KR20210054427A - Rapid-acting oral formulation of a tsaoko fructus extract and a prparing method of the same - Google Patents

Abstract

Disclosed in the present invention are an oral fast-acting formulation of an Amomum tsao-ko extract having improved bioavailability by improving solubility and dissolution rate, and a method for manufacturing the same. The present invention relates to an oral fast-acting formulation of an Amomum tsao-ko extract, comprising a solid dispersion manufactured by dissolving a composition comprising a medicinal component, the Amomum tsao-ko extract, and a hydrophilic water-soluble polymer, in an organic solvent capable of dissolving the composition, followed by spray drying the same.

Description

Rapid-acting oral formulation of a tsaoko fructus extract and a prparing method of the same}

The present invention relates to an oral fast-acting formulation composition of excess extract and a method for preparing the same.

Excess extract is a poorly soluble drug with a dissolution rate of about 40-50% in the gastrointestinal tract, although it has excellent effects in the prevention or treatment of hypertriglyceridemia. Although the dissolution rate is low and the biomembrane permeability is low, the absorption of the drug is delayed, so the bioavailability is lowered, but there is no prior art for the solubilization method and specific formulation of a formulation containing an excess extract yet.

Moreover, for the prevention or treatment of hypertriglyceridemia, a drug must be taken for a long period of time, and a fast-acting formulation administered in combination with a sustained-release formulation has been required.

The present invention discloses an oral fast-acting formulation of excess extract from this point of view.

[Prior technical literature]

Patent Document 1: Korean Patent No. 10-1691605 (Name: pharmaceutical composition and health functional food composition for the prevention or treatment of hyperlipidemia containing excess extract as an active ingredient)

An object of the present invention is to provide an oral fast-acting formulation composition of excess extract and a method for producing the same.

Other or specific objects of the present invention will be presented below.

The present inventors have used the excess extract as a water-soluble polymer, hydroxypropyl methylcellulose, to increase the bioavailability of the excess extract, which has an excellent effect in the prevention or treatment of hypertriglyceridemia, as confirmed in the Examples and Experimental Examples below, When preparing a solid dispersion by spray drying after dissolving in an appropriate solvent with pharmaceutical additives, the pH condition in the gastrointestinal tract (pH= 1.2) and in the pH conditions in the small intestine and large intestine (pH=6.8), the solubility was improved by 3.99 times (pH=1.2) and 3.18 times (pH=6.8), respectively, and the dissolution rate was improved by about 15 to 20 times. (The dissolution rate of the formulation of the comparative example was about 3% (pH=1.2) and 4.3% (pH=6.8), whereas the formulation of the present invention was about 70% under both pH conditions).

The present invention is provided based on these experimental results, and the oral fast-acting formulation composition of the excess extract of the present invention comprises a composition comprising the excess extract as a pharmaceutical ingredient and a water-soluble polymer that is hydrophilic, and an organic composition capable of dissolving the composition. It can be understood as a composition comprising a solid dispersion prepared by dissolving in a solvent and spray drying.

In the present invention, the excess extract is water, lower alcohols having 1 to 4 carbon atoms (methanol, ethanol, butanol, etc.), methylene chloride, or a mixture of excess fruits, leaves, stems, above-ground parts, roots, rhizomes, underground parts to be extracted. , Ethylene, acetone, hexane, ether, chloroform, ethyl acetate, butyl acetate, N,N-dimethylformamide (DMF), dimethyl sulfoxide (DMSO), 1,3-butylene glycol, propylene glycol, or their An extract obtained by leaching using a mixed solvent, an extract obtained using a supercritical extraction solvent such as carbon dioxide or pentane, or a fractional extract obtained by fractionating the extract. At this time, the extraction method may apply any method such as cold sedimentation, reflux, warming, ultrasonic radiation, supercritical extraction, etc. in consideration of the polarity, extraction degree, and preservation degree of the active material. In the case of a fractionated extract, a fraction obtained by suspending the extract in a specific solvent and then mixing and policing it with a solvent having a different polarity, and adsorbing the crude extract on a column filled with silica gel, etc., and then adding a hydrophobic solvent, a hydrophilic solvent, or a mixed solvent thereof. It may be a fraction obtained as a mobile phase. In addition, the extract may be a concentrated liquid form from which the extraction solvent is partially removed by a method such as freeze drying, vacuum drying, hot air drying, spray drying, or the like, or a solid state from which the extraction solvent is completely removed. Preferably, the excess extract is an extract obtained using water, ethanol, or a mixed solvent thereof as an extraction solvent, particularly an extract obtained using a mixed solvent of water and ethanol, and means a solid state from which the extraction solvent has been removed.

In addition, in the present invention, the water-soluble polymer may be any water-soluble polymer material known in the art that can act as a dispersion medium of the drug substance, specifically hydroxy propyl methyl cellulose (Hydroxy propyl methyl cellulose), methyl cellulose , Cellulose derivatives such as ethyl cellulose, hydroxypropyl methylcellulose, hydroxypropyl cellulose, sodium carboxymethylcellulose, polysaccharides such as hyaluronic acid, alginic acid, polysaccharides, and heteropolysaccharides (pectin), Polymers of polyvinylpyrrolidone, polyethylene glycol, polyvinyl alcohol, polyvinylacetate phthalate, polymethacrylate, and polymethacrylate (Commercially Eudragit), polyacrylic acid, derivatives of polymethacrylate (typically carbomers), glycerol monostearate, polyethylene oxide, poloxamer, phloxamine or a copolymer thereof, or two thereof Mixtures of the above can be used. In particular, hydroxypropyl methylcellulose, polyvinylpyrrolidone, polyvinyl alcohol, carboxymethylcellulose sodium, polyethylene oxide, polyoxyethylene and polyoxypropylene block copolymers, or a mixture of two or more thereof used in the examples below are preferred. Do. These water-soluble polymers, when spray-dried together with the excess extract, hydrophilize the environment around the excess extract, thereby increasing the solubility and dissolution rate of the excess extract, which is a medicinal ingredient, and consequently improving the bioavailability.

In the present invention, the water-soluble polymer is preferably mixed in the range of 0.5 parts by weight to 20 parts by weight, particularly 1 to 10 parts by weight, based on 1 part by weight of the excess extract as a medicinal ingredient. If the content of the water-soluble polymer is less than 0.5 parts by weight, it is difficult to expect a high solubility because the ratio of the crystalline drug is higher than the amorphous drug in the solid dispersion composition, and if it exceeds 20 parts by weight, it is difficult to expect a further solubility improvement effect. In addition, as the total dose of the solid dispersion composition is increased, it is a burden for the patient to take it, which may lower patient compliance.

In the present invention, a medicinal ingredient refers to an ingredient that can exhibit a desired activity by itself, or that itself can exhibit activity together with a carrier or additive that is not active.

In the present invention, the solvent capable of dissolving the composition containing the excess extract and the water-soluble polymer as a pharmaceutical ingredient may be any solvent, as long as it is a pharmaceutically acceptable solvent, such as dichloromethane, chloroform, ethanol, methanol, and acetone. , Isopropanol, propanol, or a mixed solvent thereof.

The formulation of the present invention contains a pharmaceutical additive that has proven pharmaceutically acceptable safety, to an objection comprising a solid dispersion prepared by dissolving a composition containing an excess extract as a pharmaceutical ingredient and a water-soluble polymer in an appropriate solvent and spray-dried. can do. Examples of such pharmaceutical additives include surfactants, diluents, binders, lubricants, disintegrants, antioxidants, flavoring agents, preservatives, sweeteners, and the like.

Surfactants may be anionic, cationic, nonionic, or amphoteric surfactants as long as they are pharmaceutically acceptable. Specifically, polyoxyethylene sorbitan fatty acid ester, sorbitan fatty acid ester, polyoxyethylene fatty acid ester, polyoxyethylene polyoxypropylene block copolymer (polyoxyethylene polyoxypropylene block copolymer), polyoxyethylene polyoxypropylene copolymer, reactant of natural or hydrogenated vegetable oil and ethylene glycol (reactant of natural or hydrogenated vegetable oil and etylene glycol), sodium dioctyl sulfosuccinate (dioctylsulfosuccinic acid sodium salt), lauryl sufonic acid sodium salt, phospholipids, propylene glycolmono or fatty acid ester, trans of natural vegetable oil triglyceride and polyalkylene polyol -Esterification reaction products, mono-, di- or mono/di glycerides, flophyllene glycol mono or di fatty acid esters with mono-, di- or mono/diglycerides One or more may be selected and used from the group consisting of mixtures of and derivatives thereof.

In addition, as pharmaceutically usable diluents, starch, microcrystalline cellulose, lactose, glucose, mannitol, alginate, alkaline earth metal salts, clay, polyethylene glycol, dicalcium phosphate, silicic anhydride, aluminum magnesium silicate, and mixtures thereof are mentioned. I can.

In addition, as pharmaceutically usable binders, polyvinylpyrrolidone, vinylpyrrolidone and vinyl acetate copolymer, cellulose derivatives such as hydroxypropylcellulose, hydroxyethylcellulose, and hydroxypropylmethylcellulose, xanthan gum, alginate, And saccharides such as gums such as gum arabic, starch, pregelatinized starch, and sucrose, and mixtures thereof.

In addition, as a disintegrant that can be used pharmaceutically, starch such as sodium glyconate, corn starch, potato starch, pregelatinized starch, modified starch, bentonite, montmorillonite, clay such as veegum, microcrystalline cellulose, hydride Celluloses such as oxypropyl cellulose and carboxymethylcellulose, algins such as sodium alginate and alginic acid, crosslinked celluloses such as croscarmellose sodium, gums such as guar gum and xanthan gum, and crospovidone ( crospovidone), effervescent agents such as sodium bicarbonate and citric acid, and mixtures thereof.

In addition, as lubricants that can be used pharmaceutically, talc, stearic acid, magnesium stearate, calcium stearate, zinc stearate, lauryl sulfate, hydrogenated vegetable oil, sodium benzoate, sodium stearyl fumarate, glyceryl monostearate, glyceryl behenate. , Glycerin fatty acid derivatives such as glyceryl palmitostearate, polyethylene glycol 4000, and mixtures thereof.

In addition, antioxidants that can be used pharmaceutically are butylated hydroxytoluene, sodium bisulfite, α-tocopherol, vitamin C (ascorbic acid), β-carotene. -carotin), tocopherol acetate, fumaric acid, nalic acid, butylated hydroxyanisole, propyl galate and sodium ascorbate ascorbate) and the like.

In addition, as a flavoring agent that can be used pharmaceutically, mixed fruit flavor, apple flavor, strawberry flavor, cherry flavor, mint flavor, vanilla flavor, yogurt flavor, drink flavor, and the like may be mentioned.

In addition, as preservatives that can be used pharmaceutically, benzoic acid, sodium benzoate, ethylparaben, methylparaben, propylparaben, and the like can be mentioned.

In addition, as sweeteners that can be used pharmaceutically, white sugar, glucose, fructose, aspartame, stevioside, sorbitol, mannitol, oligosaccharides, starch syrup, maltose syrup, and the like can be mentioned.

If necessary, in addition to the additives described above, this composition may contain water-soluble mannitol, caramel, coloring agents such as titanium oxide, fragrances such as mentha oil, orange oil, sodium carbonate, as long as the effectiveness of the formulation or active ingredient is not impaired or quality control is impaired. Other pharmaceutically usable additives, such as a pH adjusting agent such as sodium hydroxide and potassium hydroxide, and viscosity adjusting agents such as acacia, bentonite, and alginic acid, may be additionally included. These additives are listed in the Korean Pharmacopoeia or other domestic and international public notices, and any of those that have been approved for safety in the art as pharmaceutical additives can be appropriately selected and used.

When preparing the solid dispersion, the pharmaceutical additive may be added to a composition containing the excess extract as the medicinal ingredient and a water-soluble polymer. At this time, the solid dispersion is prepared by including such pharmaceutical additives.

The additives described above will be included in the formulation of the present invention in an appropriate amount according to the purpose of addition.

The composition of the present invention can be formulated in various ways. For example, uncoated tablets, coated tablets, multi-layered tablets, or nucleated tablets may be formulated as tablets, powders, granules or capsules, and preferably tablets and capsules. All of these various formulation methods are known in the art.For example, formulation of capsules is prepared by preparing a solid dispersion containing excess extract as a pharmaceutical ingredient in a capsule together with an appropriate excipient, as in the Examples below. It can be filled to prepare a capsule.

Regarding the formulation of a specific drug, for example, Remington's Pharmaceutical Sciences (19th ed., 1995) may be referred to, and the document is considered as a part of the present specification.

In another aspect, the present invention relates to a method of preparing an oral fast-acting formulation composition of excess extract.

The production method of the present invention comprises the steps of dissolving a composition comprising an excess extract as a medicinal ingredient and a hydrophilic water-soluble polymer in an organic solvent capable of dissolving the composition, and spray-drying the dissolved product to prepare a solid dispersion. Step, comprising the step of formulating by adding a pharmaceutical additive to the solid dispersion.

In the production method of the present invention, talc may be added to the melt as in the following examples in order to improve dispersibility. In this case, the amount added may be in the range of 1 part by weight to 20 parts by weight based on 100 parts by weight of the composition.

The properties of the spray-dried product vary depending on the spray drying intake temperature, exhaust temperature, drying pressure, dry injection amount, and the solid content of the spray drying liquid. When comprehensively considering the viscosity and solid content of the spray-dried liquid, the appearance and flowability of the spray-dried product, the particle size of the spray-dried product, and the particle size distribution, the spray drying is preferably performed under the following conditions.

Spray drying solution injection amount: 50 to 60 ㎖/min,

Spray drying pressure: 3 ㎏/㎠,

Spray drying intake temperature: 105 to 115°C,

Spray drying exhaust temperature: 55 to 65°C,

Others With respect to the production method of the present invention, the above-described is effective as it is with respect to the excess extract, water-soluble polymer, organic solvent, pharmaceutical additive, formulation that can be used.

As described above, the present invention can provide an oral fast-acting formulation of an excess extract with improved bioavailability by improving solubility and dissolution rate, and a method of manufacturing the same.

1 and 2 are the results of the solubility test and the dissolution rate test, respectively.

Hereinafter, the present invention will be described with reference to preferred examples and experimental examples. However, the scope of the present invention is not limited to these Examples and Experimental Examples.

<Example 1> Preparation 1 of solid dispersion containing excess extract

The excess extract was extracted for 24 hours by adding 5 times the weight of 80% ethanol to the dry excess (extraction site: fruit) powder, filtered, and the filtrate was concentrated under reduced pressure and lyophilized to obtain a powdery form.

After dissolving 100 g of excess extract and 100 g of hydroxypropyl methylcellulose, a water-soluble polymer, in 1,750 g of a 1:1 (mass ratio) mixed solvent of dichloromethane and ethanol, 10 g of talc was added to this solution and uniformly dispersed to prepare a spray-dried solution. I did. The spray-dried liquid was spray-dried under the following conditions using a spray dryer (Mobile MinorTM) to prepare a solid dispersion containing excess extract.

Spray drying solution injection amount: 50 to 60 ㎖/min,

Spray drying pressure: 3 ㎏/㎠,

Spray drying intake temperature: 105 to 115°C,

Spray drying exhaust temperature: 55 to 65°C,

<Example 2> Preparation 2 of solid dispersion containing excess extract

A solid dispersion containing excess extract was prepared in the same manner as in Example 1, except that 100 g of polyvinylpyrrolidone as a water-soluble polymer was used instead of 100 g of hydroxypropyl methylcellulose.

<Example 3> Preparation 3 of solid dispersion containing excess extract

A solid dispersion containing excess extract was prepared in the same manner as in Example 1, except that 100 g of methyl cellulose and 100 g of hydroxypropyl methyl cellulose were used instead of the water-soluble polymer.

<Example 4> Preparation 4 of solid dispersion containing excess extract

A solid dispersion containing excess extract was prepared in the same manner as in Example 1, except that 100 g of polyvinyl alcohol as a water-soluble polymer was used instead of 100 g of hydroxypropyl methylcellulose.

<Example 5> Preparation 5 of solid dispersion containing excess extract

A solid dispersion containing excess extract was prepared in the same manner as in Example 1, except that 100 g of sodium carboxymethylcellulose as a water-soluble polymer was used instead of 100 g of hydroxypropyl methylcellulose.

<Example 6> Preparation 6 of solid dispersion containing excess extract

After dissolving 100 g of excess extract, 100 g of water-soluble polymer, hydroxypropyl methylcellulose, and 50 g of polyoxyethylene polyoxypropylene block copolymer, in 1,750 g of a 1:1 (mass ratio) mixed solvent of dichloromethane and ethanol?, 10 g of precipitated calcium carbonate And uniformly dispersed to prepare a spray-dried solution. The following was spray-dried in the same manner as in Example 1 to prepare a solid dispersion containing excess extract.

<Example 7> Preparation 7 of solid dispersion containing excess extract

Except for using 100 g of hydroxypropyl cellulose and 30 g of a reaction product of natural or hydrogenated vegetable oil and ethylene glycol as a water-soluble polymer, a solid dispersion containing excess extract was prepared in the same manner as in Example 1 and under the same conditions. .

<Example 8> Formulation of solid dispersion 1

After homogeneously mixing 34.0 g of the solid dispersion composition prepared in Example 1 with 39.1 g of microcrystalline cellulose and 26.0 g of calcium carboxymethyl cellulose, granules were prepared using a roller compactor by a dry granulation method. After mixing 1.0 g of magnesium stearate as a lubricant, it was filled in an automatic capsule filling machine to prepare a capsule.

<Example 9> Formulation 2 of solid dispersion

After homogeneously mixing 38.6 g of the solid dispersion composition prepared in Example 6 with 29.0 g of microcrystalline cellulose and 21.7 g of calcium carboxymethyl cellulose, granules were prepared using a roller compactor by a dry granulation method. After mixing 0.8 g of magnesium stearate as a lubricant, it was filled in an automatic capsule filling machine to prepare a capsule.

<Example 10> Formulation of solid dispersion 3

30.5 g of the solid dispersion composition prepared in Example 7 was homogeneously mixed with 29.0 g of microcrystalline cellulose, 25.8 g of lactose, and 5.0 g of calcium carboxymethyl cellulose, and then granulated using a roller compactor by a dry granulation method. After preparing, 4.5 g of crospovidone as a disintegrant and 0.8 g of magnesium stearate were mixed as a lubricant to prepare tablets.

<Example 11> Formulation of solid dispersion 4

After homogeneously mixing 20.5 g of the solid dispersion composition prepared in Example 7 with 50.0 g of lactose and 5.0 g of calcium carboxymethyl cellulose, a dry granulation method was used to prepare granules using a roller compactor, and then a disintegrant Tablets were prepared by mixing 5.0 g of low-substituted hydroxypropyl cellulose and 0.5 g of magnesium stearate as a lubricant.

<Comparative Example>

In a mixer (High Speed Mixer), 8 kg of lactose and 4 kg of corn starch were added and mixed evenly. This mixture was mixed with 3 kg of the excess extract prepared in the same manner as in Example 1, and then kneaded in a combiner, and then assembled into a sieve No. After hot air drying at 60° C., it was sized in a No. 20 sieve to obtain granules. The prepared granules were filled in an automatic capsule filling machine to prepare capsules.

<Experimental Example 1> Solubility Comparative Experiment

The solubility of the oral test formulation including the pharmaceutical composition of the excess extract prepared by the spray drying method of the present invention and the oral comparative formulation including the pharmaceutical composition of the excess extract prepared by the conventional wet assembly method was measured and compared.

Specifically, the pH condition (pH = 1.2) in the gastrointestinal tract of the capsule test formulation containing the pharmaceutical composition of the excess extract prepared from Example 8 and the capsule comparative formulation containing the pharmaceutical composition of the excess extract prepared from the comparative example The solubility of the drug was measured under pH conditions (pH=6.8) in the small and large intestine.

The experimental method is as follows.

Taking an amount corresponding to 250 mg of the excess extract in the oral preparations prepared from Example 8 and Comparative Example, a buffer solution of pH 1.2 and pH 6.8 (the 8th revision of the Korean Pharmacopoeia, pH 1.2 solution of sodium chloride, 2.0 g of hydrochloric acid 7.0 ml and water Add 118 ml of 0.2 mol/L sodium hydroxide solution and water to 250 ml of pH 6.8 solution 0.2 mol/L potassium dihydrogen phosphate TS to make 1 L.) Add to 150 ml each. After the solution was stirred at 37° C. for 1 hour, the solubility was measured. Solubility was measured using HPLC using trans-nerolidol, an indicator component of the excess extract, after centrifugation.

The results are shown in Table 1.

Solubility and comparison at pH=1.2 and pH=6.8 (unit: ㎍/㎖) Formulation pH 1.2 pH 6.8 Comparative formulation 0.096 0.127 Test formulation 0.383 0.404 Test formulation/comparative formulation 3.99 times 3.18 times

As shown in Table 1, the solubility of the oral test formulation prepared from Example 8 of the present invention was 0.383 µg/ml and 0.404 µg/ml at pH = 1.2 and pH = 6.8, respectively, prepared from the comparative example. The solubility of the oral comparative formulation was 0.096 µg/ml and 0.127 µg/ml, respectively. In addition, when comparing the solubility, it can be seen that the solubility of the oral formulation according to the present invention is 3,99 times and 3.18 times higher at pH=1.2 and pH=6.8, respectively.

Therefore, it can be seen that the quick-acting oral preparation by the solid dispersion according to the present invention has a very high solubility in the pH conditions of the small and large intestine in the gastrointestinal tract compared to the preparation prepared by the conventional method, and it is uniformly dissolved even under various pH conditions. You can see that it is.

<Experimental Example 2> Comparative experiment of dissolution rate

The dissolution rates of the oral preparations including the fast-acting solid dispersion oral preparation of the present invention and the pharmaceutical composition of the excess extract prepared by a conventional wet assembly method were measured and compared.

The experimental method is as follows.

In the oral formulation containing the pharmaceutical composition of the excess extract prepared from Example 8 and Comparative Example, taking an amount corresponding to 60 mg of the excess extract, prepared in the same manner as in Experimental Example 1 of pH = 1.2 and pH = 6.8 500 ml of the buffer solution was added to the dissolution tester vessel and stirred at 100 rpm. The content of trans-nerolidol in the excess extract extracted therefrom by eluting by the paddle method was measured.

The dissolution rate measured at pH=1.2 is shown in FIG. 1, and the dissolution rate measured at pH=6.8 is shown in FIG.

1 and 2, the oral formulation (test formulation) prepared from Example 8 of the present invention showed a dissolution rate of 70% or more for 10 minutes at pH 1.2 and pH 6.8, and 20 minutes to 60 minutes Showed a constant dissolution rate during.

On the other hand, the oral formulation (comparative formulation) prepared from Comparative Example showed a lower dissolution rate per stirring time than the oral formulation prepared from Example 8.

Therefore, as shown in FIGS. 1 and 2, the oral formulation according to the present invention has a high dissolution rate at pH = 1.2 and pH = 6.8 compared to the oral formulation prepared from the comparative example, and in particular, it has a constant dissolution rate even at various pHs. It has excellent dissolution properties.

Claims (12)

A composition comprising an excess extract as a medicinal ingredient and a water-soluble polymer that is hydrophilic, comprising a solid dispersion prepared by dissolving the composition in an organic solvent capable of dissolving the composition and spray drying the composition.
The method of claim 1,
Formulation composition wherein the excess extract is a solid extract as an extract of water, ethanol or a mixed solvent thereof.
The method of claim 1,
The water-soluble polymer is hydroxypropyl methyl cellulose, methyl cellulose, ethyl cellulose, hydroxypropyl methyl cellulose, hydroxypropyl cellulose, sodium carboxymethylcellulose, hyaluronic acid, alginic acid. , Polysaccharide, heteropolysaccharide (pectin), polyvinylpyrrolidone, polyethylene glycol, polyvinyl alcohol, polyvinylacetate phthalate, polymethacrylate (Polymethacrylate), polymethacrylate polymer (commercially Eudragit), polyacrylic acid, polymethacrylate derivative (typically carbomer), glycerol monostearate, polyethylene oxide, poloxamer, phloxamine, A formulation composition comprising a copolymer thereof or a mixture of two or more thereof.
The method of claim 1,
Formulation composition, characterized in that the water-soluble polymer is mixed in the range of 1 to 10 parts by weight relative to 1 part by weight of the excess extract as a medicinal ingredient.
The method of claim 1,
The solvent is a formulation composition, characterized in that dichloromethane, chloroform, ethanol, methanol, acetone, isopropanol, propanol, or a mixed solvent thereof.
The method of claim 1,
The composition comprising the excess extract as a medicinal ingredient and a hydrophilic water-soluble polymer further comprises a pharmaceutical additive.
The method of claim 1,
The formulation composition further comprises a pharmaceutical additive.
The method according to claim 6 or 7,
The pharmaceutical additives are surfactants, diluents, binders, lubricants, disintegrants, antioxidants, flavoring agents, preservatives, sweeteners, colorants, fragrances, pH adjusters, and a formulation composition, characterized in that at least one of a viscosity modifier.
The method of claim 1,
Formulation composition, characterized in that the formulation is a tablet, powder, granule or capsule formulation.
Dissolving a composition comprising an excess extract as a medicinal ingredient and a hydrophilic water-soluble polymer in an organic solvent capable of dissolving the composition, spray-drying the dissolved product to prepare a solid dispersion, and the solid dispersion A method for preparing an oral fast-acting formulation composition of excess extract comprising the step of formulating by adding a pharmaceutical additive.
The method of claim 10,
A method, characterized in that talc is added to the melt.
The method of claim 10,
The spray drying method characterized in that it is carried out under the following conditions:
Spray drying solution injection amount: 50 to 60 ㎖/min,
Spray drying pressure: 3 ㎏/㎠,
Spray drying intake temperature: 105 to 115°C,
Spray drying exhaust temperature: 55 to 65°C.

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