KR20200077143A - Fast disintegrating tablets comprising oriental herbal extracts, and manufacturing method thereof - Google Patents

Abstract

The present invention relates to a fast disintegrating tablet composition containing an herb medicine extract as an active component, and a manufacturing method thereof. A fast disintegrating tablet containing a fast disintegrating tablet-induced disintegrating agent manufactured by using a vacuum dryer of the present invention has a simple manufacturing method, has excellent disintegration and solubility to be rapidly disintegrated, and also can improve compliance and convenience of taking a drug, thereby being able to be usefully used for patients, children, and the elderly who have insufficient deglutition ability.

Description

Fast disintegrating tablets comprising oriental herbal extracts, and manufacturing method thereof

The present invention relates to a fast-dissolving tablet composition, and more particularly, to a fast-dissolving tablet composition comprising a herbal extract as an active ingredient and a method for manufacturing the same.

Patients taking large amounts of medication, especially those with insufficient swallowing ability, have difficulty swallowing medication. In the case of taking the suspension, there is a problem in that the remaining amount is generated in the container (cup or pouch) or the remaining amount is consumed with water, and the accuracy of the dose is deteriorated. In other words, tablets and capsules, which generally account for the majority of oral preparations, are not easy to take in the elderly or children who have difficulty swallowing the drug, and other powders and granules are likely to remain in the oral cavity after dosing and cause discomfort, and the correct dosage Dosing is difficult.

Accordingly, it is necessary to develop a new dosage form to increase the compliance and convenience of drug administration, and to improve an accurate dosage, and studies on fast disintegrating tablets have been actively conducted to solve the above problems. In the case of fast disintegrating tablets in the oral cavity, it quickly disintegrates in the mouth to quickly develop medicinal effects and has the advantage of being easy to take when carrying, and fast disintegrating tablets disintegrate rapidly in the stomach and are absorbed through the gastric mucosa to maximize the therapeutic effect. .

In general, tablets disintegrate, disperse and dissolve in the stomach and are absorbed through the gastrointestinal mucosa, while oral disintegrating tablets disintegrate in the oral cavity during oral administration and are swallowed with saliva and then absorbed through the oral and gastrointestinal mucosa. These oral disintegrating tablets usually disintegrate within 40 seconds in the mouth without water and are convenient to take, which may be helpful for children, the elderly, and patients who have difficulty swallowing drugs.

Several agents that dissolve or disintegrate in the oral cavity are known as fast disintegrating tablets. For example, Japanese Patent Laid-Open No. 62-50445 describes an aqueous solution containing gelatin together with a pharmaceutically acceptable active ingredient, and a lyophilized matrix-type fast disintegrating agent. However, the manufacturing method according to the above publication is difficult to manufacture using a manufacturing facility of a conventional solid preparation, and thus the investment of the facility must be followed, and in actual production, there is a disadvantage that it takes more time than a general solid preparation.

In addition, U.S. Patent No. 3,885,026 discloses a method of preparing a porous tablet by volatilizing and heating a volatile excipient such as urea, urethane, ammonium carbonate, naphthalene, and then tableting and heating to volatilize the volatile excipient. However, there is a drawback that the excipients remaining in this tablet can cause fatal harm to the patient.

As described above, although studies on oral disintegrating tablets for the oral cavity have been actively conducted, the above problems still remain, and the manufacturing method is simply and quickly disintegrated, and it is necessary to develop a fast disintegrating tablet that improves compliance and convenience of drug use. This is true.

Republic of Korea Patent Publication No. 10-2010-0086140 (2010.07.30 published)

An object of the present invention is to provide a fast disintegrating tablet composition comprising a herbal extract as an active ingredient and a method for manufacturing the same.

In order to achieve the above object, the present invention a) 20 to 35% by weight of dry powder of herbal extracts; b) 5 to 15% by weight of a fast disintegrating inducing disintegrant; c) 2 to 10% by weight of disintegrant; d) 55 to 65% by weight of excipients; And e) 0.1 to 2% by weight of a lubricant, and the fast disintegrating-inducing disintegrant provides a fast disintegrating tablet composition characterized in that it is prepared by vacuum drying.

In addition, the present invention comprises the steps of: a) preparing a herbal medicine hot water extract followed by concentration and drying to produce a dry powder; b) preparing a first mixture by adding and mixing a fast disintegrating induction disintegrant, a disintegrant, and an excipient in the dry powder of step a); c) adding a lubricant to the first mixture of step b) and mixing to prepare a second mixture; And d) tableting the second mixture of step c).

The fast disintegrating tablet containing the fast disintegrating inducing disintegrant prepared using the vacuum dryer of the present invention has a simple manufacturing method, is excellent in disintegration and solubility, disintegrates quickly, and can improve the compliance and convenience of drug use. , It can be useful for patients, children, and the elderly who have insufficient swallowing ability.

1 is a flow chart showing the manufacturing process of the fast disintegrating tablet according to the present invention.

As used in the present invention, the term'fast disintegrating tablet' refers to a compression molded article having proper hardness that exhibits substantially sufficient disintegration and solubility in the oral cavity by saliva contained in the mouth without taking water.

The term'substantially sufficient disintegration and solubility' used in the present invention disintegrates or dissolves in the oral cavity for about 60 seconds to 120 seconds, preferably about 1 second to 60 seconds, more preferably about 1 second to 25 seconds. Means 'Suitable hardness' means sufficient hardness so that the molded product does not collapse in the manufacturing process and distribution process.

The present invention a) 20 to 35% by weight of dry powder of herbal extracts; b) 5 to 15% by weight of a fast disintegrating inducing disintegrant; c) 2 to 10% by weight of disintegrant; d) 55 to 65% by weight of excipients; And e) 0.1 to 2% by weight of a lubricant, and the fast disintegrating-inducing disintegrant provides a fast disintegrating tablet composition characterized in that it is prepared by vacuum drying.

The herbal medicines of a) above are licorice, jujube, ginseng, gold and silver, lotus, peppermint, gilkyung, damjuk leaves, hyunggae, dusi, allies, nutritious, peony, strong, windproof, poisonous, Angelica, ginseng, creation, ginger, mackmundong, sukjihwang , Omija, Cheonmun-dong, Bokryeong, Hubak, Galgeun, Banha, Sangjihwang, Jeonho, Broiler, Health, Doin, Baekchul, Hyangbuja, Gamguk, Cheongung, Taxi, Golden, Guruin, Ephedra, Malt, Baekji, Horseback Riding, Siho , Hwanggi, Kwakhyang, Rhubarb, Manhyeongja, Mangcho, Mokdanpi, Mokhyang, Sinsae, Sansa, Samneung, Gypsum, Seshin, Singok, Ahchul, Injinho, Perception, Jimo, Jisil, Jinpi, Cheonma, Cheongpi, Gardenia, Passer, Hwangnyeon and It may be any one or more selected from the group consisting of yellow-white, but is not limited thereto.

The rapid disintegration-inducing disintegrant of the b) can be prepared by dissolving Arabian gum in distilled water for 1 to 10 hours, and then vacuum drying for 8 to 15 hours under conditions of 40 to 60°C and 500 to 600 mmHg, but is not limited thereto. It is stated that it does not work.

The gum arabic and distilled water may be added in a weight ratio of 1: (8 to 15), but is not limited thereto.

The disintegrant of c) is croscarmellose sodium, sodium glycolate starch, crospovidone, gelatin, starch, carbomer, carboxymethylcellulose, copovidone, hydroxypropylcellulose, polyethylene oxide, povidone, calcium alginate and fumaric acid It may be any one or more selected from the group consisting of sodium aryl.

The excipient of d) in the group consisting of microcrystalline cellulose, xylitol, maltose, maltitol, mannitol, palatinose, erythritol, trehalose, glucose, sorbitol, maltodextrin, dextrose, lactose, oligosaccharides and rebaudioside A It may be any one or more selected.

The lubricant of e) may be any one or more selected from the group consisting of magnesium stearate, calcium stearate, zinc stearate, polyethylene glycol, glyceryl behenate, glyceryl palmitostearate, sodium lauryl sulfate, stearate and talc. Can.

It is noted that the disintegrating agent, excipient, and lubricant may be used without particular limitation as long as they are known in the art belonging to the present invention, and are not limited to the above descriptions.

The fast disintegrating tablet disintegrates within 1 to 25 seconds in the oral cavity, and is excellent in disintegration and solubility, thereby improving compliance and convenience of drug use.

In addition, the present invention comprises the steps of: a) preparing a herbal medicine hot water extract followed by concentration and drying to produce a dry powder; b) preparing a first mixture by adding and mixing a fast disintegrating induction disintegrant, a disintegrant, and an excipient in the dry powder of step a); c) adding a lubricant to the first mixture of step b) and mixing to prepare a second mixture; And d) tableting the second mixture of step c).

The herbal medicines of a) above are licorice, jujube, ginseng, gold and silver, lotus, peppermint, gilkyung, damjuk leaves, hyunggae, dusi, allies, nutritious, peony, strong, windproof, poisonous, Angelica, ginseng, creation, ginger, mackmundong, sukjihwang , Omija, Cheonmun-dong, Bokryeong, Hubak, Galgeun, Banha, Sangjihwang, Jeonho, Broiler, Health, Doin, Baekchul, Hyangbuja, Gamguk, Cheongung, Taxi, Golden, Guruin, Ephedra, Malt, Baekji, Horseback Riding, Siho , Hwanggi, Kwakhyang, Rhubarb, Manhyeongja, Mangcho, Mokdanpi, Mokhyang, Sinsae, Sansa, Samneung, Gypsum, Seshin, Singok, Ahchul, Injinho, Perception, Jimo, Jisil, Jinpi, Cheonma, Cheongpi, Gardenia, Passer, Hwangnyeon and It may be any one or more selected from the group consisting of yellow and white, but is not limited thereto.

The rapid disintegration-inducing disintegrant of the b) can be prepared by dissolving Arabian gum in distilled water for 1 to 10 hours, and then vacuum drying for 8 to 15 hours under conditions of 40 to 60°C and 500 to 600 mmHg, but is not limited thereto. It is stated that it does not work.

The fast disintegrating tablet composition of the present invention has various types of polymer materials, for example, povidone, methylcellulose, hydroxymethylcellulose, hydroxypropylmethylcellulose, hydroxy It may be specified that hydroxypropyl cellulose, hydroxyethyl cellulose, Eudragit, gelatin, luacomb, and xanthancomb may include one or more polymer materials, but is not limited thereto.

In order to prepare a solution for dissolving a polymer material for coating such a drug, a dissolving agent capable of properly dissolving the polymer material is required. As a dissolving agent, one or more dissolving agents selected from purified water, ethanol, isopropanol, methylene chloride, acetone, and methanol may be used. It may, but is not limited to.

Hereinafter, the present invention will be described in more detail through examples. These examples are only intended to illustrate the present invention more specifically, and it will be apparent to those skilled in the art that the scope of the present invention is not limited by these examples according to the gist of the present invention. .

Example 1: Preparation of powder of mixed herbal extract

In the present invention, gold and silver coins (1420 mg), kyokyo (1420 mg), peppermint (852 mg), gyeonggyeong (852 mg), licorice (852 mg), bile leaf (568 mg), hyeonggae (568 mg), and duo ( 712 mg), baebangja (712 mg) and nutrition angle (44 mg) were used, and a mixed herbal extract was prepared in the following manner.

After weighing and mixing each herbal medicine according to the manufacturing method, after adding purified water corresponding to 10 times the total weight of the herbal medicine and heating at 100° C. for 3 hours, using filter paper (Whatman No. 4, 25 μm) The filtrate was recovered. The collected filtrate was concentrated under reduced pressure for 6-7 hours with a rotary decompression concentrator (50℃, N-12, EYELA), and then spray-dried (180℃, 18,000 rpm, Sogang Engineering) and vacuum dryer (50℃, 600 mmHg, H It was dried with S-Tek to obtain a powder of mixed herbal extract (0.5 g).

Example 2: Preparation of fast disintegrating inducing disintegrant (treated arabia Gum; TAG)

1) TAG-1 production (containing 10% by weight of gum arabic)

10 g of gum arabic was weighed and added to 100 mL distilled water and dissolved at 500 rpm for 5 hours with a magnetic stirrer. The expanded gum arabic was dried under vacuum conditions at 50° C. and 600 mmHg for 12 hours, and then pulverized to be used as an induction disintegrant.

2) TAG-2 production (containing 10% by weight of gum arabic)

10 g of gum arabic was weighed and added to 100 mL distilled water, and dissolved at 500 rpm for 24 hours with a magnetic stirrer. The expanded gum arabic was widely spread on an enamel dish, followed by hot air drying at 40°C for 72 hours, followed by pulverization to be used as an induction disintegrant.

3) TAG-1 (containing 5% or 10% by weight of gum arabic) + mannitol mixture preparation

5 to 10 g of gum arabic was weighed and added to 100 mL distilled water, and dissolved at 500 rpm for 24 hours with a magnetic stirrer. The expanded gum arabic was widely spread on an enamel dish, dried at 40° C. for 72 hours and then ground. Each pulverized product was mixed with mannitol in a 1:1 weight ratio, grinded in a mortar and pestle, and then sifted through a No. 20 sieve to be used as an induction disintegrant.

Example 3 and Comparative Examples 1 to 3: Rapid disintegrating tablet preparation

As shown in Table 1 and Fig. 1, the dry powder of the mixed herbal extract prepared in Example 1, the disintegrant prepared in Example 2, and the excipients were first weighed and mixed first, and the lubricant was weighed to perform the second mixing. Then, tablets were quickly disintegrated by direct tableting.

Comparative Example 1 Comparative Example 2 Comparative Example 3 Example 3 Ingredient chief ingredient Dry powder of mixed herbal extracts 25
(weight%) 25
(weight%) 25
(weight%) 25
(weight%) Excipient Microcrystalline cellulose
(Avicel) 59.5
(weight%) 59.5
(weight%) 59.5
(weight%) 59.5
(weight%) Disintegrant Croscarmellose sodium
(Vivasol) 5
(weight%) 5
(weight%) 5
(weight%) 5
(weight%) Quickly disintegrating
Judo
Disintegrant TAG-2 (5% by weight) + mannitol 10
(weight%) TAG-2 (10% by weight) + mannitol 10
(weight%) TAG-2 (10 wt%) 10
(weight%) TAG-1 (10 wt%) 10
(weight%) Lubricant Magnesium stearate 0.5
(weight%) 0.5
(weight%) 0.5
(weight%) 0.5
(weight%) Sum 100
(weight%) 100
(weight%) 100
(weight%) 100
(weight%) Hardness 9.0 kp 9.2 kp 8.9 kp 8.9 kp Disintegration 40 seconds 30 seconds 20 seconds 20 seconds

Example 4: Analysis of the disintegration time of the fast disintegrating tablet

The fast disintegrating tablets prepared in Comparative Examples 1 to 3 and Example 3 were prepared with a hardness of about 9.0 kp so as not to affect the disintegration time, and the disintegration was analyzed by measuring the disintegration time after putting each in purified water at room temperature. .

As a result, when compared with Comparative Example 1 and Comparative Example 2, it was confirmed that the disintegration time was significantly shortened to 20 seconds in Example 3 in which TAG-1 prepared using a vacuum dryer was rapidly disintegrated as an induction disintegrant. In addition, in Comparative Example 1 and Comparative Example 2, the process of mixing TAG-2 with mannitol is added, whereas in Example 3, the disintegration time can be shortened only with TAG-1. It was confirmed that excellent drugs can be prepared.

In Comparative Example 2, in which TAG-2 was used as a fast disintegrating inducing disintegrant, a disintegration time of 20 seconds was exhibited, but the TAG-2 was dissolved in arabic gum in distilled water for 24 hours, and hot air dried at 40°C for 72 hours. While this is required, in the case of manufacturing TAG-1, the process of dissolving Arabian gum for 5 hours in distilled water and vacuum drying for 12 hours in a vacuum dryer at 50°C is required. TAG-1 is produced in a shorter time than TAG-2. It has the advantage of being.

The specific parts of the present invention have been described in detail above, and it is obvious that for those skilled in the art, these specific technologies are only preferred embodiments, and the scope of the present invention is not limited thereto. Accordingly, the substantial scope of the present invention will be defined by the appended claims and their equivalents.

The scope of the present invention is indicated by the following claims, and all modifications or variations derived from the meaning and scope of the claims and their equivalent concepts should be interpreted to be included in the scope of the present invention.

Claims (11)

a) 20 to 35% by weight of dry powder of herbal extract;
b) 5 to 15% by weight of a fast disintegrating inducing disintegrant;
c) 2 to 10% by weight of disintegrant;
d) 55 to 65% by weight of excipients; And
e) a lubricant containing 0.1 to 2% by weight; the rapid disintegration-inducing disintegrant comprises a fast disintegrating tablet composition characterized in that it is prepared by vacuum drying. The method according to claim 1, wherein the herbal medicine of a) is licorice, jujube, ginseng, gold silver, yeonkyo, mint, gilkyung, damjuk leaves, hyeonggae, dusi, allies, nutritious, peony, strong, windproof, poisonous, Angelica, gyeji, creation , Ginger, Macmundong, Sookjihwang, Omija, Cheonmundong, Bokryeong, Hubak, Galgeun, Banha, Saengjihwang, Jeonho, Broiler, Health, Doin, Baekchul, Hyangbuja, Gamguk, Cheongung, Taxi, Golden, Guruin, Ephedra, Malt, Baekji, Equestrian, Shiho, Jasobul, Hwanggi, Kwak Hyang, Rhubarb, Mangyeongja, Mancho, Mokdanpi, Mokhyang, Sinsae, Sansa, Samneung, Gypsum, Seshin, Shingok, Achul, Injinho, Perception, Jimo, Jisil, Jinpi, Cheonma, Cheongpi, Rapid disintegrating tablet composition, characterized in that at least one selected from the group consisting of gardenia, almond, and yellow and white. The method of claim 1, wherein the rapid disintegration-inducing disintegrant of b) is prepared by dissolving Arabian gum in distilled water for 1 to 10 hours, and then vacuum-drying for 8 to 15 hours under conditions of 40 to 60°C and 500 to 600 mmHg. Fast disintegrating tablet composition, characterized in that. The rapid disintegrating tablet composition according to claim 3, wherein the gum arabic and distilled water are added in a weight ratio of 1:(8-15). The disintegrant of claim 1, wherein the disintegrant of c) is croscarmellose sodium, sodium glycolate starch, crospovidone, gelatin, starch, carbomer, carboxymethylcellulose, copovidone, hydroxypropylcellulose, polyethylene oxide, povidone. , Fast disintegrating tablet composition, characterized in that at least one selected from the group consisting of calcium alginate and sodium stearyl fumarate. The method according to claim 1, wherein the excipient of d) is microcrystalline cellulose, xylitol, maltose, maltitol, mannitol, palatinose, erythritol, trehalose, glucose, sorbitol, maltodextrin, dextrose, lactose, oligosaccharides and rebaudio Fast disintegrating tablet composition, characterized in that at least one selected from the group consisting of side A. The method of claim 1, wherein the lubricant of e) is made of magnesium stearate, calcium stearate, zinc stearate, polyethylene glycol, glyceryl behenate, glyceryl palmitostearate, sodium lauryl sulfate, stearate and talc. Fast disintegrating tablet composition, characterized in that at least one selected from the group. The rapid disintegrating tablet composition according to claim 1, wherein the rapid disintegrating tablet has a disintegration time in the oral cavity of 1 to 25 seconds. a) preparing a herbal medicine hot water extract, followed by concentration and drying to prepare a dry powder;
b) preparing a first mixture by adding and mixing a fast disintegrating inducing disintegrant, a disintegrating agent, and an excipient in the dry powder of step a);
c) adding a lubricant to the first mixture of step b) and mixing to prepare a second mixture; And
d) a step of tableting the second mixture of step c); 10. The method of claim 9, wherein the herbal medicine of a) is licorice, jujube, ginseng, gold and silver, lotus, peppermint, gilkyung, damjuk leaves, hyeonggae, dusi, allies, nutritious, peony, strong, windproof, poisonous, Angelica, gyeji, creation , Ginger, Macmundong, Sookjihwang, Omija, Cheonmundong, Bokryeong, Hubak, Galgeun, Banha, Saengjihwang, Jeonho, Broiler, Health, Doin, Baekchul, Hyangbuja, Gamguk, Cheongung, Taxi, Golden, Guruin, Ephedra, Malt, Baekji, Equestrian, Shiho, Jasobul, Hwanggi, Kwak Hyang, Rhubarb, Mangyeongja, Mancho, Mokdanpi, Mokhyang, Sinsae, Sansa, Samneung, Gypsum, Seshin, Shingok, Achul, Injinho, Perception, Jimo, Jisil, Jinpi, Cheonma, Cheongpi, Method of manufacturing a fast disintegrating tablet composition, characterized in that at least one selected from the group consisting of gardenia, almond, and yellow and white. The method of claim 9, wherein the rapid disintegration-inducing disintegrant of b) is prepared by dissolving Arabian gum in distilled water for 1 to 10 hours, and then vacuum-drying for 8 to 15 hours under conditions of 40 to 60°C and 500 to 600 mmHg. Method of producing a fast disintegrating tablet composition, characterized in that.

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