CN1082421A - Clear away heart-fire microencapsulation and manufacture method thereof - Google Patents

Clear away heart-fire microencapsulation and manufacture method thereof Download PDF

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Publication number
CN1082421A
CN1082421A CN 93105742 CN93105742A CN1082421A CN 1082421 A CN1082421 A CN 1082421A CN 93105742 CN93105742 CN 93105742 CN 93105742 A CN93105742 A CN 93105742A CN 1082421 A CN1082421 A CN 1082421A
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radix
microencapsulation
fire
add
film forming
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金钟国
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Abstract

The invention relates to miniature Bezoar Sedative Pills and manufacture method thereof.
Feature of the present invention is with after the direct attritive powderization of crude drug as each composition of Bezoar Sedative Pills; be suspended in water and the ethanol; after water and the ethanol lixiviate; mix with its mixing or with these each compositions; after water and the ethanol lixiviate; after adding other necessary additives such as suitable film forming matter, cosolvent, spice, utilize spray dryer to make it the dry clear away heart-fire microencapsulation of making in instantaneous ground.
Clear away heart-fire microencapsulation of the present invention carries and taking convenience; particularly because the hidden overpowering odor of crude drug extract; so be easy to take; not only promptly present drug effect; and it is different with liquor; removed the big concentration step of difficulty in manufacturing engineering, so be easy to mass production and can long preservation.

Description

Clear away heart-fire microencapsulation and manufacture method thereof
The invention relates to clear away heart-fire microencapsulation and manufacture method thereof.
Bezoar Sedative Pills has been exactly the representative Chinese medicine of disease such as be used in that apoplexy, arteriosclerosis, hypertension, tachycardia, dyspnea, spirit are uneasy, heart strand disease, acute and chronic wind-engaging, autonomic nerve disorder, occurrences in human life are not known since very early; often be to use with the form of pill; the pharmacy producer of a part develops the form of liquid now, and is commercially available with the form of liquor.
According to 1985 years to the drug effect of Bezoar Sedative Pills evaluation results once more; contain Rhizoma Dioscoreae 236mg in each ball; Radix Glycyrrhizae 188mg; Radix Ginseng 94mg; Pollen Typhae 94mg; Massa Medicata Fermentata 94mg; the Semen sojae atricolor emperor rolls up 66mg; Cortex cinnamomi japonici (Ramulus Cinnamomi) 66mg; Colla Corii Asini 66mg; Radix Paeoniae 56mg; Radix Ophiopogonis 6mg; Radix Scutellariae 56mg; Radix Angelicae Sinensis 56mg; Radix Saposhnikoviae 56mg; Rhizoma Atractylodis Macrocephalae 56mg; Radix Bupleuri 47mg; Radix Platycodonis 47mg; Semen Armeniacae Amarum 47mg; Poria 47mg; Rhizoma Chuanxiong 47mg; Calculus Bovis 45mg; Cornu Saigae Tataricae 38mg; Moschus 38mg; Borneolum Syntheticum 38mg; Radix Ampelopsis 28mg is Ji Gan Ginger 28mg etc., herein can according to the prescription of Bezoar Sedative Pills or wherein the content of each composition some differences are arranged.
Bezoar Sedative Pills is as the standing medicine of emergency and give fully medicine and using, but under the situation of pill, very inconvenient for taking of emergency patient, particularly child and children's take difficulty especially, the problem that then has drug effect not bring into play very soon.In order to solve the above problems, developed the preparation of liquor various forms such as (Republic of Korea special permission 90-2845) at present already, but the form inconvenience of liquor is carried and because the intensive abnormal smells from the patient of crude drug extract, cause and take difficulty, in addition must concentrated extract in producing process, so mass production is the comparison difficulty.
The present inventor is through long result of study; found as a kind of method that increases the insoluble drug dissolubility it is that the manufacturing principle of solid being joined (elixir) is when being applied on the Bezoar Sedative Pills; then be easy to carry and take; the overpowering odor of particularly can be hidden living the crude drug extract; not only be easy to take and extremely promptly bring into play its drug effect; and overcome in producing process must spissated difficulty; so can the easily mass-produced fact; finished the present invention; therefore; the typical Chinese medicine Bezoar Sedative Pills that the objective of the invention is to make generations hand down mutually is further scientific; and provide and carry and taking convenience; the particularly hidden overpowering odor of crude drug extract; be easy to take; not only present drug effect extremely rapidly, and cancelled the concentration process in the pharmacy operation, can promptly mass-produced novel formulation Bezoar Sedative Pills microencapsulation and manufacture method thereof.
Manufacturing principle of the present invention is as follows.During the crude drug of water and the various compositions of the above-mentioned Bezoar Sedative Pills of ethanol lixiviate; then the dissolved extraction of crude drug composition is in water and ethanol or its mixed solvent; adding in this extract has affinity and don't is dissolved in alcoholic acid the third material (film forming matter) water; make it instantaneous drying; by the initial stage evaporation concentration of its lip-deep film forming matter is increased, formed film forming material layer.This film forming material layer plays the effect of selective membrane, and owing to water evaporates by diffusing through this film, but ethanol and crude drug composition can not pass this film, so remain in inside, have generated the microencapsulation of being wrapped by film forming matter.This phenomenon is owing to just more effective with instantaneous drying mode, so must use spray dryer.At this moment, be dissolved in alcoholic acid crude drug composition in this microencapsulation and just directly be dissolved in the alcohol layer, because water is evaporated by diffusing through film, so be dissolved in the inner surface that crude drug composition in the water is suspended in the alcohol layer or is present in film.
Manufacture method of the present invention is each of above-mentioned Bezoar Sedative Pills can be become the crude drug of branch; directly be processed into be suspended in water and the ethanol behind the fine powder or water and ethanol lixiviate after mix or these each composition lumped together; behind water and the alcohol extraction; after adding other necessary additives such as suitable film forming matter, surfactant, cosolvent, flavouring agent; utilize spray dryer to make it instantaneous drying, make the method for clear away heart-fire microencapsulation.
The film forming matter that uses as the present invention can be used alone or as a mixture dextrin, soluble starch, arabic gum, gelatin, sodium alginate, tragacanth gum, carbon residue glue, more skin ulcer glue and other the mixed solvent to the second alcohol and water have the material that to a certain degree dissolves and don't be dissolved in straight alcohol.
Additive as the present invention's use, in the time of can using for the surfactant of the surfactant that makes uniform sodium lauryl sulphate of suspension or polyethylene glycol oxide series and even polyethylene glycol oxide-polypropylene oxide additive compound series of surfactants class and spray drying, do not make product attached on the wall in the spray dryer and for making product have and as Colophonium, being used for flavouring agent etc. on the preparation to the moistureproof moist silica-based stabilizing agent that uses of moisture content.In addition, in order to regulate the physical property of peplos, also can use the saccharide of classes such as the macromolecular compound of classes such as sodium carboxymethyl cellulose, carboxymethylcellulose calcium, crystalline cellulose, hydroxy ethyl cellulose, hydroxy propyl cellulose, methylcellulose, polyvinyl alcohol, polyvinylpyrrolidone and white sugar, mannose, sorbose, fructose, lactose, glucose, galactose.The physical property that can regulate peplos is used in mixing by polymer substance and saccharide.
Whole compositions can be made the form of microencapsulation in original each composition right side of clear away heart-fire; also can be for being difficult to the water soluble components class in the original composition of clear away heart-fire; as class materials such as Calculus Bovis, Moschus or Cornu Saigae Tataricae; can be after other composition microencapsulations, the attritive powder of these crude drug compositions mixed with capsule make.
The clear away heart-fire microencapsulation of the present invention of Zhi Zaoing has following advantage like this; promptly because when contacting with water; almost can dissolve in moment; make original each crude drug composition of clear away heart-fire of its content dissolved or suspended; so just dissolved with the moment of taking much at one; have and promptly show drug effect the former medicine of the liquor of elephant type clear away heart-fire, but and also have long preservation, advantage such as be easy to carry.
The clear away heart-fire microencapsulation of Zhi Zaoing can perhaps also can add by behind normal excipient and the additive etc. directly with the packaged of powder like this, makes forms such as tablet and capsule according to the method for routine.
Below specify the present invention with embodiment.
Embodiment 1
With Rhizoma Dioscoreae 2630mg, Radix Glycyrrhizae 1880mg, Radix Ginseng 940mg, Pollen Typhae 940mg, Massa Medicata Fermentata 940mg, the Semen sojae atricolor emperor rolls up 660mg, Cortex cinnamomi japonici (Ramulus Cinnamomi) 660mg, Colla Corii Asini 660mg, Radix Paeoniae 560mg, Radix Ophiopogonis 560mg, Radix Scutellariae 560mg, Radix Angelicae Sinensis 560mg, Radix Saposhnikoviae 560mg, Rhizoma Atractylodis Macrocephalae 560mg, Radix Bupleuri 470mg, Radix Platycodonis 470mg, Semen Armeniacae Amarum 470mg, Poria 470mg, Rhizoma Chuanxiong 470mg, Cornu Saigae Tataricae 380mg, Borneolum Syntheticum 380mg, Radix Ampelopsis 280mg, 23 kinds of crude drugs of Ji Gan Ginger 280mg are pulverized, after the mixing, use 50%(v/v) 100ml ethanol extracted 2 hours in heat cycles formula extractor, filters.In this filtrate, add and dissolving 30g dextrin, behind the Calculus Bovis 450mg and Moschus 380mg of the powdered in advance of wherein suspending, make microencapsulation with nebulization.These goods contain 30%(weight) ethanol, per 1 ball a great deal of is 6.6g.
Embodiment 2
After pulverizing 23 kinds the crude drug of embodiment 1, mix, and use 50%(v/v) 100ml ethanol merceration 10 days, after the filtration, filtrate is used 50%(v/v once more) 100ml ethanol merceration 10 days, after the filtration, merge two filtrate.In this filtrate, add the 50g dextrin, and dissolving, behind the Calculus Bovis 450mg and Moschus 380mg of the powdered in advance of wherein suspending, make microencapsulation with nebulization.These goods contain the 35%(weight of having an appointment) ethanol, the suitable 9.3g of every ball.
Embodiment 3
After 25 kinds of crude drug attritive powderizations with embodiment 1, making it to be dispersed in 10%(v/v) in the 100ml ethanol and make suspension, to wherein adding 10g dextrin, 0.4g sodium lauryl sulphate and 2.0g white sugar, microencapsulation is made with nebulization in the dissolving back.The alcoholic acid content of these goods is less than 2%(weight), the suitable 3.0g of every ball.
Embodiment 4
Pulverize 23 kinds of crude drugs removing Calculus Bovis and Moschus in 25 kinds of crude drugs among the embodiment, after the mixing, in the heat cycles extractor, extract filtration 2 hours with 100ml water.The sodium carboxy methyl cellulose of dissolving 0.5g adds the 30ml ethanol dissolved the 30g dextrin in advance in this solution, and resuspending behind the Calculus Bovis 450mg and Moschus 380mg of attritive powderization, is made microencapsulation with spray pattern in advance.These goods contain the 30%(weight of having an appointment) the suitable 7.4g of the every ball of ethanol.
Embodiment 5
Pulverize among the embodiment 1 23 kinds of crude drugs removing Calculus Bovis and Moschus in 25 kinds of crude drugs, after the mixing, use 50%(v/v) 100ml ethanol, extraction is 2 hours in heat cycles formula extractor, and filtration.Add the 30g dextrin in this filtrate, the solution after the spraying dissolving is made microencapsulation, to wherein adding the Calculus Bovis 450mg and the Moschus 380mg of attritive powderization in advance.Contain ethanol 35% in these goods approximately, the suitable 7.0g of per 1 ball.
Embodiment 6
Pulverize 22 kinds of crude drugs removing Calculus Bovis, Moschus and Borneolum Syntheticum in 25 kinds of crude drugs among the embodiment 1, after the mixing, use 30%(v/v) 100ml ethanol, extraction is 2 hours in heat cycles formula extractor, and filters.In this filtrate, add Borneolum Syntheticum 380mg and dextrin 20g and gelatin 0.3g, dissolving, and behind the Calculus Bovis 450mg and Moschus 380mg of the attritive powderization in advance of suspending, make microencapsulation with nebulization.These goods contain the 5%(weight of having an appointment) ethanol, the suitable 4.7g of per 1 ball.
Embodiment 7
Pulverize among the embodiment 1 22 kinds of crude drugs removing Calculus Bovis, Moschus and Borneolum Syntheticum in 25 kinds of crude drugs, after the mixing, use 25%(v/v) 100ml ethanol, extraction is 2 hours in heat cycles formula extractor, and filtration.In this filtrate, add Borneolum Syntheticum 380mg, dextrin 15g, silicon dioxide 0.02g and sodium lauryl sulphate 0.4g and dissolve, behind the Calculus Bovis 450mg and Moschus 380mg of the attritive powderization in advance of suspending, make microencapsulation with nebulization.These goods contain 2%(weight) ethanol, the suitable 4.2g of per 1 ball.
Embodiment 8
After in the microencapsulation (400mg) that embodiment 7 makes, adding Pulvis Talci (about 4mg) series lubricant agent, be filled in the capsule.
Embodiment 9
In the microencapsulation (800mg) that embodiment 7 makes, add the additive of magnesium stearate (about 6mg) class, behind the tabletting, become tablet.
Embodiment 10
In the microencapsulation (4.2g) that embodiment 7 makes, behind the additive of adding Pulvis Talci (0.04g) class, be filled in the bag.
Embodiment 11
In the microencapsulation (4.2g) that embodiment 7 makes, behind the additive of adding magnesium stearate (0.04g) class, be filled in the bottle.
Experimental example 1:
The time dependent stability experiment of clear away heart-fire microencapsulation.
1) experimental technique: the preproduction of embodiment 11 was at room temperature taken care of 2 years, under UV lamp-45 degree, 45 degree and 37 degree-RH, 75% condition 6 months certainly, keeping is 2 months under 60 degree, and its character state, taste, dissolubility and content are experimentized.The character state detects by an unaided eye, taste can test have how much amount is by dispersing and dissolving for the goods of suitable 1 ball amount with the mono-component liquid (Republic of Korea's distiller) of distilled water and 50ml with trial test, dissolubility.The content test is according to health care institute's bulletin 90-42 number (90.6.5, Republic of Korea's official compendium), and Calculus Bovis quantitatively is to use the conjunction type bilirubin, and Radix Scutellariae quantitatively is to use baicalin, and Borneolum Syntheticum carries out respectively quantitatively with isoborneol and norborneol.
2) experimental result: from following data as can be seen the clear away heart-fire microencapsulation do not receive light, humidity and Temperature Influence greatly, at room temperature can stablize 2 years.

Claims (11)

1, a kind of clear away heart-fire microencapsulation; this capsule is with Rhizoma Dioscoreae, Radix Glycyrrhizae, Radix Ginseng, Pollen Typhae, Semen sojae atricolor emperor volume, Cortex cinnamomi japonici (Ramulus Cinnamomi), Colla Corii Asini, Radix Paeoniae, Radix Ophiopogonis, Radix Scutellariae, Radix Angelicae Sinensis, Radix Saposhnikoviae, the Rhizoma Atractylodis Macrocephalae, Radix Bupleuri, Radix Platycodonis, Semen Armeniacae Amarum, Poria, Rhizoma Chuanxiong, Calculus Bovis, Cornu Saigae Tataricae, Moschus, Borneolum Syntheticum, Radix Ampelopsis, Ji Gan Ginger; after the attritive powderization; lixiviate in water and ethanol and add film forming matter in the solution that obtains and make it dissolving; not adding common additive or adding under the condition of common additive, obtain after the spray drying.
2, according to the clear away heart-fire microencapsulation of claim 1; wherein can add the film forming matter of selecting by in the film forming matters such as dextrin, arabic gum, gelatin, soluble starch, sodium alginate, tragacanth gum, carbon residue glue and the skin ulcer glue of healing more than a kind; make it to dissolve, direct spray drying or add the common additive of selecting by in surfactant, cosolvent, flavouring agent, stabilizing agent and the suspending agent etc., carry out spray drying and obtain.
3, the manufacture method of clear away heart-fire microencapsulation; it is characterized in that after Rhizoma Dioscoreae, Radix Glycyrrhizae, Radix Ginseng, Pollen Typhae, Massa Medicata Fermentata, Semen sojae atricolor emperor volume, Cortex cinnamomi japonici (Ramulus Cinnamomi), Colla Corii Asini, Radix Paeoniae, Radix Ophiopogonis, Radix Scutellariae, Radix Angelicae Sinensis, Radix Saposhnikoviae, the Rhizoma Atractylodis Macrocephalae, Radix Bupleuri, Radix Platycodonis, Semen Armeniacae Amarum, Poria, Rhizoma Chuanxiong, Calculus Bovis, Cornu Saigae Tataricae, Moschus, Borneolum Syntheticum, Radix Ampelopsis, Ji Gan Ginger, the fine powder lampization; lixiviate in water and ethanol and add film forming matter in the solution that obtains; make it dissolving; not adding common additive or adding under the condition of common additive, obtain after the spray drying.
4, according to the manufacture method of the clear away heart-fire microencapsulation in the claim 3; it is characterized in that to add the film forming matter of selecting by in the film forming matters such as dextrin, arabic gum, gelatin, soluble starch, sodium alginate, tragacanth gum, carbon residue glue and the skin ulcer glue of healing more than a kind; make it dissolving, directly spray drying or further the adding carry out spray drying by the common additive of selecting in surfactant, cosolvent, flavouring agent, the stabilizing agent etc.
5; a kind of clear away heart-fire microencapsulation; this capsule is with by Rhizoma Dioscoreae; Radix Glycyrrhizae; Radix Ginseng; Pollen Typhae; Massa Medicata Fermentata; Semen sojae atricolor emperor volume; Cortex cinnamomi japonici (Ramulus Cinnamomi); Colla Corii Asini; Radix Paeoniae; Radix Ophiopogonis; Radix Scutellariae; Radix Angelicae Sinensis; Radix Saposhnikoviae; the Rhizoma Atractylodis Macrocephalae; Radix Bupleuri; Radix Platycodonis; Semen Armeniacae Amarum; Poria; Rhizoma Chuanxiong; Calculus Bovis; Cornu Saigae Tataricae; Moschus; Borneolum Syntheticum; Radix Ampelopsis is Ji after a part of crude drug attritive powderization of selecting among the Gan Ginger; lixiviate in water and ethanol and add remaining crude drug after the attritive powderization in the solution that obtains; add film forming matter again; make it dissolving; not adding common additive or adding under the condition of common additive, obtain after the spray drying.
6, according to the clear away heart-fire microencapsulation in the claim 5; wherein can add the film forming matter of selecting by in the film forming matters such as dextrin, arabic gum, gelatin, soluble starch, sodium alginate, tragacanth gum, carbon residue glue and the skin ulcer glue of healing more than a kind; make it dissolving; carry out spray drying or further add, make it spray drying and make by the additive of selecting in surfactant, cosolvent, flavouring agent, stabilizing agent and the suspending agent.
7; it is characterized in that by Rhizoma Dioscoreae according to the manufacture method of clear away heart-fire microencapsulation; Radix Glycyrrhizae; Radix Ginseng; Pollen Typhae; Shenfeng; Semen sojae atricolor emperor volume; Cortex cinnamomi japonici (Ramulus Cinnamomi); Colla Corii Asini; Radix Paeoniae; Radix Ophiopogonis; Radix Scutellariae; Radix Angelicae Sinensis; Radix Saposhnikoviae; the Rhizoma Atractylodis Macrocephalae; Radix Bupleuri; Radix Platycodonis; Semen Armeniacae Amarum; Poria; Rhizoma Chuanxiong; Calculus Bovis; Cornu Saigae Tataricae; Moschus; Borneolum Syntheticum; Radix Ampelopsis is Ji after a part of crude drug attritive powderization of selecting among the Gan Ginger; lixiviate is in water and ethanol; in the liquid that obtains, add the crude drug that is left after the attritive powderization; add film forming matter again; make it dissolving; not adding common additive or adding under the common additive, obtain after the spray drying.
8, according to the manufacture method of the clear away heart-fire microencapsulation in the claim 7; it is characterized in that to add the film forming matter of selecting by in the film forming matters such as dextrin, arabic gum, gelatin, soluble starch, sodium alginate, tragacanth gum, carbon residue glue and the skin ulcer glue of healing more than a kind; make it to dissolve and carry out spray drying or add, make it spray drying and make by the additive of selecting in surfactant, cosolvent, flavouring agent, stabilizing agent and the suspending agent.
9; the manufacture method of clear away heart-fire microencapsulation; wherein be with by Rhizoma Dioscoreae; Radix Glycyrrhizae; Radix Ginseng; Pollen Typhae; Massa Medicata Fermentata; Semen sojae atricolor emperor volume; Cortex cinnamomi japonici (Ramulus Cinnamomi); Colla Corii Asini; Radix Paeoniae; Radix Ophiopogonis; Radix Scutellariae; Radix Angelicae Sinensis; Radix Saposhnikoviae; the Rhizoma Atractylodis Macrocephalae; Radix Bupleuri; Radix Platycodonis; Semen Armeniacae Amarum; Poria; Rhizoma Chuanxiong; Calculus Bovis; Cornu Saigae Tataricae; Moschus; Borneolum Syntheticum; Radix Ampelopsis is Ji after the fine efflorescence of selecting among the Gan Ginger of a part of crude drug; lixiviate is in water and alcohol; and the adding film forming matter makes it dissolving in the liquid that obtains; do not adding common additive or adding under the condition of common additive after the spray drying; obtain microencapsulation, again in this microencapsulation that adds after the crude drug attritive powderization with remainder.
10, according to the clear away heart-fire microencapsulation in the claim 9; wherein can add the film forming matter of selecting by dextrin, arabic gum, gelatin, soluble starch, sodium alginate, tragacanth gum, carbon residue glue and the skin ulcer glue of healing etc. more than a kind; make it dissolving; carry out spray drying or adding by the common additive of selecting in surfactant, cosolvent, flavouring agent, stabilizing agent and the suspending agent; make it spray drying and obtain microencapsulation, will add in this microencapsulation after the remaining crude drug attritive powderization again.
11, the granula subtilis of clear away heart-fire microencapsulation, capsule and tablet; wherein be to add pharmaceutically spendable usually excipient in claim 1,2,5,6 and 9,10 clear away heart-fire microencapsulation, the compositions; with the method for common pharmaceutics, make the dosage form of tablet, capsule and granula subtilis.
CN 93105742 1992-04-17 1993-04-16 Clear away heart-fire microencapsulation and manufacture method thereof Pending CN1082421A (en)

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
KR6424/92 1992-04-17
KR1019920006424A KR930021196A (en) 1992-04-17 Uhwang Cheongsim microcapsules and its manufacturing method

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JP2001181192A (en) * 1999-12-24 2001-07-03 Alps Yakuhin Kogyo Kk Moisture-proof galenical extract
US6521269B2 (en) * 2000-06-01 2003-02-18 Theralife, Inc. Compositions and methods for enhancing therapeutic effects
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