KR20170076200A - Tablet containing dried extract of magnolia cortex having good stability and method for preparing the same - Google Patents

Abstract

The present invention relates to: Starch and povidone, and the dried pasty extract is obtained by mixing and drying an adsorbent material in the ethyl acetate fraction of the pasty extract, and a method for producing the same.

Description

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

The present invention relates to tablets containing dried tablets having excellent stability and a process for producing the tablets.

Magnolia cortex contains Magnolia obovata Thunberg, Magnolia officinale Rehder et Wils, and Machilus thunbergii Sieb. Et Zucc, which belong to Magnoliaceae. As a perennial herb, it is said to have the efficacy of antiseptic and antidote. It is used for the treatment of oriental dryness and abdominal pain, abdominal distension, acute enteritis, seawater, etc. as dried persimmon, digestion, subterranean, and seahorse expectorant. , As soon as it is used as a pharmaceutical ingredient.

Examples of the components of the hippophae tree so far known include β-eudesmol, magnolol, honokiol, magnocurarine, tannin and the like, Magnolol and honokiol have proven to be safer and more effective than conventional antibiotics such as chlorohexidine. Various studies have been carried out on the basis of the pharmacological action of the above-described nutritional fungus, and various uses as antimicrobial agents, cancer treatment agents, tuberculosis treatment agents, fatty liver disease treatment agents, acquired immunodeficiency diseases and hair growth agents are known.

Examples of the crude extract or the crude extract are those prepared by extracting the crude extract with water or C1 to C4 lower alcohol and then concentrating under reduced pressure or using ethyl acetate or the like, And a viscous extract having a high stickiness. Since it is adhered to a mechanism during weighing and manufacturing, it is difficult to produce an accurate amount, and a lot of effort is required to wash the adhered raw material. In the preparation process, There has been a problem in that a trouble occurs, a problem arises that the raw material comes out of the substrate and the coupling occurs at the time of coating.

Korean Patent Laid-Open Publication No. 10-2014-0095169 discloses an oral solid preparation containing an adsorbent material such as a deep-fried soft-drink extract and calcium silicate, and specifically discloses a method for producing a fat-dried extract from a deep-fried soft-drink extract , There is no consideration for a specific excipient for preparing tablets having excellent stability by adding to dried tablets.

The present invention relates to: Starch, and povidone, and the pasty dry extract is obtained by mixing and drying an adsorbent material in the ethyl acetate fraction of the pasty extract.

However, the technical problem to be solved by the present invention is not limited to the above-mentioned problems, and other matters not mentioned can be clearly understood by those skilled in the art from the following description.

The present invention relates to: Starch, and povidone, wherein the dried pasty extract is obtained by mixing and drying an adsorbent material in the ethyl acetate fraction of the pasty extract.

The weight ratio of the dried starch extract, starch and povidone may be 1: 1: 0.1 to 1: 2: 0.4.

Crospovidone, and a second adsorbent material.

The weight ratio of the dried extract, starch, povidone, crospovidone and the second adsorbent may be 1: 1: 0.1: 0.05: 0.01 to 1: 2: 0.4: 0.4: 0.05.

The tablet may be formulated at a hardness of 5 kP or more.

As a result of the disintegration test through a disintegration tester which is 29 to 32 reciprocal reciprocations per minute of purified water at 37 ± 2 ° C, when the tablets are 1000 mg or less, the tablets may be disintegrated within 1 hour.

In one embodiment of the present invention, there is provided a method for producing a dried extract of a dried beef cattle, comprising the steps of: (a) mixing an adsorbent material with an ethyl acetate fraction of a beef extract, The present invention also provides a method for producing a dried tablets containing the dried tablets, comprising the steps of: (a) mixing the dried tablets, starch, povidone and a solvent; and (b)

(c) further comprising the step of subjecting the pasta-dried extract mixture to a pressure of 1 t / cm 2 or more.

The tableting can be performed at a speed of 10 rpm to 100 rpm through a rotary tablet machine.

In the step (b), the crospovidone and the second adsorbent may be further mixed.

In the step (b), the solvent may be water or a mixed solvent containing C1 to C4 lower alcohol.

The weight ratio of the water and the C1 to C4 lower alcohols may be from 1: 1 to 3: 7.

The present invention relates to: The present invention relates to a tablet containing starch and povidone and a process for producing the starch and povidone, and a method for producing the starch and povidone. The starch and povidone are used together as an excipient, Excellent in disintegration and is useful as an oral tablet.

The inventors of the present invention conducted studies on specific excipients, disintegrants, and solvents that can be added to the dried extract to confirm that tablets having excellent stability can be prepared by using starch and povidone together as an excipient. Respectively.

Hereinafter, the present invention will be described in detail.

Superior stability Dry X  Containing tablets

The present invention relates to: Starch, and povidone, wherein the dried pasty extract is obtained by mixing and drying an adsorbent material in the ethyl acetate fraction of the pasty extract.

First, the tablets containing the dried tablets according to the present invention contain dried tablets, which are obtained by mixing and drying the adsorbed substances in the ethyl acetate fraction of the tablets extract.

The dried pasty product may have a solids content of 95% by weight or more.

The ethylacetate fraction of the crude extract is also referred to as the crude extract.

The term "soft extract" in the present invention refers to a preparation which is an extract of a herbal medicine or is made into a state like starch syrup by concentration of an extract solution. When concentrated, the composition is very viscous. .

The after-treatment soft drink extract is preferably an ethylacetate fraction which is extracted with water, C1-C4 lower alcohol or a mixture thereof, and then extracted with ethyl acetate, but is not limited thereto. More preferably, the lower alcohol used for the extraction of the pasta is ethanol or methanol, and most preferably ethanol. It is preferable to perform extraction by adding water, alcohol or a mixture thereof twice to 20 times the weight of the final product after finishing the extraction of the dried product, more preferably 3 to 10 times of the extraction, It does not. The extraction temperature is preferably 30 ° C to 100 ° C, more preferably 60 ° C to 100 ° C, but is not limited thereto. The extraction time is preferably 1 hour to 10 hours, more preferably 2 hours to 5 hours, but is not limited thereto. The extraction method may be a cold extraction, an ultrasonic extraction, or a reflux cooling extraction method, and it is preferable to use a reflux cooling extraction method, but not limited thereto. The number of times of extraction is preferably one to five times, more preferably four times, but is not limited thereto.

The ethyl acetate fraction of the L. elm extract has a very sticky property instead of conventional conformation, unlike the conventional L. extract, and thus, there is a problem that frequent tableting troubles occur in the process of tableting the tablet.

The adsorbent material may be at least one selected from the group consisting of calcium silicate, silicon dioxide, kaolin, aluminum oxide, aluminum hydroxide, aluminum phosphate, ataflite, bentonite, aluminum silicate, magnesium and saponite, It is preferably a silica adsorbing material such as silicon dioxide, more preferably calcium silicate, but is not limited thereto. In the case where calcium silicate is used as the adsorbent, it is possible to improve the tableting ability and to prevent the raw material from coming out even with a low content, and the organic solvent removal effect is also excellent. On the other hand, a cellulose adsorbing material such as microcrystalline cellulose or a saccharide such as lactose or dextrin has a significantly larger amount than calcium silicate or silicon dioxide in order to improve the tableting ability at a level similar to that of calcium silicate or silicon dioxide, There is a problem in that it is necessary to use the above.

The adsorbent material may be contained in an amount of 10 parts by weight to 100 parts by weight with respect to 100 parts by weight of the crude soft drink extract.

Next, the tablets containing the dried tablets according to the present invention contain starch and povidone as specific excipients.

The starch is preferably an excipient, but is not limited thereto, as an excipient serving as a filler. At this time, pregelatinized starch refers to starch which is prepared by heating starch with water and then rapidly dehydrating and drying the starch.

The starch may be 100 to 200 parts by weight based on 100 parts by weight of the dried extract.

Compared to microcrystalline cellulose, lactose hydrate, lactose, mannitol, Kollidon VA64, dicalcium phosphate anhydrous (DCPA) and DCPD (dicalcium phosphate dihydrate) which are commonly used excipients, the starch, It is preferred as an excipient for dry X-rays.

Also, the povidone is also referred to as polyvinylpyrrolidone, and is an excipient serving as a binder. The povidone may be 10 to 40 parts by weight based on 100 parts by weight of the dried extract. At this time, when the content of povidone is too small, there is a problem that sticking trouble such as sticking and picking occurs, and when the content of povidone is too large, disintegration property is deteriorated.

Compared to hydroxypropylcellulose, which is a commonly used excipient, povidone is preferred as an excipient for pasta-dried extracts.

That is, the weight ratio of the dried egg yolk, starch and povidone may be 1: 1: 0.1 to 1: 2: 0.4.

Next, the tablets containing the dried tablets according to the present invention may further comprise crospovidone and a second adsorbent material.

The crospovidone refers to cross-linked polyvinylpyrrolidone, which serves as a disintegrant to promote the rate of disintegration.

The crospovidone may be 5 to 40 parts by weight based on 100 parts by weight of the dried powder. At this time, when the content of crospovidone is too small, there is a problem that the disintegration property is somewhat lowered, and when the content of crospovidone is too large, the hardness is lowered.

Compared to the commonly used disintegrants, croscarmellose sodium, starch glycolate sodium, and low-substituted hydroxypropylcellulose, the crospovidone is particularly preferred as a disintegrating agent in the dried extract.

In addition, the second adsorbent material may be added to prevent stickiness, and may be the same as or different from the adsorbent material used in the preparation of the post-dried extract. The specific type of the second adsorbent material is as described above in the description section of the adsorbent material.

That is, the weight ratio of the dried egg yolk, starch, povidone, crospovidone, and the second adsorbent may be 1: 1: 0.1: 0.05: 0.01 to 1: 2: 0.4: 0.4: 0.05.

The tablets containing the dried tablets according to the present invention may be manufactured in various shapes and are preferably tablets for oral use, but are not limited thereto.

The tablet may contain other additives such as a carrier, a diluent, a lubricant, a stabilizer, an antioxidant, a flavoring agent, an antiseptic, a fragrance, a sweetener, a colorant, a pH adjuster and a viscosity adjuster in addition to the excipient, disintegrant, . ≪ / RTI > The above-mentioned other additives may be a substance which is usually used pharmacologically to such an extent as not to adversely affect the efficacy of the drug, and it is preferable to add the drug in the usual amount normally used for the preparation.

The tablets have superior surface properties and hardness, while exhibiting excellent stability, and excellent disintegrability, while suppressing tableting difficulties such as sticking.

Specifically, the tablet may be formulated at a hardness of 5 kP or more, preferably at a hardness of 10 kP or more, but is not limited thereto.

When the disintegration test is conducted through a disintegration tester which is 29 to 32 times per minute reciprocating the purified water at 37 ± 2 ° C. as a result of a disintegration test based on the disintegration test standard of the Korean Pharmacopoeia 11 Revision, It can be disintegrated.

Superior stability Dry X  Of producing purified tablets containing

The present invention also provides a method for preparing a dried extract, comprising the steps of: (a) mixing an adsorbent material with an ethyl acetate fraction of an extract of the extract, and drying the extract; The present invention also provides a method for producing a dried tablets containing the dried tablets, comprising the steps of: (a) mixing the dried tablets, starch, povidone and a solvent; and (b)

First, the method for preparing the dried tablets containing the dried tablets according to the present invention comprises a step (step (a)) of mixing the dried tablets with an adsorbent and drying the dried tablets to obtain the dried tablets.

The details of the dried pasta are as described above.

Next, the method for preparing the tablets containing the dried tablets according to the present invention comprises the step (b) of preparing the dried tablets mixture by mixing the dried tablets, starch, povidone and the solvent.

The specific contents of the starch and povidone are as described above.

The solvent is preferably a mixed solvent comprising water and a C1 to C4 lower alcohol. Specifically, the weight ratio of the water to the C1 to C4 lower alcohol is More preferably from 1: 1 to 3: 7, but is not limited thereto. At this time, if the content of the C1 to C4 lower alcohol is too small, there is a problem that the tableting disorder occurs, and when the content of the C1 to C4 lower alcohol is too large, the disintegration property is deteriorated.

At this time, the crospovidone and the second adsorbent can be further mixed, and the specific contents of the crospovidone and the second adsorbent are as described above.

Next, the method for producing the tablets containing the dried tablets according to the present invention may further comprise the step of (c) calibrating the dried tablets mixture under a pressure of 1 t / cm 2 or more. The tableting is preferably performed at a speed of 10 rpm to 100 rpm through a rotary tablet press, but is not limited thereto.

Accordingly, the present invention relates to a composition comprising: The present invention relates to a tablet containing starch and povidone and a method for producing the starch and povidone. The starch and povidone are used together as an excipient to provide excellent surface properties and hardness, And is excellent in disintegration and is useful as an oral tablet.

Hereinafter, preferred embodiments of the present invention will be described in order to facilitate understanding of the present invention. However, the following examples are provided only for the purpose of easier understanding of the present invention, and the present invention is not limited by the following examples.

[ Example ]

Production Example 1 : Nutmeg Manufacture of dry extracts

8 kg of ethanol was added to 1 kg of dried skins purchased from Kyungdong market and reflux cooled for 3 hours at 80 ℃. The reflux-cooled extract was filtered using a filter paper (Advantec no. 2 filter paper), and the filtrate was concentrated under reduced pressure using an evaporator (EYELA, N-1000, Japan) and dried to prepare a crude ethanol extract.

The crude ethanol extract was dispersed in water, and the residue was partitioned with ethyl acetate. Ethyl acetate fractions were concentrated under reduced pressure to give the fractions of ethyl acetate as fractions.

25 g of calcium silicate (Tomita Pharma, FLORITE R) was mixed, and the mixture was assembled using a 20-mesh net, dried at 60 ° C for 15 hours, The granules were prepared by passing through a net, which was then used as a dried X-ray powder.

Manufacturing example  2: excipient ( 1) of  Comparison by type

40 parts by weight of crude extract of Preparation Example 1, pre-gelatinized starch, microcrystalline cellulose, lactose hydrate, anhydrous lactose, mannitol, kollidon VA64, dicalcium phosphate anhydrous (DCPA) and dicalcium phosphate dihydrate ) And 20 parts by weight of purified water were mixed and dried at 60 DEG C for 6 hours, followed by one-time tumbling to prepare tablets. At this time, the surface properties of the tablets were observed, and the single-screw fixation resulted in the observation of the fixation disorder.

Production Example 2-1 compare
Production Example 2-1 compare
Production example 2-2 compare
Production Example 2-3 compare
Production example 2-4 compare
Production example 2-5 compare
Production Example 2-6 compare
Production example 2-7 Skins
Dry X 40 40 40 40 40 40 40 40 Pregelatinized starch 40 Microcrystalline cellulose 40 Lactose baggage 40 Anhydrous lactose 40 Mannitol 40 Co-povidone 40 DCPA 40 DCPD 40 Purified water 20 20 20 20 20 20 20 20 Surface property Great Poor Poor Poor Poor Poor Poor Poor One-shot results usually Poor Poor Poor Poor Poor Poor Poor

As shown in Table 1, in Comparative Preparations 2-1 to 2-7, the surface of the tablets was covered with the supernatant X-rays and the surface thereof was sticky, The surface of the tablets showed a dry appearance.

Sticking occurred in all of Production Example 1 and Comparative Production Examples 2-1 to 2-7, but sticking was observed compared to Comparative Production Examples 2-1 to 2-7 in Production Example 2-1 It was confirmed that there was a remarkably small occurrence.

In other words, it was confirmed that the pregelatinized starch is more suitable as the excipient (1) of the dried extract than the microcrystalline cellulose, the lactose hydrate, the anhydrous lactose, the mannitol and the copovidone.

Manufacturing example  3: excipient ( 2) of  Comparison by type

40 parts by weight of the crude extract of Preparation Example 1, 40 parts by weight of the excipient (2) of either povidone or hydroxypropylcellulose and 20 parts by weight of purified water were mixed and dried at 60 DEG C for 6 hours, . At this time, the surface properties of the tablets were observed, and the single-screw fixation resulted in the observation of the fixation disorder.

Production example 3-1 Comparative Production Example 3-1 Dried gruel 40 40 Povidone 40 Hydroxypropylcellulose 40 Purified water 20 20 Surface property Very good Poor One-shot results Great Poor

As shown in Table 2, it was confirmed that the surface of Preparative Example 3-1 showed a completely dry state, and as a result, it was confirmed that the discomfort such as sticking was substantially suppressed.

In other words, it was confirmed that povidone is more suitable as an excipient (2) for the dried extract than hydroxypropylcellulose.

Example  1: Comparison according to weight ratio of excipient (1) and excipient (2)

40 parts by weight of crude extract of Preparation Example 1, 50 to 56 parts by weight of pregelatinized starch, 3 to 9 parts by weight of povidone K30, 1 part by weight of magnesium stearate and 30 parts by weight of purified water were mixed and dried at 60 DEG C for 6 hours, A punch was attached to a rotary tablet machine (PKT-13), and tablets (1,000 T or more) were prepared by pressing at a speed of 40 rpm under a pressure of 1 t / cm 2. At this time, the tableting disability was observed and the disintegration rate was measured by measuring the disintegration time based on the disintegration test method of the Korean Pharmacopoeia 11th revision.

Example 1-1 Examples 1-2 Example
1-3 Examples 1-4 Examples 1-5 Examples 1-6 Examples 1-7 Dried gruel 40 40 40 40 40 40 40 Pregelatinized starch 56 55 54 53 52 51 50 Povidone 3 4 5 6 7 8 9 Stearic acid
magnesium One One One One One One One Purified water 30 30 30 30 30 30 30 Tableting result
(Over 1,000T) Sticking occurs Picking
Occur Great Great Great Great Great Disintegration time 5 minutes 10 minutes 30 minutes 40 minutes More than 1 hour More than 1 hour More than 1 hour

As shown in Table 3, it was observed that when the povidone content was more than 5 parts by weight, the tableting discomfort was suppressed with respect to 40 parts by weight of the dried powdery extract. However, when the povidone content was 7 parts by weight or more, It was confirmed that the degradation of the sea water was deteriorated.

Example  2: Disintegrant  Comparison by type

40 parts by weight of the crude extract of Preparation Example 1, 43 to 53 parts by weight of pregelatinized starch, 6 parts by weight of povidone K30, crospovidone, croscarmellose sodium, sodium starch glycolate and hydroxypropylcellulose having a degree of substitution 5 parts by weight of the release agent, 1 part by weight of magnesium stearate and 30 parts by weight of purified water as a solvent were mixed and dried at 60 DEG C for 6 hours. Then, the punch was attached to a rotary tablet machine (PKT-13) (1,000 T or more). At this time, the tableting disability was observed and the disintegration rate was measured by measuring the disintegration time based on the disintegration test method of the Korean Pharmacopoeia 11th revision.

Example 2-1 Example 2-2 Example
2-3 Examples 2-4 Example 2-5 Examples 2-6 Example
2-7 Examples 2-8 Skins
Dry X 40 40 40 40 40 40 40 40 Pregelatinized starch 53 48 48 48 48 50 49 43 Povidone 6 6 6 6 6 6 6 6 Crospovidone 5 3 4 10 cross
Camelos
salt 5 Starch glycolate sodium 5 Low substitution degree
Hydroxy
Propyl cellulose 5 Stearic acid
magnesium One One One One One One One One Purified water 30 30 30 30 30 30 30 30 Disintegration time 40 minutes 10 minutes
Within 40 minutes 50 minutes 40 minutes 30 minutes 10 minutes 10 minutes
Within

As shown in Table 4, when povidone is contained as a disintegrant as in Example 2-2, Example 2-6, Example 2-7, and Example 2-8, disintegration is excellent by shortening disintegration time .

In other words, it was confirmed that crospovidone is preferable to disintegration of dried cucumber extracts, compared with sodium croscarmellose, sodium starch glycolate and low-substituted hydroxypropylcellulose.

Example  3: Comparison according to solvent

40 parts by weight of crude extract of Preparation Example 1, 48 parts by weight of pregelatinized starch, 6 parts by weight of povidone K30, 5 parts by weight of crospovidone, 1 part by weight of magnesium stearate and 0 to 30 parts by weight of purified water and 0 to 30 parts by weight of ethanol The mixed solvent was mixed and dried at 60 DEG C for 6 hours. Then, punches were attached to a rotary tablet machine (PKT-13), and tablets (10,000 T or more) were prepared by pressing at a speed of 40 rpm under a pressure of 1 t / cm 2. At this time, the tableting disability was observed and the disintegration rate was measured by measuring the disintegration time based on the disintegration test method of the Korean Pharmacopoeia 11th revision.

Example 3-1 Example 3-2 Example
3-3 Example 3-4 Example 3-5 Examples 3-6 Examples 3-7 Dried gruel 40 40 40 40 40 40 40 Pregelatinized starch 48 48 48 48 48 48 48 Povidone 6 6 6 6 6 6 6 Crospovidone 5 5 5 5 5 5 5 Stearic acid
magnesium One One One One One One One Purified water 30 21 18 15 12 9 0 ethanol 0 9 12 15 18 21 30 Tableting result
(10,000T or more) Picking occurs Picking
Occur Picking
Occur Great Great Great Great Disintegration time 10 minutes
Within 10 minutes
Within 10 minutes
Within 10 minutes
Within 10 minutes
Within 20 minutes 40 minutes

As shown in Table 5, it was observed that when the content of ethanol in the mixed solvent was 50% by weight or more, the tableting disability was suppressed, but when the content of ethanol in the mixed solvent was 70% by weight or more, there was.

Example  4: Comparison according to the content of the second adsorbent material

40 parts by weight of dried powdery extract of Preparation Example 1, 0 to 5 parts by weight of calcium silicate (Tomita Pharma, FLORITE R), 48 to 43 parts by weight of pregelatinized starch, 6 parts by weight of povidone K30, 5 parts by weight of crospovidone, 1 part by weight, purified water in an amount of 12 parts by weight and ethanol in an amount of 18 parts by weight were mixed and dried at 60 DEG C for 6 hours, and then punches were attached to a rotary tablet machine (PKT-13) Tablets (30,000 T or more) were prepared by tabletting. At this time, the tablet hardness was measured as a result of tableting, and storage was carried out for one week at a temperature of 40 ° C and a humidity of 75% to confirm the occurrence of stickiness.

Example 4-1 Example 4-2 Example 4-3 Example 4-4 Example 4-5 Dried gruel 40 40 40 40 40 Calcium silicate 0 One 2 3 5 Pregelatinized starch 48 47 46 45 43 Povidone 6 6 6 6 6 Crospovidone 5 5 5 5 5 Magnesium stearate One One One One One Purified water 12 12 12 12 12 ethanol 18 18 18 18 18 Purification hardness 12kp 12kp 10kp 8kp 5kp Stickiness occurs Occur Not occurring Not occurring Not occurring Not occurring

As shown in Table 6, when the content of calcium silicate was more than 1 part by weight, it was confirmed that no stickiness occurred in 40 parts by weight of the dried powdery extract, but it was confirmed that when the calcium silicate content was too large, the tablet hardness was lowered I could.

Particularly, in Example 4-2, the surface properties of tablets were observed over 3 months, and the tableting disability was observed. The disintegration time was measured by measuring the disintegration time on the basis of the Disintegration Test Method of the Korean Pharmacopoeia 11 . Further, the tablet hardness was measured as a result of tableting, and occurrence of stickiness was confirmed at a temperature of 40 캜 and a humidity of 75%.

Early 1 month 3 months Surface property Great No change No change Heart failure Great - - Disintegration time Within 10 minutes Within 10 minutes Within 10 minutes Purification hardness 12kp 12kp 12kp Stickiness occurs Not occurring Not occurring Not occurring

As shown in Table 7, in the case of Example 4-2, tablets having an excellent surface property of tablets and being able to inhibit tableting disorders, excellent disintegrability and hardness, had no stickiness and were stable for a long time .

Comparative Example  One

40 parts by weight of the crude extract of Preparation Example 1, 40 parts by weight of at least one of pregelatinized starch, microcrystalline cellulose, lactose hydrate, anhydrous lactose, mannitol, Kollidon VA64, DCPA (dicalcium phosphate anhydrous) and DCPD (dicalcium phosphate dihydrate) 57 parts by weight of the excipient (1) and 3 parts by weight of magnesium stearate were mixed, punches were attached to a rotary tablet machine (PKT-13) and tableted (1,000 T or more) by pressing at a speed of 40 rpm under a pressure of 1 t / . At this time, we observed the impaired tableting result.

Comparative Example 1-1 Comparative Example 1-2 Comparative Example 1-3 Comparative Example 1-4 Comparative Example 1-5 Comparative Example 1-6 Comparative Example 1-7 Comparative Example 1-8 Comparative Example 1-9 Dried gruel 40 40 40 40 40 40 40 40 40 Pregelatinized starch 57 Pending
cellulose 22 57 Lactose baggage 35 57 Anhydrous lactose 57 Mannitol 57 Co-povidone 57 DCPA 57 DCPD 57 Stearic acid
magnesium 3 3 3 3 3 3 3 3 3 Tableting result Sticking
Occur Sticking
Occur Sticking
Occur Sticking
Occur Sticking
Occur Sticking
Occur Sticking
Occur Sticking
Occur Sticking
Occur

That is, in the case of Comparative Examples 1-1 to 1-9 in which no solvent was used, it was confirmed that sticking occurred and a tableting trouble occurred.

Comparative Example  2

40 parts by weight of crude extract of Preparation Example 1, 37 to 52 parts by weight of microcrystalline cellulose, 5 to 20 parts by weight of a second adsorbent of at least one of calcium silicate, silicon dioxide and talc, and 3 parts by weight of magnesium stearate were mixed, A punch was attached to a rotary tablet machine (PKT-13), and tablets (1,000 T or more) were prepared by pressing at a speed of 40 rpm under a pressure of 1 t / cm 2. At this time, we observed the impaired tableting result.

Comparative Example 2-1 Comparative Example 2-2 Comparative Example 2-3 Comparative Example 2-4 Comparative Example 2-5 Dried gruel 40 40 40 40 40 Microcrystalline cellulose 52 47 47 47 37 Calcium silicate 5 10 Silicon dioxide 5 Talc 10 20 Magnesium stearate 3 3 3 3 3 Tableting result Sticking
Occur Sticking
Occur Sticking
Occur Sticking
Occur Sticking
Occur

That is, in the case of Comparative Examples 2-1 to 2-5 in which no solvent was used, it was confirmed that even if the second adsorbing material was included, sticking occurred and a tableting trouble occurred.

Comparative Example  3

40 parts by weight of crude extract of Preparation Example 1, 24 parts by weight of microcrystalline cellulose, 20 to 35 parts by weight of lactose hydrate, 0 to 10 parts by weight of calcium silicate, 1 part by weight of magnesium stearate and 30 parts by weight of purified water, After drying for a period of time, punches were attached to a rotary tablet machine (PKT-13), and tablets (1,000 T or more) were prepared by pressing at a speed of 40 rpm under a pressure of 1 t / cm 2. In this case,

Comparative Example 3-1 Comparative Example 3-2 Comparative Example 3-3 Dried gruel 40 40 40 Microcrystalline cellulose 24 24 24 Lactose baggage 35 30 20 Calcium silicate 0 5 10 Magnesium stearate One One One Purified water 30 30 30 Tableting result Sticking occurs Sticking occurs No puncture

In the case of Comparative Example 3-1 and Comparative Example 3-2, a solvent was used, but starch and povidone were not used together as an excipient. On the other hand, in the case of Comparative Example 3-3, it was confirmed that the tableting itself was impossible due to the excessive amount of the second adsorbent material.

It will be understood by those skilled in the art that the foregoing description of the present invention is for illustrative purposes only and that those of ordinary skill in the art can readily understand that various changes and modifications may be made without departing from the spirit or essential characteristics of the present invention. will be. It is therefore to be understood that the above-described embodiments are illustrative in all aspects and not restrictive.

Claims (12)

Xylose drying x; Starch and povidone,
The dried eggplant extract was prepared by mixing and drying an adsorbent material in an ethyl acetate fraction of a dried eggplant extract
Highly stable dried X-containing tablets.
The method according to claim 1,
The weight ratio of the dried starch, starch and povidone is 1: 1: 0.1 to 1: 2: 0.4
Highly stable dried X-containing tablets.
The method according to claim 1,
Further comprising crospovidone and a second adsorbent material
Highly stable dried X-containing tablets.
The method of claim 3,
The weight ratio of the dried powder of starch, starch, povidone, crospovidone and the second adsorbent material is 1: 1: 0.1: 0.05: 0.01 to 1: 2: 0.4: 0.4: 0.05
Highly stable dried X-containing tablets.
The method according to claim 1,
The tablets were prepared with a hardness of 5 kP or more
Highly stable dried X-containing tablets.
The method according to claim 1,
As a result of a disintegration test through a disintegration tester which is 29 to 32 reciprocal reciprocations per minute in purified water of 37 ± 2 ° C, when the tablets are 1000 mg or less, the tablets are disintegrated within 1 hour
Highly stable dried X-containing tablets.
(a) mixing an adsorbent material with the ethyl acetate fraction of the crude extract to produce a dried extract of the pasty; And
(b) mixing the dried pasty extract, starch, povidone and a solvent to prepare a dried pasty mixture;
A method for producing a tablets containing an X-ray dry extract excellent in stability.
8. The method of claim 7,
(c) further comprising the step of subjecting the dried pasty extract mixture to a pressure of 1 t / cm 2 or more
A method for producing a tablets containing an X-ray dry extract excellent in stability.
9. The method of claim 8,
The tableting is performed at a speed of 10 rpm to 100 rpm through a rotary tablet machine
A method for producing a tablets containing an X-ray dry extract excellent in stability.
8. The method of claim 7,
In step (b), crospovidone and the second adsorbent are further mixed
A method for producing a tablets containing an X-ray dry extract excellent in stability.
8. The method of claim 7,
In the step (b), the solvent is a mixed solvent comprising water and a C1 to C4 lower alcohol
A method for producing a tablets containing an X-ray dry extract excellent in stability.
12. The method of claim 11,
The weight ratio of the water and the C1 to C4 lower alcohols is from 1: 1 to 3: 7
A method for producing a tablets containing an X-ray dry extract excellent in stability.