KR102240935B1 - Techniques for improving the disintegration and storage stability of tablet containing fingerroot extract as an active ingredient - Google Patents

Abstract

The present invention relates to a tablet containing a finger root extract as an active ingredient (pharmacological component, main component), and the unique tablet provided by the present invention contains a high component of finger root extract (panduratin-based compound), It not only exhibits excellent physical properties such as required appropriate disintegration, drug stability, and aging stability, but also has excellent properties in terms of efficient manufacturing process/distribution, such as tabletting and handling ease (hardness and friability-related physical strength, etc.).

Description

{Techniques for improving the disintegration and storage stability of tablet containing fingerroot extract as an active ingredient}

The present invention relates to a tablet peculiar to the present invention that contains a finger root extract as an active ingredient (pharmacological component, main component) and has excellent physical properties in various aspects such as tabletting property, disintegrating property, and aging stability.

In the case of manufacturing tablet products that are widely used in the pharmaceutical and health functional food industries, each component powder is mixed and then compressed and tableted using a tablet press, depending on the physical properties of the main ingredient (pharmacological ingredient). There are many differences in the composition of the tablets. Tablets are generally manufactured by adding an additive to the main component material, and by formulating with the additive, it is intended to increase the quality and economy while maintaining the stability, safety or homogeneity of the formulation. That is, additives are substances that are additionally used to increase the usefulness of stability, safety and quality when formulating pharmaceuticals or health functional foods.

Depending on the main component and the composition of the additives contained in each tablet, there are restrictions on the physical properties of individual tablets, and so on, these tablet composition techniques are closely controlled. As an additive, it is used for the purposes of excipients, stabilizers, preservatives, buffers, flavoring agents, suspending agents, emulsifying agents, fragrances, solubilizing aids, coloring agents, thickeners, and the like, if necessary. The additives used do not show direct pharmacological action at the dosage of the formulation and are safe, and should not alter the therapeutic effect of the formulation or interfere with the test. The choice of additives depending on the active ingredient is very important in the design of high-quality formulations (tablets). Additives improve the stability of the formulation, improve the bioavailability, maintain the quality of the formulation during storage or use, and control the physical properties of the drug to improve drug economy. In particular, incompatibility between the active ingredient (especially a drug) and an additive is often a problem, i.e., an undesirable interaction that changes the physical, chemical or therapeutic properties of the drug formulation (or formulation) is the main ingredient. It can occur between the drug and the additive.

For example, crosscarmellose sodium is previously used in a way that a small amount is added in tablets in which the main component of the tablet, various excipients (fillers), and binders are combined.'Huang WX et al. 2006 (Non-Patent Literature 1)' reported that croscarmellose sodium had an effect on the release of Metformin drugs, and thus was not suitable for formulations of components such as Metformin.

In addition, when an excessive amount of disintegrant is used, the dissolution of the tablet may be accelerated, but the possibility of negatively affecting the stability of the tablet by attracting moisture in the air increases, which may cause the storage period to be shortened. That is, the disintegrant may negatively affect tablet stability (especially, storage stability) through a method such as attracting moisture in the air. Accordingly, Korean Patent Registration No. 10-1752700 (Patent Document 1) adopted a special form of provision in which a tablet containing an excessive amount of disintegrant is incorporated into the capsule.

In addition, in the manufacture of tablets, it is required to satisfy not only excellent moldability, but also formulation characteristics such as moderate hardness and low brittleness.The hardness and disintegration properties are opposite to each other, and in general, the hardness is increased. In order to do so, if the molding pressure is increased, the disintegration time becomes longer. On the contrary, if the molding pressure is decreased to shorten the disintegration time, the hardness tends to decrease.

Therefore, in providing tablets, various additives such as excipients, stabilizers, preservatives, buffers, suspending agents, emulsifiers, solubilizers, and thickeners are mixed for each purpose little by little for the excellent characteristics of the tablet. to be. However, as the number of substances actually increases, not only the economic feasibility of manufacturing a product decreases, but also becomes a factor of occurrence of unpredictable variables in certain situations when using a formulation.

Meanwhile, as interest in the quality of life and wellness increases along with the improvement of living standards, various new health functional food materials are being discovered. As a representative example of this, fingerroot is in the spotlight, and its extract is known to contain a large amount of panduratin-based compounds. These panduratin compounds, that is, fingerroot extract, are known to have various functions such as improving exercise capacity, reducing blood fat, anti-fatigue, strengthening muscles, reducing blood sugar, reducing cholesterol, and reducing weight.

Accordingly, attempts have been made to provide a fingerroot extract (i.e., panduratin-based compound) in tablet form to facilitate ingestion, but disintegration, drug stability, stability over time, tabletting ability, and large-scale production required by the pharmaceutical formulation Research on the aspects of manufacturing characteristics such as ease of handling (storage, packaging, distribution, etc.), constant hardness, and wear rate are insufficient.

Panduratin-based compounds do not dissolve well in water, and thus precise control according to the types and contents of other additives is required in order to produce tablets having desirable physical properties. As a prior study, Korean Patent Registration No. 10-1695443 (Patent Document 2) has attempted to manufacture panduratin tablets using L-arginine as a disintegrant, but the disintegration rate is also used when L-arginine is used as a disintegrant. Was reported to be about 40 to 55 minutes. This is a level that still requires improvement, considering that the standard set by the disintegration test method among the general test methods of the Korean Health Functional Food Code is about 30 minutes. In addition, it was confirmed that physical properties such as stability over time were poor when L-arginine was used (see Experimental Example 1 of the present specification).

As described above, it is difficult to satisfy both the pharmaceutical properties and manufacturing properties required for the fingerroot extract tablet, and thus, purification of excellent physical properties is still required.

Korean Patent Registration 10-1752700 Korean Patent Registration 10-1695443

Huang WX et al, Elimination of metformin-croscarmellose sodium interaction by competition. Int J Pharm. 2006 Mar 27;311(1-2):33-9.

Accordingly, the present inventors overcome the limitations of the prior art, and specifically cross-linked carboxymethylcellulose for tablets containing fingerroot extract (panduratin-based compound) as a main component, is used as an agent for improving aging stability (stability over 24 months or longer). It was identified for the first time that it has a special use as a), and thus it contains a fingerroot extract (panduratin-based compound) component (especially in a high content), and provides adequate disintegration properties, drug stability, and aging stability, etc. In addition to exhibiting excellent physical properties, the present invention was completed by producing excellent tablets in terms of efficient manufacturing process/distribution, such as tabletting properties and ease of handling (hardness and wear-related physical strength, etc.).

Therefore, the object of the present invention,

In the tablet containing fingerroot (fingerroot) extract as an active ingredient,

The tablet is to provide a tablet comprising cross-linked carboxymethylcellulose as an agent for improving stability over time and a disintegrant.

In order to achieve the above object, the present invention is in the tablet containing a fingerroot (fingerroot) extract as an active ingredient, the tablet includes cross-linked carboxymethylcellulose (Cross-linked carboxymethylcellulose) as a stability improver and disintegrant over time It provides a tablet characterized in that.

Hereinafter, the present invention will be described in detail.

The term "finger root (fingerroot)" in the present invention are a type of plant of ginger (Zingiberaceae family), beam Essen suberic hunger plate dura other (Boesenbergia pandurata), rhizome, such kaem Feria plate dura other (Kaempferia pandurata) (rhizome Means).

In one preferred embodiment, the finger root extract (particularly, panduratin-based compound) used in the present invention is purified water suitable for food processing, alcohol (preferably, C1-C6 alcohol), subcritical or super It can be obtained by extraction and purification using any one solvent selected from the group consisting of a critical fluid and a mixed solvent thereof, or can be obtained by separating and purifying the whole fingerroot plant from oil obtained by directly pressing.

For example, as an extraction solvent, ethanol, methanol, propanol, isopropanol, butanol, acetone, ether, benzene, chloroform, ethyl acetate, Various solvents, such as methylene chloride, hexane, cyclohexane, and petroleum ether, can be used individually or in mixture.

In one embodiment, in the present invention, the fingerroot extract may be prepared in the form of dry X, soft X, liquid X, tincture, or the like according to a conventional X preparation method.

In one preferred embodiment, the finger root extract in the present invention may be to use a dry extract (solid extract).

In one embodiment, the finger root extract used in the present invention may preferably mean a panduratin-based compound.

In yet another embodiment, a mixture of only panduratin-based compounds may be used for preparing tablets. In the present invention, the panduratin-based compound is, but is not limited to, panduratin A (formula 1), isopanduratin A (formula 2), and 4-hydroxypaduratin A. , Chemical formula 3) and the like.

<Formula 1>

<Formula 2>

<Formula 3>

Individual separation and purification of panduratin-based compounds from fingerroot extracts can be performed by using column chromatography filled with various synthetic resins such as silica gel or activated alumina, and high-performance liquid chromatography (HPLC) alone or in parallel. Although it can be used, the method of extraction and separation and purification of the panduratin derivative is not necessarily limited to the above method.

In providing a tablet containing (especially, high content) finger root extract, cross-linked carboxymethylcellulose (CMC) as well as a disintegrant has a special effect as a finger root extract tablet-specifically, as a aging stability enhancer. It was the first to be identified as having. In other words, even when a tablet is prepared and provided by mixing only cross-linked carboxymethylcellulose (CMC) as a single additive in addition to the main component, the tablet not only satisfies the disintegration property required for the pharmaceutical formulation, but also forms formability, drug stability, and stability over time. It exhibits excellent physical properties such as (especially storage stability), appropriate hardness and friability, and low friability, and is also excellent in terms of efficient manufacturing process/distribution such as tabletting property and ease of handling. This characteristic of the present invention is contrasted with the fact that the excipient component occupies a large proportion in the additive in the tablets provided previously. In general, since the role of the excipient is to impart the proper size and hardness of the tablet, it is known that when only the disintegrant is used alone, the size of the tablet is not properly formed, and it is difficult to show the appropriate hardness. In addition, when using a disintegrant generally used in the manufacture of tablets in the past, compared to the poor stability over time of the finger root extract tablet, the unique effect of the present invention has remarkable technical specificity.

In particular, in the conventional manufacturing of tablets, there is a technical difficulty in achieving'combination of disintegration properties with physical properties such as hardness and storage stability' or'optimal balance between physical properties such as hardness and storage stability' and disintegration properties. Contrary to this known, according to the present invention, not only disintegration occurs within 30 minutes, but also has hardness and abrasion characteristics to the extent that tablets maintain a certain quality during handling (processes of manufacturing, packaging, storage, distribution, etc.) It is characterized by doing. In addition, the tablets of the present invention at the same time have excellent aging stability (storage stability).

In particular, cross-linked-CMC can be used as a stability enhancer (enhancer) over time for not only disintegration but also finger root extract tablets (panduratin-based compound tablets), it is the earliest disclosed in the present invention. This is in contrast to the conventional cross-linked-CMC was not used as a single additive in the field of tablet manufacturing, and has remarkable technical significance. Substantially, a separate excipient may not be required in the tablet of the present invention, or a small amount of excipient may be included in the composition in order to improve material flow or/and tabletting properties in the process desired by those skilled in the art.

Therefore, the present invention

In the tablet containing fingerroot (fingerroot) extract as an active ingredient,

The tablet provides a tablet comprising cross-linked carboxymethylcellulose as an agent for improving stability over time and a disintegrant.

That is, the present invention,

Fingerroot extract; And it provides an oral tablet composition comprising a cross-linked carboxymethylcellulose (Cross-linked carboxymethylcellulose).

In the present invention, the crosslinked carboxymethyl cellulose may be used in the form of a known salt thereof, and the type of the salt is not particularly limited. In one embodiment, in the present invention, cross-linked sodium carboxymethylcellulose may be used.

Preferably, the tablet of the present invention is technically characterized in that the weight ratio of crosslinked carboxymethyl cellulose: fingerroot extract is 1: 2 to 7. If the addition amount of crosslinked carboxymethyl cellulose is greater than 1:2 in the ratio, tablet tabletability is poor, and if the amount of crosslinked carboxymethyl cellulose is less than 1:7 in the ratio, disintegration does not occur.

For example, in the tablet of the present invention, the weight ratio of crosslinked carboxymethyl cellulose: fingerroot extract is 1:2.0, 1:2.1, 1:2.2, 1:2.3, 1:2.4, 1:2.5, 1:2.6, 1:2.7 , 1:2.8, 1:2.9, 1:3.0, 1:3.1, 1:3.2, 1:3.3, 1:3.4, 1:3.5, 1:3.6, 1:3.7, 1:3.8, 1:3.9, 1 :4.0, 1:4.1, 1:4.2, 1:4.3, 1:4.4, 1:4.5, 1:4.6, 1:4.7, 1:4.8, 1:4.9, 1:5.0, 1:5.1, 1:5.2 , 1:5.3, 1:5.4, 1:5.5, 1:5.6, 1:5.7, 1:5.8, 1:5.9, 1:6.0, 1:6.1, 1:6.2, 1:6.3, 1:6.4, 1 It may be :6.5, 1:6.6, 1:6.7, 1:6.8, 1:6.9 or 1:7.0.

In a more preferred embodiment, the tablet of the present invention is characterized in that the weight ratio of crosslinked carboxymethyl cellulose: fingerroot extract is 1: 3 to 7.

In a more preferred embodiment, the tablet of the present invention is characterized in that the weight ratio of crosslinked carboxymethyl cellulose: fingerroot extract is 1: 4 to 7.

In one embodiment, most preferably, the tablet of the present invention may be characterized in that the weight ratio of crosslinked carboxymethyl cellulose: fingerroot extract is 1: 5 to 6.

The tablet of the present invention is not particularly limited in the content of the finger root extract as long as it satisfies the above-described technical characteristics. For example, in the tablet of the present invention, the content of the fingerroot extract may be 10 to 90% (w/w) based on the total weight of the tablet. Specifically, in the tablet of the present invention, the fingerroot extract is 10, 15, 20, 25, 30, 35, 40, 45, 50, 55, 60, 65, 70, 75, 80, 85 or 90% of the total weight of the tablet. It may be included as (w/w).

Preferably, in the tablet of the present invention, the content of the fingerroot extract may be 30 to 80% (w/w) based on the total weight of the tablet.

In one embodiment, as an example, the fingerroot extract may be included in an amount of 30 to 50% (w/w) based on the total weight of the tablet.

In another embodiment, the tablet of the present invention may contain a high content of fingerroot extract. In this embodiment, as a preferred example, the fingerroot extract may be contained in an amount of 50 to 80% (w/w) based on the total weight of the tablet.

In a more preferred example, the fingerroot extract may be included in an amount of 60 to 80% (w/w) based on the total weight of the tablet.

In one embodiment, the present invention

Fingerroot extract; And

It provides a tablet characterized in that it comprises (or consists essentially of) cross-linked carboxymethyl cellulose.

The tablets of the present invention may optionally contain additional additives as long as the above-described properties are satisfied.

As an example, a lubricant may be additionally included in a range that does not negatively affect advantageous properties such as disintegration, stability over time, hardness, friability, and tabletability of the tablet of the present invention. The lubricant is used for the purpose of making the powder material flow well in the tablet press, preventing sticking to equipment such as punches, and giving gloss to the tablet, as long as it does not affect the advantageous properties of the tablets of the present invention. , Although the type is not particularly limited, for example, one or more selected from the group consisting of stearic acid, magnesium stearate, and calcium stearate may be used.

The lubricant may be included in an amount of 1 to 2% (w/w) based on the total weight of the tablet, and if it is contained less than 1% (w/w), it is not good because the frictional force of the device increases during tableting, and 2% (w/w) is not good. w) Excessive use may negatively affect tabletting.

In another example, the tablet of the present invention may further contain an excipient. In the present invention, excipients are mainly used to impart an appropriate size of the tablet and facilitate flowability during tableting, and may additionally impart hardness within a range that does not impair the advantageous properties of the present invention. The excipient is used in a category that does not negatively affect the advantageous properties such as disintegration, stability over time, hardness, friability, and tabletability of the tablet of the present invention. Although not particularly limited, for example, one or more selected from the group consisting of crystalline cellulose, maltodextrin, lactose, starch, chicory root extract powder, indigestible maltodextrin and isomalt may be used.

In one embodiment, for example, in the tablet of the present invention, crystalline cellulose may be used as an excipient.

In another embodiment, for example, in the tablet of the present invention, crystalline cellulose and maltodextrin may be used in combination as excipients. In this case, a person skilled in the art may appropriately mix and use the two substances so as to show appropriate flowability and tabletability during the process according to the properties of the main raw material.This combination is well known in the art, and the person skilled in the art determines the degree of mixing the excipients according to the desired flowability. Can be arbitrarily adjusted.

The excipient is included in the remaining amount excluding the content (% (w/w)) of essential ingredients based on the total weight of the tablet of the present invention. Therefore, the content of the excipient may not be included in the composition depending on the properties of the raw material used, or may contain 0.1 to 99%, but the content is preferably adjusted according to the features of the present invention.

In the above embodiment, the present invention is an example

Fingerroot extract;

Crosslinked carboxymethyl cellulose; And

Optionally, there is provided a tablet, characterized in that it consists of (essentially) a lubricant, an excipient, or a mixture thereof.

In the present invention, the term'optionally comprising/consisting of' means not only including the indicated substance in the composition (the tablet composition of the present invention) as desired by those skilled in the art, but also the indicated substance not present in the composition. This means that you can select a configuration (that is, it does not contain).

In other words, the present invention as an embodiment

Fingerroot extract;

Crosslinked carboxymethyl cellulose; And

Optionally any one selected from the group consisting of lubricants, excipients and mixtures thereof

It provides a tablet, characterized in that consisting of (essentially).

In another embodiment, the present invention

In the tablet containing finger root extract, excipient, lubricant and disintegrant,

The tablet provides a tablet comprising cross-linked carboxymethylcellulose as an agent for improving stability over time and a disintegrant.

In another aspect, the present invention

In the tablet consisting of fingerroot extract, excipient, lubricant and disintegrant (essentially), the tablet comprises cross-linked carboxymethylcellulose as a stability improver and disintegrant over time. Provides.

In one preferred embodiment, the present invention

In a tablet comprising (or consisting essentially of) fingerroot extract and crosslinked carboxymethyl cellulose, optionally further comprising a lubricant, excipient or mixture thereof,

The finger root extract is contained in 30 to 80% (w / w) based on the total weight of the tablet,

In the tablet, the weight ratio of crosslinked carboxymethyl cellulose: fingerroot extract is 1: 2 to 7 (more preferably 1: 3 to 7, even more preferably 1: 4 to 7), including crosslinked carboxymethyl cellulose in an amount corresponding to It provides a tablet characterized in that (or consisting essentially of).

As one more specifically preferred embodiment, the present invention

Based on the total weight of the tablet

30 to 80% (w/w) fingerroot extract;

Cross-linked carboxymethylcellulose in an amount corresponding to the weight ratio of cross-linked carboxymethyl cellulose: fingerroot extract is 1: 2 to 7 (more preferably 1: 3 to 7, even more preferably 1: 4 to 7) ;

1 to 2% (w/w) lubricant; And

It provides a tablet, characterized in that it consists of (essentially) the balance of excipients.

As another preferred embodiment, the present invention provides a tablet containing a high content of finger root extract. In the present invention, cross-linked carboxymethylcellulose as an essential component is not only suitable for tabletting fingerroot extract, but also on the basis of a unique discovery that simultaneously achieves the effect of improving the stability over time as well as disintegration of the tablet.

As an example of such a tablet, the present invention

Based on the total weight of the tablet

60 to 80% (w/w) fingerroot extract; And

Cross-linked carboxymethyl cellulose: characterized in that it comprises (or consists essentially of) cross-linked carboxymethyl cellulose in an amount corresponding to the weight ratio of the finger root extract 1: 4 to 7 (more preferably 1: 5 to 6) Provide tablets.

As another example for the purification of the high content of finger root extract, the present invention

In a tablet comprising (or consisting essentially of) fingerroot extract and crosslinked carboxymethyl cellulose, optionally further comprising a lubricant, excipient or mixture thereof,

The finger root extract is contained in an amount of 60 to 80% (w/w) based on the total weight of the tablet,

In the tablet, the weight ratio of crosslinked carboxymethyl cellulose: fingerroot extract is 1: 4 to 7 (more preferably 1: 5 to 6) in an amount corresponding to the crosslinked carboxymethyl cellulose (or consists essentially of) It provides a tablet made of.

As another example for the purification of the high content of finger root extract, the present invention

Based on the total weight of the tablet

60 to 80% (w/w) fingerroot extract;

Crosslinked carboxymethyl cellulose: crosslinked carboxymethyl cellulose in an amount corresponding to the weight ratio of the fingerroot extract of 1: 4 to 7 (more preferably 1: 5 to 6);

1 to 2% (w/w) lubricant; And

It provides a tablet, characterized in that it consists of (essentially) the balance of excipients.

As another example for a tablet containing finger root extract, the present invention

Fingerroot extract;

Crosslinked carboxymethyl cellulose; And

Optionally, it is a tablet comprising a lubricant, an excipient, or a mixture thereof, wherein the excipient is not included in the tablet, or the content of the excipient is less than (preferably, less than) the content of the crosslinked carboxymethyl cellulose based on the weight. A tablet (tablet composition) is provided.

As another example for the purification of the high content of finger root extract, the present invention

In a tablet comprising (or consisting essentially of) fingerroot extract and crosslinked carboxymethyl cellulose, and optionally further comprising a lubricant, an excipient, or a mixture thereof,

The fingerroot extract is contained in 60 to 80% (w/w) (more preferably 75 to 80% (w/w)) based on the total weight of the tablet,

In the tablet, the weight ratio of crosslinked carboxymethyl cellulose: fingerroot extract is 1: 4 to 7 (more preferably 1: 5 to 6),

The excipient is not included in the tablet or provides a tablet (tablet) composition, characterized in that it is included in the weight of crosslinked carboxymethyl cellulose or less (preferably less than).

As another example for the purification of the high content of finger root extract, the present invention

In a tablet comprising (or consisting essentially of) a fingerroot extract, a crosslinked carboxymethyl cellulose and a lubricant, and optionally further comprising an excipient,

The fingerroot extract is contained in 60 to 80% (w/w) (more preferably 75 to 80% (w/w)) based on the total weight of the tablet,

In the tablet, the weight ratio of crosslinked carboxymethyl cellulose: fingerroot extract is 1: 4 to 7 (preferably 1: 5 to 6),

The excipient is not included in the tablet or provides a tablet (tablet) composition, characterized in that it is included in the weight of crosslinked carboxymethyl cellulose or less (preferably less than). In a preferred example, the lubricant in the tablet may be included in an amount of 1 to 2% (w/w) based on the total weight of the tablet, but may not be limited as long as the features are satisfied.

Although not limited thereto, in one embodiment, the tablets of the present invention may be uncoated tablets.

In one more preferred embodiment, the tablets of the present invention may be those produced by direct compression.

In a further embodiment, the tablets of the present invention may be those prepared by a dry granulation method (dry granulation method).

In another embodiment, the tablets of the present invention may be coated tablets. In this embodiment the present invention

A coating layer containing a hydrophilic polymer; And

It provides a tablet, characterized in that consisting of a core (core) comprising a finger root extract and cross-linked carboxymethyl cellulose.

In the core of the tablet, additional additives may be optionally included within a range that does not negatively affect the advantageous properties of the tablet of the present invention. Preferably, it may additionally include one or more selected from the group consisting of excipients and lubricants, and specific types and contents thereof are understood with reference to the foregoing.

In the coating layer of the tablet, the hydrophilic polymer is used as the main coating agent. Hydrophilic polymer types suitable for coating tablets are well known in the art, and are not limited thereto, but the hydrophilic polymer suitable for the present invention is preferably at least one selected from the group consisting of hydroxypropylmethylcellulose, hydroxypropylcellulose, and ethylcellulose. Can be.

The amount of the hydrophilic polymer is not particularly limited as long as it is used in tablet coating in the art, and as an example, it may be used in an amount of 3 to 5% (w/w) based on the total weight of the tablet of the present invention.

In one embodiment, the tablet of the present invention may preferably be one using hydroxypropylmethylcellulose as a hydrophilic polymer. For example, hydroxypropylmethylcellulose may be contained in an amount of 3.5 to 5%, and when hydroxypropylmethylcellulose is less than 3.5%, the viscosity of the coating composition is low, resulting in poor coating properties, which takes a long time to coat In this case, when it exceeds 5%, the viscosity of the coating composition increases rapidly, so that it may be difficult to apply a coater.

In the tablet of the present invention, the coating layer may additionally contain an emulsifier in addition to the hydrophilic polymer as the main coating agent. Although not limited thereto, suitable emulsifiers for the present invention include acetylated monoglycerides, Myvacet, polyethylene glycol, glycerol, triacetin, and stearic acid. ) It may be one or more selected from the group consisting of.

The amount of the emulsifier is not particularly limited as long as it is used for coating tablets in the art, and as an example, may be used in an amount of 0.01 to 1% (w/w) based on the total weight of the tablet of the present invention. If the emulsifier is not added, layer separation of the coating composition may occur, and if more than 1% is added, film film formation may not occur well during coating, which is not good.

As one embodiment for coated tablets, the present invention

A coating layer comprising 3 to 5% (w/w) of hydrophilic molecules and 0.01 to 1% (w/w) of an emulsifier based on the total weight of the tablet; And

A tablet comprising (or consisting essentially of) a fingerroot extract and a crosslinked carboxymethyl cellulose, and optionally comprising a lubricant, an excipient, or a mixture thereof, wherein the fingerroot extract comprises a total weight of the tablet. It is contained in an amount of 30 to 80% (w/w) based on, and the weight ratio of crosslinked carboxymethyl cellulose: fingerroot extract in the tablet is 1: 2 to 7 (more preferably 1: 3 to 7, even more preferably 1: 4) It provides a tablet characterized in that it comprises a cross-linked carboxymethyl cellulose in an amount corresponding to 7).

In the coated tablet, as an example of a more preferred tablet, the present invention

A coating layer comprising 3 to 5% (w/w) of hydrophilic molecules and 0.01 to 1% (w/w) of an emulsifier based on the total weight of the tablet; And

Fingerroot extract 30 to 80% (w / w), cross-linked carboxymethyl cellulose: the weight ratio of the finger root extract 1: 2 to 7 (preferably 1: 3 to 7, even more preferably 1: 4 to 7) It provides a tablet, characterized in that it consists of a core composed of a content of crosslinked carboxymethyl cellulose, a lubricant 1 to 2% (w/w), and a residual amount of excipients (essentially).

As another preferred embodiment, the present invention provides a coated tablet containing a high content of finger root extract. Although not limited thereto, as one embodiment for the finger root extract high content coated tablet, the present invention

A coating layer comprising 3 to 5% (w/w) of hydrophilic molecules and 0.01 to 1% (w/w) of an emulsifier based on the total weight of the tablet; And

A tablet comprising (or consisting essentially of) a fingerroot extract and crosslinked carboxymethyl cellulose, and optionally comprising a lubricant, an excipient or a mixture thereof, and further comprising a core,

The fingerroot extract is contained in an amount of 60 to 80% (w/w) based on the total weight of the tablet, and the weight ratio of crosslinked carboxymethyl cellulose: fingerroot extract in the tablet is 1: 4 to 7 (more preferably 1: 5 to It provides a tablet, characterized in that it contains cross-linked carboxymethyl cellulose in an amount corresponding to 6).

In the finger root extract high content coated tablet, as an example of a more preferred tablet, the present invention

A coating layer comprising 3 to 5% (w/w) of hydrophilic molecules and 0.01 to 1% (w/w) of an emulsifier based on the total weight of the tablet; And

Fingerroot extract 60 to 80% (w/w), crosslinked carboxymethyl cellulose: crosslinked carboxymethyl cellulose in an amount corresponding to a weight ratio of fingerroot extract of 1: 4 to 7 (more preferably 1: 5 to 6), It provides a tablet, characterized in that it consists of a core composed of 1 to 2% (w/w) of a lubricant and (essentially) the balance of excipients.

In another embodiment, the coated tablet of the present invention is

A coating layer containing a hydrophilic polymer; And

A tablet comprising a core comprising a fingerroot extract, crosslinked carboxymethyl cellulose, and optionally a lubricant, an excipient, or a mixture thereof,

The excipient is not included in the tablet, or a tablet (tablet composition), characterized in that the content of the excipient is less than (preferably, less than) the content of crosslinked carboxymethyl cellulose based on the weight.

As one of the preferred examples of the above embodiment, the coated tablet of the present invention

A coating layer comprising 3 to 5% (w/w) of hydrophilic molecules and 0.01 to 1% (w/w) of an emulsifier based on the total weight of the tablet; And

A tablet comprising (or consisting essentially of) a fingerroot extract and crosslinked carboxymethyl cellulose, and optionally comprising a lubricant, an excipient or a mixture thereof, and further comprising a core,

The fingerroot extract is contained in an amount of 60 to 80% (w/w) (more preferably 75 to 80% (w/w)) based on the total weight of the tablet, and in the tablet cross-linked carboxymethyl cellulose: weight ratio of finger root extract A 1: 4 to 7 (more preferably 1: 5 to 6), and the excipient is not included in the tablet or is included in the weight of crosslinked carboxymethyl cellulose or less (preferably less than). to provide.

As one of the preferred examples of the above embodiment, the coated tablet of the present invention

A coating layer comprising 3 to 5% (w/w) of hydrophilic molecules and 0.01 to 1% (w/w) of an emulsifier based on the total weight of the tablet; And

A tablet comprising (or consisting essentially of) a fingerroot extract, a crosslinked carboxymethyl cellulose and a lubricant, and optionally comprising a core further comprising an excipient,

The fingerroot extract is contained in an amount of 60 to 80% (w/w) (more preferably 75 to 80% (w/w)) based on the total weight of the tablet, and in the tablet cross-linked carboxymethyl cellulose: weight ratio of finger root extract A 1: 4 to 7 (more preferably 1: 5 to 6), and the excipient is not included in the tablet or is included in the weight of crosslinked carboxymethyl cellulose or less (preferably less than). to provide. In a preferred example, the lubricant in the tablet may be included in an amount of 1 to 2% (w/w) based on the total weight of the tablet, but may not be limited as long as the features are satisfied.

In one preferred embodiment, the tablets provided in the present invention are formulations for oral administration.

The tablets of the present invention may be provided in a general health functional food tablet standard, but are not limited thereto, but may be provided in units of 200mg to 2000mg.

The tablet having a composition peculiar to the present invention described above is characterized in that it disintegrates within 30 minutes (meaning hereinafter) based on an uncoated tablet. The uncoated tablet of the present invention exhibits a disintegration time of 5 to 30 minutes. For example, the uncoated tablet of the present invention is 5 minutes, 6 minutes, 7 minutes, 8 minutes, 9 minutes, 10 minutes, 11 minutes, 12 minutes, 13 minutes, 14 minutes, 15 minutes, 16 minutes, 17 minutes, 18 minutes, It may have a disintegration time of 19 minutes, 20 minutes, 21 minutes, 22 minutes, 23 minutes, 24 minutes, 25 minutes, 26 minutes, 27 minutes, 28 minutes, 29 minutes or 30 minutes.

In another preferred embodiment, the tablet having a composition specific to the present invention described above is characterized in that it disintegrates within 60 minutes (meaning hereinafter) based on a coated tablet. The coated tablet of the present invention may exhibit a disintegration time of 20 minutes to 60 minutes. For example, the coated tablet of the present invention is 20 minutes, 21 minutes, 22 minutes, 23 minutes, 24 minutes, 25 minutes, 26 minutes, 27 minutes, 28 minutes, 29 minutes, 30 minutes, 31 minutes, 32 minutes, 33 minutes, 34 It may have a disintegration time of minutes, 35 minutes, 36 minutes, 37 minutes, 38 minutes, 39 minutes 40 minutes, 45 minutes, 50 minutes, 55 minutes, or 60 minutes.

In the present invention, the term "stability over time" means that the stability of the formulation is not impaired over time and lasts, and may preferably mean storage stability.

The tablet of the present invention is characterized by having a aging stability (storage stability) of 24 months or more. Currently, since a maximum of 24 months is announced as a shelf life of health functional foods, only 24 months are set as the reference point, and practically, the tablet of the present invention is not limited to having a aging stability of up to 24 months. The tablets of the present invention can be stably stored for 120 days to 36 months. Considering the currently announced shelf life criteria, more preferably the tablets of the present invention can be stably stored for 120 days to 24 months. In one embodiment, although not limited thereto, the storage or storage may be preferably performed at a temperature of 20 to 25° C. and a relative humidity of 40 to 50%RH.

In addition, the present invention

In the finger root extract tablet manufacturing method,

It provides a method for producing a finger root extract tablet having improved stability over time, characterized by adding (mixing) cross-linked carboxymethyl cellulose to the finger root extract (or including the step of adding this).

The characteristics of the manufacturing method of the present invention are understood in accordance with the technical characteristics of the tablet composition described in the present specification.

The tablet of the present invention (high) contains a finger root extract (especially a panduratin-based compound), and exhibits excellent physical properties such as appropriate disintegration properties, drug stability, and aging stability, as well as tabletting properties and handling. It is excellent in terms of efficient manufacturing process/distribution such as ease (hardness and physical strength related to wear rate, etc.).

Hereinafter, the present invention will be described in detail.

However, the following examples are merely illustrative of the present invention, and the contents of the present invention are not limited to the following examples.

Tablet manufacturing method

1) Preparation of finger root extract (panduratin-based compound extract)

First, the dried finger root ( Boesenbergia pandurata ) was pulverized with a mixer, and then 100 g of the pulverized finger root sample was added to 500 mL of ethanol, and an extract was prepared while stirring at 50° C. for 30 minutes. The extracted sample was filtered through Whatman No. 2 filter paper, and the filtered extract was concentrated with a vacuum rotary concentrator to remove the solvent component, and then freeze-dried to remove moisture to obtain a fingerroot extract (powder).

2) Comparative Examples and Examples of Uncoated Tablet Manufacturing Method

The uncoated tablets of each of the comparative examples and examples were blended with the types of components and contents indicated in each table, and then tableted. The total weight of the tablet was 600 mg. First, all raw materials except for a lubricant (typically, magnesium stearate, etc.) were mixed for 10 minutes, and then a lubricant was added before tableting, mixed for 5 minutes, and tableted to prepare uncoated tablets. All were prepared using a tablet tablet press of SEJONG (Korea) KDIT-200 model in the same manner.

3) Comparative Examples and Examples of Coated Tablet Manufacturing Method

Coated tablets of each of the comparative examples and examples were prepared by coating them with hydroxypropyl methylcellulose and Myvacet after tableting in an uncoated state as described above. Hydroxypropyl methylcellulose was used as the main coating agent, and Mibaset was used as a coating aid.

Specifically, first, hydroxypropyl methylcellulose and mibaset were dissolved in a mixture of purified water and alcohol. The mixture thus obtained was applied to the uncoated tablet and coated. At this time, SEJONG (Korea) 8FC-130FS was used for the coating of the tablet.

4) Competency evaluation

The tabletting properties include lamination (a phenomenon in which the tablet is peeled in layers), capping (a phenomenon in which the upper part of the tablet is peeled in a hat shape), sticking (a phenomenon in which a groove is formed on the tablet surface), and weight deviation. It was judged on the basis of. Lamination, capping, and sticking were judged by a technician visually reviewing the manufactured tablet, and if there was no abnormality, it was judged as good, otherwise it was judged as bad. The weight deviation was judged as good if the weight deviation was 3% or less through the micro scale, and bad if the weight deviation exceeded 3%.

5) Hardness measurement

The hardness of the tablets was measured using a digital hardness tester of the D-63150 Heusenstamm model of ERWEKA GmbH (Germany), and was taken as an average value of 10 samples (manufactured tablets) measured every 10 minutes.

6) Disintegration (measurement of disintegration time)

The disintegration rate of tablets was measured according to the disintegration test method among general test methods of the Health Functional Food Code. It was tested in water at 37±2℃. Take 6 tablets as a sample, put it in a disintegration tester (KUK JE ENG Co. (domestic) KDIT-200 model), and perform vertical motion 30 times per minute until the sample is completely disintegrated. Observation and disintegration time were measured.

According to the health functional food code disintegration test method, the result is determined by performing vertical motion for 30 minutes in the case of uncoated tablets and then observing, even if the residue of the sample is not in the glass tube, the sea surface is If it is in the form of a material of the same shape), it is considered to be suitable. In the case of coated tablets, when observed after moving up and down for 60 minutes, it is considered suitable if the sample remains in the glass tube or is a film. Based on this disintegration conformity criterion, the stage without residues or the stage on the sea level was determined as the time of completion of the final disintegration time, measured and recorded in minutes. The disintegration time of the six samples was taken as the average value.

7) Measurement of change over time

After putting the tablets in a petri dish, the lid was not covered, and the tablets were stored in a temperature of 20 to 25°C and a relative humidity of 40 to 50% RH, and changes with time were observed.

8) Measurement of friability

The friability was measured using the KUK JE (Korea) friability tester FRIABILATOR KTF-25. Ten samples (tablets) were placed in the tester and rotated for 5 minutes, and then the degree of friability was measured as a ratio of change in weight compared to before putting the samples (tablets) into the tester.

Experimental Example 1: Material composition for manufacturing tablets that simultaneously satisfy excellent tabletting properties and tablet properties, and evaluation of properties of manufactured products accordingly

1-1. Manufacture of uncoated tablets

In general, in order to satisfy the beneficial properties in terms of ingestion and absorption in the body and advantageous properties (physical properties) during manufacture, handling, distribution, and storage, careful control is required in consideration of the action of other additives in addition to the main component. .

The present inventors tested the composition of various additives in order to identify a more suitable additive composition for providing a fingerroot extract (active ingredient). Representatively important examples are comparatively shown in Table 1 below. Use crystalline cellulose or/and maltodextrin by selecting an excipient that does not affect the evaluation of the physical properties of the main substance of the test object, such as L-arginine, Calcium carboxymethyl cellulose, and Cross-linked sodium carboxymethyl cellulose, on the tablet of the fingerroot extract. I did.

Classification Raw material name Comparative example
One Comparative Example 2 Comparative Example 3 Comparative Example 4 Comparative Example 5 Comparative Example 6 Comparative example
7 Example
One Example
2 chief ingredient Fingerroot extract 30 30 30 30 30 30 30 30 30 Excipient Crystalline cellulose 45 35 20 35 20 45 45 45 45 Excipient Maltodextrin 24 19 19 19 19 19 9 19 14 Lubricant Magnesium stearate One One One One One One One One One Disintegrant L-Arginine - 15 30 - - - - - - Disintegrant L-arginine hydrolyzed product - - - 15 30 - - - - Disintegrant Calcium carboxymethyl cellulose - - - - - 5 15 - - Disintegrant Cross-linked sodium carboxymethyl cellulose - - - - - - - 5 10 Disintegrant: Fingerroot extract
Weight ratio - 1:2 1:1 1:2 1:1 1:6 1:2 1:6 1:3 Sum 100 100 100 100 100 100 100 100 100

* In the table above, the unit of each value is% w/w (except for ratio display)

In Table 1, the hydrolyzed L-arginine (corresponding to Comparative Examples 4 and 5) refers to a raw material dried after adding 12% (w/w) of purified water to the L-arginine raw material and mixing.

1-2. Evaluation of tabletting and tableting properties

The tabletting properties, hardness, and disintegration test results for the tablet preparations are shown in Table 2 below, and the results of the aging change test are shown in Table 3 below.

division Comparative example
One Comparative example
2 Comparative example
3 Comparative example
4 Comparative example
5 Comparative Example 6 Comparative example
7 Example
One Example
2 Tabletting Good Good Good Good Good Good Good Good Good Hardness
(kg/cm ² ) 17-18 17-19 18-20 19~21 19~21 21~22 21~22 19-20 18-20 Disintegration time 60 minutes
More than 60 minutes
More than 60 minutes
More than 60 minutes 46 minutes 60 minutes
More than 55 minutes 29 minutes 23 minutes

Day 1 Day 7 Day 14 Day 30 Day 60 Day 120 Comparative Example 1 - - - - - - Comparative Example 2 - - - - - - Comparative Example 3 - - Tablet splitting Tablet burst Tablet burst Tablet burst Comparative Example 4 - - - - - Tablet splitting Comparative Example 5 - Tablet splitting Tablet burst Tablet burst Tablet burst Tablet burst Comparative Example 6 - - - - - - Comparative Example 7 - - - - - - Example 1 - - - - - - Example 2 - - - - - -

In the examples shown above (all uncoated tablets), it was possible to manufacture tablets with good levels of hardness and tabletting properties. Specifically, the detailed characteristics are as follows.

As shown in Comparative Example 1, in the case of manufacturing a tablet by adding only an excipient as a basic tablet manufacturing method, tabletting properties, hardness, etc. showed appropriate physical properties, but the disintegration time was 60 minutes or more, and the active ingredient (fingerroot Extract) was found to be unfavorable for absorption in the body.

Thus, as shown in Comparative Example 2 and Comparative Example 3, a tablet was prepared by adding L-arginine as a disintegrant. As shown in Comparative Example 2 and Comparative Example 3, there was a disintegration delay problem that still took more than 60 minutes of tablet disintegration time even after treatment with L-arginine.In particular, as the L-arginine treatment content increased, the tablet cracked and burst during storage. This occurred, and it was confirmed that the stability over time was low.

In addition, as an example in which the hydrolyzed L-arginine product was added as a disintegrant, in Comparative Examples 4 and 5, the disintegration delay problem was somewhat improved rather than tablets using the L-arginine raw material as it is (Comparative Examples 2 and 3). Although it was confirmed, it still did not meet the criteria for disintegration test (30 minutes undecided), and as the content of L-arginine hydrolyzate increased, the tablet cracking and bursting occurred during storage, and the stability over time was confirmed to be low.

When comparing Comparative Examples 2 and 4, and Comparative Examples 3 and 5, respectively, the L-arginine content is substantially the same, but disintegration depending on the processing state (e.g., hydrotreating) of the raw materials before tabletting. It was confirmed that it affects the stability over time of and tablets. However, in this context, even when considering the experimental results including Comparative Examples 2 to 5, that is, considering the raw material processing state when L-arginine is added, L-arginine simultaneously causes disintegration delay and purification stability problems. It was confirmed that it has a limit that cannot be solved.

As shown in Comparative Example 6 and Comparative Example 7, when preparing tablets by adding calcium carboxymethyl cellulose as a disintegrant, there is still a limit to solving the disintegration delay problem because the disintegration test method criteria are still not met. Confirmed that there is.

On the other hand, the present inventors confirmed that when cross-linked sodium carboxymethyl cellulose (represented as cross-linked sodium carboxymethyl cellulose, cross-linked-CMC) is added as a disintegrant, it not only satisfies the criteria of the disintegration test method, but also remarkably excellent in terms of stability over time. In particular, as compared in Examples 1 and 2, compared with the content of the disintegrant used in the other comparative examples, the cross-linked-CMC in the tablet of the present invention is included in a smaller amount, but the disintegration properties and stability over time are appropriate. The characteristics are displayed at the same time. In particular, these tablet characteristics were also found in tablets consisting only of finger root extract and cross-linked-CMC. When using a disintegrant commonly used in manufacturing other tablets, finger root extract tablets have poor aging stability, whereas finger root extract tablets have poor aging stability. In the purification of the root extract, it was specifically confirmed that cross-linked-CMC can impart excellent aging stability characteristics. In general, since the role of the excipient in tablet manufacturing is to impart the proper size and hardness of the tablet, when only the disintegrant is used alone, the size of the tablet is not properly formed, and it is difficult to show the appropriate hardness.

Not only the disintegration (and release effect), but also the stability over time of the fingerroot extract tablet is remarkably improved when provided in combination with crosslinked-CMC.It is the first to be disclosed, and in particular, a similar substance, CMC salt (i.e., the carboxymethylcellulose calcium) The material composition of the present invention proves to be an unexpected invention in that it gives a completely different level of effect by simultaneously achieving long-term stability stability, advantageous disintegration, and hardness unlike the case of using Example).

Experimental Example 2: Comparison of purification characteristics according to material composition ratio

2-1. Preparation of uncoated and coated tablets

Based on the tablet composition identified in Experimental Example 1, fingerroot extract tablets were prepared to which cross-linked sodium carboxymethyl cellulose (CMC) was added as a stabilizer and disintegrant over time. Various tablets having different compositions (uncoated tablets and coated tablets, etc.) were prepared, and representatively important examples are comparatively shown in Table 4 below.

division Raw material name Example
3 Example
4 Example
5 Example
6 Comparative Example 8 Comparative Example 9 Comparative Example 10 chief ingredient Fingerroot extract 10 30 10 30 30 60 60 Excipient Crystalline cellulose 40 40 40 40 45 25 25 Excipient Maltodextrin 44 24 43.1 23.1 23 9 8.1 Lubricant Magnesium stearate One One One One One One One Disintegrant Cross-linked sodium carboxymethyl cellulose
(Bridge-CMC) 5 5 5 5 One 5 5 Cross-linked-CMC: finger root extract weight ratio 1:2 1:6 1:2 1:6 1:30 1:12 1:12 Coating agent hydroxypropyl methylcellulose - - 0.8 0.8 - - 0.8 Coating agent ^* Mibasset - - 0.1 0.1 - - 0.1 Sum 100 100 100 100 100 100 100

` ^* Mibasset: acetylated monoglycerides

* In the table above, the unit of each value is% w/w (except for ratio display)

2-2. Evaluation of tabletting and tableting properties

The tabletting properties, hardness, friability, and disintegration test results for the tablet preparations are shown in Table 5 below, and the results of the aging change test are shown in Table 6 below.

division Example
3 Example
4 Example
5 Example
6 Comparative example
8 Comparative example
9 Comparative example
10 Tabletting Good Good Good Good Good Good Good Hardness (kg/cm ² ) 17-18 17-18 18-20 18-20 19-20 15~17 15~17 Friction degree (%) 0.077 0.094 0.081 0.092 0.131 0.134 Najeong
Disintegration time 6 minutes 27 minutes - - 52 minutes 60 minutes
More than - Coated tablet
Disintegration time - - 7 minutes 27 minutes - - 60 minutes
Excess

Day 1 Day 7 Day 14 Day 30 Day 60 Day 120 Example 3 - - - - - - Example 4 - - - - - - Example 5 - - - - - - Example 6 - - - - - - Comparative Example 8 - - - - - - Comparative Example 9 - - - - - - Comparative Example 10 - - - - - -

As a result of the comparative experiment for various examples, the tablets peculiar to the present invention are not only tabletting properties specifically when the weight ratio of finger root extract to cross-linked-CMC (ie, cross-linked-CMC: finger root extract weight ratio) is 1: 2 to 7 In addition, it was confirmed that remarkably advantageous refining properties can be achieved simultaneously with respect to hardness, friability, disintegration rate, and stability over time. Additionally, for tablets containing various amounts of finger root extract, it was confirmed that more desirable tablet characteristics were achieved when the cross-linked-CMC: finger root extract weight ratio was in the range encompassing about 1:3 to 7.

This effect of the present invention is well shown in the experimental results of the uncoated and coated tablets of Examples 3 to 6. Specifically, the tablets according to the present invention were capable of producing tablets with good hardness, friability, and tabletability (no abnormality). In addition, it was confirmed that there was no cracking or bursting of the tablet even after a long period of time, and it was found to have excellent stability over time. In addition, in particular, it was found that the disintegration rate satisfies the criteria for the disintegration test method (especially within 30 minutes of the uncoated standard). It was confirmed that such disintegration properties were not substantially affected by the presence or absence of coating of the tablet, which was well compared to the uncoated tablets of Examples 3 and 4 and the coated tablets of Examples 5 and 6. appear. In particular, the tablet characteristics of the present invention were also found in the tablet consisting of only fingerroot extract and crosslinked-CMC (each ratio condition is the same as in Table 4 and above).

Comparative Examples 8 to 10 had slightly lower hardness and slightly higher friability compared to the present invention. It was judged that this level was not an abnormality in the quality of the product. The tabletting property was also good, but unlike the present invention, the disintegration time did not meet the disintegration test method reference time at all and took a long time.

As a result, it was confirmed that the tablet made of the unique composition of the present invention is a form capable of simultaneously solving the problems of disintegration delay and tablet stability. In addition, the present invention has an advantage in terms of productivity due to excellent tablet characteristics and tabletting properties, and is easy to handle. Therefore, excellent quality can be maintained even in the distribution process.

Experimental Example 3: Preparation of tablets with high content of fingerroot extract according to the present invention and evaluation of excellence in purification

3-1. Preparation of uncoated and coated tablets

Based on the tablet composition of the present invention identified in Experimental Example 2, tablets containing a high content of fingerroot extract were produced. Various tablets (uncoated tablets and coated tablets, etc.) were prepared according to the present invention, and representatively important examples are shown in Table 7 below.

division Raw material name Example
7 Example
8 Example
9 Example
10 Example
11 Example
12 Example
13 Example
14 chief ingredient Fingerroot extract 60 70 75 80 60 70 75 80 Excipient Crystalline cellulose 20 10 5 3.1 20 10 5 3.1 Excipient Maltodextrin 8.1 8.1 3.1 - 8.1 8.1 3.1 - Lubricant Magnesium stearate One One One One One One One One Disintegrant Cross-linked sodium carboxymethyl cellulose 10 10 15 15 10 10 15 15 Cross-linked-CMC: finger root extract weight ratio 1:6 1:7 1:5 1:5.33 1:6 1:7 1:5 1:5.33 Coating agent hydroxypropyl methylcellulose 0.8 0.8 0.8 0.8 Coating agent ^* Mibasset 0.1 0.1 0.1 0.1 Sum 99.1 99.1 99.1 99.1 100 100 100 100

* In the table above, the unit of each value is% w/w (except for ratio display)

3-2. Evaluation of tabletting and tableting properties

The tabletting properties, hardness, friability, and disintegration test results for the tablet preparations are shown in Table 8 below, and the results of the change with time are shown in Table 9 below.

division Example 7/
Example 11 Example 8/
Example 12 Example 9/
Example 13 Example 10/
Example 14 Tabletting Good Good Good Good Hardness (kg/cm ² ) 15 to 17 14 to 17 14 to 16 13 to 15 Friction degree (%) 0.135 0.141 0.140 0.142 Disintegration time (najeong) 32 minutes 35 minutes 25 minutes 29 minutes Disintegration time (coated tablet) 34 minutes 36 minutes 25 minutes 31 minutes

Day 1 Day 7 Day 14 Day 30 Day 60 Day 120 Example 7 - - - - - - Example 8 - - - - - - Example 9 - - - - - - Example 10 - - - - - - Example 11 - - - - - - Example 12 - - - - - - Example 13 - - - - - - Example 14 - - - - - -

The characteristics of the high content of the fingerroot extract tablets according to the present invention are typically shown in the above tables. As shown in Examples 7 to 14, the tablets (uncoated tablets and coated tablets) according to the present invention not only have good hardness, friability, and tabletting properties (no abnormality), but also have excellent stability over time and maximize Even in this case, it was confirmed that the disintegration rate was excellent by disintegrating all in the 30 minutes (that is, less than 40 minutes).

As a result of the above experiment, when the finger root extract is contained in a high content, usually when the weight ratio of cross-linked-CMC: finger root extract is in the range of 1: 4 to 7, a previously known finger root extract (panduratin-based compound ) It was confirmed that it has better disintegration than tablets and satisfies the aging stability characteristics.

In particular, in the case of Example 9 in which the weight ratio of crosslinked-CMC: fingerroot extract was 1.5:7.5 (1:5) and Example 10 in which 1.5:8 (1:5.33) was used, in 20 minutes (i.e., 30 minutes or less) It was confirmed that the disintegration time was shortened. This is a result that the addition ratio of crosslinked-CMC is very important depending on the content of the fingerroot extract, and this result was not significantly affected on the coating of the tablet. That is, when the finger root extract is included in a high content (60% (w/w) to 80% (w/w)), the weight ratio of finger root extract to cross-linked-CMC (ie, cross-linked-CMC: finger root extract weight ratio) is 1 : In the case of 5 to 6, it was confirmed that advantageous properties such as tabletting property, hardness, friability, and stability with time were more satisfied, as well as disintegration within 30 minutes (hereinafter), enabling the production of more excellent tablets. These results were the same regardless of whether the tablet was coated or not. The effects of the present invention can be confirmed through Examples 9, 10, 13, 14, and the like. In addition, in Examples 9, 10, 13, and 14, there is a compositional characteristic that the content of the excipient is less than the content of crosslinked carboxymethyl cellulose.

In addition, as a result of testing the maximum duration of the tablet of the present invention in an additional experiment, the tablet of the present invention could be stably stored for more than 24 months.

In particular, the above-described purification characteristics of the present invention were also found in tablets consisting only of fingerroot extract and crosslinked-CMC (each ratio condition is the same as in Table 7 and above).

As described above, the present invention relates to a tablet containing a finger root extract as an active ingredient (pharmacological ingredient, main ingredient), and the unique tablet provided by the present invention contains a high content of finger root extract (panduratin-based compound). In addition, not only exhibits excellent physical properties such as appropriate disintegration, drug stability, and aging stability required by the formulation, but also excellent physical properties in terms of efficient manufacturing process/distribution such as tabletting and handling ease (physical strength related to hardness and wear rate) As a result, it has high industrial applicability.

Claims (8)

In a tablet containing fingerroot extract as an active ingredient,
The tablet contains cross-linked carboxymethylcellulose as a stability improving agent and disintegrant over time,
Cross-linked carboxymethyl cellulose: a tablet, characterized in that the weight ratio of the finger root extract is 1: 2 to 7.
delete The tablet according to claim 1, wherein the content of the fingerroot extract is 30 to 80% (w/w) based on the total weight of the tablet.
The tablet according to claim 1, wherein the tablet disintegrates within 30 minutes based on an uncoated tablet.
The tablet according to claim 1, wherein the tablet exhibits a aging stability of 24 months or more.
The method of claim 1, wherein the crosslinked carboxymethyl cellulose is
Tablets, characterized in that the cross-linked sodium carboxymethylcellulose (Cross-linked sodium carboxymethylcellulose).
The method of claim 1, wherein the tablet
A coating layer containing a hydrophilic polymer; And
Tablet, characterized in that consisting of a core (core) comprising a finger root extract and cross-linked carboxymethyl cellulose.
The tablet according to claim 7, wherein the tablet has a disintegration time of 60 minutes or less as a coated tablet.