include a substance having medicinal properties in the cigarette tobacco. U.S. Patent 4,498,495 includes interferon in the cigarette tobacco to administer it directly to the smoker's lungs.

Taurine (or 2-aminoethanesulfonic acid) is a low-toxic amino acid possessing some known pharmacological properties that may be useful in the therapy for the treatment of congestive heart failure, but taurine activity is very low and cannot effectively used as a drug. Taurine amides showing mucolytic, hepatoprotective, detoxicant and normolipemizing properties are described in European Patent Application 307,788.

RE Gordon et al. describes in an article titled Taurine protects hamster bronchioles from acute NO2-induced change, AJP (Dec. 1986), the use of taurine in the lining of hamsters, resulting in an improvement in protection against the adverse effects of nitrogen dioxide NO2, which is a component of the urban pollution, and that is included in the tobacco smoke. According to a hypothesis described in the article, taurine is distributed through the animal tissue and contributes to various forms of biochemical reactions to stabilize membranes, remove free radicals and prevent peroxidation. The protective effect of taurine on membranes and against toxic compounds such as oxidants is also described in GE Gaull Taurine as a conditionally necessary nutrient in humans, J. of Am. College of Nutrition

5: 121-125 (1986), whic h considers such effects in human subjects.

Recently, the intravenous administration of taurine in patients who have undergone coronary artery bypass surgery has been shown to reduce myocardial damage by producing an antioxidant and with a cleansing effect. Reference can be made to Ferreira et al., Reduction of reperfusion injury by myocardial revascularization with taurine pills, University of Milan, 15-20. July 1990.

It has also been demonstrated that the administration of dimethyl sulfoxide, in atomized form, by inhalation, is effective in the treatment of smoke-induced pulmonary injury. Reference can be made to Kimura et al. in Treatment of Smoke-Induced Pulmonary Injury by Nebulized Dimethyl Sulfoxide, Alan R. Riss, Inc. (1988). These results are based on animal studies.

Other published test results have established the usefulness of taurine in producing anti-mutagenic effects by inhibiting various putative carcinogenic agents that may cause DNA alterations. These agents contain reactive free radicals. Reference can be made to Laidlaw et al. in Anti-mutagenic effects of taurine - a bacterial assay system, Cancer Research, 49, 66006604 (Dec. 1989).

An object of the present invention is a device for administering taurine to smokers, by inhalation.

More particularly, an object of the invention is to provide a cigarette filter comprising a filtration material for filtering smoke from burning tobacco passing through said filtration material, and apparatus for including taurine in said filtration material and introducing it into the smoke as it passes through said filtration material.

This is achieved according to the invention by a device for administering taurine by inhalation, consisting of a cigarette filter, characterized by a filtration material for filtering the smoke from burning tobacco passing through said filtration material, and means for including taurine in said filtration mat erial and introducing it. into the smoke passing through said filtration material.

According to a preferred embodiment, the device according to the present invention comprises:

a filtration material for filtering the smoke from burning tobacco as it passes through said filtration material;

at least one rupture capsule containing water or an aqueous solution placed in said filtration material such that the capsule ruptures at a pressure on the filter and the water or aqueous solution is distributed into the filtration material.

Taurine may be in the form of a powder included in the filtration material, which further contains at least one capsule containing water or an aqueous solution, or in the form of a solution contained in the capsule (s) included in the filtration material. When taurine is in powder form, it is preferably connected to microcapsules containing water distributed in the filtration material.

The featured features of the present invention will be described in detail in the following description, taken in connection with a preferred embodiment, with reference to the accompanying drawings, which show:

Fig. 1 is a longitudinal section of the filter end of a cigarette comprising the device according to the invention; 2 is a sectional view of a filter showing a second embodiment of the invention; FIG. 3 is a sectional view of a filter showing a third embodiment of the invention.

As shown in FIG. 1, the device according to the invention comprises a filter end 1 of a cigarette comprising a paper 2 which forms a packaging material containing tobacco 3 and a filter consisting of a filtering material 4, such as hard-packed cellulose or similar fibers.

According to the present invention, the device for introducing taurine into filtration material is provided in the form of finely divided taurine powder 5 which is uniformly distributed through the filtration material 4. The powder, which should have the consistency of light talcum powder, is automatically drawn into the smoke as it passes. from the burning tobacco 3 through the filtration material 4 to the smoker's lungs.

If necessary, according to the invention, a solution of taurine can be distributed through the filtering material 4 by rolling the filter 1 between the fingers to crush and rupture the walls of the microspheres 6, containing distilled water, a physiological saline solution or a non-toxic aqueous solution. Thus, by crushing the microspheres by applying a slight pressure on the filter and rolling it between the fingers, a rupture of the thin wall, for example made of epoxy resin or any other inert substance, occurs and thus the aqueous solution or water contained therein is distributed. through the filtration material 4 to form a solution with the taurine powder since taurine is water soluble.

The presence of a taurine solution in the filtration material, which is passed by fast-running smoke, which is hot, emits some evaporation and atomization from the solution, which is then transported into the smoker's lungs.

2 and 3 show two other embodiments of the present invention, where the same references are used to denote the same parts as in FIG. 1.

FIG. 2 shows a rupture capsule 7 having a waterproof wall containing a taurine solution 8 located in the center of the filtration material 4 near the tobacco connection site. By pressing the filter near said junction, the capsule is crushed, the walls burst, and the taurine solution is distributed through the filtration material.

Fig. 3 shows a third embodiment of the filter according to the present invention, in which an oval shaped capsule 9 is placed in the space, within the paper 2, between the tobacco 3 and the filtering material 4. Markings or references 10 are provided on the outer surface of the paper 2 such as the smoker can locate the area where he will squeeze the cigarette to crush the capsule 9 and break the capsule walls. Although most of the taurine solution 8 seeps into the filtration material 4 and into the adjacent tobacco 3, a small portion of the solution remains in the space between the tobacco 3 and the filtration material 4, where it is used as a moisturizing agent and the introduction of the taurine. solution into the smoke passing through the filter.

The embodiments shown in FIG. 2 and 3 may also be modified by providing the capsules 7 and 9 with distilled water or other aqueous solution, and the taurine powder is applied to the filtration material 4. According to the invention, the filter may be as shown in FIG. 1, and it does not contain the fissile microspheres, but only contains powdered taurine.

A particular advantage that results from the presence of taurine in the filter, either in the form of powder or in the form of a solution, is that the dissolution temperature of taurine is 300 ° C. Thus, by adding taurine to the tobacco filling, substantially the desired object of the invention is wiped out, since taurine will be dissolved as the burning tobacco moves forward toward the filter. Thus, the invention differs from US patent no.

No. 4,498,485, which describes the administration of a pharmacologically active substance, such as interferon, into the cigarette tobacco.

The presence of even small amounts of taurine in the cigarette smoke provides an effective taurine delivery system.

When delivered to the lungs, taurine has an advantageous antioxidant effect, as is known from the description above. This effect is enhanced when the administration of taurine takes place in the presence of the smoke of a burning cigarette, which gives an antioxidant effect. Although taurine is intended to act mainly in the lungs, it can also act directly on the smoke by a buffer action, before the smoke reaches the smoker's lungs.

Furthermore, the administration of taurine by inhalation, using the device of the present invention, differs substantially from the administration by oral route, i.e. as a food additive, and does not result in the same effects. When taurine is administered orally as usual, it is exposed to the acidic fluid in the stomach and absorbed into the gastrointestinal system. In contrast, according to the invention, taurine comes into direct contact with the internal walls of the lungs. As mentioned above, the effect of taurine is enhanced, even with relatively small amounts of taurine added to the cigarette filter.

It has been noted that the administration of taurine using the device of the invention provides a protective effect against the harmful effects of the smoke coming from the burning tobacco, verified by the tests of bronchospasm induced by ultrasonic atomization of distilled water. A decrease in bronchospasm is observed when taurine is regularly administered using the device.

The taurine solution contained in the capsules of the device shown in FIG. 2 and 3 is preferably a solution having a taurine content of 0.2% to 2.0% by weight. The water-containing microspheres of the device shown in FIG. 1, must be introduced into the filtration material in such an amount that the concentration of the resulting taurine solution is about 100 mg / ml. The total amount of taurine present in the filter generally comprises between 25 mg and 200 mg, and preferably between 50 mg and 120 mg.