KR20090131584A - Fast dissoluble effervescent tablet containing mastic - Google Patents

Abstract

PURPOSE: An effervescent and rapid disintegrating tablet containing mastic and water soluble polymer is provided to reduce weakness of table such as sticking and dissolve the drug in small amount of water. CONSTITUTION: An effervescent and rapid disintegrating tablet contains mastic which is sap extract of Pistasia lentiscus, water soluble polymer, sugar or their mixture. The tablet contains acid and carbonate. The tablet further contains sweetener. The water soluble polymer is contained in 0.2-10 weight parts based on mastic weight. The tablet contains 20-70 weight% of solid dispersion, 5-10 weight% of organic acid, and 5-15 weight% of carbonate.

Description

Fast dissoluble effervescent tablet containing mastic}

The invention Helicobacter pylori ( Helicobacter) is a causative agent of gastric ulcer and duodenal ulcer pyroli ) is a fast disintegrating tablet containing a mastic having a bactericidal effect.

Mastic is a sap extracted from Pistasia lentiscus , a kind of pistachio tree growing on the island of Chios, Greece. It has a unique fragrance and is hardly soluble in water. . Mastic has long been known to have the effect of inhibiting or killing the growth of Helicobacter pyroli, which is known as a causative agent of gastritis, gastric ulcer and duodenal ulcer. come.

However, such a mastic has a disadvantage in that tableting disorders such as sticking are likely to occur during the manufacture of tablets due to its physical properties, and the disintegration or dissolution rate is very slow due to poor water solubility.

In addition, since mastic has a specific bitter and astringent taste, it is more preferable to solve such unpleasant taste in terms of patient compliance.

Therefore, the technical problem to be achieved by the present invention is to provide a tablet containing a mastic that tableting disorders such as sticking are improved and the disintegration or dissolution rate of the mastic which is an active ingredient is improved.

In order to achieve the above technical problem, the present invention is a solid dispersion of mastic, which is an sap extract of Pistasia lentiscus , preferably solid dispersion of mastic and a water-soluble polymer. An effervescent fast disintegrating tablet comprising a sieve is provided.

In general, effervescent fast disintegrating tablets, or fast disintegrating effervescent tablets, are prepared in the form of tablets and when bubbling in the oral cavity or when a small amount of water is added, bubbles are formed while foaming in the water so that the active ingredients contained in the tablets are rapidly converted into aqueous solutions. By being manufactured, it is possible to easily ingest the components contained in the foam tablets.

The present invention is to prepare a solid dispersion of mastic (mastic oil or mastic resin), when producing a foamed fast disintegrating tablet with a variety of sticking, such as sticking occurs when the mastic is produced by a conventional tablet manufacturing method Not only can the tableting disorder be significantly improved, but the main ingredient can significantly improve the disintegration or dissolution time of the mastic, and the improved solubility is prevented by preventing the recrystallization of the mastic by humidity, temperature and light even after solubilization. It is based on the fact that it can be kept during storage.

The present invention provides a composition capable of solubilizing an effective mastic to Helicobacter pylori, which is known as a major causative agent of gastric ulcer and duodenal ulcer, and preventing recrystallization of the active ingredient.

The present invention also rapidly disintegrates or dissolves the tablets by oral administration through the technique according to the present invention, even when taken with very small amounts of water, and elutes the active ingredient by dissolving the active ingredient to disinfect them. And effervescent fast disintegrating tablets capable of exhibiting a therapeutic effect.

Therefore, the expandable fast disintegrating tablet of the present invention includes a solid dispersion of mastic, and preferably a solid dispersion of mastic and a water-soluble polymer.

As a method for preparing a solid dispersion, a solid dispersion manufacturing method commonly known in the art may be used. For example, using a solvent (eg, methanol, ethanol, isopropanol, acetone, ethyl acetate or a mixture thereof) in which both the main component and the water-soluble polymer, the sugar or a mixture thereof, which are the solid dispersion forming medium are dissolved, are used. A solution for forming a solid dispersion by preparing a solution containing a solid dispersion forming medium, followed by drying, a melting method for melting the main component and the solid dispersion forming medium using heat and then cooling the same together to form a solid dispersion, and mixing them. One method or the like can be used.

Water-soluble polymers that form a solid dispersion with mastic and maintain the solid dispersion include polyvinylpyrrolidone, hydroxypropylcellulose, hydroxypropylmethylcellulose, vinylpyrrolidone-vinylacetate air Copolymer, Polyvinyl Alcohol, Polyvinyl Alcohol-Polyethylene Glycol Copolymer, Hydroxymethyl Cellulose, Hydroxyethyl Cellulose, Hydroxymethyl Cellulose, Polyvinylacetate, Polyalkene Oxide, Polyalkeneglycol, Polyoxyethylene-Poly Oxypropylene polymer, diethylaminoacetate, aminoalkyl methacrylate copolymer, sodium alginate, gelatin and the like can be used alone or in combination, and considering the ease of solid dispersion formation with mastic, improvement of tableting disorder, etc. Polyvinylpyrrolidone, hydroxypropylmethylcellulose or mixtures thereof are preferred. .

In addition, as a sugar that forms a solid dispersion with mastic and maintains the solid dispersion, mannitol, sorbitol, white sugar, glucose, xylitol, inositol, lactose, fructose, and the like may be used. However, the water-soluble polymer is more preferable as a medium for forming a solid dispersion in terms of tableting disorder, recrystallization of mastic, solubilization of mastic, and the like.

In such a solid dispersion, the water-soluble polymer is preferably contained in an amount of 0.2-10 parts by weight based on the weight of the mastic in terms of improving tableting disorder, improving solubility of the mastic, and preventing recrystallization. When used in less than 0.2 parts by weight relative to the mastic weight, it is difficult to prevent recrystallization of the solubilized active ingredient mastic, and when used in excess of 10 parts by weight, the viscosity is strong during the formulation process, making the work process difficult.

Such a solid dispersion is preferably included 20-70% by weight relative to the total weight of the tablet according to the present invention. When the solid dispersion containing mastic, which is an active ingredient, is generally added in an amount less than 20% by weight, the effect is difficult to expect. On the contrary, when it is added in excess of 70% by weight, the content ratio of other components such as organic acid and carbonate is reduced. It is difficult to expect rapid disintegration.

Tablets according to the invention are also essential ingredients for exhibiting effervescent properties such as organic acids, inorganic acids or mixtures thereof; And carbonates.

Such organic acids include citric acid, tartaric acid, malic acid, adipic acid, ascorbic acid, succinic acid, sulfamic acid, capric acid, lauric acid, formic acid, glutamic acid, glycolic acid, malic acid, malistic acid, and oleic acid. Or mixed.

As such inorganic acid, hydrochloric acid, phosphoric acid, sulfuric acid, or the like may be used alone or in combination.

Such acid is preferably added at 5-10% by weight relative to the total weight of the tablet. If the organic acid is added at less than 5% by weight, foaming performance may deteriorate and disintegration may be delayed. If it is added in excess of 10% by weight, the hardness of the tablet may be lowered, and it may be easily condensed. Foaming and swelling can occur.

As the carbonate salt, sodium bicarbonate, sodium carbonate, sodium sesquicarbonate, calcium carbonate, potassium carbonate, magnesium carbonate, calcium hydrogen carbonate, potassium hydrogen carbonate and the like can be used alone or in combination, improving dissolution or disintegration of tableting disorders and mastic. Sodium bicarbonate is more preferred in this regard.

Such carbonate is preferably added at 5-15% by weight based on the total weight of the tablet. If the amount is less than 5% by weight, the foaming capacity is lowered, so that the tablet does not disintegrate quickly. If it is added in excess of 15% by weight, foaming is damaged during the distribution process, and the packaging material is damaged or the foaming performance is reduced when taken orally. Can be.

Effervescent fast disintegrating tablets of the present invention may also further comprise sweetening agents, flavoring agents and the like to improve the unpleasant taste of the mastic.

As such sweeteners, purified white sugar, aspartame, acesulfame K, stevioside, saccharin, or the like may be used alone or in combination.

In addition to the above components, the foamed fast disintegrating tablet of the present invention may further contain a lubricant, a binder, a filler, and the like within the scope of not impairing the object of the present invention. As the lubricant, silicon dioxide, colloidal silicon dioxide, magnesium stearyl acid, talc, stearyl fumarate, stearyl acid, sodium lauryl sulfate, polyethylene glycol, and the like can be used alone or in combination. Polyethyleneglycol is most preferred for preparing into fast disintegrating foamed tablets.

As a result, the present invention provides a foamed fastener comprising 20-70% by weight of a solid dispersion comprising mastic and a water-soluble polymer, 5-10% by weight of an organic acid, 5-15% by weight of a carbonate, and a balance of sweeteners, fillers, lubricants, and the like. It provides a degradable tablet.

The fast disintegrating foam tablets according to the invention can be prepared in various sizes up to about 500 mg to 3 g, and these tablets disintegrate substantially completely within two minutes.

The present invention solubilizes a mastic known to be excellent in killing effect of Helicobacter pylori, which is a causative agent of gastritis, gastric ulcer and duodenal ulcer, and solves a problem in that it is not easy to commercialize by material properties by preparing a fast disintegrating foam tablet. Tablets according to the invention are new formulations containing safe natural plant antimicrobial components with little side effects.

Hereinafter, examples and the like will be described in detail to help understand the present invention. However, embodiments according to the present invention can be modified in many different forms, the scope of the invention should not be construed as limited to the following examples. Embodiments of the present invention are provided to more fully describe the present invention to those skilled in the art.

<Example 1>

500 g of mastic and 500 g of polyvinylpyrrolidone were added to 10000 g of ethanol and completely dissolved using a stirrer. Solid dispersion was prepared by confirming complete dissolution and spray drying using a fluidized bed coater. The instrument conditions for producing the solid dispersion were as follows.

Equipment: GPCG 3 Type

Supply temperature: 60 ℃

Exhaust temperature: 40 ℃

Nozzle Diameter: 1.0 mm

Injection speed: 30 g / min

<Example 2>

500 g of mastic and 500 g of hydroxypropylmethylcellulose were added to a mixed solution of 7000 g of ethanol and 3000 g of methylene chloride, and completely dissolved using a stirrer. Solid dispersion was prepared by confirming complete dissolution and spray drying using a fluidized bed coater. Instrument conditions for producing the solid dispersion were the same as in Example 1.

<Example 3>

1000 g of the solid dispersion prepared in Example 1, 150 g of citric acid, 250 g of sodium bicarbonate, 450 g of xylitol, 55 g of stevioside, 45 g of microcrystalline cellulose, and 25 g of peppermint micron were mixed and finally 25 g of polyethylene glycol was added. After mixing, tablets with a total weight of 2 g were prepared using a rotary tablet press. Prior to preparation, the remaining excipients except the solid dispersion and peppermint micron were used after drying. When mixing each component, the relative humidity was adjusted to 50% or less to prevent tableting disorder.

<Example 4>

1000 g of the solid dispersion prepared in Example 2, 150 g of citric acid, 250 g of sodium bicarbonate, 450 g of xylitol, 55 g of stevioside, 45 g of microcrystalline cellulose, and 25 g of peppermint micron were mixed and finally 25 g of polyethylene glycol was added. After mixing, tablets with a total weight of 2 g were prepared using a rotary tablet press. All manufacturing methods were carried out in the same manner as in Example 3.

Comparative Example 1

500 g of mastic, 135 g of microcrystalline cellulose, 25 g of sodium bicarbonate, 50 g of polyvinylpyrrolidone, 50 g of xylitol, 30 g of peppermint micron and 10 g of magnesium stearate were mixed and prepared by tableting in the same manner as in Example 3. All manufacturing methods were carried out in the same manner as in Example 3.

<Experiment 1> Comparison of the ease of preparation and disintegration time of fast disintegrating tablet

During the tableting process of the above examples, the tablet forming performance was evaluated in four stages: poor (-), normal (+), good (++) and good (+++), and when the tablet was placed in 100 ml of water, Disintegration time was evaluated as disintegration time. The results are shown in Table 1 below.

division Tablet molding performance (tableting evaluation) Disintegration time Example 3 +++ 30 seconds Example 4 +++ 45 sec Comparative Example 1 + 17 minutes 22 seconds

As shown in Table 1, Comparative Example 1 was a phenomenon that the powder stuck to the punch and the die during tableting, the disintegration time was also very long compared to Examples 3 and 4.

Claims (8)

An effervescent fast disintegrating tablet comprising a solid dispersion of a sap extract of Pistasia lentiscus and a water-soluble polymer, a sugar, or a mixture thereof. The method of claim 1, wherein the water-soluble polymer is polyvinylpyrrolidone, hydroxypropyl cellulose, hydroxypropylmethylcellulose, vinylpyrrolidone-vinylacetate copolymer, polyvinyl alcohol, polyvinyl alcohol-polyethylene glycol copolymer, Hydroxymethyl cellulose, hydroxyethyl cellulose, hydroxyethyl cellulose, polyvinylacetate, polyalkene oxide, polyalkenglycol, polyoxyethylene-polyoxypropylene polymer, diethylaminoacetate, aminoalkyl methacrylate co Effervescent fast disintegrating tablet, characterized in that any one or more selected from the group consisting of polymer, sodium alginate and gelatin. The method of claim 1, wherein the tablet is an acid; And carbonates. The acid according to claim 3, wherein the acid is an organic acid, citric acid, tartaric acid, malic acid, adipic acid, ascorbic acid, succinic acid, sulfamic acid, capric acid, lauric acid, formic acid, glutamic acid, glycolic acid, malic acid, and malist. Effervescent fast disintegrating tablet, characterized in that any one or more selected from the group consisting of acid and oleic acid. 4. The expandable fast disintegrating tablet according to claim 3, wherein the carbonate is at least one selected from the group consisting of sodium bicarbonate, sodium carbonate, sodium sesquicarbonate, calcium carbonate, potassium carbonate, magnesium carbonate, calcium hydrogen carbonate and potassium hydrogen carbonate. . The effervescent fast disintegrating tablet according to claim 3, wherein the composition contains a sweetening agent. The rapid disintegrating tablet according to claim 1, wherein the water-soluble polymer is contained in an amount of 0.2-10 parts by weight based on the weight of the mastic. The effervescent fast disintegrating tablet according to claim 3, wherein the tablet comprises 20-70 wt% of solid dispersion, 5-10 wt% of organic acid, and 5-15 wt% of carbonate.