KR20080108227A - Quickly disintegrating tablet produced by direct dry-tabletting - Google Patents

Abstract

It is intended to provide a quickly disintegrating tablet, which has a practically appropriate tablet hardness while sustaining the disintegrability, and a process for producing the same by the direct dry-tabletting method wherein a material mixture powder before tabletting has a high flowability owing to well designed combination of an active ingredient with auxiliary ingredient(s) and, therefore, can be smoothly flown out from the hopper of a tabletting machine, no capping occurs during tabletting and the obtained tablets show little deviation in weight. Namely, a quickly disintegrating tablet produced by the direct dry-tabletting method characterized by containing (a) an active ingredient and (b)as a dissolution aid, at least one member selected from the group consisting of acid selected from among citric acid, tartaric acid, malic acid, lactic acid and ascorbic acid or alkali metal salts thereof; alkali metal hydrogencarbonates; and alkali metal carbonates, together with (c) a filler, (d) a binder, (e) a disintegrating agent, (f) a fluidizer, and (g) as a lubricant, a lubricant comprising a combination of magnesium stearate with a sucrose fatty acid ester. ® KIPO & WIPO 2009

Description

QUICKLY DISINTEGRATING TABLET PRODUCED BY DIRECT DRY-TABLETTING}

The present invention relates to a dry direct-type fast disintegrating tablet having a hardness of practical tablets while maintaining fast disintegration by devising a combination of an active ingredient and a blending component, and a method for producing the same.

In recent years, the demand for the development of fast disintegrating tablets in the oral cavity has been increased for reasons such as ease of administration in medical solid preparations. Tablets as fast disintegrating tablets in the oral cavity include (1) disintegration within 30 seconds by the disintegration test method of the Japanese pharmacy room, (2) disintegration within 60 seconds in the oral cavity, and (3) wear and tear test at 200 rotations The hardness and the like of which no noticeable damage is confirmed is required.

As a method for producing fast disintegrating tablets in the oral cavity, a wet granulation method and a dry granulation method have been conventionally proposed. As a wet granulation method, for example, (1) with respect to a tablet component containing a saccharide as an active ingredient and an excipient, the surface of the particles of the saccharide is moistened using 0.3 to 7% by weight of water, Method for producing an orally disintegrating tablet having a disintegration time of 0.05 to 3.0 minutes by the disintegration test method described in Article 12 of the Japanese Pharmacy Room by tableting and drying the mixture containing the same (Patent Document 1) It is.

In addition, as a dry granulation method, for example, (2) a tablet which is administered orally without dispersing in water before administration, and is a mixed material of a mixture containing an active substance in the form of fine crystals or fine particles coated to mask the taste and an excipient. Rapidly disintegrating multiparticulate tablets obtained by direct compression of P has been proposed (Patent Document 2). In this case, the mixture containing the excipient includes at least one disintegrant and at least one swelling agent or at least one solubilizer selected from starch, processed starch or microcrystalline cellulose and which does not generate high viscosity in contact with water. Tablets are fast disintegrating multiparticulate tablets that do not contain blowing agents and free organic acids and disintegrate in less than 60 seconds without chewing in the presence of saliva in the oral cavity.

Furthermore, as a composition by a dry granulation method, it is (3) meloxycam as an active ingredient; Oligosaccharides and / or polysaccharides; One or more of pharmaceutically acceptable additives selected from the group consisting of surfactants, hydrotropes, alkalizers, hydrocolloids and polymers; And a pharmaceutical composition (patent document 3) consisting of any excipient, carrier and / or preparation has been proposed.

In addition, as the same dry tableting method, for example, (4) it rapidly disintegrates in the oral cavity containing at least one of mannitol, disintegrant, cellulose, lubricant, starch and lactose, and has sufficient strength practically. Orally disintegrating compositions (Patent Document 4) or (5) melancholy or pharmaceutically acceptable salts thereof, starch or multiple starches, flow promoters and at least one additional excipient As a rapidly disintegrating tablet, at least one of the additional excipients is a water-soluble direct dry press method (direct blow method), for example, a blend of meloxycam, lactose, starch and silicon dioxide hydrate, and the components are mixed in a conventional mixer for 30 minutes. It is prepared by mixing by, followed by adding magnesium stearate and blending the composition again for 5 minutes (Patent Document 5).

Patent Document 1: Japanese Patent No. 3069458

Patent Document 2: Japanese Patent No. 2820319

Patent Document 3: Japanese Patent Publication No. 2001-513563

Patent Document 4: Japanese Patent Application Laid-Open No. 2000-273039

Patent Document 5: Japanese Patent Publication No. 2004-525975

However, these conventional methods, for example, in the wet granulation method of (1), use 0.3 to 7% by weight of water with respect to the tablet component containing the active ingredient and the sugar to wet and dry the surface of the particles of the sugar. Troublesome handling is required. In the dry granulation method of (2), when the active ingredient (active ingredient) is coated and is in a fine crystal state, the fine granules are coated, and when the active ingredient is in a fine granule state without an active ingredient, the active ingredient is coated. For example, fine granules may be formed by extrusion granulation, processing in a fan, air fluidized bed, or the like, and in the above (3), meloxycam and oligosaccharides and / or polysaccharides (eg, For example, it is an effervescent tablet using the composition which copolymerized cyclodextrin, microcrystalline cellulose, lactose, and starch), and its manufacturing method, and complicated operation was required.

The dry tableting method is a method of forming a tablet by mixing the drug and other excipients, etc., and then directly tableting the mixture (direct tableting method), and is a simple method of preparing a tablet in two processes of mixing and tableting. However, due to the combination of drug types, mixed components, etc., the fluidity of the mixture is lowered, for example, so that the powder mixture does not flow out of the hopper of the tableting machine, which makes tableting impossible or lowers the yield by capping, A significant increase in the weight deviation was observed, or there was a problem that the hardness of the tablets could not be maintained if the tablets were disintegrated.

In fact, the present inventors found that in the case of tablets by the dry method of the drug used in the dry method, for example, meloxycam, the smaller the particle diameter of Meloxycham, the faster the elution rate of Meloxycham from the resulting tablet, but It is experienced that tableting obstacles, such as sticking, occur easily.

The present invention improves the fluidity of the mixed powder before tableting by devising a combination of the active ingredient and the compounding ingredient, so that the outflow property from the hopper of the tableting machine is good, while suppressing the occurrence of capping, and consequently, the weight variation of the tablet. It is an object of the present invention to provide a fast disintegrating tablet having a small, practical tablet hardness while maintaining the disintegration property of the tablet, and a production method by the dry direct method.

MEANS TO SOLVE THE PROBLEM As a result of earnestly examining in order to solve the said subject, the present inventors can solve these problems by devising the combination of an active ingredient and a compounding ingredient, especially selecting a specific thing as a dissolution aid, and selecting a specific lubricant. It discovered what was new and came to complete this invention.

In particular, the present invention can provide an effective fast disintegrating tablet containing meloxycam by selecting Meloxycam, which is a nonsteroidal anti-inflammatory and analgesic agent, as an active ingredient.

That is, the present invention provides, as its basic form, (a) an active ingredient, (b) an acid selected from citric acid, tartaric acid, malic acid, lactic acid and ascorbic acid or its alkali metal salt as a dissolution aid; Alkali metal hydrogencarbonates; And at least one member selected from the group consisting of alkali metal carbonates, and (c) excipients, (d) binders, (e) disintegrants, (f) glidants and (g) glidants as magnesium stearate and sucrose fatty acids. It is a dry type | mold quick disintegrating tablet which further contains the lubricant which consists of a combination of ester.

More specifically, in the present invention, the alkali metal salts of acids are sodium citrate, potassium citrate, sodium stannate, potassium stannate, sodium malate, potassium malate, sodium lactate, potassium lactate, sodium ascorbate or potassium ascorbate, alkali metal carbonate It is a dry, instantaneous fast disintegrating tablet wherein the anti-inflammatory is sodium bicarbonate or potassium bicarbonate and the alkali metal carbonate is sodium carbonate or potassium carbonate.

More specifically, in the present invention, the dissolution aid of (b) comprises a combination of both sodium citrate and sodium bicarbonate, and the excipient of (c) is lactose, erythritol, D-mannitol, xylitol, and multitol. It is a dry type direct instant disintegrating tablet which is at least one selected from the group consisting of sugars, synthetic aluminum silicate, sodium hydroxypropyl starch, crystalline cellulose, hydroxypropyl starch, anhydrous calcium hydrogen phosphate and reduced maltose syrup.

In the present invention, the binder (d) is at least one member selected from the group consisting of crystalline cellulose, powdered cellulose, low-substituted hydroxypropyl cellulose, and carmellose, and the disintegrating agent of (e) is crospovidone and carmel It is at least 1 sort (s) chosen from the group which consists of roth, carmellose calcium, and carboxymethyl starch sodium, and the said fluidizing agent of (f) is a dry type | mold quick disintegrating tablet whose hard silicic acid (silicon dioxide) is hard.

Most specifically, the present invention is a dry-type instant disintegrating tablet in which the active ingredient (a) is meloxycam, specifically, the following components;

The active ingredient of (a) is meloxycamp,

Dissolution aids of (b) include sodium citrate and sodium bicarbonate,

excipients of (c) include lactose and erythritol,

The binder of (d) is crystalline cellulose,

Disintegrants of (e) are crospovidone,

The fluidizing agent of (f) includes light silicic anhydride (silicon dioxide),

The glidant of (g) is a dry, direct-acting tablet that consists of magnesium stearate and a sucrose fatty acid ester.

In another aspect, the present invention provides (a) meloxycam, (b) sodium citrate and sodium bicarbonate, (c) excipient, (d) binder, (e) disintegrant and (f) glidant as dissolution aids. It is a manufacturing method of the dry spontaneous fast disintegrating tablet characterized by mixing, (g) further adding and mixing magnesium stearate and sucrose fatty acid ester as a lubricant, and then tableting the obtained mixture directly.

That is, the present invention is an acid or a alkali metal salt thereof selected from citric acid, tartaric acid, malic acid, lactic acid and ascorbic acid as a dissolution aid to be added in addition to the active ingredient / excipient; Alkali metal hydrogencarbonates; And a lubricant containing at least one selected from the group consisting of alkali metal carbonates, and a lubricant comprising a combination of both magnesium stearate and sucrose fatty acid ester as lubricants. It is to provide a dry direct-type fast disintegrating tablet having the desired fast disintegration and moderate hardness.

(Effects of the Invention)

According to the present invention, the flowability of the mixed powder containing the active ingredient before tableting is good, and therefore, the flowability of the mixed powder from the hopper of the tableting machine is good, the occurrence of capping is suppressed, and consequently, the tablet has little variation in weight. There is provided a disintegratable tablet and a production method by the dry direct method.

The fast disintegrating tablets obtained by the present invention have the desired disintegration rate, have the practical hardness of tablets, and the manufacturing method has the advantage of being inexpensive and simple manufacturing method.

There is no restriction | limiting in particular as a drug active ingredient used for the dry instant disintegrating tablet of this invention, For example, a nonsteroidal antipyretic analgesic anti-inflammatory agent, a vitamin agent, an antihistamine, an antitussive agent, a fungicide, an antacid, a herbal medicine, a gastric mucosa repair agent, an analgesic Antispasmodics, constipation treatments, H2 receptor antagonists, ulcers, antagonists, antibiotics, arrhythmia treatments, gastrointestinal drugs, expectorants, antispasmodic drugs, and central nervous system stimulants.

Especially, it can apply preferably to a nonsteroidal antipyretic analgesic anti-inflammatory agent.

Below, the dry type | mold quick disintegrating tablet of this invention is demonstrated, for example as Meloxycam as a representative example.

Meloxycam is a pale yellow powder, very difficult to dissolve in methanol and ethanol and hardly soluble in water. In addition, it is a non-steroidal anti-inflammatory and analgesic with no bitter taste, and it is orally administered once a day as a tablet containing 10 mg as a disease for rheumatoid arthritis, deformed arthrosis, back pain, periarthritis of the shoulder, and shoulder pain syndrome and anti-inflammatory and analgesic. It is becoming.

The smaller the particle diameter of the medicinal agent of Meloxycum used for the dry spontaneous fast disintegrating tablet of the present invention is preferable, and in consideration of improving the solubility in the case of tableting, an appropriate particle size can be used. Preferably, the average particle diameter is 20 μm or less.

As a dissolution aid used with the said active ingredient, an acid or its alkali metal salt, alkali metal hydrogencarbonate, or alkali metal carbonate is mentioned. Such acids are selected from the group consisting of citric acid, tartaric acid, malic acid, lactic acid and ascorbic acid in the present invention. Thus, the alkali metal salts of the acids are sodium citrate, potassium citrate, sodium stannate, potassium stannate, sodium malate, Potassium malate, sodium lactate, potassium lactate, sodium ascorbate, potassium ascorbate, and the like.

Examples of the alkali metal hydrogen carbonate as the dissolution aid include sodium bicarbonate or potassium bicarbonate, and the alkali metal carbonate includes sodium carbonate or potassium carbonate.

These dissolution aids can be used in combination of one or more. Particular preference is given to a combination of both sodium citrate and sodium hydrogen carbonate.

Although the compounding quantity of the dissolution adjuvant in this invention changes with the active ingredient to be used, the kind of dissolution adjuvant, etc., it cannot be specifically limited, For example, it uses a hydroxycam as an active ingredient, and citric acid as a dissolution adjuvant for this In the case where both sodium and sodium bicarbonate are combined in combination, the amount of the dissolving aid expressed in weight% is preferably about 0.5 to 6% by weight based on the total amount of sodium citrate and sodium bicarbonate per tablet.

In the case of combining both sodium citrate and sodium bicarbonate, the most preferable compounding ratio of sodium citrate and sodium bicarbonate is 0.3-1.9 mol of sodium bicarbonate, preferably 0.57-1.78 mol to 1 mol of sodium citrate. More preferably, it is about 0.7-1.6 mol.

The blending amount of the tablets of sodium citrate and sodium hydrogen carbonate blended by the combination by the molar ratio is preferably combined so that the pH of the solution is between 4 and 8.5 when one tablet is dissolved in 900 mL of distilled water. The range of pH more preferable is mix | blended so that it may become pH range of 5.0-8.0, Especially preferably, pH6.5-7.5.

In addition, when using melocampal as an active ingredient, it turned out that it is good to mix this pH so that it may become slightly alkaline side.

Even when a dissolution aid other than sodium citrate and sodium hydrogen carbonate is employed as the dissolution aid, the preferred compounding amount of each component as the dissolution aid is the same as above, and when one tablet is dissolved in 900 mL of distilled water, the pH of the solution is 4 to 8.5, Preferably it is 5.0-8.0, Especially preferably, it is mix | blended so that it may become pH6.5-7.5.

In the fast disintegrating tablet provided by the present invention, excipients include sugars such as lactose, erythritol, D-mannitol, xylitol, and multitol, synthetic aluminum silicate, hydroxypropyl starch sodium, crystalline cellulose, and hydroxypropyl starch. And anhydrous calcium hydrogen phosphate, reduced maltose syrup, and the like. Especially, it is preferable to use erythritol which can be used as a lactose and a mating agent.

The compounding amount per tablet of the excipient to be blended is 20 to 70% by weight, preferably 30 to 70% by weight, more preferably about 60% by weight.

In the fast disintegrating tablet provided by the present invention, examples of the binder include crystalline cellulose, powdered cellulose, low-substituted hydroxypropyl cellulose, carmelose and the like. Preferably, it is a crystalline cellulose, for example, Seolas PH101 and Seolas PH302 (made by Asahi Kasei Chemicals Co., Ltd.).

The blending amount per binder of the binder to be used is 5 to 20% by weight, preferably about 10% by weight.

In the fast disintegrating tablet provided by the present invention, at least one selected from the group consisting of crospovidone, carmellose, carmellose calcium, and carboxymethyl starch sodium may be mentioned as the disintegrant. Preferably crospovidone.

The compounding amount of the disintegrating agent per tablet is 5 to 20% by weight, preferably about 15% by weight.

Hard silicic acid anhydrous (silicon dioxide) is mentioned as a fluidizing agent. Preferably, Adosorida 101 [brand name, Furo Into Sangyo Co., Ltd. product] is mentioned.

The compounding amount per tablet of the fluidizing agent is 0.5 to 3% by weight, preferably about 0.5 to 1.5% by weight.

The fast disintegrating tablet provided by the present invention is characterized by using a combination of both magnesium stearate and sucrose fatty acid ester as a lubricant. As sucrose fatty acid ester, For example, Sugar ester B-370F or Safhof J-2203F [The fine grinding | pulverization of B-370 using sucrose behenic acid ester as a lubricant; Mitsubishi Kagaku Food Co., Ltd.] etc. are mentioned.

The blending ratio of magnesium stearate and sucrose fatty acid ester is preferably 1: 1 to 2 by weight, preferably 1: 1 to 1.4.

Moreover, the compounding quantity per tablet as whole quantity of a lubricating agent is 1.0 to 3 weight%, Preferably it is about 1.0 to 2.0 weight%.

When the active ingredient has a bitter taste, a masking agent for masking such a bitter taste can be blended according to a commercial method. Examples of such masking agents include sweeteners such as aspartame and tautman or flavoring agents such as 1-menthol, dry coat vanilla, brown sugar flavor, dry coat peppermint and grapefruit coat. The compounding quantity of these masking agents can increase and decrease its usage suitably according to the active ingredient to contain.

The dry direct instant disintegrating tablet provided by this invention can be prepared, for example by the manufacturing method by the following processes.

This method is roughly composed of two steps of a first step of mixing each component constituting the tablet, followed by a second step of tableting, and each step itself is simple and efficient that can be carried out according to a commercial method. It is a preparation method of a tablet.

The detail is as follows.

[Step 1]

First, a predetermined amount of the following components, (a) active ingredient, (b) dissolution aid, (c) excipient, (d) binder, (e) disintegrant and (f) glidant according to the conventional method, for example, a mixer [Brand name, Borecontena mixer; Kotobukiki Kenko Co., Ltd. product] is used for mixing.

The mixing time at this time varies depending on the type of additive used, the amount of use, and the like, but is not particularly limited, but preferably 5 to 40 minutes, more preferably 5 to 30 minutes.

Subsequently, (g) lubricant is further added to the mixture and mixed.

The mixing time at this time should just be a time which can fully mix a lubricant, and although it does not specifically limit depending on the usage-amount of the said mixture, Usually, it is 2 to 10 minutes, Preferably it is 2 to 4 minutes. In mixing, you may further add a mating agent, for example, erythritol, as desired.

Second Process

In this way, the dry direct tableting tablet of the present invention made into the target by dry compression using the prepared mixture is prepared.

The fragrance used in the fast disintegrating tablet provided by the present invention can be added at any one of the first step and the second step, but is preferably added at the second step.

In addition, the sweetener used for the tablet of this invention can be added anywhere in the said 1st process or a 2nd process.

Although the dry spontaneous fast disintegrating tablet for which this invention aims by the above is provided, the obtained tablet has the hardness of a practical tablet, maintaining the desired fast disintegration property.

(Example)

Hereinafter, the present invention will be described in more detail in the following examples.

Furthermore, in Examples 1-9, the tablet which added both sodium citrate and sodium hydrogencarbonate together as a dissolution adjuvant was used, using Meloxycam whose average particle diameter obtained by grind | pulverizing with a grinder according to a conventional method is 4-15 micrometers. Although the preparation method of is illustrated, this invention is not limited to these Examples.

In addition, also in the comparative example, meloxycam which has each particle diameter is prepared and used.

Examples 1-9:

Each component was mixed and compressed into tablets according to the formulations shown in Table 1 below, to obtain dry direct- instant disintegrating tablets.

In the table, (a) is an active ingredient, (b) is a dissolution aid, (c) is an excipient, (d) is a binder, (e) is a disintegrant, (f) is a fluidizing agent, and (g) is a lubricant (H) is a mating agent, (i) is a sweetener, and (j) is a fragrance.

Representative manufacturing operations are shown in the formulation of Example 1.

(a) Meloxycam (active ingredient; 8.00 g), (b) sodium citrate (dissolution aid; 8.00 g), sodium hydrogencarbonate (dissolution aid; 2.00 g), (c) lactose (excipient; 62.00 g), ( d) crystalline cellulose [binder; 20.00 g, Zeoras PH302, manufactured by Asahi Kasei Chemicals Co., Ltd.], (e) crospovidone [disintegrant; 30.00 g, crospovidone XL, manufactured by ISP Co., Ltd.] and (f) hard silicic anhydride [fluidizing agent; 2.60 g of Furo Intokyo Co., Ltd.] was mixed for 30 minutes, followed by (g) magnesium stearate (lubricant; 1.40 g) and sucrose fatty acid ester [lubricant; 2.00 g, Sugar ester B-370F, Mitsubishi Kasei Foods Co., Ltd.] were further added, and it mixed for 3 minutes.

In mixing, erythritol (coating agent; 60.00 g), aspartame (sweetening agent; 4.00 g), and 1-menthol (fragrance; 0.10 g) were added.

By tableting the obtained mixture directly, 375 mg weight tablet containing 15 mg of active ingredients was obtained.

Also about each Example, each tablet was prepared according to the above. However, in Examples 8 and 9, it is a tablet of 250 mg weight containing 10 mg of active ingredients.

About the obtained tablet, the hardness of the tablet, the disintegration time (minutes) by the disintegration test method of the Japanese pharmacy room, and the abrasion degree by the 200 degree-of-wear test were measured, and also it showed in the table.

Example 10:

In the manufacturing method of Example 7, tablets containing 15 mg of the active ingredient (total weight: 375 mg) were prepared by the same formulation, except that meloxycam and sodium citrate were 4 parts by weight and 1 part by weight of sodium bicarbonate.

As a result, although the elution was faster than the tablet of the comparative example 3 mentioned later, it felt a little bitter taste.

Example 11:

In the preparation method of Example 7, tablets containing 15 mg of the active ingredient (total weight: 375 mg) were prepared by the same formulation, except that meloxycam and sodium citrate were 3 parts by weight and 2 parts by weight of sodium bicarbonate.

As a result, although eluting was quicker than the tablet of the comparative example 4 mentioned later, it felt a little bitter taste.

Example 12:

In the preparation method of the tablet of Example 3, tablets containing 15 mg of the active ingredient are obtained by tableting the mixture obtained by the same method, except that brown sugar flavor (0.2 g) or dry coat peppermint (0.2 g) is added as a fragrance. : 375 mg) was prepared. The properties such as elution behavior for these tablets do not change at all with those of Example 3, and the taste of these tablets was good.

In addition, in Example 11 and Example 12, unpleasant bitterness was alleviated when tablets were prepared by adding aspartame as a sweetener and 1-menthol as a flavoring agent.

Comparative Examples 1 to 6:

Each component was mixed and compressed into tablets according to the formulation shown in Table 2 below, to obtain dry direct- instant disintegrating tablets.

About each obtained tablet, it tested similarly to the said Example, and showed the result in the table | surface together.

In Comparative Examples 1 to 4, Meloxycamp having an average particle diameter of 60 to 80 µm was used as a dissolution aid. In Comparative Example 1, only sodium hydrogen carbonate was 0.25 parts by weight based on 1 part by weight of Meloxycam, and Comparative Examples 1 to 4 were citric acid. It is each tablet which added only 1, 2.5, and 5 weight part of sodium only with respect to 1 weight part of meloxycamps, respectively.

About each of these tablets, "V. Elution behavior was confirmed in accordance with the section "Elution test".

As a result, commercial tablets eluted an average of 85% or more within 60 minutes, but each tablet of Comparative Examples 1 to 4 did not elute an average of 85% or more within 6 hours of the prescribed time.

As a cause of the difference in elution behavior with commercially available tablets, first of all, the difference in the physical property values of the raw meloxycam was considered. Then, it examined whether improvement was made by making particle diameter small.

Comparative example 5 and 6 are each tablet which used 1 and 1.25 weight part of sodium citrate with respect to 1 weight part of hydroxycamphams, respectively, using the meloxycamp with an average particle diameter of 7-15 micrometers, as a dissolution aid. As a result, the dissolution behavior was found to be similar to that of a commercially available product by using Meloxycam with a small average particle diameter and adding a dissolution aid. Elution of more than 85% on average within 6 hours was not found.

In addition, although tableting was performed using magnesium stearate or sucrose fatty acid ester alone as a lubricant, capping occurred and the yield decreased, which was not practical.

From the above result, although the particle size of Meloxycam was used and the dissolution adjuvant was further added, it was confirmed that it was effective in making the elution behavior similar to a commercial item, but sufficient elution behavior was not yet acquired.

On the other hand, the tablet of Examples 1-9 uses meroxica which has an average particle diameter of 4-15 micrometers, and uses both sodium citrate and sodium hydrogencarbonate as a dissolution adjuvant, and a desired dissolution behavior is obtained by this. The specificity of the present invention is well understood in this respect.

As described above, according to the present invention, dry instantaneous rapid disintegrating tablets having a hardness of practical tablets, in particular, instantaneous rapid disintegrating tablets containing meloxycam, are provided, and their dissolution behavior is good. The medical value is tremendous.

Claims (10)

(a) an active ingredient; (b) as a dissolution aid, it contains an acid selected from citric acid, tartaric acid, malic acid, lactic acid and ascorbic acid or at least one member selected from the group consisting of alkali metal salts, alkali metal hydrogencarbonates, and alkali metal carbonates: (c A) a lubricant comprising (d) a binder, (e) a disintegrant, (f) a glidant, and (g) a lubricant, a lubricant comprising a combination of magnesium stearate and a sucrose fatty acid ester. Collapsible tablets. The method of claim 1, wherein the alkali metal salt of the acid is sodium citrate, potassium citrate, sodium stannate, potassium stannate, sodium malate, potassium malate, sodium lactate, potassium lactate, sodium ascorbate or potassium ascorbate; Alkali metal hydrogencarbonates are sodium bicarbonate or potassium bicarbonate; Dry metal instantaneous rapid disintegrating tablet, characterized in that the alkali metal carbonate is sodium carbonate or potassium carbonate. The dry instant disintegrating tablet according to claim 1, wherein the dissolution aid of (b) comprises a combination of sodium citrate and sodium bicarbonate. The excipient according to any one of claims 1 to 3, wherein the excipient of (c) is a sugar such as lactose, erythritol, D-mannitol, xylitol, multitol, synthetic aluminum silicate, and hydroxypropyl starch sodium. Dry crushing fast disintegrating tablet, characterized in that at least one selected from the group consisting of crystalline cellulose, hydroxypropyl starch, anhydrous calcium hydrogen phosphate, reduced maltose syrup. The binder according to any one of claims 1 to 4, wherein the binder of (d) is at least one member selected from the group consisting of crystalline cellulose, powdered cellulose, low-substituted hydroxypropyl cellulose, and carmelose. Dry direct instant disintegrating tablets. The disintegrant according to any one of claims 1 to 5, wherein the disintegrant of (e) is at least one selected from the group consisting of crospovidone, carmellose, carmellose calcium, and carboxymethyl starch sodium. Dry direct instant disintegrating tablets. 7. The dry instantaneous rapid disintegrating tablet according to any one of claims 1 to 6, wherein the fluidizing agent of (f) is hard silicic anhydride (silicon dioxide). 8. The dry instant disintegrating tablet according to any one of claims 1 to 7, wherein the active ingredient (a) is meloxycam. Dry spontaneous fast disintegrating tablet comprising the following components. The active ingredient of (a) is meloxycamp, Dissolution aids of (b) include sodium citrate and sodium bicarbonate, excipients of (c) include lactose and erythritol, The binder of (d) is crystalline cellulose, Disintegrants of (e) are crospovidone, The fluidizing agent of (f) includes light silicic anhydride (silicon dioxide), The glidants of (g) are magnesium stearate and sucrose fatty acid esters. (a) meloxycam, (b) sodium citrate and sodium bicarbonate as dissolution aids, (c) excipients, (d) binders, (e) disintegrants and (f) glidants; (g) further adding and mixing magnesium stearate and sucrose fatty acid ester as glidants; The tableting process of the obtained mixture is carried out directly, The manufacturing method of the dry spontaneous fast disintegrating tablet of Claim 8 or 9.