UA84688C2 - Drug for treatment of erectile disfunction - Google Patents

Abstract

The invention relates to medicine, in particular to the use of sildenafil trigluconate as a drug for treatment of erectile disfunction.

Description

patients personally. In addition, in 20-309 men - a description of the methods of obtaining the remedy according to the erection achieved in this way acquired signs of priapism (i.e., it was accompanied by persistent pain), - a description of experiments to check the effective and long-term use of the indicated method of infertility of the remedy on experimental models and medko caused fibrosis in the injection sites and the need for their surgical treatment with the corresponding recommendations for its use. myself

The same shortcomings (Orsi. Horpinchenko) reveal 1) The method of obtaining sildenafil trigluconate during intracavernous administration of other shaft dilators, for example, chlorpromazine, phento- Sildenafil trigluconate was obtained: lamin, moxicillin, vasointestinal peptide - or from the basis of sildenafil by adding in her and their combinations. water-alcohol solution of gluconic acid (z

Less traumatic treatment of erectile di- calculation of mol of gluconate anions per 1 mol of sysfunction by transurethral administration of ldenafil) followed by evaporation of alprostadil solution, i.e. prostaglandin E1 (orsi. niks under vacuum and drying of the target product in

Horpinchenko ei ai). desiccators over dispersed calcium oxide,

Unfortunately, it provides a full-fledged erection not - or from available on the pharmaceutical market in more than 3095 men. sildenafil citrate by adding to its aqueous

The path to a practically acceptable treatment with an alcohol solution of the appropriate amount of gluconate of erectile dysfunction in men was opened when the company "Rii7eg" created a vasodilator on the basis of the reaction mass with sodium (or potassium) and careful mixing before the appearance of a precipitate of sodium citrate in sildenafil citrate. Erection after application (or potassium). After that, the sediment was separated by filtering this drug by men according to direct prescription, and the target product was isolated from the filtrate, ching, that is, as a vasodilator, was detected as described above. accidentally. But then, on the basis of sildenafil citrate, the tablet "Viagra" was created, and sildenafil trigluconate is specially designed for the treatment of erectile dysfunction (Orsii Gorpinchenko, EI). This means of the speed of action of the proposed means in comparison is the closest in technical essence to the proposed sildenafil citrate action was used with the means. while perfusion of isolated blood strips

Indeed, the oral use of vascular tablets (namely rat aorta) with aqueous solutions of "Viagra" in 63-8295 patients causes a rather persistent of these drugs (see Sperelakis N. Zlect - erection for a time sufficient for full-fledged staterophysiology of vascular smooth muscles. - In the book: Act of Physiology and Pathophysiology of the Heart, in 2 volumes.

However, sildenafil citrate as such has to- M.: Medicine. - 1988, vol. 2, p. 428-470). This method has low bioavailability. Thus, dependence on is considered adequate for determining the activity of the patient's stomach and the acidity of the solution of erectile dysfunction treatment IV.V. of cranial juice is absorbed only from 40 to 60905 pe- Frolkis, V.V. Bezrukov, L.T. Malaya et al. Mecharorally administered dose. Since the path from the gastrointestinal tract to the bloodstream is quite long, the waiting period and pathogenetic treatment of cardiovascular diseases is rarely less than 40 minutes, which is very vascular system// Blood circulation and hemostasis. - inconvenient The use of high (of course not 2003, Me2, p. 42-48). less than 5 Ωg) of single doses of the active substance with the aim of measuring erectile activity was the expression - compensation of the indicated deficiencies causes undesirable side effects in the abundance of dilator reactions of the perfused strips of these patients, namely (taking into account the effective doses headache (from 17 to 3095), dyspepsia (from 17 to EDvo-0.016:20.003mM/l for silde-20965 trigluconate) and a violation of color perception (within nafil and ED5o-0.03630.004mM/l for silde-9-1195 citrate) (SO Mozbu'z, 2000).denafil).

The basis of the invention is the task by The obtained results are shown in the graph. changes in the qualitative composition are created on the basis of silde- The specific method of obtaining experimental nafil such a means for the treatment of erectile di- data for plotting the graph is clear from the function that would have increased bioavailability and the examples below. therefore, it would provide the necessary therapeutic Example 1. A strip of rat aorta initially per- effect even in relatively small doses. were fused with standard Krebs solution.

This problem is solved by the use of triglucon- After the stabilization of the length of the strip (due to the 6-nate sildenafil as a means for the treatment of erectile dysfunction), potassium chloride was added to the solution in the concentration of dysfunction. 10bMM/l which led to contraction (spasm)

As will be shown later, trigluconate silde- vessels. Then trinafil was added to the perfusion solution. Sildenafil gluconate at a concentration of 107 mM/l and lower doses than sildenafil citrate was added to the perfusion solution. registered relaxation of the vessel at 8095 in relation to

A brief description of the illustrations of the original length, which indicates a vividly expressed

The attached graph shows the dilator and dilator effect of the agent according to the invention. reaction of strips cut from the aorta of rats to the effect of Example 2. A strip of a rat aorta was first treated with sildenafil pertrigluconate and sildenafil citrate. were fused with standard Krebs solution.

The best options for implementing the invention After the stabilization of the length of the strip (after 6-

Next, the essence of the invention is explained: min.) concentrated potassium chloride was added to the solution

106MM/l, which led to contraction (spasm) of transdermal or urethral applications and vessels. Then cit-rectal suppositories were added to the perfusion solution. rate of sildenafil in a concentration of 107mM/l and registered the industrial suitability of the vessel relaxation by 5295 in relation to the output. The means according to the invention can be easily produced. This is much less than industrially grown and used for the application of sildenafil trigluconate. effective treatment of erectile dysfunction in

C. Methodological recommendations for the use of doses that are significantly lower compared to the citrate of sildenafil for the treatment of erectile dysfunction. Yes, experimental data show that

The tool according to the invention can be used depending on the concentration of triglu- for the treatment of erectile dysfunction in the form of sildenafil conats for more than 5095 effective tablets, used reg o5 or preferably more than sildenafil citrate. ngual (sublingual), as well as in the form of an aerosol. It is clear that reducing doses will allow for inhalation, spray, capsules, drops, injections to weaken (and sometimes completely eliminate) the manifestation of negative bilateral effects. va petes tsa ethnic tini inn babysitter sh currants nen i KK checks n kkunineninnnnksnknkoy

Meaning:

OTO Yara tet von - in the same days

ES popolooonon ap r-n sildenafipu citrah.

In ho shu ryttia inn: that Sildenafil urigluvanyat - ; Pn nannya za - peee nt ttsinyuinntyutnnnnn sh 20 PI zha Sudno rey Z : nt z H za - nyni penya

Z z z po V V KO V V o 17 voFovo ziooo obo 10060 concentration of substances

Computer layout V. Klyukin Signature Circulation 28 approx.

Ministry of Education and Science of Ukraine

State Department of Intellectual Property, str. Urytskogo, 45, Kyiv, MSP, 03680, Ukraine

SE "Ukrainian Institute of Industrial Property", str. Glazunova, 1, Kyiv - 42, 01601