Medicinal products containing finasteride

 

(57) Abstract:

The invention can be used in medicine, in particular as a drug in the form of tablets containing the active ingredient finasteride, lactose, starch, calcium stearate and a binder, and is characterized by the fact that the tablet contains as a binder ethoxylated ether sorbitan General formula

< / BR>
where v+x+y+z= 20; R - monopalmitate, monooleate, trioleate, linoleate, and has a shell consisting of methylcellulose, titanium dioxide and ethoxylated ether sorbitan the above formula, the following ratio of ingredients, wt. %: core: finasteride 3-4, lactose 80-88, ethoxylated ether sorbitan 0.5 to 1.5, calcium stearate 0.5 to 1.5, starch - the rest is up to 100%; shell: ethoxylated ether sorbitan 28-36, titanium dioxide 2-6, methylcellulose - the rest is up to 100%. The invention allows to obtain a simple and accessible form of the medicinal product in the form of tablets containing as active ingredient finasteride, shell, increases the strength of the tablets in the manufacture, stability during storage and provides stability and uniformity of the release of finasteride. table 2.

The invention relates to medicine, in Ho-Aza-5-androst-EN-17 carboxamid.

Finasteride (synonyms - proscar money, finast, proscar, finasteride), a synthetic azasteroid connection with the specific ability to inhibit 5-reductase and convert testosterone into dihydrotestosterone. The use of finasteride is able to inhibit the growth of the prostate, improve the balance of urine when its hypertrophy, reduce the symptoms associated with BPH. Allowed in the country and registered in the RF Ministry of health (Mashkovsky M. D. Medicines. - M., 2000).

Know the use of finasteride to treat acne, female hirsutism, and particularly benign prostatic hyperplasia (U.S. Pat. USA 4760071).

Generalized experience of the conducted research shows that the only accepted pills drug able to reduce the volume of the prostate in benign hyperplasia is finasteride, despite the fact that the drug is very expensive, and its use long-term (0.5 to 2 years).

There are various dosage forms on the basis of finasteride in the form of tablets, capsules and other known under the brand name PROSCAR (U.S. Pat. USA 4732897, 4859681).

Known composition finasteride for oral or parenteral p is get to add as filler lactose, subjected to spray drying, and magnesium stearate. Preparation on the basis of finasteride with/or without the addition of auxiliary active compounds can be obtained in the form of tablets or pills by mixing solid, powdered carrier such as sodium citrate, calcium carbonate and a binder such as polyvinylpyrrolidone, gelatin or cellulose derivatives, adding, if necessary, lubricants such as magnesium stearate or polyethylene glycol. As other forms application, you can use the closed capsules, for example, hard gelatin, and closed soft gelatin capsules containing razmestiteli or plasticizer, such as glycerol. The sealed capsules contain the active ingredient finasteride in the form of granules, a mixture of fillers, such as lactose, starch, cellulose derivatives or highly dispersed silicic acid. In soft capsules the active substance is preferably dissolved or suspended in suitable liquids, such as vegetable oil or liquid polyethylene glycol. Finasteride can be used parenterally. In this case we use the solution of active substance in sesame (sesame) oil or olive mA is blacki.

There is little dosage forms in the form of tablets and capsules, which takes into account the need to ensure their easy swallowing patients, despite the variety of existing known dosage forms of pharmaceuticals for taking them inside.

The authors focused on the development of such a dosage form, which is easy to deal with, especially the elderly and children, who have difficulty swallowing medications. For these purposes, suitable drugs that dissolve inside the mouth. However, they are almost a little because of such defects as:

complex stage production,

- limited use of active constituent substances,

- the difficulty of treatment with these drugs because of their lack of hardness associated with the rapid disintegration and dissolution in the oral cavity.

To eliminate the above disadvantages apply known solid dosage form consisting of a nucleus containing different active substances, and the shell of the polymer, which disguise the taste of medicines and prevent the selection of drug in the oral cavity, but release the medicine after swallowing. The polymer shell is running, neprimechatel, talatalatat cellulose, carboxymethylcellulose.

The closest technical solution to the claimed composition is a solid pharmaceutical composition of the medicinal product finasteride in the form of tablets (U.S. Pat. RF 2173152). In addition to finasteride tablet contains starch, lactose and magnesium stearate as a binder gum, carboxymethylcellulose, polyethylene glycol.

The main disadvantage of this drug is poor (less than 75% within 45 min) release of the active principle, the poor quality of the drug due to the low strength of the tablets in the manufacture.

The purpose of this invention is to provide a simple and accessible form of the medicinal product in the form of tablets containing as active ingredient finasteride, shell, increasing the strength of the tablets in the manufacture.

This goal is achieved through the use of a medicinal product in the form of tablets containing the active ingredient finasteride, lactose, starch, calcium stearate and binder. This tablet contains as a binder ethoxylated ether sorbitan General formula

< / BR>
where v+x+y+z= 20, R - monopalmitate, m is th ether sorbitan the above formula, in the following ratio of ingredients, wt.%:

core:

Finasteride - 3-4

Lactose - 80-88

Ethoxylated ether sorbitan - 0,5-1,5

Calcium stearate 0.5 to 1.5

Starch - the Rest is up to 100%

shell:

Ethoxylated ether sorbitan - 28-36

Titanium dioxide - 2-6

Methylcellulose - the Rest is up to 100%

The technical result obtained by implementing the present invention is the achievement of the required quality, in particular a satisfactory strength, stability during storage, the desired rate of release, regardless of the activity of the gastric and intestinal juices and intestinal motility.

For all formulations of the drug used following the General method of manufacture.

An example implementation of the invention by a method of wet granulation.

Mix the sifted powders finasteride, starch, ethoxylated ether sorbitan moisturize 3% starch paste, mix to a uniform distribution of moisture. The granulate is dried at a temperature of 45oC for 30 minutes, granularit on the device for producing granules through a sieve with the hole diameter of 1.5 mm and dried to a residual moisture content of 1-2%. After dry granuloma film-forming composition, containing methylcellulose, titanium dioxide, ethoxylated ether sorbitan specified formula. Layering is carried out to obtain a satisfactory film thickness. The obtained tablets with an average weight 0,1550 g satisfy the requirements of the pharmaceutical agent. The results are presented in table 1.

Used ethoxylated ether sorbitan, in which:

in the 1 - R - monooleate,

in the 2 - R - linoleate,

in the 3 - R - trioleate,

part 4 - R - monopalmitate.

Studies have shown that the proposed tool provides stability and uniformity of the release of finasteride in the storage of not less than 3 years. The amount of finasteride, released from the tablet (prototype-based), manufactured by MERCK, 3 hours is 57,512,5%, while the same indicator for the claimed composition is 50,76,0%.

The quality indicators derived drugs are summarized in table 2.

In the group treated with finasteride the claimed composition was observed increase in maximum urinary flow rates of 32.5%, figure J-PSS and the volume of the prostate decreased on average by 20 and 32%, respectively.

Likeart and a binder, wherein the tablet contains as a binder ethoxylated ether sorbitan General formula

< / BR>
where v+x+y+z= 20;

R - monopalmitate, monooleate, trioleate, linoleate,

and has a shell consisting of methylcellulose, titanium dioxide and ethoxylated ether sorbitan above formula in the following ratio of ingredients, wt. %:

core:

Finasteride - 3-4

Lactose - 80-88

Ethoxylated ether sorbitan - 0,5-1,5

Calcium stearate 0.5 to 1.5

Starch - the Rest is up to 100%

shell:

Ethoxylated ether sorbitan - 28-36

Titanium dioxide - 2-6

Methylcellulose - the Rest is up to 100%

 

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