PHARMACEUTICAL COMPOSITION FOR TREATMENT OF LUNG OBSTRUCTIONS

Abstract: The present invention relates to a pharmaceutical composition for a therapeutic and/or prophylactic treatment of lung obstructions, whereby the therapeutically active part of the composition consists of a therapeutically active amount of at least one beta adrenergic agonist and a therapeutically active amount of at least one active thyroid hormone.

Description: PHARMACEUTICAL CXDMPOSITi SI FOR TREATMENT]? OF LUNG OBSTRUCTIONS DESCRIPTION Techni ca I field The present invention relates to a pharmaceutical composition having therapeutical and/or prophylacti c effect against ob¬ struct i ona I conditions in the lungs. The object of the present invention is to obtain a possibility to improve the therapeutical and prophy lact ca I treatment of obstruct iona I conditions of the lungs, such asthma and cronical bronchit s by increasing the effect of beta-adrenergic ago¬ nists, as well as unspeci f i cal ly widen the bronchii . Background of the invention It is previously known to use beta-adrenerg c agonists, so called beta-stimulators, and more particularly beta-2-sti mu- lators, in treating asthmatic conditions, whereby a beta-2- stimulator is normally administered locally to the bronchii and, there, by means of its stimulating effect on the beta- receptors present creates a widening of the bronchii and the¬ reby provides for a more easy breathing mechanism. -9 It is further known that isoprenaline in increasing doses (10 -4 to 10 M) increases the activity of adenylate cyclase in cells of normal as well as hypothyroi di c , as well as hypert h roid i pati ent s . Description of the present invention It has now surpringly been shown possible to be able to increa- se the effect of adrenergic beta-receptor agonists by means of the present invention which is characterized in that the com¬ position comprises a theraeut i ca I ly active amount of a beta- adrenergic agonist, as well as a therapeutically active amount of at least one active thyroid hormone. Further characteristics are evident from the accompanying c lai ms . Suitable beta-adrenergic agonists are preferably salbutamole, terbutaline, phenotrole, epinephrine, i sop rena I ne , orcipre- naline, and riniterole, as well as other unspecific beta-2- agonists and specific beta-2-agoni sts . The active compounds are generally used in salt form, such as hydrochloric, sulphate. Suitable active thyroid hormones are thyroxine, t ri odoth ro- nine, di iodothyroni ne, and other active analogues of thyronine. The compositions according to the present invention have turned out to be active preferably in the treatment of asthmatic con¬ ditions, cronicaL bronchitis, and other diseases involving an obstruction of the lungs. The invention wi ll be described more in detai l in the following with reference to some examples however, without being restric¬ ted thereto. Example 1 Terbutaline sulphate and t r i odothyron ine were granulated to¬ gether using ethano L /water together with 1-2% of sorbitan, cal¬ culated on the weight of the therapeutically active compounds, as a granulating agent, dried and then ground to a fine powder having a particle size suitable for being administered in the form of an inhalation aerosole for the Local treatment of the lungs. The molar ratio of terbutaI ine: tr i iodothyroni ne was 50:50. At the treatment of an asthmatic patient the dai ly dose of ter¬ butaline could be decreased with 40 % by weight at acute asth¬ matic attacks. At dai ly maintenance dose used for prophylactic reasons, which was 50 % by weight of a normal terbutaline dose the number of asthmatic attacks could be considerably reduced. This proves that the present composition possesses a therapeu¬ tic effect as well as a prophylactic effect. E x a mp l e 2 Salbutamole and thyroxine were treated in the same way as in the Example 1 above for the formulation of an aerosole for lo¬ cal administration to the bronchii . The molar ratio of sa I butamo le : thyrox i ne was 60:40. At the treatment of an asthmatic patient the same good results were obtained as when using the composition according to Examp- le 1. The therapeutic and prophylactic dose could thus be lo¬ wered to the corresponding degree. By means of the present invention the dai ly therapeutical dose of beta-adrenergic agonists can thus be lowered with up to 60% when discussing terbutaline. The relation between beta-adrenergic stimulator to thyroid hor¬ mone ar 100:1, preferably 10:1 and down to 1 :1. Suitable single doses are 1 to 1000 .ug of active compound, suitably 10 to 500 ug. The composition can be administered 1 to 3 times a day de¬ pending on the status of the patient. The active compounds can be administered together with every suitable inert di luent and expedient to the formation of an aerosole being distributed through an inhaler to the bronchii . The compositions can also be produced in the form of a solution intended for injection in the case a larger acute dose has to be administered to for example an unconscious patient in order to rapidly improve the lung status. In such cases the co po- nents are dissolved in the form of watersoluble salts in an isotonic saline solution which is injected, preferably intra¬ venously, for a more rapid effect. Other types of administration than aerosole powder and inject- able solutions may exist, preferably at a prophylactic treat¬ ment when the composition can be administered in the form of tablets, pi lls, rectal pi lls, or granules, coated or uncoated.

Claims: CLAIMS 1. Pharmaceutical composition for a therapeutic or prophylactic treatment of lung obstructions, characterized in that it, besi¬ des inert diluents and expedients consists of a therapeuti ca l- ly active amount of at least one beta adrenergic agonist and a therapeutically active amount of at least one active thyroid hormone . 2. Pharmaceutical composition according to claim 1, characteri- zed in that the ingoing amount of beta adrenergic agonist is reduced with up to 60% in relation to the situation when the agonist is used alone for the same indication. 3. Pharmaceut cal composition according to claim 1, characteri- zed in that the ingoing amount of active thyroid hormone is re¬ duced with up to 60% in relation to the situation when the hoi— mone is used alone. 4. Pharmaceu ical composition according to claims 1 to 3, cha- racterized in that the beta adrenergic agonist is selected from the group consisting of salbutamole, terbutaline, phenoterole, epinephrine, i soprena I ine, o rci prena I ine, riniterole and other unspecific and specific beta-2-adrenergi c agonists. 5. Pharmaceutical composition according to claims 1 to 3, cha¬ racterized in that the active thyroid hormone is selected from the group consisting of thyroxine, tr iodothyroni ne, diiodo- thyronine, and other active thyronine analogues. 6. Pharmaceut cal composition according to claims 1 to 5, cha¬ racterized in that it is present in the shape of an administ¬ ration form suitable for inhalation. 7. Pharmaceutical composition according to claims 1 to 5, cha- racterized in that it is present in the shape of an injectable solution. 8. Pharmaceutical composition according to claims 1 to 5, cha¬ racterized in that it is present in the shape of an administra¬ tion form for peroral use. 9. Pharmaceutical composition according to claims 1 to 8, cha¬ racterized in that the molar ratio between the ingoing beta adrenergic agonist and the thyroid hormone is 100:1 - 1:1, pre¬ ferably 10:1 - 1:1. 10. Pharmaceutical composition according to claims 1 to 9, cha¬ racterized in that the single dose of active components is 1 to 1000 #ug, preferably 10 to 500 .ug, when administered in the form of an inhalation composition.

Inventors: SMITH ULF PER GUSTAV, WESSLAU CHRISTIAN, SMITH, ULF, PER, GUSTAV, WESSLAU, CHRISTIAN
Applicants: SMITH ULF PER GUSTAV, WESSLAU CHRISTIAN, SMITH, ULF, PER, GUSTAV, WESSLAU, CHRISTIAN
Application year: 1989
Main classification: A61K45
IPC codes: A61K31, A61K38, A61K45, A61P11, A61P25