Pharmaceutical compositions containing androst-5-ene-3-17th-diol, and its use

 

Androst-5-ene-3-17th-diol (5-diol) is used to treat or reduce the likelihood of osteoporosis or menopausal symptoms, or other disorders caused by activity of the estrogen receptor, and conditions that respond positively to treatment with dehydroepiandrosterone (DHEA). 5-Diol provides the optimal ratio of estrogenic activity to androgenic activity and lower maximum androgenic activity compared to DHEA. 5-Diol is particularly suitable for the treatment of conditions where the required estrogenic activity with minimal androgenic activity. 14 C. and 6 C.p. f-crystals, 18 ill.

Description text in facsimile form (see graphic material)

Claims

1. The pharmaceutical composition that provides increased concentrations of sex steroids, consisting mainly of a pharmaceutically acceptable diluent or carrier and a therapeutically effective amount of androst-5-ene-317th-diol or prodrug, is present either as a single active ingredient or osterone, sulfate dehydroepiandrosterone, progestin and estrogen, and prodrugs of any of the above compounds, where any prodrug is a pharmaceutically inactive derivative of the active ingredient, which is enzymatically or spontaneously transformed in vivo to the active ingredient.

2. The pharmaceutical composition according to p. 1, containing a therapeutically effective amount of estrogen.

3. The pharmaceutical composition according to p. 1, containing a therapeutically effective amount of progestin.

4. The pharmaceutical composition according to p. 2, containing a therapeutically effective amount of progestin.

5. The pharmaceutical composition according to p. 1, containing a compound selected from the group consisting of dehydroepiandrosterone and dehydroepiandrosterone sulfate.

6. The pharmaceutical composition according to p. 1, further containing a pharmaceutically acceptable diluent or carrier for percutaneous introduction or insertion through the mucous membrane, where the specified androst-5-ene-317th-diol or prodrug is present in a concentration of, part 2 - 20% of the total weight of the pharmaceutical composition.

7. The kit contains a first container comprising an active derivative of the active ingredient and which is spontaneously or enzymatically converted in vivo to the active ingredient, and at least one additional container, comprising at least one active ingredient selected from the group consisting of progestin, estrogen, dehydroepiandrosterone, dehydroepiandrosterone sulfate, and prodrugs of any of the above compounds.

8. therapeutic method of treating or reducing the likelihood of the formation of low or unbalanced concentrations of sex steroids, including the stage of introduction to a patient in need, a therapeutically effective amount of androst-5-ene-317th-diol or its prodrug, which is pharmaceutically inactive derivative of the active ingredient and which is spontaneously or enzymatically converted in vivo to the active ingredient.

9. The method according to p. 8, which additionally provides for the introduction of at least one additional active ingredient selected from the group consisting of dehydroepiandrosterone and dehydroepiandrosterone sulfate as part of combination therapy.

10. A method of treating or reducing the likelihood of menopausal symptoms, including stage injection to a patient in need, a therapeutically effective is which is pharmaceutically inactive derivative of the active ingredient and which is spontaneously or enzymatically converted in vivo to the active ingredient, moreover, this prodrug is not deformat of androstenediol.

11. A method of treating or reducing the likelihood of vaginal atrophy, including the stage of introduction to a patient in need, a therapeutically effective amount of androst-5-ene-317th-diol or its prodrug, which is pharmaceutically inactive derivative of the active ingredient and which is spontaneously or enzymatically converted in vivo to the active ingredient.

12. A method of treating or reducing the likelihood of hypogonadism, including the stage of introduction to a patient in need, a therapeutically effective amount of androst-5-ene-317th-diol or its prodrug, which is pharmaceutically inactive derivative of the active ingredient and which is spontaneously or enzymatically converted in vivo to the active ingredient.

13. A method of treating or reducing the likelihood of osteoporosis, including the stage of introduction to a patient in need, a therapeutically effective amount of androst-5-ene-317th-diol or its prodrug, which Yao is converted in vivo to the active ingredient.

14. A method of treating or reducing the likelihood of low libido, including the stage of introduction to a patient in need, a therapeutically effective amount of androst-5-ene-317th-diol or its prodrug, which is pharmaceutically inactive derivative of the active ingredient and which is spontaneously or enzymatically converted in vivo to the active ingredient.

15. A method of treating or reducing the likelihood of skin atrophy, including the stage of introduction to a patient in need, a therapeutically effective amount of androst-5-ene-317th-diol or its prodrug, which is pharmaceutically inactive derivative of the active ingredient and which is spontaneously or enzymatically converted in vivo to the active ingredient.

16. A method of treating or reducing the likelihood of urinary incontinence, including the stage of introduction to a patient in need, a therapeutically effective amount of androst-5-ene-317th-diol or its prodrug, which is a pharmaceutically active inactive derivative hinge or reduce the likelihood of dry skin, including the stage of introduction to a patient in need, a therapeutically effective amount of androst-5-ene-317th-diol or its prodrug, which is pharmaceutically inactive derivative of the active ingredient and which is spontaneously or enzymatically converted in vivo to the active ingredient.

18. A method of treating breast cancer, uterine cancer, ovarian cancer or endometriosis, including the stage of introduction to a patient in need, a therapeutically effective amount of androst-5-ene-317th-diol or its prodrug, which is pharmaceutically inactive derivative of the active ingredient and which is spontaneously or enzymatically converted in vivo to the active ingredient, in combination with an antiestrogen and at least one of the following compounds: androgen, DHEA, an aromatase inhibitor, an inhibitor 17-hydroxysteroid-dehydrogenase, agonist or antagonist releasing hormone luteinizing hormone.

19. A method of treating breast cancer, uterine cancer, ovarian cancer or endometriosis, including the stage of introduction of the patient who needs it the following communications: an antiestrogen, the androgen inhibitor of the aromatase inhibitor 17-hydroxysteroid-dehydrogenase, agonist or antagonist releasing hormone luteinizing hormone.

20. A method of treating or reducing the likelihood of diseases selected from the group consisting of obesity, cardiovascular disease, atherosclerosis, insulin resistance, loss of muscle mass, loss of energy or fatigue, memory loss, Alzheimer's disease, introducing a therapeutically effective amount of the pharmaceutical composition under item 1, where deformat of androstenediol is not used as prodrugs of androst-5-ene-317th-diol.

 

Same patents:

The invention relates to medicine, in particular to clinical medicine, and can be used for the prevention and recovery of cardiac arrhythmias in patients with coronary artery disease

The invention relates to medicine and can be used to provide emergency assistance in hypertensive crisis

The invention relates to medicine and can be used as a tool for emergency medical self-care for acute heart failure

The invention relates to new sulfadimethoxine compounds of formula I, where R(1)-R(9) and have the values listed in the description with+channel blocking action, as well as pharmaceutical compositions based on them

The invention relates to medicine and refers to the funds that affect the cardiovascular system

The invention relates to medicine and refers to the funds that affect the cardiovascular system

The invention relates to medicine and for the prevention and treatment of arteriosclerosis
The invention relates to medicine, namely cardiology, and for the treatment of patients with the syndrome sick sinus
The invention relates to medicine, namely cardiology, and for the treatment of patients with the syndrome sick sinus

The invention relates to the derivatives of dihydronaphthalene formula I, where R1represents hydrogen, hydroxyl or alkyloxy, R2represents hydrogen, lower alkyl, aralkyl or phenyl, and R3represents pyridyl or imidazolyl

The invention relates to new non-steroidal compounds which are high-affinity modulators of steroid receptors

The invention relates to medicine, namely to gynecology
The invention relates to medicine

The invention relates to medicine, in particular to pharmacology concerns the pressed tablets desogestrel made by dry granulating method, and method of manufacturing of tablets, capsules or granules, containing desogestrel, by roller compaction or by moulding blanks, in which desogestrel optionally with other active compounds and/or fillers in the first step of the method is then pressed at high pressure, after which the second stage breaks up the particles and in the third stage of these particles produce tablets or fill their capsules with known methods

The invention relates to benzothiophene compounds of formula I, where R1-H, - OH, -O(C1-C4alkyl), - EA6H5-, OCO(C1-C6alkyl), or-OSO2(C2-C6alkyl);

R2IS-H, -OH, -O(C1-C4alkyl), EA6H5, CCA(C1-C6alkyl) , -OSO2(C2-C6alkyl), or halogen; R3- 1-piperidinyl, 1-pyrrolidinyl, methyl-1-pyrrolidinyl, dimethyl-1-pyrrolidinyl, 4-morpholino, dimethylamino, diethylamino, diisopropylamino or 1 hexamethyleneimino; n = 2 or 3; Z Is-O - or-S-, or their pharmaceutically acceptable salts

The invention relates to medicine

The invention relates to pharmaceutical industry and medicine and relates to products containing derivatives of gamma-aminobutyric acid and affecting the cardiovascular system
Up!