KR20150062919A - Tablet containing panduratin and manufacturing method thereof - Google Patents

Abstract

The present invention relates to a tablet containing panduratin, which has good performance of disintegrating tablets and filling a vessel of the tablet, and a manufacturing method thereof. Specifically, in the present invention, provided is a tablet, which includes panduratin as an active ingredient and arginine used for promoting disintegration wherein the tablet containing panduratin has proper disintegration with ease of package and is accordingly easily taken with water. In addition, the tablet stability is maintained, when being packaged, stored and taken, thereby having no problems or inconvenience.

Description

BACKGROUND OF THE INVENTION 1. Field of the Invention The present invention relates to panduratin containing tablets,

The present invention relates to panduratin-containing tablets having excellent properties in disintegration of tablets, small amounts of tablets in a container, storage stability, and taking, and a method for producing the same.

Pandur Latin is a component contained in the finger root ( Boesenbergia pandurata ), a food used in Southeast Asia and Thai ginger. Panduratin has the effect of inhibiting gene expression associated with lipid synthesis. It also has an anti-obesity effect by increasing the fat oxidation and exothermic action. For example, an adult who has a body mass index (BMI) of 25 or more consumed panduratin for 12 weeks, reduced body weight by 2.2 kg, and decreased body fat by 1.15%.

Korean Registered Patent Novel Use of Panduratin Derivative or Boesenbergia panurata Extract (Patent Registration No. 10-1135132) discloses that a panduratin derivative is closely related to metabolic diseases such as body weight, body fat, and lipid content And it has been shown that it exerts excellent effects on metabolic diseases such as obesity, hyperlipidemia, hypercholesterolemia and diabetes. In addition, in Boesenbergia pandurata Attenuates Diet-Induced Obesity by Activated AMP-Activated Protein Kinase and Regulating Lipid Metabolism ( Int. J. Mol. Sci. , 13 (1), 994-1005, doi: 10.3390 / ijms13010994) high-fat diets) have been shown to be effective in relieving obesity.

However, studies on the disintegration, packaging ease, and stability required for pharmaceutical preparations such as panduratin-containing tablets are still poor.

Accordingly, a problem to be solved by the present invention is to provide panduratin containing tablets having appropriate disintegration properties, being easy to be packed, securing the stability of tablets during storage, and being easy to take with drinks.

There is a problem in that the size of the tablets is inevitably reduced in order to satisfy the daily intake standard (600 mg) of panduratin and to contain these tablets in a moderately small container.

On the other hand, panduratin does not dissolve well in a solvent (water) and a large amount of additives should be used in order to prepare tablets having desirable physical properties. However, when the size of the tablet becomes smaller, the additive such as excipient and disintegrant can not be used much, and as a result, it is difficult to secure the desirable physical properties of the tablet.

In order to achieve good disintegration even when the content of panduratin is very high, the present inventors have conducted studies using various disintegration accelerators such as starch 1500 (TM), sodium hydroxide, L-lysine hydrochloride and the like, When arginine is contained, the disintegration property is remarkably improved, and the disintegration property can be secured satisfactorily while keeping the size of the tablet small.

Accordingly, in order to solve the above problems, the present invention provides a panduratin tablet comprising panduratin as an active ingredient and arginine for promoting disintegration.

Preferably, the content of panduratin in the tablet according to the present invention is at least 50% by weight based on the total weight of the tablet, and more preferably the content of panduratin is 60-80% by weight based on the total weight of the tablet.

Further, one aspect of the present invention is based on the following technical idea. When filling the elliptical tablet having a long length with a small amount (for example, 1 to 5 tablets) in a small volume container (see FIG. 1), the tablets are placed in the cap higher than the container height, Is damaged or caught. However, if the containers containing the tablets are enlarged to a large extent, not only the manufacturing cost is increased but also the tablets are greatly shaken in the process of packaging and moving.

To solve this problem, we tried to make tablets slip during packaging. For this purpose, commonly used coating materials such as stearic acid, magnesium stearate and the like were used. In this case, the purpose of the glueing can be achieved, and the phenomenon of breakage of the tablets during packing is improved, but when the liquid composition such as the Yakult liquid is contained in the container containing the tablets, the tablets easily stick to the container again.

In the case of stearic acid, magnesium stearate, etc., since the melting point is high, it is difficult to form a relatively thin film without a completely missing part. Therefore, it is difficult to form a liquid composition or an inner moisture- But it is not limited to this theoretical mechanism.

The inventors of the present invention discovered that the various problems were simultaneously solved by coating the tablets with wax, preferably by coating the wax with a hydrophilic polymer, followed by secondary coating with wax. One aspect of the invention is based on this surprising discovery.

Based on the foregoing theoretical assumptions, it may be desirable to warm the wax above the melting point of the wax during the wax coating process so that the wax entirely surrounds the tablet, but the invention is not limited to this theoretical assumption.

Preferably, the hydrophilic polymer used in the primary coating is selected from the group consisting of polyvinyl alcohol (PVA) (e.g., OPADRY (TM)), hydroxypropylmethylcellulose (HPMC), hydroxypropylcellulose (HPC), polydextrose And sodium-carboxymethylcellulose (Na-CMC), and more preferably polyvinyl alcohol may be used. Preferably, the wax used in the secondary coating may be carnauba wax, bees wax or a mixture thereof, and more preferably carnauba wax may be used.

By coating the tablets with wax, the frictional force is reduced and the tablets naturally collapse even in small flows, so that breakage or pinching can be avoided. The wax may be used in an amount of 0.5 to 4% by weight, preferably 1 to 3% by weight based on the total weight of the composition. When the wax is less than 0.5 wt% based on the total weight of the composition, the amount of the coating is insufficient, so that the tablets adhere to the container at the time of drinking. When the wax is more than 4 wt%, the wax is coated on the surface of the tablet inappropriately. In the case of such a content, the stability of the tablet from the liquid composition contained in the same container as the tablet can be ensured during filling, storage, movement and taking.

The tablets of the present invention are packaged in 1 to 5 definite units in a packaging container. Preferably, the length of the longest side of the cross section of the tablet is longer than the height of the inside of the container containing the tablet, and the total volume of tablets or tablets contained in one container is at least 40% by volume of the internal volume of the container containing the tablet , More preferably at least 50 vol%, and even more preferably at least 60 vol%. The effect of the present invention can be further exerted if it is contained in such a container.

The present invention also relates to a method for producing a pandurant comprising: (S1) granulating panduratin and arginine powder; (S2) adding a lubricant to the granules, and then tableting to prepare tablets; And (S3) coating the tablet. The present invention also provides a method for preparing panduratin tablet. The coating step may be a primary coating using a hydrophilic polymer and a secondary coating by spinning the wax on the primary coated tablet. Preferably, during the coating of the wax, it is preferable to warm the wax to rise above the melting point.

In addition, the present invention is a small-sized container product in which tablets packed in units of 1 to 5 tablets are packed, wherein a length of the longest side of the tablets is longer than a height of the inside of the container to be packaged, and a total volume of the tablets or tablets Characterized in that the tablets are coated with wax, wherein the tablets are packed with wax in an amount of 40 vol% or more of the volume of the container inside the container. In particular, preferably, the total volume of the tablets or tablets is at least 50% by volume, more preferably at least 60% by volume based on the volume of the container inside the container, and the effect of the present invention can be further maximized. When the liquid composition is contained together, the effects of the present invention can be further exerted.

Preferably, the tablet contained in the product is a hydrophilic polymer and can be primary coated, secondary coated with wax. Preferably, the types of the hydrophilic polymer and the wax are as mentioned above.

Such a small-sized container product does not break the tablets when the coated tablets are packed into the containers, and when the tablets are drunk with the beverages in the containers, the tablets do not stick to the containers and are easy to drink.

The panduratin containing tablets of the present invention may contain one or more other ingredients selected from the group consisting of additional disintegrants, disintegration accelerators, excipients, fillers, lubricants, flavors, colorants, etc., . These components may be those commonly known in the art to which the present invention belongs.

The panduratin-containing tablets of the present invention have appropriate disintegration properties, are easy to be packed, secure storage stability, and are easy to take with drinks.

BRIEF DESCRIPTION OF THE DRAWINGS The accompanying drawings, which are incorporated in and constitute a part of the specification, illustrate exemplary embodiments of the invention and, together with the description of the invention, It should not be construed as limited.
BRIEF DESCRIPTION OF THE DRAWINGS Figure 1 is a schematic diagram showing a container in which a tablet according to the present invention is filled;

Hereinafter, embodiments of the present invention will be described in detail to facilitate understanding of the present invention. However, the embodiments according to the present invention can be modified into various other forms, and the scope of the present invention should not be construed as being limited to the following embodiments. Embodiments of the invention are provided to more fully describe the present invention to those skilled in the art.

≪ Preparation of Example 1 >

According to the following Table 1, panduratin-containing coated tablets were prepared by the tablet production method commonly used in the field of the present invention. More specifically, the raw materials on the blending ratio were weighed, and the powder was granulated using a fluidized bed granulator. The tablets were then prepared by further mixing the lubricants and then tableting. 1 tablet of panduratin was about 300mg. Then, the coating was firstly coated with polyvinyl alcohol (OPADRY (TM)), and the precoated tablet was rotated while spraying wax, followed by secondary coating.

Ingredients (% by weight) Example 1 Comparative Example 1 Comparative Example 2 Comparative Example 3 Comparative Example 4 Comparative Example 5 Comparative Example 6 Comparative Example 7 Comparative Example 8 Panduratin extract 75.00 75.00 75.00 75.00 75.00 75.00 75.00 75.00 75.00 L-arginine 20.28 - - - - - - - - Starch 1500 - 20.28 - - - - - - - Sodium hydroxide - - 20.28 - - - - - - L-lysine hydrochloride - - - 20.28 - - - - - Crystalline cellulose - - - - 20.28 - - - - Sodium citrate - - - - - 20.28 - - - Anhydrous crystalline glucose - - - - - - 20.28 - - Vitamin C - - - - - - - 20.28 - Calcium carbonate - - - - - - - - 20.28 Magnesium stearate 0.80 0.80 0.80 0.80 0.80 0.80 0.80 0.80 0.80 Polyvinyl alcohol (OPADRY ™) 2.70 2.70 2.70 2.70 2.70 2.70 2.70 2.70 2.70 Violet collar 0.22 0.22 0.22 0.22 0.22 0.22 0.22 0.22 0.22 Carnauba wax 1.00 1.00 1.00 1.00 1.00 1.00 1.00 1.00 1.00

Experimental Example 1: Evaluation of disintegrability

The disintegration rate of the tablet was measured in the following manner. The disintegration rate was measured according to the Disintegration Test in the Korean Register of Pharmacopoeia. Six test specimens were taken at 37 ° C in water, placed in a disintegration tester (JISICO®), and subjected to up-and-down movement 30 times per minute until the specimen completely disintegrated and the disintegration time was measured. The disintegration rates of Example 1 and Comparative Examples 1 to 8 are shown in Table 2 below.

Example 1 Comparative Example 1 Comparative Example 2 Comparative Example 3 Comparative Example 4 Comparative Example 5 Comparative Example 6 Comparative Example 7 Comparative Example 8 Disintegration rate (min) 40 to 55 120 or more 90-120 90-120 Does not melt Does not melt Does not melt Does not melt 90-120

The present inventors studied a variety of prescriptions to evaluate the degree of disintegration in order to improve the disintegration effect of the panduratin extract, but it was difficult to obtain satisfactory disintegration time. On the other hand, the disintegration rate of Example 1 according to the present invention was extremely good, about 40 to 55 minutes.

Experimental Example 2: Evaluation of ease of filling

Comparative Example 9, which was not secondarily coated with carnauba wax, was prepared in the same manner as in Example 1. Specific components of Example 1 and Comparative Example 9 are shown in Table 3 below.

Ingredients (% by weight) Example 1 Comparative Example 9 Panduratin extract 75.00 76.00 L-arginine 20.28 20.28 Magnesium stearate 0.80 0.80 Polyvinyl alcohol (OPADRY ™) 2.70 2.70 Violet collar 0.22 0.22 Carnauba wax 1.00 -

When the tablets of Example 1 and Comparative Example 9 were filled in a small container cap (see FIG. 1) capable of holding two tablets in each case (free fall of the filling method), the tablets were broken or stuck due to the volume characteristics of the caps The ease of charging was evaluated. Each time, 10 times were repeatedly charged, and the number of times of occurrence of breakage or pinch phenomenon of tablets was evaluated.

Example 1 Comparative Example 9 Breaking or pitting of tablets 0 times 9 times

As a result of evaluation, the tablets of Comparative Example 9 leaned or overlapped with each other, and the tablets were broken or stuck frequently due to friction when they were combined with the lid.

On the other hand, the tablet of Example 1 secondary coated with Carnauba wax did not cause any breakage or pinching due to the cap of the container due to natural friction by reducing the frictional force.

Experimental Example 3: Evaluation of ease of use

Tablets of Example 1 and Comparative Example 9 prepared with the ingredients shown in Table 3 were placed in a container (see Fig. 1) together with Yakult, and the container was tilted to about 130 ° to evaluate the ease of taking the Yakult when drinking the Yakult.

The tablets were melted and adhered to the container to evaluate whether or not the tablets adhered to the container. The tablets were evaluated for ease of use as ∘, usually Δ, and poor as X, as shown in Table 5.

Example 1 Comparative Example 9 Ease of taking ○ X

As a result of the experiment, the tablets of Comparative Example 9 were found to have difficulty in taking the moisture or the Yakult solution in the container into the tablets, causing the tablets to stick to the containers. The tablet of Comparative Example 9 was not coated sufficiently with the polyvinyl alcohol alone. On the other hand, Example 1 did not cause discomfort because the tablets did not dissolve upon administration.

Claims (14)

A panduratin tablet characterized by comprising panduratin as an active ingredient and arginine for promoting disintegration. The tablet according to claim 1, wherein the content of panduratin is at least 50% by weight based on the total weight of the tablet. The tablet according to claim 2, wherein the content of panduratin is 60-80% by weight based on the total weight of the tablet. The tablet according to claim 1, wherein the tablet is a hydrophilic polymer and is secondarily coated with a wax after the first coating. The method of claim 4, wherein the hydrophilic polymer is selected from the group consisting of polyvinyl alcohol (PVA), hydroxypropylmethylcellulose (HPMC), hydroxypropylcellulose (HPC), polydextrose, and sodium-carboxymethylcellulose -CMC). ≪ / RTI > The tablet according to claim 4, wherein the wax is carnauba wax, beeswax or a mixture thereof. The tablet according to claim 4, wherein the wax is 0.5 to 4% by weight based on the total weight of the composition. The tablet according to any one of claims 1 to 7, wherein the tablets are packaged in 1 to 5 definitive units in a packaging container. The tablet according to claim 8, wherein the longest side of the cross section of the tablet is longer than the height of the inside of the container in which the tablets are contained,
Wherein the total volume of the tablets or tablets contained in one container is at least 40% by volume of the internal volume of the container containing the tablets. The tablet according to claim 9, wherein the total volume of the tablets or tablets contained in one container is at least 60% by volume of the internal volume of the container containing the tablets. (S1) granulating panduratin and arginine powder;
(S2) adding a lubricant to the granules, and then tableting to prepare tablets; And
(S3) coating the tablet
≪ / RTI > The method of claim 11, wherein the coating step is a primary coating using a hydrophilic polymer, and a secondary coating is performed by spinning the wax while spraying the primary coated tablet. 13. The method of claim 12, wherein the wax is carnauba wax, beeswax, or a mixture thereof. Wherein the length of the longest side of the cross section of the tablet is longer than the height of the inside of the container to be packaged and the inside of the container containing the total volume of the tablets or tablets A packaged container product comprising tablets of 40 vol% or more by volume,
Characterized in that the tablet is coated with wax.

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