Please wait...



Goto Application


Note: Text based on automatic Optical Character Recognition processes. Please use the PDF version for legal matters

[ EN ]
Techni ca I field
The present invention relates to a pharmaceutical composition having therapeutical and/or prophylactic effect against obstruct 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 agonists, 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 thereby provides for a more easy breathing mechanism.

-9 It is further known that isoprenaline in increasing doses (10
to 10 M) increases the activity of adenylate cyclase in cells of normal as well as hypothyroi di c , as well as hy pert 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 composition comprises a ther aeut 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 conditions, cronicaL bronchitis, and other diseases involving an obstruction of the lungs.

The invention will be described more in detail in the following with reference to some examples however, without being restricted thereto.

Example 1
Terbutaline sulphate and t r i odothyron ine were granulated together using ethano L /water together with 1-2% of sorbitan, calculated 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 terbuta I i ne : t r i iodothyroni ne was 50:50.

At the treatment of an asthmatic patient the daily dose of terbutaline could be decreased with 40 % by weight at acute asthmatic attacks. At daily 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 therapeutic 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 local administration to the bronchii.

The molar ratio of sa I butamo le : t hyrox 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 lowered to the corresponding degree.

By means of the present invention the daily 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 hormone 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 depending on the status of the patient.

The active compounds can be administered together with every suitable inert diluent 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 intravenously, for a more rapid effect.

Other types of administration than aerosole powder and inject-able solutions may exist, preferably at a prophylactic treatment when the composition can be administered in the form of tablets, pills, rectal pi lls, or granules, coated or uncoated.