JPH06107555A - Oriental bezoar microcapsule and preparation thereof - Google Patents

Abstract

PURPOSE: To provide a Goou-Seishin microcapsule which is convenient to carry and take, is easy to take for its capability of concealing the strong taste of crude drug extract, extremely rapidly exhibits effects and is preservable for a long period. CONSTITUTION: The Goou-Seishin microcapsule is obtd. by finely pulverizing the crude drugs which are the respective components of Goou-Seishinngan (a Chinese herb medicine: Goou is Bezoar Bovis, Seishinngan is the pill or powder formulated to provide mental stability by eliminating the cause for palpitations, anxiety at the time of sleeping, etc.), suspending the powder in water and ethanol or precipitating the powder with the water and ethanol and mixing the same or joining the respective components and precipitating the mixture with the water and ethanol, adding suitable materials to be filmed, dissolution assistants, aromatic sugar and other necessary additives to the mixture, then instantaneously drying the mixture by utilizing a spray drier. Such a difficulty that the thickening is needed during production stages does not exist and the mass production is easy, unlike the case of liquid.

Description

Detailed Description of the Invention

[0001]

BACKGROUND OF THE INVENTION 1. Field of the Invention The present invention relates to beef yellow Qingshin microcapsules and a method for producing the same.

[0002]

2. Description of the Related Art Ushio Hyoseishinmaru has long been known for stroke, arteriosclerosis, hypertension, heart palpitations, dyspnea, anxiety, angina,
It is a typical herbal medicine that has been used for acute chronic astonishment, autonomic imbalance, unknown human resources, etc., and is sometimes used in the form of pills.Currently, some pharmaceutical companies have developed a liquid form and used it in the form of a liquid drug. It is commercially available.

According to the 1985 re-evaluation of drug efficacy, Ushio Hyoshinshin Maru has 263 mg of Yamayaku, 188 mg of licorice, and 9 ginseng.
4mg, Guangxi 94mg, Shinkyoku 94mg, Soybean Imperial Roll
66mg, cinnamon 66mg, Ag 66mg, peony
6 mg, Bakumon winter 56 mg, yellow rice 56 mg, toki
56 mg, windproof 56 mg, white syrup 56 mg, sago 47
mg, Chinese bellflower 47mg, Apricot kernel 47mg, Furei 47m
g, river cucumber 47 mg, beef yellow 45 mg, goose horn 3
8 mg, musk 38 mg, Borneolum 38 mg, white brick 2
One round contains 8 mg, ginseng 28 mg and the like, and this formulation may have some differences according to the beef Huangseishinmaru's formulation or the content of each component thereof.

[0004]

[Outer 1] Ushihokushinshinmaru is used as an emergency medicine or a reserve medicine, but in the case of pills, it is inconvenient for emergency patients to take, and especially for infants and children, it is difficult to take and the drug effect appears late, so there is a problem.
In order to solve such problems, liquid medicine (Korean Patent 9
0-2845) and other various forms of preparations have been developed, but it is difficult to take liquid medicines due to the inconvenience and strong taste of the crude drug extract, and it is also necessary to concentrate the extract during the manufacturing process. Mass production is difficult because of the difficulties that must be met.

[0005]

As a result of a long-term study, the present inventor has found that applying the manufacturing principle of a solid elixir to Gyuhokuseishinmaru as a method for increasing the solubility of a poorly soluble drug is convenient for carrying and taking. , Found that not only the strong taste of crude drug extract can be masked, it is easy to take and the drug effect is very quick, and also mass production is easy because there is no difficulty to concentrate during the manufacturing process. Then, the present invention was completed. Therefore, the traditional Chinese herbs, which have been in succession for generations, have been further stepped up to science, and are convenient to carry and to take, especially because the strong taste of the crude drug extract is hidden and easy to take, and the drug effect appears very quickly. In addition, it is an object of the present invention to provide a new preparation of beef huangshinshingan microcapsules and a method for producing the same, which is a new preparation that can be rapidly mass-produced because there is no concentration step during the manufacturing process.

[0006]

The principle of the present invention is as follows. If the crude drug, which is each component of the above-mentioned beef yellow Seishin-maru, is precipitated with water and ethanol, the crude drug component is dissolved and extracted in water or ethanol or a mixed solvent thereof, and this extract has an affinity for water but ethanol. If an insoluble third substance (coating substance) is added and instantaneously dried, the concentration of the coating substance increases on the surface due to the initial evaporation and a coating substance layer is formed. This coating material layer acts as a selective membrane, water passes through diffusion and evaporates, and ethanol and herbal ingredients cannot pass through this membrane, so that it remains inside and microcapsules encapsulated by the coating material are formed. To be done. Since such a phenomenon occurs efficiently in the instant drying method, it is essential to use a spray dryer. At this time, the crude drug component that is soluble in ethanol is dissolved in the ethanol layer as it is in this microcapsule, and water passes through the membrane by diffusion and evaporates, so the crude drug component that is soluble in water is suspended in the ethanol layer. Be present on the inner surface.

[0007] In the production method of the present invention, the crude drug which is each component of the above-mentioned Beef Huangseishinmaru is finely powdered as it is and suspended in water and ethanol, or it is precipitated with water and ethanol and mixed, or Each component of the above is combined and extracted with water and ethanol, and after adding appropriate coating substances, surfactants, solubilizers, flavoring agents and other necessary additives, it is dried instantaneously using a spray dryer. Then, the beef yellow Qingshin microcapsules are manufactured.

The coating substance used in the present invention includes dextrin, soluble starch, gum arabic, gelatin, sodium alginate, tragacanta gum, xanthan gum,
Guar gum and other substances that are dissolved to some extent in a mixed solvent of ethanol and water and are not dissolved in pure ethanol are used alone or in combination.

The additives used in the present invention include sodium lauryl sulfate used to make the suspension uniform,
Or a surfactant such as a polyoxyethylene series surfactant or a polyoxyethylene-polyoxypropylene addition compound series surfactant, etc., and the product does not adhere to the vessel wall in the spray dryer during spray drying. It is possible to use a stabilizer such as silicon dioxide, which is used for the product to have a moisture-proof property against moisture, and a flavoring agent which can be used in the preparation such as ranger fragrance. In addition, in order to control the physical properties of the coating, carboxymethyl cellulose and thorium, carboxymethyl cellulose calcium, crystalline cellulose, hydroxyethyl cellulose, hydroxypropyl cellulose,
It is also possible to use polymer compounds such as methyl cellulose, polyvinyl alcohol, polyvinyl pyrrolidone and the like and sugars such as sucrose, mannitol, sorbitol, fructose, lactose, glucose and galactose. It is also possible to control the physical properties of the coating by using a polymer substance and a saccharide as a mixture.

[0010] Each component of Gyuhuangseishinmaru can be made into a microcapsule form as a whole, and the ingredients of gyuhuangshinshinmaru are those which are difficult to dissolve in water, for example, substances such as beef huang, musk or wort horn. It can also be manufactured by microencapsulating the remaining ingredients and then mixing fine powders of these crude drug ingredients with the microcapsules.

The thus-produced beef yellow Qingshin microcapsules of the present invention are almost instantaneously dissolved upon contact with water to dissolve or suspend the herbal medicine component of the contents, Beef yellow Qingshin gan, so that it can be taken. It has the advantages of being dissolved at almost the same moment and exhibiting a rapid drug effect like the liquid type Ushi Huangshinshin-maru, and it has the advantage of being able to be stored for a long time and easy to carry.

The thus-produced beef yellow cypress heart microcapsules are packed in the powder form as it is, or tablets, capsules, fine granules and the like are added in the usual manner by adding usual excipients and additives. It can also be made into a dosage form.

The invention is embodied in the following examples.

[0014]

The present invention will be described in more detail below with reference to examples of the present invention and comparative examples thereof, but the present invention is not limited to these examples.

Example 1 Mountain herb 2630 mg, licorice 1880 mg, carrot 94
0mg, Guangxi 940mg, Shinkyoku 940mg, Soybean Emperor Roll 660mg, Cinnamon 660mg, Aguri 660m
g, peony 560mg, barley winter 560mg, yellow rice
560mg, Toki 560mg, Windbreak 560mg, Shiroshu 560mg, Saiko 470mg, Kikyo 470mg, Apricot kernel 470mg, Furei 470mg, Kawakyu 470
50% (v / v) ethanol 10 after crushing and combining 23 kinds of herbal medicines of mg, ram sheep horn 380mg, Borneolum 380mg, white brick 280mg, and garlic 280mg.
Extract with 0 ml of a heating circulation type extractor for 2 hours and filter. To this filtrate, 30 g of dextrin was added and dissolved, and 450 mg of beef yellow and 380 mg of musk which had been finely powdered were suspended, and then microcapsules were produced by a spraying method. This product contains 30% by weight of ethanol, and 6.6 g corresponds to one whole circle.

Example 2 The 23 kinds of crude drugs of Example 1 were crushed and combined to obtain 50% (v
/ V) After being cold-precipitated with 100 ml of ethanol for 10 days and filtered, the filtrate was again filtered with 50% (v / v) ethanol 100.
The two filtrates were combined by cold precipitation filtration in ml for 10 days. Add 50 g of dextrin to the filtrate and dissolve,
Finely powdered beef yellow 450 mg and musk 380 mg
After suspending, the microcapsules are manufactured by a spraying method.
This product contains about 35% by weight of ethanol, and 9.3 g corresponds to one whole circle.

Example 3 Twenty-five crude drugs of Example 1 were finely powdered to 10% (v /
v) 10 g of dextrin and 0.4 g of sodium lauryl sulfate in a suspension prepared by dispersing in 100 ml of ethanol.
Then, 2.0 g of sucrose is added and dissolved, and then microcapsules are manufactured by a spraying method. This product contains less than about 2% by weight of ethanol, and 3.0 g corresponds to one whole circle.

EXAMPLE 4 Twenty-three kinds of crude drugs in Example 1 except ginseng and 23 kinds of crude drugs except for musk were crushed and combined, and then extracted and filtered with 100 ml of water for 2 hours by a heating circulation type extractor. To this filtrate, 0.5 g of sodium carboxymethyl cellulose was dissolved, and 30 ml of ethanol in which 30 g of dextrin was dissolved in advance was added to obtain 450 mg of beef yellow powder and musk 380 which were finely powdered in advance.
After suspending mg, microcapsules are manufactured by a spray method. This product contains approximately 30% by weight of ethanol, 7.
4 g corresponds to one round.

Example 5 [0025] Twenty-five herbal medicines of the first example, twenty-three kinds of herbal medicines excluding musk were crushed and combined, and then 50% (v / v) ethanol 100 ml was used to heat a circulating extractor 2 Filter by time extraction. A microcapsule is produced by a spraying method using a solution obtained by adding 30 g of dextrin to the filtrate and dissolving it, and 450 mg of beef yellow and 380 mg of musk which are finely powdered in advance are added thereto. This product contains about 35% by weight of ethanol, and 7.0 g is equivalent to one whole circle.

Example 6 Twenty-two kinds of crude drugs of Example 1 except for Gyu-Yo, Musk and Borneolum were crushed and combined to obtain 30% (v / v).
Extract and filter with 100 ml of ethanol for 2 hours with a heating circulation type extractor. To this filtrate, 380 mg of Borneolum, 20 g of dextrin and 0.3 g of gelatin are put and dissolved, and 450 mg of beef yellow and 380 mg of musk which have been finely powdered in advance are suspended, and then microcapsules are produced by a spraying method. This product contains about 5% by weight of ethanol, and 4.7 g is 1
It is the corresponding amount.

Example 7 25 kinds of crude drugs of Example 1 22 kinds of crude drugs except beef yellow, musk and camphor were ground and combined, and then 25% (v / v)
Extract and filter with 100 ml of ethanol for 2 hours with a heating circulation type extractor. 380 mg of Borneolum and 1 of dextrin were added to this filtrate.
5g, 0.02g of silicon dioxide and 0.4g of sodium lauryl sulfate were added and dissolved, and beef powder 4 was finely powdered in advance.
After suspending 50 mg and 380 mg of musk, microcapsules are produced by a spraying method. This product contains about 2% by weight of ethanol, and 4.2 g corresponds to one whole circle.

Example 8 The microcapsules (400 mg) prepared in Example 7 are filled with a lubricant such as talc (about 4 mg) to fill the capsules.

Example 9 The microcapsules (800 mg) prepared in Example 7 are tableted by adding an additive such as magnesium stearate (about 6 mg) into tablets.

Example 10 The microcapsules (4.2 g) prepared in Example 7 are filled in a bag by adding an additive such as talc (0.04 g).

Example 11 The microcapsules prepared in Example 7 (4.2 g) are bottled with an additive such as magnesium stearate (0.04 g).

Experimental Example 1: Stability experiment with time-dependent change of beef yellow cypress heart microcapsules 1) Experimental method: The trial product of Example 11 was stored at room temperature for 2 years under UV irradiation.
1 amp-45 degrees, 45 degrees and 37 degrees-RH 75% was stored for 6 months and 60 degrees for 2 months, and the properties, taste, solubility and content were tested. The appearance is macroscopic, the taste is scrutinized, and the solubility is purified water and 50 mg of 1 liquid (Korean drug).
The content test was conducted by the Public Health Center Notification No. 90-42 (90.6.5.
According to the Korean National Standards), bovine yellow quantitation was determined with bound bilirubin, yellow quantitation with baicalin, and Borneolum with isoborneol and norborneol. 2) Experimental results: As shown in Table 1, beef yellow Qingshin microcapsules are not affected by light, humidity and temperature and are stable at room temperature for 2 years.

[0027]

[Table 1]

[0028]

INDUSTRIAL APPLICABILITY The beef yellow cypress round microcapsule of the present invention is a new preparation which is convenient to carry and to take, in particular, the strong taste of the crude drug extract is masked and is easy to take, and the drug effect is exhibited very quickly. Method is suitable for rapid mass production of these microcapsules.

Claims (11)

[Claims] 1. Mountain herbs, licorice, carrots, ginger yellow, Shinkyoku, soybean roll, cinnamon skin, Ag, peony, barley winter, yellow rice, toki, windbreak,
White powder, saiko, bellflower, apricot kernel, 苯 苓, river cucumber, beef yellow, ginseng horn, musk, borneol, white brick, and licorice are finely pulverized and added to water and alcohol. Beef yellowish heart microcapsules obtained by spray-drying by dissolving and dissolving with usual additives or adding usual additives. 2. One or more coating substances selected from coating substances such as dextrin, gum arabic, gelatin, soluble starch, sodium alginate, tragacanta gum, xanthan gum and guar gum are added and dissolved, and spray-dried as it is or The beef yellow cypress heart microcapsule according to claim 1, obtained by spray-drying a conventional additive selected from a surfactant, a solubilizing agent, a flavoring agent, a stabilizer, a suspending agent and the like. 3. Mountain herb, licorice, carrot, ginger yellow, sacred song, soybean roll, cinnamon skin, Ag, peony, barley winter, yellow rice, toki, windbreak,
White powder, saiko, bellflower, apricot kernel, 苯 苓, river cucumber, beef yellow, ginseng horn, musk, borneol, white brick, and licorice are finely pulverized and added to water and alcohol. A method for producing microcapsules of beef yellow quince, which is characterized in that the microcapsules are dissolved by spraying and dried by spraying with or without addition of usual additives. 4. One or more coating substances selected from coating substances such as dextrin, gum arabic, gelatin, soluble starch, sodium alginate, tragacanta gum, xanthan gum and guar gum are added and dissolved, and spray-dried as it is or The method for producing beef yellow Qingshin microcapsules according to claim 3, wherein usual additives selected from surfactants, solubilizers, flavors, stabilizers, suspending agents and the like are further added and spray-dried. 5. Mountain herbs, licorice, carrots, ginger yellow, sacred songs, soybean rolls, cinnamon skin, Ag, peony, barley winter, yellow rice, toki, windbreak,
Fine powder of some crude drugs selected from Shirasu, Saiko, Kikyo, Apricot kernels, 苯 苓, Kawakyu, Beef yellow, yan mutton, musk, dragon brain, white brick, and kangaraku Microbeads obtained from the obtained liquid by finely powdering the rest of the herbal medicine, adding a coating substance to dissolve it, and adding no usual additives or adding ordinary additives and spray-drying. 6. One or more coating substances selected from coating substances such as dextrin, gum arabic, gelatin, soluble starch, sodium alginate, tragacanta gum, xanthan gum and guar gum are added and dissolved, and then spray-dried or an interface. The beef yellow Qingshin microcapsule according to claim 5, which is produced by further adding an additive selected from an activator, a solubilizing agent, a flavoring agent, a stabilizer, a suspending agent and the like, and spray-drying. 7. Mountain herbs, licorice, carrots, ginger yellows, Shinkyoku, soybean rolls, cinnamon, Ag, peony, barley winter, yellow rice, toki, windbreak,
Fine powder of some crude drugs selected from Shirasu, Saiko, Kikyo, Apricot kernels, 苯 苓, Kawakyu, Beef yellow, yan mutton, musk, dragon brain, white brick, and kangaraku The remaining herbal medicines are finely pulverized and added to the obtained liquid, and a coating substance is added and dissolved therein, and ordinary additives are not added or ordinary additives are added and spray-dried. Manufacturing method. 8. One or more coating substances selected from coating substances such as dextrin, gum arabic, gelatin, soluble starch, sodium alginate, tragacanta gum, zantane gum and guar gum are added and dissolved, and then spray-dried, or 8. The method for producing beef yellow Qingshin microcapsules according to claim 7, wherein an additive selected from a surfactant, a solubilizing agent, a flavoring agent, a stabilizer, a suspending agent and the like is added and spray-dried. 9. Mountain herbs, licorice, carrots, ginger yellow, sacred songs, soybean rolls, cinnamon skin, Ag, peony, barley winter, yellow dust, toki, windbreak,
Fine powder of some crude drugs selected from Shirasu, Saiko, Kikyo, Apricot kernels, 苯 苓, Kawakyu, Beef yellow, yan mutton, musk, dragon brain, white brick, and kangaraku Beef yellow Seishin micro was prepared by adding the coating substance to the obtained liquid and dissolving it, and adding the usual crude drug to the microcapsules obtained by spray-drying with or without adding the usual additives. capsule. 10. A coating substance of at least one selected from dextrin, gum arabic, gelatin, soluble starch, sodium alginate, tragacanta gum, zantane gum, guar gum, etc. is added, dissolved and spray-dried, or a surfactant, The microbeads of Gyuhuang Qingshin according to claim 9, wherein the rest of the crude drug is finely powdered and added to microcapsules obtained by adding usual additives selected from a solubilizing agent, a flavoring agent, a stabilizer, a suspending agent, etc. and spray-drying. capsule. 11. Tablets and capsules prepared by adding the excipients conventionally used in pharmaceutically to the microcapsules of Huangjing Qingshin according to any one of claims 1, 2, 5, 6, 9 or 10 by a conventional pharmaceutical method. And a tablet, capsule or fine granule of beef huangshinshin microcapsule manufactured in the form of fine granule.