TWI307625B - New use of flibanserin - Google Patents

Description

1307625 A7 B7 V. DESCRIPTION OF THE INVENTION (Inventive Description European Patent Application EP-A-526434 discloses the compound 1-[2-(4-(3-trifluoromethyl))piperidinium in the form of the hydrochloride salt. 1-yl)ethyl b 2,3-dihydro-1H-benzimidazol-2-one (Frebencillin), and its chemical structure is as follows:

Fulbencillin exhibits affinity for the 5-HT1A & 5-HT2 receptor. It is therefore useful as a therapeutic agent for the treatment of various diseases such as depression, schizophrenia and anxiety. In studies of male or female patients suffering from sexual dysfunction, it has been found that Fulbencillin, which is in the form of a pharmaceutical acceptable acid addition salt, exhibits an increased demanding property. Accordingly, the present invention relates to the use of flubenzcillin in the form of a pharmaceutically acceptable acid addition salt to prepare a medicament for the treatment of a desired condition. A preferred embodiment of the present invention relates to the use of fenriberin in the form of a pharmaceutical acceptable acid addition salt as it is, in the treatment of a disease selected from the group consisting of an under-required disease, a loss of sexual desire, a sexual demand, a decrease in sexual demand, and a sexual demand. The medical use of a disease that suppresses and loses sexy 'sexy confusion and cold feeling. The best in the present invention is the case of the pharmaceutical acceptable acid addition salt form of fenriberin in the preparation of a treatment selected from the group consisting of insufficiency of insufficiency, the demand for the paper size of the paper, the Chinese National Standard (CNS) A4 specification ( 210 X 297 mm) 1307625 V. Description of the invention (loss, sexual demand, way.

= hair: the best specific example is about the case of medical acceptance of acid plus disease self-contained F = Benxilin found in the material reached in men and women. Ranjie Yue, the other object of the present invention, is preferably a medicine-accepting acid drug: the following:: ί, Flebexillin in the preparation of a treatment for female sexual dysfunction, whether it is a lifelong problem or need, And the pathologically unrelated, u-management and drug production - mental production, organ _ physical and drug production - and mentally produced ' or unknown", can be found to have a beneficial effect. Fulbencillin can be used in the form of its pharmaceutically acceptable acid addition salt. Suitable acid addition salts include, for example, acid additions selected from the group consisting of succinic acid 'hydrobromic acid, acetic acid, fumaric acid, maleic acid, toluene acid, lactic acid, citric acid, hydrochloric acid, sulfuric acid, tartaric acid, and citric acid. As the salt, an acid addition salt of the above mixture can also be used. From the above acid addition salts, preferred are the hydrochlorides and hydrobromides, especially the hydrochlorides. Fulbencillin, which may be used in the form of its pharmaceutically acceptable acid addition salt, may be added to the general pharmaceutical preparation in %, liquid or spray form, as appropriate. The composition may be in the form of, for example, oral, rectal, parenteral or nasal inhalation; it preferably comprises, for example, a capsule, a lozenge, a dragee, a ampule, a test, and a nasal spray. -5- This paper size applies to China National Standard (CNS) Α4 specifications (2ΐ〇χ297 public) 1307625 A7 ______ B7 ____ V. Description of invention (3) Activated ingredients can be added to the general use of pharmaceutical compositions In the agent or carrier, for example, talc, gum arabic, lactose, gelatin, magnesium stearate, corn powder, aqueous or non-aqueous carrier, polyvinylpyrrolidone, semi-synthetic glyceride of fatty acid, benzylammonium chloride , sodium phosphate, EDTA, Tween 80. The composition #father is formulated in the form of a dosage unit, and each dosage unit is suitable for supplying a single dose of the active ingredient. The daily acceptable dosage range is from 0.1 to 4, preferably from 1. to 300, more preferably from 2 to 200 mg. Each dosage unit will usually contain from 001 mg to 丨〇〇 mg, preferably from 1 to 5 mg. Suitable lozenges can be used, for example, by binding the active substance to known excipients (for example, inert diluents such as calcium carbonate, calcium phosphate or lactose), disintegrating agents (such as corn starch or alginic acid), such as starch. Or gelatin, a lubricant such as magnesium stearate or talc and/or a delayed release agent such as carboxymercaptocellulose, cellulose acetate phosphate, or polyvinyl acetate. Tablets can also include many layers. The coated tablet can be prepared by coating a core similar to the manufacture of a tablet, such as a sponge or a shellac, gum arabic, talc, by a substance commonly used for tablet coating. , titanium dioxide or sugar. The core may also contain many layers in order to achieve delayed release or to avoid incompatibility. A similar money coating may comprise a plurality of layers for delayed release, and the above-described excipients may be used for the tablet. The (iv) or glycyrrhizin containing the active substance of the present invention or a combination thereof may additionally contain a sweetener such as saccharin, sweetener, glycerin or sugar, and a flavoring agent such as a flavoring agent such as a scent or an organic extract. It can also contain suspension or increase

1307625 A7

The agent "such as methyl cellulose reduction, wetting agent such as a fat product, or a preservative such as p-hydroxy benzoic acid vinegar. Or a stabilizer such as "?' such as the addition of a preservative such as a p-hydroxyl injection into an ampoule or a metal tetraacetate in a vial, and the addition of one or more active substances or actives such as active substances and inertia A carrier such as lactose is prepared in a gelatin capsule. The capsule of the conjugate may be mixed by sorbitol, and a suitable suppository may be prepared, for example, by providing a natural fat or polyethylene glycol or The following examples are used to illustrate the invention, but the scope of the pharmaceutical formulation is not limited to the following:

Each of the money 100 mg 240 mg 340 mg 45 mg 15 mg 740 mg A) Lozenges Fulbencillin hydrochloride Lactose corn starch Polyethylene p Pilo bite net magnesium stearate fine grinding activity The substance, lactose and some corn starch are mixed together. The mixture was sieved and then wetted with an aqueous solution containing polyvinylpyrrolidone, kneaded, wet granulated and dried. The remaining corn starch and stearic acid towns are sieved and mixed together. The compressed mixture is made into the appropriate shape and size. The paper size is applicable to the Chinese National Standard (CNS) A4 specification (210 X 297 mm). 1307625 A7 B7 V. Invention Description (5) Key agent. B) Lozenges Each lozenge Fulbencillin hydrochloride 80 mg Corn starch 190 mg Lactose 55 mg Microcrystalline cellulose 35 mg Polyethylene p ratio 11 Each biting ketone 15 mg sodium-carboxymethyl starch 23 mg hard Magnesium citrate 2 mg 400 mg The finely divided active substance, part of corn starch, lactose, microcrystalline cellulose and polyvinylpyrrolidone are mixed together, and the mixture is sieved and blended with the remaining corn starch and water to form granules. It is then dried and sieved. Sodium-carboxymethyl starch and magnesium stearate are added and mixed, and the mixture is compressed to form a bond of an appropriate size. C) Coated ingots Each coated key Fulbencillin hydrochloride 5 mg Corn starch 41.5 mg Lactose 30 mg Polyethylene p ratio • Biting I 3 mg Magnesium stearate 0.5 mg 80 mg Active substance, corn The powder of the temple, the lactose and the polyethylene P are more than the ketones of the B. The paper size is applicable to the Chinese National Standard (CNS) A4 specification (210 x 297 mm) I307625

This combination is wetted with water. The damp material is pushed to the mesh of the mesh of millimeters and dried at 45 c and the granules are passed through the same screen. After the magnesium stearate was mixed therein, the tablet core having a diameter of 6 mm was compressed in a granulator. In a known manner, the tablet core is produced by substantially covering the sugar and talc. The final coated ingot is brightened with wax. 150 mg per capsule 268.5 mg 1.5 mg D) Capsules

Fulbencillin Hydrochloride Corn Starch Magnesium Stearate 420 mg Pack Mix the material with cornstarch and moisten with water. The wetted material is sieved and dried. The dried granules are sieved and mixed with magnesium stearate. The final mixture was placed in a hard gelatin capsule of Size 1. Order

E) Ampoule solution Fulbencillin hydrochloride 50 mg Sodium hydride 50 mg Water for injection at its own pH or optionally at pH 5.5 to 6.5 Dissolve the active substance in water and add vaporized sodium to form isotonic The resulting solution was filtered to remove coke concentrate and the filtrate was transferred to an ampoule under sterile conditions, followed by sterilization and thaw sealing. -9- This paper scale applies to Chinese National Standard (CMS) A4 Specification (210X297 public) 1307625 A7 B7 V. Invention Description (F) Suppository Fulbencillin Hydrochloride 50mg Solid Fat 1 650mg 1700mg Hard Fat melt. The milled active material was evenly dispersed therein at 40 °C. Cool to 38 ° C and pump into a slightly cooled suppository mold. -10- This paper scale applies to China National Standard (CNS) A4 specification (210X 297 mm)

Claims (1)

A8 B8 C8 1307625 A use of fenriberin in the form of a pharmaceutically acceptable salt form for the manufacture of a medicament for the treatment of a disorder of therapeutic need. 2. The use of the first application of the patent scope is characterized in that the sexual demand disorder is selected from the group consisting of diseases with low sexual demand, loss of sexual demand, lack of sexual demand, decreased sexual demand, inhibitory demand, loss of sexual desire, sexual desire disorder and Cold sensation. 3. The use of item 1 or 2 of the patent application is characterized in that the sexual demand disorder is selected from the group consisting of diseases with low inclusive demand, loss of demand, lack of sexual demand, decreased demand for sex, and inhibitory demand. 4. For the use of the first paragraph of the patent application, it is used to prepare medicines for the treatment of female sexual dysfunction. 5. The use of the first or second aspect of the patent application, characterized in that the Flebexillin is used in the form of a pharmaceutically acceptable acid addition salt selected from the group consisting of an acid formed. Diacid, hydrobromic acid, acetic acid, fumaric acid, maleic acid, terephthalic acid, lactic acid, phosphoric acid, hydrochloric acid, sulfuric acid, tartaric acid, citric acid and mixtures thereof" 6 as claimed in the first or second patent scope Its use is characterized by the use of fenribillin at a dose of 0.1 to 400 mg per ounce. -11 - This paper size applies to China's Home Ownership (CNS) A4 specification (210 X 297). _> Application for the 案 案 091119956 category (the above columns are filled by this Bureau) %. More 4 ' ·; C4 Patent Specification Chinese novelty of FLIBANSERIN English NEW USE OF FLIBANSERIN Name Nationality 1. FRANCO BORSINI FRANCO BORSINI 2. Kennedy Evans KENNETH ROBERT EVANS 1. Italy ITALY 2. Canada CANADA Residence, Residence 1. PANORAMAWEG 23, 88339 BAD WALDSEE, GERMANY, Bayside, Bahia, Germany. B. WALDSEE, GERMANY 2. 89 JOSEPH DUGGAN ROAD, TORONTO, ONTARIO M4L 3x5, CANADA III. Applicant's Name (Name) Nationality Smile J Residence (Company i Representative Name Deer Bailingjia Ingelheim Pharmaceutical Company BOEHRINGER INGELHEIM PHARMA GMBH & CO. KG Germany German Ingers D-55216 177 BINGER STRASSE 173, D-55216 INGELHEIM AM RHEIN, GERMANY 1. Hans Harmon 2. Detroit HEINZ HAMMANN DIETER LAUD 正 N Paper-scale operation applies two quasi (CNS) off grid (2i〇x29 Lake