BE1021240B1 - TRANEXAMIC ACID TABLETS - Google Patents

Abstract

TRANEXAMIC ACID TABLETS. The present invention relates to a tablet comprising tranexamic acid for the treatment or prevention of bleeding such as caused by fibrinolysis or fibrinogenolysis, drug-induced fibrinolysis, general fibrinolysis and local fibrinolysis. The tablet is designed to minimize swallowing difficulties associated with dysphagia and provide a means for an accurate dosage of tranexamic acid to a patient. The invention also relates to a method for producing the tranexamine tablets.

Description

Tranexamic acid tablets

TECHNICAL DOMAIN

The invention relates to the technical domain of tranexamic acid tablets and methods of making said tablets, to the optimization of the design of the tablet to minimize swallowing problems associated with dysphagia, and to provide a way for an accurate dosage of tranexamic acid to patients.

BACKGROUND

Tranexamic acid is a synthetic derivative of the amino acid lysine. It is often used in the treatment and prevention of excessive blood loss during operations and other medical conditions.

Currently, the drug is on the market as tablets comprising 500 mg or 650 mg tranexamic acid or as an intravenous preparation. In clinical studies on postoperative blood-saving effectiveness of oral versus intravenous tranexamic acid after full knee prosthesis surgery, oral tranexamic acid was presented as a superior blood-saving strategy compared to intravenous drug administration.

The average daily dose for a patient is between 1 gram and 4.5 grams of tranexamic acid. From a patient-friendly point of view, the fewer tablets the patient has to take, the better. Although side effects are rare, it is better to provide an accurate dose based on the needs and circumstances of the patient. Smaller doses are needed in children and patients with renal insufficiency. With the current 500 mg tablets, the patient almost always takes more medication than is actually necessary and must take several tablets to achieve an effective dose of tranexamic acid.

There is a need for a delivery system that can optimize the amount of tranexamic acid administered to the patient. The use of half a tablet is also accompanied by complications, problems with breaking the tablet occur. The tablet does not break exactly in half, which leads to an incorrectly administered dose. Storing the unused half of the tablet also causes problems. Half the tablet is not stored in an inert atmosphere and moisture from the air can reach the tablet, causing the tablet to start to disintegrate and in some cases, the active ingredient will start to degrade.

The more pills people have to take, the more mistakes people make when they are given. Every year in Europe alone, 194,500 people die from misuse of medicines. 20 to 30 percent of patients abuse drugs when treating a medical condition. In prevention, 30 to 40 percent of patients use their medicines in a wrong way, and in the treatment of chronic conditions almost 50 percent misuse their medicines.

Another problem with current tablets is that some people have problems swallowing them. 40 percent of patients complain about difficulty swallowing tablets and 8 percent admit to skip a dose of the prescribed medication. 4 percent stopped treatment because the tablets were difficult to swallow. Problems swallowing tablets is a recognized medical condition and is called dysphagia.

Large tablets have been shown to prolong the esophagus transit and sometimes get stuck to the wall of the esophagus for a period of time. This can cause the tablet to already start to disintegrate into the esophagus, resulting in pain, even localized esophagitis and worse, leading to serious complications such as ulcers, narrowing and perforation.

When patients think that tablets are difficult to swallow, some of them bend their heads back to facilitate swallowing. This position opens the windpipe, making it easier for the tablet to enter. When tablets are inhaled, they can cause respiratory problems, pneumonia and lung tissue death.

There remains a need in the art for a system for tranexamic acid that can be dosed correctly, patient-friendly and easy to swallow, which overcomes the aforementioned problems.

SUMMARY OF THE INVENTION

In a first aspect, the invention provides a tablet comprising tranexamic acid for the treatment or prevention of bleeding. Bleeding may be caused by fibrinolysis or fibrinogenolysis, drug-induced fibrinolysis, general fibrinolysis (in prostate cancer and pancreatic cancer) and local fibrinolysis such as occurs under the following conditions: prostatectomy and bladder surgery, menorrhagia, epistaxis, cervical cervix, trauma (trauma) hyphema, hereditary angioneurotic edema, dental extraction in haemophilia patients, hip or knee prosthesis surgery and heart surgery.

The tablet is designed to minimize swallowing problems associated with dysphagia. The tablet has a diameter of at most 10 mm and preferably this diameter is at most 8 mm. Tablets with a diameter of up to 10 mm are experienced as easy to swallow.

The tablet is shaped so that it has no flat surfaces, so that all surfaces are curved. In a preferred embodiment, the shape of the tablet is spherical or a caplet shape. Tablets with flat surfaces adhere more easily to the inner wall of the esophagus and this prolongs the esophagus transit causing the aforementioned problems.

In a preferred embodiment, the tablet is film-coated. This film coating further improves the ease of swallowing. It can happen that the tablet adheres to the inner wall of the esophagus. The film coating properties can be adjusted to influence the release properties of the active ingredient tranexamic acid. Preferably the tablet is an immediate release, a delayed release or an enteric release.

In a preferred embodiment, the tablet comprises approximately 250 mg, 500 mg, 750 mg or 1000 mg of tranexamic acid. Preferably the tablet comprises 750 mg of tranexamic acid. Having a series of tablets of different strengths allows a more accurate dose of tranexamic acid to the patient. It is not necessary to break the tablet to obtain a desired amount of tranexamic acid.

Preferably, tranexamic acid is present in the tablet in 50 to 90 weight percent of the total tablet weight, more preferably in 60 to 80 weight percent of the total tablet weight and most preferably in about 75 weight percent of the total tablet weight.

In a second aspect, the invention provides a method for manufacturing a tablet, comprising the following steps:

A1) mixing tranexamic acid, a first amount of binder and disintegrant; A2) adding matrix polymer previously dissolved in water; A3) granulating the resulting mixture thereby providing granulated compounds; A4) mixing the granulated compounds with a lubricant and a second amount of binder; A5) pressing the lubricated and granulated compounds into a tablet form; A6) optionally applying a film coating on the outer surface of the tablets.

In a preferred embodiment of the invention, binder is added in two different phases of the method of manufacturing a tablet. In a preferred embodiment, the total amount of binder used is divided into 50-75% in step A1 and 25-50% in step A4. In a more preferred preferred embodiment, 50 percent of the total amount of binder used is added in step A1 and the remaining 50 percent is added to the blend in step A4.

In a third aspect, the invention provides a tablet that can be obtained by an above-mentioned method. The tablets are preferably obtained by a method according to the invention. A two-step distribution of binder over the production steps provides a homogeneous distribution of the active ingredient over the tablet.

DETAILED DESCRIPTION OF THE INVENTION

Unless defined otherwise, all terms used in the invention, including technical and scientific terms, have the meaning as generally understood by one skilled in the art to which this invention belongs. For further guidance, term definitions are included to better value the teachings of the present invention.

As used herein, the following terms have the following meaning: "A", "de" and "it" as used herein refer to both the singular and plural unless the context clearly dictates otherwise. As an example, "a tablet" refers to one or more than one tablets. "Approximately" as used herein that refers to a measurable value, such as a parameter, an amount, a duration, and related, is intended to include variations of +/- 20% or less, preferably +/- 10% or less , more preferably +/- 5% or less, even more preferably +/- 1% or less, and even more preferably +/- 0.1% or less of the declared value, insofar as such variations are suitable for in the described invention. However, it is to be understood that the value to which the "approximately" determination refers refers to itself specifically. "Include", "comprising" and "comprising" and "includes" as used herein are synonymous with "contents", "including", "includes" or "contain", "contain", "contain" and are inclusive or open terms that specify the presence of what follows, for example, component, and do not exclude or prevent the presence of other non-cited components, properties, elements, members, steps, known in the art or described therein.

Quoting numeric ranges by end points includes all numbers and fractions included within that range, as well as the cited end points.

The term "weight%" or "weight%" (weight percent), throughout and throughout the description, unless otherwise defined, refers to the relative weight of the component in question based on the total weight of the formulation.

The term "capsule / caplet shape" refers to an elongated oval shape or a beam shape with rounded edges so that the overall shape has no flat surfaces.

In a first aspect, the invention provides a tablet comprising tranexamic acid for the treatment or prevention of bleeding. Bleeding or bleeding escaping from the circulatory system can be caused by fibrinolysis or fibrinogenolysis, drug-induced fibrinolysis, general fibrinolysis such as in prostate cancer and pancreatic cancer, and local fibrinolysis such as occurs in the following conditions: prostatectomy and bladder surgery, menorrhagia, conparisation of epistaxis cervix, traumatic hyphema, hereditary angioneurotic edema, dental extraction in haemophilia patients, hip or knee prosthesis surgery and heart surgery.

A tablet according to an embodiment of the invention is designed to minimize swallowing problems associated with dysphagia. The tablet has a diameter of at most 10 mm and preferably this diameter is at most 8 mm. Studies have shown that tablets with a diameter of up to 10 mm and preferably at most 8 mm are experienced as easy to swallow.

The shape of the tablet has no flat surfaces, which means that all surfaces are curved. Examples of tablet forms without flat surfaces are capsule, caplet forms and spheres. In a preferred embodiment, the shape of the tablet is spherical or a caplet shape. Tablets without flat surfaces attach less easily to the inner wall of the esophagus. This reduces the time of the esophagus transit and alleviates the above problems.

In a preferred embodiment, the outer surface of the tablet is film-coated. The film coating further enhances easy swallowing and prevents the tablet from adhering to the inner wall of the esophagus.

The film coating properties can be adjusted to further influence the release properties of the active ingredient. In a preferred embodiment, the tablet is an immediate release, a delayed release, or an energetic release.

The shape of the tablet, the diameter of the tablet and the film coating of the tablet are selected in such a way that dysphagia is kept to a minimum. This also makes it possible to predict the time required for the tablet to reach the stomach. The combination of film coating, shape and composition of the tablet is preferably in such a way that the tablet disintegrates when it reaches the stomach and releases the active ingredient in a rapid manner.

In a preferred embodiment, the tablet comprises approximately 250 mg, 500 mg, 750 mg or 1000 mg of tranexamic acid. Having a series of tablets of different strengths allows a more accurate dose of tranexamic acid to the patient.

Preferably, tablets comprise 750 mg of tranexamic acid. Since a posology often requires the administration of 1.5 g of tranexamic acid, two 750 mg tablets can be used. To date, patients had to use three 500 mg tablets or one and a half tablets of 1000 mg. The number of tablets can be reduced in this way. Therapy compliance can therefore be improved. Avoiding breaking the tablets is advantageous to obtain an accurate dosage of the active ingredient. It can also prevent premature release of the active ingredient.

Preferably, tranexamic acid is present in the tablet in 50 to 90 weight percent of the total tablet weight, more preferably in 60 to 80 weight percent of the total tablet weight and most preferably about 75 weight percent. In a preferred embodiment, tablets comprise 750 mg of tranexamic acid and this amount is in total at least 50 percent, preferably at least 60, 70, 80 or 90 percent by weight of the total tablet weight.

The tablet composition comprises a binder. Preferably, the binder is selected from the list of dextrates, dextrin, dextrose, fructose, iactitol, lactose, maltitol, maitose, mannitol, sorbitol, sucrose, erythritol, and xylitol acacia, alginic acid, 2-propionic acid homopolymer known under the trade name CARBOMER , microcrystalline cellulose, carboxymethyl cellulose, cellulose, dextrin, ethyl cellulose, gelatin, polydextrose, polyethylene oxide, sodium alginate and combinations thereof.

The binder guarantees the mechanical stability of the tablet and holds all the different components together.

Preferably the binder is present in an amount of 1 to 40 percent, more preferably 10 to 25 percent, even more preferably 15 to 20 percent, and most preferably about 17 percent by weight of the total tablet weight.

The tablet further comprises a disintegrant. Preferably the disintegrant is selected from the list of a polyvinylpyrrolidone, a carboxymethylcellulose, a starch, a starch glycolate or combinations thereof. In a preferred embodiment, the disintegrant comprises a cross-linked polyvinylpyrrolidone, a sodium carboxymethyl cellulose, a cross-linked sodium carboxymethyl cellulose, a modified starch, a sodium starch glycolate or combinations thereof. Preferably the binder is a cellulose, most preferably microcrystalline cellulose. A cellulose suitable for use in the present invention is commercially available under the brand name Avicel. In another embodiment, the binder is preferably polyvinylpyrrolidone.

The disintegrant swells and dissolves when the tablet gets wet, breaking up the tablet in the digestive tract and releasing the active ingredient.

Preferably, the disintegrant is present in an amount of 0.1 to 10 weight percent of the total tablet weight, more preferably in an amount of 1 to 5 weight percent of the total tablet weight and most preferably in an amount of about 2 weight percent of the total tablet weight.

The tablet further comprises a lubricant. Preferably the lubricant is selected from the list of sodium stearate, stearic acid, polyethylene glycol, talc, polyoxypropylene-polyoxyethylene block polymers, magnesium stearate, sodium stearyl fumarate, colloidal silica, anhydrous silica or a combination of these components. Preferably the lubricant is selected from the list of magnesium stearate, talc and / or silica.

The presence of a lubricant simplifies ejecting the tablet from the mold after the tablet is pressed. It also prevents the powdery mixture from sticking to parts of the press. It improves product flows by reducing friction between particles. It can further reduce dysphagia.

Preferably the lubricant is present in an amount of 1 to 20% by weight of the total tablet weight, more preferably in an amount of 5 to 15% by weight of the total tablet weight, even more preferably in an amount of 3 to 10% by weight of the total tablet weight tablet weight and most preferably in an amount of about 5 weight percent of the total tablet weight.

The tablet composition further comprises a matrix polymer. Preferably the matrix polymer is selected from the list of dextran, hydroxyethyl cellulose or polyethylene oxide, and combinations thereof.

The matrix polymer acts as a matrix-forming agent. Preferably, the matrix polymer is present in 1 to 20 weight percent of the total tablet weight, more preferably in 2 to 10 weight percent of the total tablet weight, even more preferably 2.5 to 5 weight percent, and most preferably about 3 weight percent of the total tablet weight tablet weight.

In a preferred embodiment, a tablet according to an embodiment of the invention for use in the treatment or prevention of bleeding comprises: - 60-80 wt% tranexamic acid; - 10-25% binder; 1-5% by weight a disintegrant; 1-20 wt% lubricant; and, 1-20 wt% matrix polymer, the weight being expressed as a percentage of the total weight of the tablet; characterized in that the tablet has a maximum diameter of 10 mm and all surfaces are curved.

In a more preferred embodiment, a tablet according to an embodiment of the invention for use in the treatment or prevention of bleeding comprises: 70-75 wt% tranexamic acid; 15-20% binder; about 2% by weight of disintegrant; about 5 wt% lubricant; and - about 3% by weight matrix polymer, the weight being expressed as a percentage of the total weight of the tablet; characterized in that the tablet has a maximum diameter of 10 mm and all surfaces are curved.

In a most preferred embodiment, a tablet according to an embodiment of the invention for use in the treatment or prevention of bleeding comprises: 50-90 wt% tranexamic acid; 1-40% binder; 1-5% by weight of disintegrant; 5-15% lubricant; and, 2-10% by weight matrix polymer, the weight being expressed as a percentage of the total weight of the tablet; characterized in that the tablet has a maximum diameter of 10 mm and all surfaces are curved.

In a preferred embodiment, the amount of tranexamic acid, binder, disintegrant, lubricant, and matrix polymer is 100% by weight of the total tablet weight.

In a second aspect, the invention provides a method for manufacturing a tablet with a composition and shape described above, comprising the following steps:

A1) mixing tranexamic acid, a first amount of binder and disintegrant; A2) adding matrix polymer previously dissolved in water; A3) granulating the mixture to provide granulated compounds; A4) mixing the granulated compounds with a lubricant and a second amount of binder; A5) pressing / pressing the lubricated and granulated compounds into a tablet form; A6) optionally applying a film coating on the outer surface of the tablets.

A wet granulation method according to an embodiment of the invention offers the advantage that the active ingredient tranexamic acid is homogeneously distributed over the tablet mass.

In a preferred embodiment, the invention provides a method for manufacturing a tablet according to an embodiment of the invention, comprising the following steps: B1) mixing tranexamic acid, a first amount of binder and disintegrant in a granulating vessel; B2) adding matrix polymer previously dissolved in water; B3) passing the mixture through a granulator; B4) mixing the granulated compounds with a lubricant and a second amount of binder; B5) pressing / pressing providing the tablet; B6) optionally applying a film coating on the outer surface of the tablet.

In a preferred embodiment, the total amount of binder is divided between step A1 and step A4. Preferably 50% or 55%, more preferably 60% or 65%, and most preferably 70 or 75% of the total amount used in the composition is used in step A1; the remainder is used in step A4.

In a preferred embodiment of the invention, step A1 and / or B1 uses only 50 percent of the total amount of binder. The remaining 50 percent of the total amount of binder used in the formulation is added to the blend in step A4 and / or B4.

In a preferred embodiment, the various components pass through a 1 mm screen before mixing the components in steps A1, A4, B1 and B4.

In a preferred embodiment, the granulated compound obtained through steps A3 and B3 passes through a 1.5 mm screen before step A4 is started.

In a preferred embodiment, the binder has a grain size of at least 100 µm or 110 µm, preferably 120 µm or 130 µm, more preferably 140 µm or 150 µm, even more preferably 160 µm or 170 µm and most preferably of about 180 pm.

In a third aspect, the invention provides a tablet obtainable or obtained by the above method. Tablets obtained by a method according to an embodiment of the invention, wherein binder is distributed over two steps in the preparation, exhibit a homogeneous distribution of the active ingredient over the matrix of the tablet. This is advantageous to provide an accurate tranexamic acid dosage.

The present invention will now be described in more detail with reference to non-limiting examples.

EXAMPLES

Example 1: Tablet compositions according to embodiments of the invention 1. Pass the tranexamic acid and the various components through a 1 mm sieve. 2. Mix tranexamic acid, binder (50% or 100% of the total number used) and disintegrant. 2. Add an amount of matrix polymer that was previously dissolved in water to make a wet mass. 3. Pass the wet mass through a granulator, dry, and then pass it through a 1.5 mm sieve. 4. Mix the granulated compounds with lubricant and the rest of the binder; i.e., 50%, when 50% binder is used to granulate.

Table 1: tablet composition

Various parameters to define compressibility and flow properties, including apparent density, shaking weight, Carr Index and Haussner Index, have been determined. The criteria used to classify the Haussner Index values are provided in Table 2. A summary can be found in Table 3.

Based on the results provided in Table 3, it follows that the distribution of the binder over two steps improves the classification from suitable to acceptable / good. It can also be concluded that a binder with a particle size of 180 µm is preferable to 50 µm. Granules 3 and 4 are preferred.

Table 2: dassification criteria

Table 3: preparation properties

Example 2: Tablet preparations according to embodiments of the invention

Various sizes and shapes were tested during the development process. Preferred tablet shapes and sizes are provided in Table 4. These tablets are made using a composition as shown in Example 1.

Table 4: shape and dimensions of tablets

Example 3: Alternative tablet compositions according to the invention

A few more tablets were prepared according to the procedure description in Example 1. The compositions are shown in Table 5. Prepared tablet strengths were resp. 250, 500, 750 and 1000 mg of tranexamic acid.

Table 5: Tablet compositions

Example 4: Medical use of tablets according to the invention

Tablets made according to a process of the invention are administered orally. The posology is determined individually and depends on age, condition to be treated, body weight, other medication taken by the patient, general health of the patient, whether the patient has kidney problems and other disorders.

The general dosing principle is as follows: For adults, the recommended standard dosage is 0.75 to 1.5 grams of tranexamic acid in tablet form, 2 to 3 times a day. For children, the dose is calculated according to body weight at 15-25 mg / kg per dose.

For adults this corresponds to 1 or 2 tablets containing 750 mg of tranexamic acid, 2 or 3 times a day.

Example 5: Medical use of tablets according to the invention

For the treatment of local fibrinolysis caused by prostatectomy, tablets prepared according to a process of the invention are administered orally. The posology is individual and depends on age, condition to be treated, body weight, other medication taken by the patient, general health of the patient, whether the patient has kidney problems and other disorders.

The dosing principle is as follows: After initial pre- or post-operative tranexamic acid injection, 0.75-1.5 g Tranexamic acid tablet orally 2 to 3 times a day until third postoperative day or until macroscopic hematuria is no longer present. This corresponds to 1 or 2 tablets containing 750 mg of tranexamic acid or 1 tablet containing 1000 mg of tranexamic acid 2 or 3 times a day.

Example 6: Medical use of tablets according to the invention

For the treatment of local fibrinolysis caused by menorrhagia: tablets prepared according to a process of the invention are administered orally. The posology is individual and depends on age, condition to be treated, body weight, other medication taken by the patient, general health of the patient, whether the patient has kidney problems and other disorders.

The dosing principle is as follows: 0.75-1.5 g of tranexamic acid in tablet form 3 to 4 times a day for as long as necessary up to 4 days. The dosage can be increased with very heavy menstrual bleeding. Treatment with Tranexamic acid should not be started until menstrual bleeding has begun. This corresponds to 1 or 2 tablets containing 750 mg of tranexamic acid or 1 tablet containing 1000 mg of tranexamic acid 3 or 4 times a day.

Example 7: Medical use of tablets according to the invention

For the treatment of local fibrinolysis caused by epistaxis: tablets prepared according to a process of the invention are administered orally. The posology is individual and depends on age, condition to be treated, body weight, other medication taken by the patient, general health of the patient, whether the patient has kidney problems and other disorders.

The dosing principle is as follows: 0.75-1.5 g of tranexamic acid in tablet form three times a day for 4-10 days. This corresponds to 1 or 2 tablets containing 750 mg of tranexamic acid or 1 tablet of 1000 mg of tranexamic acid 3 times a day.

Example 8: Further medical use of tablets according to the invention

For the treatment of local fibrinolysis caused by cervix conization: tablets prepared according to a process of the invention are administered orally. The posology is individual and depends on age, condition to be treated, body weight, other medication taken by the patient, general health of the patient, whether the patient has kidney problems and other disorders.

The dosing principle is as follows: Postoperatively 0.75-1.5 g tranexamic acid three times a day for 12 to 14 days. This corresponds to 1 or 2 tablets containing 750 mg tranexamic acid or 1 tablet of 1000 mg tranexamic acid 3 times a day for 12 to 14 days.

Example 9: Further medical use of tablets according to the invention

For the treatment of local fibrinolysis caused by traumatic hyphema: tablets prepared according to a process of the invention are administered orally and the posology is individual and depends on age, condition to be treated, body weight, other medication the patient takes, general health of the patient, whether the patient has kidney problems and other disorders.

The dosing principle is as follows: 0.75-1 g tranexamic acid three times a day for 6 days. This corresponds to 1 tablet containing 750 mg of tranexamic acid or 1 tablet containing 1000 mg of tranexamic acid 3 times a day.

Example 10: Further medical use of tablets according to the invention

For the treatment of local fibrinolysis caused by hereditary angioneurotic edema: tablets prepared according to a process of the invention are administered orally and the posology is individual and depends on age, condition to be treated, body weight, other medication the patient takes, general patient's health, or the patient has kidney problems and other conditions.

The dosing principle is as follows: when an attack occurs, 0.75-1.5 g of tranexamic acid is administered three times a day for a few days. Prophylactic dosage is 0.75-1.5 g Tranexamic acid three times daily adjusted to the lowest effective dose. This corresponds to 1 or 2 tablets containing 750 mg of tranexamic acid or 1 tablet of 1000 mg of tranexamic acid 3 times a day.

Example 11: Further medical use of tablets according to the invention

For the treatment of local fibrinolysis caused by hemophilia: tablets prepared according to a process of the invention are administered orally and the posology is individual and depends on age, condition to be treated, body weight, other medication the patient takes, general health of the patient, or the patient has kidney problems and other conditions.

The dosing principle is as follows: when managing dental extractions, 0.75-1.5 g of tranexamic acid every eight hours. The dose is based on 25 mg / kg. This corresponds to 1 or 2 tablets containing 750 mg of tranexamic acid or 1 tablet containing 1000 mg of tranexamic acid every 8 hours.

Tablets made according to a process of the invention provide a way for accurate dosing of tranexamic acid to a patient. The invention also relates to a method for producing the aforementioned tranexamic acid tablets.

It is to be understood that the present invention is not limited to any form of realization described above and that certain modifications may be added to the examples shown without revaluing the appended claims.

Claims (15)

CONCLUSIONS A tablet for use in the treatment or prevention of bleeding, comprising: - tranexamic acid; a binder; - a disintegrant; a lubricant; and a matrix polymer, characterized in that the tablet has a diameter of at most 10 mm and all surfaces are curved. Tablet according to claim 1, characterized in that the tablet comprises 750 mg of tranexamic acid. Tablet according to claim 1, characterized in that the tablet comprises 1000 mg of tranexamic acid. Tablet according to any one of claims 1-3, characterized in that the binder is present in an amount of 1 to 40% by weight of the total tablet weight. Tablet according to any one of claims 1-4, characterized in that the disintegrant is present in an amount of 0.1 to 10% by weight of the total tablet weight. Tablet according to any one of claims 1-5, characterized in that the lubricant is present in an amount of 1 to 20% by weight of the total tablet weight. A tablet according to any one of claims 1-6, characterized in that the matrix polymer is present in an amount of 1 to 20% by weight of the total tablet weight. Tablet according to any one of claims 1-7, characterized in that the tablet has a diameter of at most 8 mm. A tablet according to any one of claims 1-8, characterized in that the tablet has a caplet shape. The tablet of any one of claims 1-9, characterized in that the tablet has an outer film envelope. A tablet according to any one of claims 1-10, characterized in that in the treatment or prevention of bleeding, the bleeding is caused by fibrinolysis or fibrinogenolysis, drug-induced fibrinolysis, general fibrinolysis and local fibrinolysis as occurring in the following disorders : prostatectomy and bladder surgery, menorrhagia, epistaxis, cervical congestion, traumatic hyphema, hereditary angioneurotic edema, tooth extraction in haemophilia patients, hip or knee prosthesis surgery and heart surgery. A method for producing a tablet according to any of claims 1-11, comprising the steps of: A1) mixing tranexamic acid, a first amount of binder and disintegrant; A2) adding matrix polymer previously dissolved in water; A3) granulating the resulting mixture thereby providing granulated compounds; A4) mixing the granulated compounds with a lubricant and a second amount of binder; A5) pressing the lubricated and granulated compounds into a tablet form; A6) optionally applying a film coating on the outer surface of the tablets. A method according to claim 12, characterized in that the total amount of binder used is divided into 50-75% in step A1 and 25-50% in step A4. A method according to claim 13, characterized in that 50% of the total amount of binder is used in step A1, and the remaining 50 percent of the total amount of binder is added in step A4. A tablet according to any of claims 1 to 11 obtainable by a method according to any of claims 12 to 14.