CN1824014A - Blood pressure reducing preparation and its making method - Google Patents

Blood pressure reducing preparation and its making method Download PDF

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Publication number
CN1824014A
CN1824014A CNA200510134413XA CN200510134413A CN1824014A CN 1824014 A CN1824014 A CN 1824014A CN A200510134413X A CNA200510134413X A CN A200510134413XA CN 200510134413 A CN200510134413 A CN 200510134413A CN 1824014 A CN1824014 A CN 1824014A
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preparation
active component
medicine
chinese medicine
water
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刘露
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Beijing Fukangren Bio Pharm Tech Co Ltd
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Beijing Fukangren Bio Pharm Tech Co Ltd
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Abstract

A composite Chinese medicine in the form of dripping pill and soft capsule for treating headache, dizziness, red eye, tinnitus, hypertension, and its preparing process are disclosed.

Description

Antihypertensive formulation and new preparation method
Technical field:
The present invention relates to a kind of Chinese medicine composition and preparation technology thereof, particularly a kind of to be used for due to liver-yang, the flaming up of liver-fire headache dizzy, conjunctival congestion tinnitus, the prescription of hypertension and preparation technology thereof.
Background technology:
Headache is dizzy due to liver-yang, the flaming up of liver-fire, conjunctival congestion tinnitus, and hypertension is clinically to see symptom more, the traditional Chinese medical science is often taked nourishing kidney, liver heat removing, the means of pathogenic fire purging are treated it, and evident in efficacy.Chiang ya wan is that it represents medicine.But in the practice, because this medicine is medical material to be beaten powder be used as medicine in preparation, cause impurity many, shortcoming such as dosage is big has a strong impact on its clinical practice.
The preparation of process extraction process preparation of the present invention is easy to dissolving and absorption than elite and thick putting that ordinary pill more can collect medicine, and curative effect is fast, and administration time is short, and therefore, curative effect is better.
The purpose of this invention is to provide a kind of therapeutic domain wide, easily accept, easily absorb, the preparation technology of efficient, low dosage, the Chinese medicine dripping pills that has no side effect, soft capsule, granule, chewable tablet, mixture, it is dizzy that its pill that makes can be used for curing mainly due to liver-yang, the flaming up of liver-fire headache, conjunctival congestion tinnitus, hypertension.
Summary of the invention:
The present invention relates to a kind of prescription and preparation technology thereof of Chinese medicine preparation, it is characterized in that, the preparation of per 1000 dosage units is prepared from by following proportion raw material:
100~800 parts of 30~240 portions of Flos Sophorae Immaturus of 100~800 parts of Radix Gentianae of Concha Margaritifera
40~320 parts of 50~400 parts of Radix Achyranthis Bidentataes of 100~800 portions of Radix Rehmanniae of Spica Prunellae
Preferably:
200 parts of 60 portions of Flos Sophorae Immaturus of 200 parts of Radix Gentianae of Concha Margaritifera
80 parts of 100 parts of Radix Achyranthis Bidentataes of 200 portions of Radix Rehmanniae of Spica Prunellae
In more than forming, the weight of medicine is calculated with crude drug, and per 1 part can be 1 gram, also can be kilogram or ton, if be unit with gram, this prescription composition can be made into 1000 doses of pharmaceutical preparatioies.Described 1000 doses of fingers, the final drug preparation of making, as make 1000 of soft capsule preparations, drop pill 1000 balls, granule 1000g etc., also can make big packing as granule, as 100~500 bags, specifically can be 100 bags, 125 bags, 200 bags, 250 bags, 500 bags etc., every bag can be used as taking dose 1 time.
More than form, can be made into the preparation of 50~1000 taking doses,, make 125 bags, take 1~2 bag at every turn, can take altogether 62.5~125 times as granule.
More than form to be by weight as proportioning, when producing, can increase or reduce according to corresponding proportion, as large-scale production can be unit with the kilogram, or be unit with the ton, small-scale production can be unit with the milligram also, weight can increase or reduce, but the constant rate of the raw medicinal herbs weight proportion between each composition.
The raw material of Chinese medicine of said ratio extracts processing through new technology of the present invention, obtain the active constituents of medicine of preparation of the present invention, add suitable excipient as required and make suitable medicinal any dosage form, said preparation can be various suitable dosage forms such as drop pill, capsule, granule, tablet, mixture, powder, unguentum.
The above new technology of the present invention may further comprise the steps:
Method a:(technology 1.)
(1) get the Radix Gentianae medical material, pulverize, with 6~15 times of amount methanol percolation extract or 30~60 ℃ of water-baths in warm macerating extract, merge extractive liquid,, 30~60 ℃ of decompression and solvent recoveries get extractum, and are standby;
(2) get Concha Margaritifera and smash and be decocted first 0.5~3.0 hour, add the residue medical material again and decoct with water 2~6 times, each 0.5~3.5 hour, collecting decoction filtered, and filtrate is condensed into thick paste, promptly gets water extract;
(3) above active component lumps together the active constituents of medicine into preparation of the present invention, and this active component is suitable for preparing various preparations such as drop pill of the present invention and soft capsule.
Method b:(technology 2.)
(1) getting the Radix Gentianae medical material beats powder and is used as medicine;
(2) get Concha Margaritifera and smash and be decocted first 0.5~3.0 hour, add the residue medical material again and decoct with water 2~6 times, each 0.5~3.5 hour, collecting decoction filtered, and filtrate is condensed into thick paste, promptly gets water extract;
(3) above active component lumps together the active constituents of medicine into preparation of the present invention, and this active component is suitable for preparing the various preparations except that drop pill and soft capsule of the present invention.
The active constituents of medicine of the preparation of the present invention that above method obtains can be prepared into preparation of the present invention through further processing.
Preparation of the present invention, different dosage form method difference below is the preparation method of several preferred dosage form.
(1) preparation of drop pill
Drop pill of the present invention, wherein the ratio of active component and adjuvant is 1: 0.5~10, and preferred ratio is 1: 2~4, and most preferred ratio is 1: 3.The above adjuvant be specially molecular weight polyethylene glycol between 400 to 10000 Polyethylene Glycol and their mixture, as PEG400 (PEG400), Macrogol 2000, Macrogol 4000, polyethylene glycol 6000 or their mixture or other suitable other auxiliary elements of making drop pill, as glycerol, gelatin or stearic acid sodium etc.
Following steps are taked in the preparation of drop pill of the present invention:
1. be ready to following raw material: active component, adjuvant and/or other inactive ingredients;
2. with the above-mentioned raw materials mix homogeneously;
3. add the transconversion into heat material, move into the drip irrigation of drop pill machine, medicinal liquid splashes in the liquid sub liquid paraffin by water dropper, removes liquid paraffin, selects ball, promptly.
(2) preparation of soft capsule
Soft capsule preparation of the present invention is that active component and pharmaceutically useful organic solvent and the material of making soft capsule shell are formed.Organic solvent wherein is selected from PEG400, Tween 80, glycerol, propylene glycol, isopropyl alcohol, dehydrogenation soybean oil, vegetable oil, aromatic oil, the material of wherein making soft capsule shell is gelatin or arabic gum, water, plasticizer and antiseptic, the weight ratio of gelatin or arabic gum and plasticizer is 1.0: 0.4~1.0 in the soft capsule shell, and the weight ratio of gelatin and water is 1.0: 0.8~1.2; The content of active component is 50mg~500mg in every soft capsule.
The preparation method of preparation of the present invention, the process following steps:
A. get gelatin, glycerol, pure water adds thermosol, adds an amount of antiseptic, preparation rubber;
B. get active component and be dissolved in organic solvent, add suitable quantity of water, be prepared into soft capsule through encapsulating machine.
(3) preparation process of granule is as follows: with the gained active component, add a certain amount of correctives, filler, lubricant, granulate, promptly get granule.
(4) preparation method of chewable tablet is as follows: with the gained active component, add a certain amount of correctives, filler, lubricant, granulate, and drying, tabletting promptly gets chewable tablet.
Filler described in the preparation of granule, chewable tablet is selected from one or more the mixture in lactose, sucrose, dextrin, starch, microcrystalline Cellulose, mannitol, pregelatinized Starch, sorbitol, the xylitol etc.;
Described correctives one of is selected from Rhizoma et radix valerianae, Fructus Pruni pseudocerasi, Fructus Vitis viniferae, Fructus Citri tangerinae, Fructus Citri Limoniae, Herba Menthae, Fructus Fragariae Ananssae, Fructus Musae, Fructus Ananadis comosi, honey peach essence, maltose alcohol, saccharin sodium, protein sugar, sucrose, aspartame, the stevioside or wherein several mixture;
Suitable lubricant comprises wherein one or more such as magnesium stearate, Pulvis Talci, micropowder silica gel.
Following data declaration beneficial effect of the present invention by experiment:
In order to prove the Clinical feasibility that changes after the technology, we have carried out its main pharmacodynamics, toxicologic study to this medicine, observe its therapeutical effect, and the clinical experimental basis that provides is provided.
1, to the hypertensive influence of rat experiment
Get 32 of healthy rats, be divided into 4 groups (seeing Table 1) at random, 8 every group, survey normotensive value with the rat measuring cell, continuous measurement 3d averages.Every rat subcutaneous injection every day androlin 5mg is total to 10d, and measuring blood pressure 3 times is averaged.Press the listed dosage gastric infusion of table 1, matched group is irritated equal-volume water, and 10d continuously surveys the 4th, 8, the 12d blood pressure then, averages, and sees Table 1.The result shows that each extractum group and matched group comparison can significantly reduce rat blood pressure, see table 1 for details.
The hypertensive influence of table 1 pair rat experiment (x ± s, n=8)
Group Dosage (g/kg) Mean blood pressure (KPa)
Before giving hormone After giving hormone After the administration
Matched group - 13.8±0.41 17.1±0.65 16.7±0.73
QINGXUAN JIANGYA PIAN technology is 2. extractum group of extractum group technology 1. 1.2 0.46 0.62 14.0±0.42 13.6±0.35 14.1±0.27 17.1±0.68 16.9±0.75 17.2±0.55 14.1±0.54 ** 13.8±0.56 ** 14.5±0.67 *
Annotate: compare with the blank group *P<0.05, *P<0.01 (down together)
2, to the influence of mice autonomic activities
Choose 40 of healthy mices, body weight 16~20g, male and female half and half are divided into 4 groups at random, press the gastric infusion of dosage shown in the table 2, matched group is given equal-volume water, and 5d puts into the autonomic activities analyzer with mice behind the 6d administration 30min continuously, stablize 5min, survey the movable number of times of mice in the 10min, can significantly reduce mice autonomic activities number of times, the results are shown in Table 2.
The influence of table 2 pair mice autonomic activities (x ± s)
Group Number of animals (only) Dosage (g/kg) The autonomic activities number of times
Matched group technology 1. extractum group technology 2. the extractum group is stable 10 10 10 10 - 0.92 1.24 20mg 94.3±23.2 68.4±19.8 ** 69.6±20.1 ** 59.2±15.8 **
3, to the influence of the inductive mouse sleep time of pentobarbital sodium
Get 40 of healthy male mices, grouping and administration experiment 2 together, after last is irritated stomach 30min, press 35mg/kg for each treated animal, the lumbar injection pentobarbital sodium, injection volume is 0.2ml/20g, serves as the sleep index with the mice righting reflex loss, observes and is tried thing to the pentobarbital sodium prolongation effect of the length of one's sleep.The result shows that each extractum group is compared with matched group, and the effect of significant prolongation mouse sleep time is arranged, and shows that Chinese hawthorn blood-pressure-reducing extractum has the sleep of coordination effect.
4, toxicological study
Acute toxicity test shows that rat oral gavage extract of the present invention fails to measure LD 50
Long term toxicity test: rat grouping, extract of the present invention is irritated stomach, every day three times, connect and annotate 90d, the result, administration group rat and control rats movable, search for food, drinking-water, body weight and multinomial observation indexs such as substantial viscera pathologic finding and histopathology detect, result of the test is not all found any toxicity; Hemogram and hepatic and renal function index and the equal no significant difference of matched group.
The blood vessel irritation of this medicine, allergy and hemolytic test all are negative.
In sum, preparation of the present invention, dropping pill formulation particularly of the present invention and soft capsule preparation are that headache is dizzy due to a kind of good treatment liver-yang, the flaming up of liver-fire, conjunctival congestion tinnitus, the medicine of hypertension, and change preparation technology, can obviously strengthen its nourishing kidney, liver heat removing, clinical efficacies such as pathogenic fire purging, its hypotoxicity in addition, prolonged application safety, therefore, be worth clinical application.
The specific embodiment:
Further specify the present invention by the following examples, include but not limited to the following example.
Embodiment 1:
The preparation method of drop pill of the present invention:
Prescription:
Concha Margaritifera 150g Radix Gentianae 45g Flos Sophorae Immaturus 150g
Spica Prunellae 150g Radix Rehmanniae 75g Radix Achyranthis Bidentatae 60g
PEG4000 100g
Make 1000 balls
Preparation method:
(1) get the Radix Gentianae medical material, pulverize, extract with 8 times of amount methanol percolation, merge extractive liquid,, 50 ℃ of decompression and solvent recoveries get extractum, and are standby;
(2) get Concha Margaritifera and smash and be decocted first 1.5 hours, add the residue medical material again and decoct with water 3 times, each 1.5 hours, collecting decoction filtered, and filtrate is condensed into thick paste, promptly gets water extract;
(3) with above-mentioned extract obtained, the PEG4000 that adds recipe quantity puts into the vessel in heating dissolving, and jolting makes and dissolves into uniform solution, inserts in the fluid reservoir.Keep 80 ℃ the system of dripping temperature, and a control speed, condensed fluid is a liquid paraffin, drips system promptly.
Embodiment 2:
Preparation of soft capsule method of the present invention:
Prescription:
Concha Margaritifera 740g Radix Gentianae 222g Flos Sophorae Immaturus 740g
Spica Prunellae 740g Radix Rehmanniae 370g Radix Achyranthis Bidentatae 296g
PEG400 500g
Make 1000
Preparation method:
(1) get the Radix Gentianae medical material, pulverize, extract with 8 times of amount methanol percolation, merge extractive liquid,, 50 ℃ of decompression and solvent recoveries get extractum, and are standby;
(2) get Concha Margaritifera and smash and be decocted first 1.5 hours, add the residue medical material again and decoct with water 3 times, each 1.5 hours, collecting decoction filtered, and filtrate is condensed into thick paste, promptly gets water extract;
(3) with above-mentioned extract obtained, add an amount of PEG400 and mix and mixing, add the PEG400 of surplus then, promptly get medicinal liquid.It is standby in addition to join gelatin solution by certain prescription.The condition that control is suitable is regulated content weight, obtains soft capsule in the soft capsule machine.
Embodiment 3:
The preparation method of granule of the present invention:
Prescription:
Concha Margaritifera 800g Radix Gentianae 240g Flos Sophorae Immaturus 800g
Spica Prunellae 800g Radix Rehmanniae 400g Radix Achyranthis Bidentatae 320g
Make 1000g
Preparation method:
(1) getting the Radix Gentianae medical material beats powder and is used as medicine;
(2) get Concha Margaritifera and smash and be decocted first 1.5 hours, add the residue medical material again and decoct with water 3 times, each 1.5 hours, collecting decoction filtered, and filtrate is condensed into thick paste, promptly gets water extract;
(3) above active component is merged, add aspartame 5.0g, dextrin 260.0g, granulate, drying sprays into essence 5.0g, promptly gets granule 1000g.
Embodiment 4:
The preparation method of chewable tablet of the present invention:
Prescription:
Concha Margaritifera 440g Radix Gentianae 132g Flos Sophorae Immaturus 440g
Spica Prunellae 440g Radix Rehmanniae 220g Radix Achyranthis Bidentatae 176g
Make 1000
Preparation method:
(1) getting the Radix Gentianae medical material beats powder and is used as medicine;
(2) get Concha Margaritifera and smash and be decocted first 1.5 hours, add the residue medical material again and decoct with water 3 times, each 1.5 hours, collecting decoction filtered, and filtrate is condensed into thick paste, promptly gets water extract;
(3) above active component is merged, add aspartame 3.0g, mannitol 100.0g, granulation, drying adds magnesium stearate 3.0g, mixing, and tabletting promptly gets 1000 of chewable tablet.

Claims (10)

1, a kind of Chinese medicine preparation is characterized in that per 1000 dosage units are made by the following weight proportion raw material:
100~800 parts of 30~240 portions of Flos Sophorae Immaturus of 100~800 parts of Radix Gentianae of Concha Margaritifera
40~320 parts of 50~400 parts of Radix Achyranthis Bidentataes of 100~800 portions of Radix Rehmanniae of Spica Prunellae.
2, the compound preparation of claim 1 is characterized in that, per 1000 dosage units are made by the following weight proportion raw material:
200 parts of 60 portions of Flos Sophorae Immaturus of 200 parts of Radix Gentianae of Concha Margaritifera
80 parts of 100 parts of Radix Achyranthis Bidentataes of 200 portions of Radix Rehmanniae of Spica Prunellae.
3, claim 1 or any one Chinese medicine preparation of 2 are drop pill, capsule, granule, tablet, mixture, powder, unguentum.
4, the Chinese medicine preparation of claim 3 through described raw material is extracted processing, obtains active component, adds suitable adjuvant as required and makes.
5, the Chinese medicine preparation of claim 4 is characterized in that, described active component prepares through following steps:
Method a:(technology 1.)
(1) get the Radix Gentianae medical material, pulverize, with 6~15 times of amount methanol percolation extract or 30~60 ℃ of water-baths in warm macerating extract, merge extractive liquid,, 30~60 ℃ of decompression and solvent recoveries get extractum, and are standby;
(2) get Concha Margaritifera and smash and be decocted first 0.5~3.0 hour, add the residue medical material again and decoct with water 2~6 times, each 0.5~3.5 hour, collecting decoction filtered, and filtrate is condensed into thick paste, promptly gets water extract;
(3) above active component lumps together the active constituents of medicine into preparation of the present invention, and this active component is suitable for preparing various preparations such as drop pill of the present invention and soft capsule.
Method b:(technology 2.)
(1) getting the Radix Gentianae medical material beats powder and is used as medicine;
(2) get Concha Margaritifera and smash and be decocted first 0.5~3.0 hour, add the residue medical material again and decoct with water 2~6 times, each 0.5~3.5 hour, collecting decoction filtered, and filtrate is condensed into thick paste, promptly gets water extract;
(3) above active component lumps together the active constituents of medicine into preparation of the present invention, and this active component is suitable for preparing the various preparations except that drop pill and soft capsule of the present invention.
6, the Chinese medicine preparation of claim 5 is characterized in that:
Described drop pill, wherein the ratio of active component and adjuvant is 1: 0.5~10, described adjuvant be molecular weight between 400 to 10000 Polyethylene Glycol and their mixture, be selected from PEG400 (or 600), Macrogol 2000, Macrogol 4000, polyethylene glycol 6000 or their mixture.
Its preparation method is: active constituents of medicine and proper auxiliary materials behind 60~115 ℃ of mix homogeneously, are regulated the water dropper size with control drop pill weight, are that the coolant system of dripping forms with dimethicone or liquid paraffin, and coolant temperature is-10~5 ℃.
7, the Chinese medicine preparation of claim 5 is characterized in that:
Described soft capsule, its content is made up of active component and suitable substrate, and wherein the content of active component is 50mg~500mg in every soft capsule; Substrate wherein is selected from wherein one or more of PEG400, Tween 80, glycerol, propylene glycol, isopropyl alcohol, dehydrogenation soybean oil, vegetable oil, aromatic oil, animal wet goods.
Its preparation method is: with active constituents of medicine and proper auxiliary materials mix homogeneously, obtain uniform suspension and/or solution, regulate content weight, compacting, dry getting final product.
8, the Chinese medicine preparation of claim 5 is characterized in that:
The preparation process of described granule is as follows: with above-mentioned extract obtained, add a certain amount of filler, correctives, lubricant, granulate, promptly get granule;
The preparation method of chewable tablet is as follows: with above-mentioned extract obtained, adds a certain amount of filler, correctives, lubricant, granulates, and drying, tabletting promptly gets chewable tablet.
9, the Chinese medicine preparation of claim 8 is characterized in that:
Described filler is selected from one or more the mixture in lactose, sucrose, dextrin, starch, microcrystalline Cellulose, mannitol, pregelatinized Starch, sorbitol, the xylitol etc.;
Described correctives one of is selected from Rhizoma et radix valerianae, Fructus Pruni pseudocerasi, Fructus Vitis viniferae, Fructus Citri tangerinae, Fructus Citri Limoniae, Herba Menthae, Fructus Fragariae Ananssae, Fructus Musae, Fructus Ananadis comosi, honey peach essence, maltose alcohol, saccharin sodium, protein sugar, sucrose, aspartame, the stevioside or wherein several mixture;
Suitable lubricant comprises wherein one or more such as magnesium stearate, Pulvis Talci, micropowder silica gel.
10, the preparation method of any one Chinese medicine preparation of claim 1~9 is characterized in that, the process following steps:
Described raw material of Chinese medicine is extracted processing, obtain active component, add suitable adjuvant and make; Wherein said active component prepares through following steps:
Method a:(technology 1.)
(1) get the Radix Gentianae medical material, pulverize, with 6~15 times of amount methanol percolation extract or 30~60 ℃ of water-baths in warm macerating extract, merge extractive liquid,, 30~60 ℃ of decompression and solvent recoveries get extractum, and are standby;
(2) get Concha Margaritifera and smash and be decocted first 0.5~3.0 hour, add the residue medical material again and decoct with water 2~6 times, each 0.5~3.5 hour, collecting decoction filtered, and filtrate is condensed into thick paste, promptly gets water extract;
(3) above active component lumps together the active constituents of medicine into preparation of the present invention, and this active component is suitable for preparing various preparations such as drop pill of the present invention and soft capsule.
Method b:(technology 2.)
(1) getting the Radix Gentianae medical material beats powder and is used as medicine;
(2) get Concha Margaritifera and smash and be decocted first 0.5~3.0 hour, add the residue medical material again and decoct with water 2~6 times, each 0.5~3.5 hour, collecting decoction filtered, and filtrate is condensed into thick paste, promptly gets water extract;
(3) above active component lumps together the active constituents of medicine into preparation of the present invention, and this active component is suitable for preparing the various preparations except that drop pill and soft capsule of the present invention.
Described drop pill, wherein the ratio of active component and adjuvant is 1: 0.5~10, described adjuvant be molecular weight between 400 to 10000 Polyethylene Glycol and their mixture, be selected from PEG400 (or 600), Macrogol 2000, Macrogol 4000, polyethylene glycol 6000 or their mixture.
Its preparation method is: active constituents of medicine and proper auxiliary materials behind 60~115 ℃ of mix homogeneously, are regulated the water dropper size with control drop pill weight, are that the coolant system of dripping forms with dimethicone or liquid paraffin, and coolant temperature is-10~5 ℃.
Described soft capsule, its content is made up of active component and suitable substrate, and wherein the content of active component is 50mg~500mg in every soft capsule; Substrate wherein is selected from wherein one or more of PEG400, Tween 80, glycerol, propylene glycol, isopropyl alcohol, dehydrogenation soybean oil, vegetable oil, aromatic oil, animal wet goods.
Its preparation method is: active constituents of medicine is mixed with proper auxiliary materials, obtain uniform suspension and/or solution, regulate content weight, compacting, dry getting final product.
CNA200510134413XA 2005-12-15 2005-12-15 Blood pressure reducing preparation and its making method Pending CN1824014A (en)

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Application Number Priority Date Filing Date Title
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Cited By (2)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
CN100509002C (en) * 2006-12-21 2009-07-08 中国科学院南海海洋研究所 Marine medicine for treating hypertension, preparation process and dispersible tablet thereof
CN106474219A (en) * 2016-11-11 2017-03-08 天津蚓福生物科技开发有限公司 Blood fat reducing pressed candy

Cited By (2)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
CN100509002C (en) * 2006-12-21 2009-07-08 中国科学院南海海洋研究所 Marine medicine for treating hypertension, preparation process and dispersible tablet thereof
CN106474219A (en) * 2016-11-11 2017-03-08 天津蚓福生物科技开发有限公司 Blood fat reducing pressed candy

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