CN103549422A - Konjac controlled-release colloidal particle - Google Patents

Konjac controlled-release colloidal particle Download PDF

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Publication number
CN103549422A
CN103549422A CN201310533378.3A CN201310533378A CN103549422A CN 103549422 A CN103549422 A CN 103549422A CN 201310533378 A CN201310533378 A CN 201310533378A CN 103549422 A CN103549422 A CN 103549422A
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konjaku
coating material
controlled release
controlled
release
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张芝庭
张涛涛
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GUIZHOU SHENQI DRUG RESEARCH INSTITUTE
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GUIZHOU SHENQI DRUG RESEARCH INSTITUTE
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    • AHUMAN NECESSITIES
    • A23FOODS OR FOODSTUFFS; TREATMENT THEREOF, NOT COVERED BY OTHER CLASSES
    • A23LFOODS, FOODSTUFFS, OR NON-ALCOHOLIC BEVERAGES, NOT COVERED BY SUBCLASSES A21D OR A23B-A23J; THEIR PREPARATION OR TREATMENT, e.g. COOKING, MODIFICATION OF NUTRITIVE QUALITIES, PHYSICAL TREATMENT; PRESERVATION OF FOODS OR FOODSTUFFS, IN GENERAL
    • A23L2/00Non-alcoholic beverages; Dry compositions or concentrates therefor; Their preparation
    • A23L2/02Non-alcoholic beverages; Dry compositions or concentrates therefor; Their preparation containing fruit or vegetable juices
    • AHUMAN NECESSITIES
    • A23FOODS OR FOODSTUFFS; TREATMENT THEREOF, NOT COVERED BY OTHER CLASSES
    • A23LFOODS, FOODSTUFFS, OR NON-ALCOHOLIC BEVERAGES, NOT COVERED BY SUBCLASSES A21D OR A23B-A23J; THEIR PREPARATION OR TREATMENT, e.g. COOKING, MODIFICATION OF NUTRITIVE QUALITIES, PHYSICAL TREATMENT; PRESERVATION OF FOODS OR FOODSTUFFS, IN GENERAL
    • A23L33/00Modifying nutritive qualities of foods; Dietetic products; Preparation or treatment thereof
    • A23L33/20Reducing nutritive value; Dietetic products with reduced nutritive value
    • A23L33/21Addition of substantially indigestible substances, e.g. dietary fibres
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K36/00Medicinal preparations of undetermined constitution containing material from algae, lichens, fungi or plants, or derivatives thereof, e.g. traditional herbal medicines
    • A61K36/18Magnoliophyta (angiosperms)
    • A61K36/88Liliopsida (monocotyledons)
    • A61K36/888Araceae (Arum family), e.g. caladium, calla lily or skunk cabbage
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K47/00Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient
    • A61K47/30Macromolecular organic or inorganic compounds, e.g. inorganic polyphosphates
    • A61K47/32Macromolecular compounds obtained by reactions only involving carbon-to-carbon unsaturated bonds, e.g. carbomers, poly(meth)acrylates, or polyvinyl pyrrolidone
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K47/00Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient
    • A61K47/30Macromolecular organic or inorganic compounds, e.g. inorganic polyphosphates
    • A61K47/36Polysaccharides; Derivatives thereof, e.g. gums, starch, alginate, dextrin, hyaluronic acid, chitosan, inulin, agar or pectin
    • A61K47/38Cellulose; Derivatives thereof
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K9/00Medicinal preparations characterised by special physical form
    • A61K9/14Particulate form, e.g. powders, Processes for size reducing of pure drugs or the resulting products, Pure drug nanoparticles
    • A61K9/16Agglomerates; Granulates; Microbeadlets ; Microspheres; Pellets; Solid products obtained by spray drying, spray freeze drying, spray congealing,(multiple) emulsion solvent evaporation or extraction

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  • Health & Medical Sciences (AREA)
  • Chemical & Material Sciences (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Engineering & Computer Science (AREA)
  • Natural Medicines & Medicinal Plants (AREA)
  • Medicinal Chemistry (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Epidemiology (AREA)
  • Animal Behavior & Ethology (AREA)
  • General Health & Medical Sciences (AREA)
  • Public Health (AREA)
  • Veterinary Medicine (AREA)
  • Nutrition Science (AREA)
  • Mycology (AREA)
  • Food Science & Technology (AREA)
  • Polymers & Plastics (AREA)
  • Inorganic Chemistry (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Alternative & Traditional Medicine (AREA)
  • Biotechnology (AREA)
  • Botany (AREA)
  • Medical Informatics (AREA)
  • Microbiology (AREA)
  • Medicinal Preparation (AREA)

Abstract

The invention relates to a konjac controlled-release colloidal particle. The colloidal particle is prepared from fine konjac powder through a gastric-soluble and fat-soluble controlled-release coating material according to a conventional coating and pelleting technology. The invention provides the konjac controlled-release colloidal particle which is used in beverage and solves the problems that a fine konjac powder health-care product in the prior art is high in side effects, and bad in absorption effect; the konjac controlled-release colloidal particle is fewer in side effects, good to absorb, can be used in beverage, and is beneficial to human digestion and absorption after being acted under the gastric acid environment, and helpful to enhancing the effect of the fine konjac powder.

Description

A kind of konjaku controlled release micelle
Technical field
The present invention relates to a kind of konjaku controlled release micelle, belong to field of health care products.
Background technology
(formal name used at school: Amorphophalmskonjac/Amorphophallus), You Cheng Amorphophalus rivieri taro, is commonly called as konjaku, Thunder God rifle, Kun Betel is perennial root stem tuber herbaceous plant to konjaku Wei Amorphophalus rivieri.The underground stem tuber of konjaku is oblate, just like large size water chestnut, nutrition is very abundant, contains the mineral matter elements such as multivitamin and potassium, phosphorus, selenium, also contains the SKGM that necessary for human is wanted, and has the feature of low in calories, low fat and high-cellulose.In the prior art, konjaku is used for food processing industry, and for extracting glucomannan composition.In the prior art, konjaku powder is generally used in food processing.Konjaku powder is added to water gelatinization to be become transparent, colourless, tasteless dextrin and adds in grain and food, can increase its viscosity, elasticity and extensibility, its water imbibition is strong, color and luster, mouthfeel are good, water conservation, fresh-keeping, storage tolerance, and lower, effective than the cost that adds other vegetable protein, Chicken Albumin and starch; As products such as konjak noodle, konjaku bread, konjaku cake and konjaku vermicelli.In konjaku, the glucomannan of content maximum has powerful expansive force, has the sticky toughness that surpasses any natural plant gum, both can fill stomach and intestine, eliminates hunger, again because of institute's heat content seldom, therefore can control body weight, have the effect of lipopenicillinase.Therefore, the value of konjaku maximum is its glucomannan composition at present, is unique Main Economic crop that glucomannans can be provided in a large number.Yet, how to realize the convenient utilization of active ingredient in konjaku and effectively absorb and become a difficult problem of the prior art.
According to < < Compendium of Materia Medica > >, record, before more than 2000 year, our ancestors just cure the disease with konjaku.Konjaku contains several amino acids and mineral trace element and abundant food fiber, and to preventing and treating diabetes, hypertension has special efficacy.Konjaku low-heat, low fat, low sugar, be applicable to prevention and treat the crowd of colon cancer, breast cancer, obesity, the multiple common chronic disease that can also prevent and treat multiple stomach digestive system.In the prior art, also have and take the medicament that konjaku makes as raw material, but its side effect is larger, the assimilation effect in human stomach is not ideal.A kind of capsules of Moyuqing for regulating digestive function as disclosed in CN1679880B, to using honeysuckle, cordate houttuynia, purslane, konjaku powder, Radix Isatidis as raw material, the health-caring capsule being prepared into by suitable proportioning, its raw material mostly is cold Chinese medicine, is unsuitable for weakness of the spleen and the stomach crowd and uses; Purslane does not take in pregnant woman, the person of having loose bowels; Radix Isatidis is empty to body, without the malicious person of excess fire heat, avoid clothes.Visible, the disclosed capsules of Moyuqing for regulating digestive function of this technical scheme should not be used for a long time as health products.And for example the disclosed a kind of konjak extractive powder capsule of CN101108227A is enclosed with glucomannans content and is more than or equal to 70% konjaku powder in gastric solubility capsule.The deficiency of this technical scheme is that konjaku powder is unfavorable for absorption of human body with the capsule that conventional capsule manufacture craft is made.
Summary of the invention
The object of the present invention is to provide a kind of konjaku controlled release micelle, the side effect that solved konjaku powder health products in prior art is large, the bad problem of assimilation effect, and a kind of konjaku controlled release micelle can be used in beverage is provided.
Technical scheme of the present invention thes contents are as follows:
A controlled release micelle is that stomach dissolution type, fat-soluble sustained release coating material for konjaku powder are made to colloidal solid according to conventional dressing granulating process.
Konjaku controlled release micelle of the present invention, sustained release coating material used comprises stomach dissolution type, fat-soluble cellulose acetate, ethyl cellulose and acrylic copolymer.
Further, above-mentioned sustained release coating material comprises:
Eudragit E (No. 4) EudragitE;
By EudragitRL and EudragitRS bi-material mixing gained controlled release coat film;
Ethyl acrylate-methyl methacrylate (2:1) copolymer release controlling coating material (trade name EudragitNE30D).
Konjaku controlled release micelle of the present invention, sustained release coating material used is Eudragit E (No. 4) EudragitE.
Konjaku controlled release micelle of the present invention is for the application of beverage.
Beneficial effect of the present invention: compared with prior art, the present invention makes konjaku powder controlled release micelle of sustained release coating material, obtained good health-care effect, its side effect is little, good absorbing, can be used in beverage, under gastric acid environment, acts on, be conducive to human body and digest and assimilate, strengthened the effectiveness of konjaku powder.Medicinal component in konjaku powder can clear out and be deposited on cardiovascular metabolism of lipid and cholesterol; The too much person of edible animal acid food effectively absorbs the active ingredient of konjaku powder, can reach the effect of food acid, soda balance.In konjaku powder, contain the favourable pectin of human body, alkaloid, 17 seed amino acids and trace element, contain a kind of natural antibiotic, the helping digestion of can whetting the appetite, remove enteron aisle rubbish, intestinal enzymes secretion is increased, accelerate to remove deposit on intestines wall, it is excreted as early as possible.Konjaku powder, after entering stomach, digests and slow releasing function by stomach, can form semi-transparent film clothing, is attached on intestines wall, hinders the absorption of various harmful substances, particularly carcinogen.And, food fiber in konjaku powder absorbs after moisture expansion at stomach, volume increases, strengthen satiety, Soluble Fiber has formed colloidal state, delayed glucose and fatty absorption, made gradually blood sugar and blood lipid level decline, thereby can effectively prevent and treat the generation of hyperglycaemia, high fat of blood class disease.This may be because, food fiber is glycolysis in intestines, causes pH value in intestines to decline, affect anaerobic bacteria flora metabolic activity becomes the antitumorigenic factor and originates; Food fiber can also promote that cholesterol is converted into cholic acid, reduces cholic acid and recycles by liver, thereby reduce cholesterol, thereby can restrain cholesterol and rise; In addition, the mucus albumen in konjaku powder can play the effect of prevention of arterial sclerosis.
The specific embodiment
Below in conjunction with embodiment, further explain the present invention, but content of the present invention is not limited to the following stated.
A kind of konjaku controlled release micelle of the present invention is that stomach dissolution type, fat-soluble sustained release coating material for konjaku powder are made to colloidal solid according to conventional dressing granulating process.Sustained release coating material used comprises stomach dissolution type, fat-soluble cellulose acetate, ethyl cellulose and acrylic copolymer.Sustained release coating material comprises: Eudragit E (No. 4) EudragitE; By EudragitRL and EudragitRS bi-material mixing gained controlled release coat film; Ethyl acrylate-methyl methacrylate (2:1) copolymer release controlling coating material (trade name Eudragit NE30D).Wherein, most preferred sustained release coating material is Eudragit E (No. 4) Eudragit E.
Konjaku controlled release micelle of the present invention, for beverage, can obtain the products such as fruit granular suspended drink, instant edible, and be conducive to digest and assimilate.Because the method for making of konjaku controlled release micelle of the present invention is special, insoluble in beverage, can preserve for a long time, and after beverage enters in stomach, can under gastric acid environment, digest, the Novel edible approach of having opened up konjaku powder class health products, is not only conducive to take and absorb, and is also conducive to the popularization of konjaku powder class health products.
The konjaku powder that the present invention is used; its main component is glucomannans; be the legal CAS[37220-17-0 of being numbered] product of/INS425; main component is mannose and glucose with the-strong high molecular weight non-ionic mannosan (glucomannan) closing of Isosorbide-5-Nitrae, has on a small quantity with-1; 4 keys and bond structure; along on average having 1 acetyl group every 9~19Ge Tang units on glucomannans main chain, it contributes to the dissolving of glucomannans, mean molecule quantity 200,000~2,000,000.Konjaku powder is generally white or cream light brown yellow powder, and in the hot water that to dispersible in pH value be 4.0~7.0 or cold water and form high viscosity solution, heating and mechanical agitation can improve solubility; As added the alkali of moderate in solution, even if can form also undissolved thermally-stabilised gel of heat intensive.In addition, be in addition the yellowish konjaku powder to brown powder, its basic odorless, tasteless.Its aqueous solution has very strong hangover (wire drawing) phenomenon, and denseness is very high, and fibrous matter is had to certain capacity of decomposition, water-soluble, is insoluble to ethanol and grease.
Konjaku powder is that the piece root of konjaku flour (You Amorphophalus rivieri Amorphophallus is dry by peeling, section, dry, pulverize, gained fine powder sieves) use ethanol, benzinums etc. carry out physical modification, water-soluble to improve, dissolve viscosity, the performances such as dissolution velocity, for this reason can be by piece undercut sheet, after pulverizing, be dipped in ethanol, drying under reduced pressure at 60 ℃, with petroleum ether degreasing, hydro-oxidation sodium liquid filters after dissolving, filtrate with in hydrochloric acid and after add again lead acetate and extract, get filtrate, pass into hydrogen sulfide to remove lead ion, add ethanol precipitation, after centrifugation, use acetone drying, it is first crude product, use again dissolution of sodium hydroxide, filter, with concentrating with rear in hydrochloric acid, with ethanol, precipitate, the fine work of using acetone drying again after centrifugal and obtaining, therefore be called " konjaku powder ".Active ingredient in konjaku powder is released more, and the effects such as it has replenishes the calcium, balance salinity, clean stomach, whole intestines, toxin expelling are stronger, can be promoting blood circulation and removing blood stasis, removing toxicity for detumescence, wide intestines defaecation, resolving phlegm and softening hard masses; Cure mainly scrofula subcutaneous nodule, damage the diseases such as the stasis of blood is swollen, constipation stomachache, abscess of throat, swelling and aching of gum.
In the present invention, adopt stomach dissolution type, fat-soluble sustained release coating material that mill taro fine powder is carried out to dressing, make colloidal solid, added in beverage, can under the effect of human body hydrochloric acid in gastric juice, digest, can reach the effect of controlled release, give full play to the pharmacy effect of konjaku powder.The present invention's sustained release coating material used comprises stomach dissolution type, fat-soluble cellulose acetate, ethyl cellulose and acrylic copolymer.
Controlled release preparation be by clothing film regularly, outwards discharge quantitatively, evenly a kind of formulation of medicine, make blood concentration constant, without " peak valley " phenomenon, thereby bring into play better curative effect.The controlled release form of making by packaging technique, be control and regulate formulation Chinese traditional medicine rate of release in vivo and in vitro by coating membrane, so the selection of coating material is, the composition of coating membrane has determined the success or failure of slowly-releasing and the controlled-release function of this preparation to a great extent.Sustained release coating material is high molecular polymer normally, be mostly insoluble in water or water insoluble, but water is penetrable; The interference that it is nontoxic, not to be subject to liquid in intestines and stomach, has good filming performance and mechanical performance.Although the research of the sustained release coating material of tool release-controlled film function report is a lot, that stands that time and climate law change test has cellulose acetate, ethyl cellulose and an acrylic copolymer.
Cellulose acetate (Cellulose acetate, CA) is to take a small amount of sulfuric acid as catalyst with cotton or wood-fibred, makes through part or all of acetylation with glacial acetic acid and acetic acid mixed liquor.For the normally cellulose diacetate of slowly-releasing and controlled release preparation, its average molecular mass is about 50000, for white loose granule, bar or flakelike powder, nontoxic, water insoluble, ethanol, acid, aqueous slkali; Be dissolved in the organic solvents such as acetone, chloroform, methyl acetate and dioxane, the filming performance that solution tool is good.
Ethyl cellulose (ethylcellulose, EC) be with paper pulp or cotton fiber through alkali treatment gained alkali fiber, then ethylize and make with chloroethanes.Ethyl cellulose is white runny particle or powder, water insoluble, gastro-intestinal Fluid, glycerine and propane diols, and alkaline-resisting and salting liquid, but not acidproof; Oxidative degradation easily occurs in the sun, should be housed in the closed container of lucifuge, be placed in the dry place of 7 ℃~32 ℃, but compare with other many celluloses, it is the most stable that ethyl cellulose belongs to.Ethyl cellulose can be used as adhesive, the sustained-release matrix material of tablet and is widely used as thin film coating material, is more slowly-releasing and controlled release coat for tablet, pilule etc.During due to the independent dressing of ethyl cellulose, the clothing membrane permeability forming is poor, often mix application with some water miscible filmogens as methylcellulose, hydroxypropyl cellulose, Hydroxypropyl methylcellulose, osmosis type acrylic resin etc., to obtain the coating membrane of suitable Release Performance.
Polyacrylic resin (polyacrylic resin) is the general designation of methacrylic acid copolymer and methacrylate copolymer, wherein, adopts the fat-soluble polyacrylic resin that solubility property is stomach dissolution type to be used as control release type coating material of the present invention.Eudragit E (No. 4) Eudragit E for example, and by Eudragit RL and Eudragit RS bi-material mixing gained controlled release coat film, and for example ethyl acrylate-methyl methacrylate (2:1) copolymer release controlling coating material (trade name Eudragit NE30D).Eudragit E is dissolved in ethanol, acetone, and isopropyl alcohols etc., have aqueous dispersion latax, at acid pH, dissolve.The commercially available prod of Eudragit RL and two kinds of polymer of Eudragit RS is white fine powder or transparent grain, all can be dissolved in acetone, carrene, methyl alcohol and mixed solvent as in equivalent isopropyl alcohol/acetone and isopropyl alcohol/carrene etc.; Make and close clarification or the micro-turbid solution that 12.5% isopropyl alcohol/acetone (60/40) forms, trade name is called Eudragit RL12.5 and Euragit RS12.5.Eudragit NE30D is a kind of white size whey dispersion liquid that contains 30% decentralized photo made from emulsion polymerization method, tool low viscosity.
With health-care effect test example, further explain the health-care effect of konjaku controlled release micelle of the present invention below:
1. test grouping:
Of all ages, sex, select 30 routine diabetes patients, 30 routine fat personages, 30 routine habitual constipation patients, 30 routine patients with gastric disease, the high patient of 30 example three; Be divided at random 3 groups, every group has 10 routine diabetes patients, 10 routine fat personages, 10 routine habitual constipation patients, 10 routine patients with gastric disease, the high patient of 10 example three.
2. test method:
Regularly take following health products respectively for every group, in every 0.3g, every day 1 time, each 3; Make every group of taking dose identical, until every group of tested uninterruptedly taking after 2 months, symptom of each group of observed and recorded is improved situation, according to invalid, improve, obviously improve grade III Standard and add up improvement situation, and calculate efficient, to determine the konjaku powder class health products of best results:
Group 1: konjaku controlled release micelle disclosed by the invention;
The disclosed a kind of capsules of Moyuqing for regulating digestive function of group 2:CN1679880B;
The disclosed a kind of konjak extractive powder capsule of group 3:CN101108227A.
Efficient computational methods:
Figure BDA0000406557150000062
3. result of the test:
The health care result of the test of each group is as shown in table 1.
Table 1 is respectively organized health-care effect
Figure BDA0000406557150000061
Known by contrasting, the health-care effect of organizing the konjaku controlled release micelle of 1 employing is better than organizing 2 and group 3 capsules of Moyuqing for regulating digestive function and the konjak extractive powder capsules that adopt.This means, the present invention is better than take in prior art the health product that konjaku powder is produced as raw material.

Claims (5)

1. a konjaku controlled release micelle, is characterized in that, is stomach dissolution type, fat-soluble sustained release coating material for konjaku powder are made to colloidal solid according to conventional dressing granulating process.
2. a kind of konjaku controlled release micelle according to claim 1, is characterized in that, described sustained release coating material comprises stomach dissolution type, fat-soluble cellulose acetate, ethyl cellulose and acrylic copolymer.
3. according to the arbitrary described a kind of konjaku controlled release micelle of claim 1~2, it is characterized in that, described sustained release coating material comprises:
Eudragit E (No. 4) EudragitE;
By EudragitRL and EudragitRS bi-material mixing gained controlled release coat film;
Ethyl acrylate-methyl methacrylate (2:1) copolymer release controlling coating material (trade name EudragitNE30D).
4. according to the arbitrary described a kind of konjaku controlled release micelle of claim 1~2, it is characterized in that, described sustained release coating material is Eudragit E (No. 4) EudragitE.
5. according to the application of the arbitrary described a kind of konjaku controlled release micelle of claim 1~2, it is characterized in that, for the application of beverage.
CN201310533378.3A 2013-10-31 2013-10-31 Konjac controlled-release colloidal particle Pending CN103549422A (en)

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Cited By (1)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
CN106031414A (en) * 2015-03-11 2016-10-19 李文军 Konjak powdery particle, preparation method and applications thereof

Citations (5)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
CN1280829A (en) * 2000-05-23 2001-01-24 吴承亚 Konjak-glucomannan capsule
JP2001078916A (en) * 1999-09-13 2001-03-27 Lion Corp Spongy material
CN1513380A (en) * 2003-07-22 2004-07-21 解克俭 Berverage made from devilstongue
CN101108227A (en) * 2006-07-18 2008-01-23 张茂玉 Konjak extractive powder capsule
CN101229149A (en) * 2007-01-26 2008-07-30 上海医药工业有限公司 Meclofenoxate hydrochloride stomach-floating sustained release capsule and preparing method thereof

Patent Citations (5)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
JP2001078916A (en) * 1999-09-13 2001-03-27 Lion Corp Spongy material
CN1280829A (en) * 2000-05-23 2001-01-24 吴承亚 Konjak-glucomannan capsule
CN1513380A (en) * 2003-07-22 2004-07-21 解克俭 Berverage made from devilstongue
CN101108227A (en) * 2006-07-18 2008-01-23 张茂玉 Konjak extractive powder capsule
CN101229149A (en) * 2007-01-26 2008-07-30 上海医药工业有限公司 Meclofenoxate hydrochloride stomach-floating sustained release capsule and preparing method thereof

Cited By (1)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
CN106031414A (en) * 2015-03-11 2016-10-19 李文军 Konjak powdery particle, preparation method and applications thereof

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Application publication date: 20140205