CN100435809C - Ginseng bupleurum drop pill for treating liver disease and its preparation method - Google Patents
Ginseng bupleurum drop pill for treating liver disease and its preparation method Download PDFInfo
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- CN100435809C CN100435809C CNB200510002243XA CN200510002243A CN100435809C CN 100435809 C CN100435809 C CN 100435809C CN B200510002243X A CNB200510002243X A CN B200510002243XA CN 200510002243 A CN200510002243 A CN 200510002243A CN 100435809 C CN100435809 C CN 100435809C
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- polyethylene glycol
- leaf
- stem
- radix bupleuri
- total saponins
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- 230000007062 hydrolysis Effects 0.000 description 1
- 238000006460 hydrolysis reaction Methods 0.000 description 1
- 230000002218 hypoglycaemic effect Effects 0.000 description 1
- 230000036039 immunity Effects 0.000 description 1
- 230000004957 immunoregulator effect Effects 0.000 description 1
- 230000002757 inflammatory effect Effects 0.000 description 1
- 230000005764 inhibitory process Effects 0.000 description 1
- 230000003834 intracellular effect Effects 0.000 description 1
- 210000001503 joint Anatomy 0.000 description 1
- 229940043353 maltol Drugs 0.000 description 1
- 235000012054 meals Nutrition 0.000 description 1
- 230000029052 metamorphosis Effects 0.000 description 1
- 239000004531 microgranule Substances 0.000 description 1
- 229960005181 morphine Drugs 0.000 description 1
- 210000002200 mouth mucosa Anatomy 0.000 description 1
- 208000031225 myocardial ischemia Diseases 0.000 description 1
- TZBAVQKIEKDGFH-UHFFFAOYSA-N n-[2-(diethylamino)ethyl]-1-benzothiophene-2-carboxamide;hydrochloride Chemical compound [Cl-].C1=CC=C2SC(C(=O)NCC[NH+](CC)CC)=CC2=C1 TZBAVQKIEKDGFH-UHFFFAOYSA-N 0.000 description 1
- 210000005036 nerve Anatomy 0.000 description 1
- 239000002664 nootropic agent Substances 0.000 description 1
- 230000001777 nootropic effect Effects 0.000 description 1
- 229940100243 oleanolic acid Drugs 0.000 description 1
- 229920001542 oligosaccharide Polymers 0.000 description 1
- 230000003647 oxidation Effects 0.000 description 1
- 238000007254 oxidation reaction Methods 0.000 description 1
- 239000003208 petroleum Substances 0.000 description 1
- 239000000825 pharmaceutical preparation Substances 0.000 description 1
- 230000000144 pharmacologic effect Effects 0.000 description 1
- 150000002989 phenols Chemical class 0.000 description 1
- 229920000573 polyethylene Polymers 0.000 description 1
- 239000000843 powder Substances 0.000 description 1
- 238000003825 pressing Methods 0.000 description 1
- HZLWUYJLOIAQFC-UHFFFAOYSA-N prosapogenin PS-A Natural products C12CC(C)(C)CCC2(C(O)=O)CCC(C2(CCC3C4(C)C)C)(C)C1=CCC2C3(C)CCC4OC1OCC(O)C(O)C1O HZLWUYJLOIAQFC-UHFFFAOYSA-N 0.000 description 1
- YQUVCSBJEUQKSH-UHFFFAOYSA-N protochatechuic acid Natural products OC(=O)C1=CC=C(O)C(O)=C1 YQUVCSBJEUQKSH-UHFFFAOYSA-N 0.000 description 1
- 150000003254 radicals Chemical class 0.000 description 1
- 238000007670 refining Methods 0.000 description 1
- 201000005404 rubella Diseases 0.000 description 1
- 229930192014 saikosaponin Natural products 0.000 description 1
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- 210000004116 schwann cell Anatomy 0.000 description 1
- 239000007787 solid Substances 0.000 description 1
- 235000014347 soups Nutrition 0.000 description 1
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- 239000004094 surface-active agent Substances 0.000 description 1
- 210000004243 sweat Anatomy 0.000 description 1
- 230000002194 synthesizing effect Effects 0.000 description 1
- DKVBOUDTNWVDEP-NJCHZNEYSA-N teicoplanin aglycone Chemical compound N([C@H](C(N[C@@H](C1=CC(O)=CC(O)=C1C=1C(O)=CC=C2C=1)C(O)=O)=O)[C@H](O)C1=CC=C(C(=C1)Cl)OC=1C=C3C=C(C=1O)OC1=CC=C(C=C1Cl)C[C@H](C(=O)N1)NC([C@H](N)C=4C=C(O5)C(O)=CC=4)=O)C(=O)[C@@H]2NC(=O)[C@@H]3NC(=O)[C@@H]1C1=CC5=CC(O)=C1 DKVBOUDTNWVDEP-NJCHZNEYSA-N 0.000 description 1
- 231100000419 toxicity Toxicity 0.000 description 1
- 230000001988 toxicity Effects 0.000 description 1
- WKOLLVMJNQIZCI-UHFFFAOYSA-N vanillic acid Chemical compound COC1=CC(C(O)=O)=CC=C1O WKOLLVMJNQIZCI-UHFFFAOYSA-N 0.000 description 1
- TUUBOHWZSQXCSW-UHFFFAOYSA-N vanillic acid Natural products COC1=CC(O)=CC(C(O)=O)=C1 TUUBOHWZSQXCSW-UHFFFAOYSA-N 0.000 description 1
- 239000000341 volatile oil Substances 0.000 description 1
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Landscapes
- Medicines Containing Plant Substances (AREA)
- Medicinal Preparation (AREA)
Abstract
The present invention discloses an oral preparation prepared from pure Chinese medicine for treating liver diseases, particularly a medical composition oral preparation prepared from the total saponin of ginseng stems and leaves and bupleurum root extracts which comprise bupleurum root saponin as raw materials. The present invention aims to make up the insufficiency of the existing medicinal preparation for treating liver diseases, and provides an oral preparation-shengchai gankang dripping pill for treating liver diseases, which has the advantages of high biological utilization rate, quick medicine release, rapid effect taking, no pollution of the production and low production cost. The shengchai gankang dripping pill provided by the present invention is prepared from the total saponin of the ginseng stems and leaves and the bupleurum root extracts which comprise the bupleurum root saponin as the raw materials and an equal amount of medicinal carriers in a certain proportion.
Description
Technical field
The present invention relates to a kind of pure oral preparation of Chinese traditional medicinal for the treatment of hepatopathy, particularly with stem and leaf of Radix Ginseng total saponins and contain Radix Bupleuri to make the Radix Bupleuri extract of glycosides be the drug composition oral preparation that raw material and a certain proportion of pharmaceutically suitable carrier are prepared from together.
Background technology
Point out according to the speech of the neat Xiao Qiu of health ministry Department of Disease Control in " the national viral hepatitis control seminar " on April 27th, 2004:
*1992---nineteen ninety-five whole nation viral hepatitis seroepidemiological survey demonstration:
Hepatitis A viral infection rate 80.9% calculates that the whole nation has 9.7 hundred million people to infect the hepatitis A poison approximately.
The hepatitis B virus infection rate is 57.6%, and the hepatitis B virus carrying rate is 9.8%, calculates that the whole nation has 6.9 hundred million people once to infect hepatitis B
Virus, wherein 1.2 hundred million people carry hepatitis B virus for a long time.
……
*---2003, annual report hepatitis neopathy about 70---nineteen ninety-five is between 900,000 people, counts the first place according to various statutory report class AB infection disease notifications then.
*2003, whole nation report viral hepatitis 92.4 ten thousand examples accounted for infection disease notification 35.7% of the number of always falling ill; The hepatitis B case history is 710,000 people, accounts for 28% of national statutory report infectious disease total number of persons.
……
Be not difficult to find out that from the authoritative numeral of above these officials the existence of China's hepatopathy can be described as extremely general, it brings to such an extent that harm can not be ignored certainly for people's life.
And the Radix Ginseng of Chinese medicine and Radix Bupleuri are owing to have many good characteristics, in the traditional field of Chinese medicines of China, occupy crucial status, and have widely and to use, discovering especially in recent years, effective ingredient in Radix Bupleuri and the Radix Ginseng, for the treatment hepatopathy original effect is arranged, the defence and the treatment expert that therefore more and more are subjected to hepatopathy pay attention to.
1. Radix Bupleuri is the root of umbelliferae bupleurum BupleurumchinenesBC., bitter in the mouth, little suffering, and property is flat, and having induces sweat brings down a fever, the effect of dispersing the stagnated live-QI to relieve the stagnation of QI, elevate a turnable ladder yang-energy.It is swollen etc. to cure mainly anemopyretic cold, pertussis, stagnation of liver-QI costalgia, rubella, sore joint.Main chemical compositions Radix Bupleuri root contains volatile oil, and (stem and leaf contains flavonoid to saikoside for saikosaponins, SS) a, c, d, s and polysaccharide.Play 80～nineties of 20th century research that China's medical circle has just begun the Herba Sidae Rhombifoliae soup anti-hepatic fibrosis, and find that SS is one of its main effective ingredient.
In sum, SS is by himself antiinflammatory and immunoregulatory biological nature, realize its intervention to hepatic fibrosis mechanism, deny the inflammatory mediator that Schwann Cells and sinusoidal endothelial cell discharge at first, stop its startup and aggravation effect in liver fibrosis process by antiinflammatory action minimizing hepatic stellate cell, Ke; Next suppresses stellate cell activator, plays the fibrosis pivotal role.In addition, SS scalable cytokine makes network be in a kind of balance, stops cascade of cytokines effect in the hepatic fibrosis, causes the ECM over-deposit, and forms hepatic fibrosis.
(quote certainly---Zhu Lanxiang, Liu Shizeng, Gu Zhenlun. the pharmacological action of saikoside and the application of anti-hepatic fibrosis. the 33rd the 10th phase of volume of Chinese herbal medicine ChineseTraditionalandHerbalDrugs2002)
2. Radix Bupleuri is China's Chinese medicine and conventional Chinese medicine, have soothing the liverly allay sorrow, the effect of elevate a turnable ladder yang-energy.China's pharmacopeia regulation Radix Bupleuri (Bulperum Chinese DC) and Radix Bupeuri Scorzonerfolii. (claiming Radix Bupleuri Scorzonerifolii again, B.Scorzone ri folium Wild.) are the former plant of Chinese medicine certified products.The main effective ingredient of Radix Bupleuri is a saikoside.What up to the present, accepted extensively by the world of medicine is that saikoside has antiinflammatory, protects the liver, reduces physiologically actives such as blood cholesterol and blood fat.In recent years research and application show that saikoside treatment chronic nephropathy has good effect, and action principle and mechanism also progressively disclose.
(quote certainly---Zhang Xiangnian, Zhang Xiangbo. the physiologically active of saikoside and the application in the treatment nephropathy. ACAD J GCP the 16th the 2nd phase of volume of June in 2000)
3. Radix Ginseng has the number of chemical composition, and every kind of composition has its characteristics separately again aspect pharmacology.The ginsenoside can be divided into 3 classes by the structure of aglycon; Oleanolic acid type such as ginsenoside Ro mainly contain antiinflammatory, antiplatelet release action.Protopanoxadiol type such as ginsenoside Rb1 and Rb2 show as central nerve inhibition, reduce intracellular Ca2+, antioxidation, removing free radical and improve effect such as myocardial ischemia reperfusion injury, and the protopanoxadiol saponins does not have hemolytic activity.Protopanaxatriol's saponins has hemolytic activity.Protopanaxatriol's type saponin such as Rg1 then show as central nervous excitation, and nootropics promotes effects such as synthesizing of protein, DNA and RNA; Re is the arrhythmia effective ingredient, can suppress morphine and bring out the effects such as drug resistance that mice produces.Rg2 can suppress effects such as rabbit platelet release reaction.In the non-saponin component, that the alkynol compounds has is anticancer, pain relieving, antiinflammation; Phenolic compound such as vanillic acid, maltol etc. have antioxidation; The biological activity of polysaccharide composition is mainly aspect 4: (1) can the enhancing human body immunity ability; (2) can be used for the assistant medicament of anti-curing oncoma; (3) can obviously suppress hepatic injury due to the carbon tetrachloride; (4) hypoglycemic activity.The oligopeptide class has anti-fat-splitting activity.In addition, contain glycoprotein in the Radix Ginseng and have antivirus action, ginseng protein has the aixs cylinder of promotion and generates the effect of increase brain cell quantity.
(quote certainly---Dou Deqiang, Jin Ling, Chen Yingjie. the chemical constituent of Radix Ginseng and the progress of pharmacologically active and prospect. Shenyang Pharmaceutical University's journal the 16th the 2nd phase of volume of April in 1999)
Though Radix Ginseng and Radix Bupleuri have many good characteristics, have very important and application widely at the traditional field of Chinese medicines of China, it is rare only to form the medicine for the treatment of hepatopathy with this two flavors medicine.
The ginseng bupleurum sheet that records for national drug tentative standard WS-10722 (ZD-0722)-No. 2002 is as follows:
Prescription: stem and leaf of Radix Ginseng saponin 33.4g, Radix Bupleuri 834g, starch 102.65g makes 1000.
Function cures mainly: the QI invigorating soothing liver-QI.Be used for acute and chronic hepatitis and belong to deficiency of vital energy liver depression person.
Yet, owing to reasons such as technologies of preparing, exist all after the oral formulations of most drug is taken that dissolve scattered time limit is long, dissolution is low, absorption is relatively poor, problem such as liver sausage first pass effect and bioavailability are lower, thereby influence the performance of drug effect, also directly affect therapeutic effect.
In addition, dosage forms such as conventional tablet, capsule can produce bigger dust pollution in preparation process, can staff's health be worked the mischief to a certain extent, also can cause certain pollution to environment simultaneously.
Moreover the production technology of drop pill is simple, and production cost is lower, and is common at below 50% of tablet according to measuring and calculating, thereby makes patient's drug cost reduce greatly, helps improving the ability of seeking medical advice of extensive patients, also helps improving the general health level of society.
As seen drop pill is as a kind of new pharmaceutical preparation, the above many disadvantages that can overcome conventional oral formulations to a great extent and had.So far do not find in the liver disease field any relevant report of the drop pill that is prepared from relevant for the effective ingredient that utilizes Radix Ginseng, Radix Bupleuri involved in the present invention.
Summary of the invention
Purpose of the present invention is to replenish the existing deficiency that is used for the treatment of the liver disease drug preparation, and a kind of bioavailability height is provided, release fast, produce effects fast, produce pollution-free, and the lower oral formulations ginseng bupleurum drop pill that is used for the treatment of hepatopathy of production cost.Ginseng bupleurum drop pill involved in the present invention is with stem and leaf of Radix Ginseng total saponins and contain Radix Bupleuri to make the Radix Bupleuri extract of glycosides be that raw material and a certain proportion of pharmaceutically suitable carrier are prepared from together.Be prepared by the following technical solutions, can obtain ginseng bupleurum drop pill involved in the present invention:
[preparation method]
1. the Radix Bupleuri extract that contains saikoside---get by extracting in the Radix Bupleuri, for containing the extract of saikoside, extracting method is as follows: Radix Bupleuri is added decocting in water three times, and 3 hours for the first time, 2 hours for the second time, 1 hour for the third time, collecting decoction filtered, and filtrate is crossed D
101Macroporous resin column washes with water to the sugar-free reaction, uses 75% ethanol elution, and eluent reclaims ethanol and is condensed into thick paste, and drying under reduced pressure is pulverized, and must contain the Radix Bupleuri extract of saikoside.
Radix Bupleuri extract also can adopt other extracting method to obtain, and only provides an example here, is not limited thereto a kind of extracting method, also can use the finished product saikoside of plant produced according to the equal principle of medicament contg.
2. stem and leaf of Radix Ginseng total saponins---Chinese phonetic alphabet Renshen Jingye Zongzaogan
English name: General Ginsenoside in extract of Ginseng stems and leaves
According to 2002 the 7th fascicle P7-4 of the national drug standards, WS-10001-(HD-0591)-2002 record, this product is the extract of Stem and leaf of Radix Ginseng, presses dry product and calculates, and contains the ginsenoside Rg
1(C
42H
72O
14) must not be less than 7.0%, contain ginsenoside Re (C
48H
82O
18) must not be less than 23.0%.
Character: this product is faint yellow or pale brown color amorphous powder, and is little smelly; Bitter in the mouth; The tool hygroscopicity.
This product is easily molten in methanol or ethanol, dissolves in water, and is almost insoluble in ether or petroleum ether.
3. substrate---Polyethylene Glycol
1500, Polyethylene Glycol
2000, Polyethylene Glycol
4000, Polyethylene Glycol
6000, one or more the mixture in pharmaceutically suitable carrier such as polyoxyethylene stearate 40 esters, betacyclodextrin, poloxamer, carboxymethyl starch sodium, sodium lauryl sulphate, stearic acid, sodium stearate;
4. proportioning---with g or kg is unit, by weight, and stem and leaf of Radix Ginseng total saponins: Radix Bupleuri extract=2.6: 2.3; Medicinal mixture: substrate=1: 1～1: 5;
Wherein: use Radix Bupleuri to make glycosides or contain Radix Bupleuri when making the extract of glycosides, the principle that should equate according to medicament contg, calculate the weight that should use.
5. according to the given ratio of prescription, accurately take by weighing stem and leaf of Radix Ginseng total saponins, Radix Bupleuri extract and substrate, the substrate that is taken by weighing is placed heating while stirring in the heating container, treat complete fusion, put into stem and leaf of Radix Ginseng total saponins, Radix Bupleuri extract again, continue to stir until the pharmaceutical composition fused solution that obtains containing stem and leaf of Radix Ginseng total saponins, Radix Bupleuri extract and substrate and/or emulsion and/or suspension standby;
6. adopt homemade or general drop pill machine (as the TZDW-1 type drop pill machine of Changzheng Tianmin High Science ﹠ Technology Co., Ltd., Beijing's production), and the temperature control system of adjustment drop pill machine, make the water dropper temperature heating of drop pill machine and remain on (60～90) ℃, the temperature cooling of condensing agent also remains on (40～-5) ℃;
7. treating that the temperature of condensing agent in dropping-pill machine head and the condensation column is stable respectively is in above second step during desired state of temperature, to contain the pharmaceutical composition fused solution of stem and leaf of Radix Ginseng total saponins, Radix Bupleuri extract and substrate and/or emulsion and/or suspension and place in the water dropper storage vat of drop pill machine, splash in the condensing agent by water dropper with suitable speed.Condensing agent can be any one or any two or more mixture in liquid paraffin, methyl-silicone oil, the vegetable oil;
8. will shrink the drop pill taking-up of molding by the outlet of drop pill machine, remove the surface condensation agent, be drying to obtain.
Beneficial effect
Point out according to the speech of the neat Xiao Qiu of health ministry Department of Disease Control in " the national viral hepatitis control seminar " on April 27th, 2004:
*1992---nineteen ninety-five whole nation viral hepatitis seroepidemiological survey demonstration:
Hepatitis A viral infection rate 80.9% calculates that the whole nation has 9.7 hundred million people to infect the hepatitis A poison approximately.
The hepatitis B virus infection rate is 57.6%, and the hepatitis B virus carrying rate is 9.8%, calculates that the whole nation has 6.9 hundred million people once to infect hepatitis B
Virus, wherein 1.2 hundred million people carry hepatitis B virus for a long time.
……
*---2003, annual report hepatitis neopathy about 70---nineteen ninety-five is between 900,000 people, counts the first place according to various statutory report class AB infection disease notifications then.
*2003, whole nation report viral hepatitis 92.4 ten thousand examples accounted for infection disease notification 35.7% of the number of always falling ill; The hepatitis B case history is 710,000 people, accounts for 28% of national statutory report infectious disease total number of persons.
……
Be not difficult to find out that from the authoritative numeral of above these officials the existence of China's hepatopathy can be described as extremely general, it brings to such an extent that harm can not be ignored certainly for people's life.
And the Radix Ginseng of Chinese medicine and Radix Bupleuri are owing to have many good characteristics, in the traditional field of Chinese medicines of China, occupy crucial status, and have widely and to use, discovering especially in recent years, effective ingredient in Radix Bupleuri and the Radix Ginseng, for the treatment hepatopathy original effect is arranged, the defence and the treatment expert that therefore more and more are subjected to hepatopathy pay attention to.
The existing Radix Ginseng Radix Bupleuri oral formulations that is used for the treatment of hepatopathy has only the ginseng bupleurum tablet, and its product comes out at home.But domestic also do not have any manufacturer about the ginseng bupleurum drop pill so far, do not meet any relevant report yet.
Yet, owing to reasons such as technologies of preparing, exist all after the oral formulations of most drug is taken that dissolve scattered time limit is long, dissolution is low, absorption is relatively poor, problem such as liver sausage first pass effect and bioavailability are lower, thereby influence the performance of drug effect, also directly affect therapeutic effect.
In addition, dosage forms such as conventional tablet, capsule can produce bigger dust pollution in preparation process, can staff's health be worked the mischief to a certain extent, also can cause certain pollution to environment simultaneously.
Moreover the production technology of drop pill is simple, and production cost is lower, and is common at below 50% of tablet according to measuring and calculating, thereby makes patient's drug cost reduce greatly, helps improving the ability of seeking medical advice of extensive patients, also helps improving the general health level of society.
Ginseng bupleurum drop pill involved in the present invention is compared with its tablet, has following beneficial effect:
1. ginseng bupleurum drop pill involved in the present invention; utilize surfactant polyethylene etc. to be substrate; make glycosides and contain Radix Bupleuri with ginseng stem-leaf total and make the Radix Bupleuri extract of glycosides and make solid dispersion; making medicine be molecule, colloid or microcrystalline state is scattered in the substrate; the total surface area of medicine increases, and substrate is hydrophilic, and medicine is had wetting action; can make that medicine is rapidly molten to loose into microgranule or solution, thereby make the dissolving of medicine and absorb and accelerate.Thereby improved bioavailability, brought into play efficient, quick-acting effects etc.Compare with the administering mode of traditional oral formulations, exist essential distinction.Drop pill with the solid dispersion technology preparation can adopt oral and sublingual administration, and effective ingredient is fully contacted with mucomembranous surface, absorbs by mucomembranous epithelial cell, directly enters blood circulation.Owing to directly enter blood circulation without gastrointestinal tract and liver, avoided first pass effect effectively, also avoided gastrointestinal irritation, thereby it is rapid to have an onset, bioavailability height, characteristics such as side effect is little, and medication is convenient.
2. ginseng bupleurum drop pill involved in the present invention, volume is little, and is in light weight, is convenient to carry.After containing entrance cavity, contact promptly with saliva and to dissolve rapidly, and absorb by oral mucosa, not only rapid-action, and the influence of not taken food, promptly ante cibum, all can containing take after meal.
3. production technology, the equipment of preparation drop pill are simple, easy to operate, the automaticity height, and labor intensity is low, the production efficiency height.Workshop does not have dust simultaneously, helps labor protection and environmental protection yet.The preparation drop pill need adopt high-tech means and equipment, and active constituents of medicine is uniformly dispersed in substrate, and dosage is accurate, and the ball method of double differences is different little than tablet, and usually production cost is greatly about with below 50% of kind tablet.
4. ginseng bupleurum drop pill involved in the present invention is by after solid drugs active component and substrate heating, being melt into liquid state, splash into refining forming in the not miscible condensed fluid, therefore, the stability of drug height, not facile hydrolysis, oxidation, and operation is to carry out under liquid state, no dust pollution, be not subject to the influence of crystal formation, thereby guaranteed the quality of medicine, increased stability.
In sum, ginseng bupleurum drop pill involved in the present invention has the advantage of triple effect (quick-acting, efficient, long-acting), three little (taking dose is little, toxicity is little, side effect little), five convenience (convenient for production, store convenience, convenient transportation, easy to carry, easy to use).
The specific embodiment
Now with several groups of specific embodiments, be described further with regard to the preparation method of ginseng bupleurum drop pill of the present invention.
First group: the test of single-matrix
1. the Radix Bupleuri extract that contains saikoside---the Radix Bupleuri extract that contains saikoside that obtains by [preparation method] 1;
2. stem and leaf of Radix Ginseng total saponins---commercially available finished product;
3. substrate---Polyethylene Glycol
1500, Polyethylene Glycol
2000, Polyethylene Glycol
4000, Polyethylene Glycol
6000, pharmaceutically suitable carrier such as polyoxyethylene stearate 40 esters, betacyclodextrin, poloxamer, carboxymethyl starch sodium, sodium lauryl sulphate, stearic acid, sodium stearate;
4. proportioning---with g or kg is unit, by weight, and stem and leaf of Radix Ginseng total saponins: Radix Bupleuri extract=2.6: 2.3; Medicinal mixture: substrate=1: 1～1: 5.
5. the process that provides according to [preparation method] 5～8 is prepared, and can obtain the ginseng bupleurum drop pill of different size.
[result of the test]
Test 1: for observe stem and leaf of Radix Ginseng total saponins, Radix Bupleuri extract and different substrates when 1: 1 the proportioning prepared ginseng bupleurum drop pill in qualitative difference, according to 1: 1 ratio, with stem and leaf of Radix Ginseng total saponins, Radix Bupleuri extract respectively with Polyethylene Glycol
1500, Polyethylene Glycol
2000, Polyethylene Glycol
4000, Polyethylene Glycol
6000, pharmaceutically suitable carrier such as polyoxyethylene stearate 40 esters, betacyclodextrin, poloxamer, carboxymethyl starch sodium, sodium lauryl sulphate, stearic acid, sodium stearate matches, adopt homemade drop pill machine, be prepared according to the step of stipulating in the preparation method, can obtain 11 pharmaceutical compositions experiments that contain stem and leaf of Radix Ginseng total saponins, Radix Bupleuri extract and different substrates, and obtain 11 groups of different experimental results and see Table 1.
Test 2: for observe stem and leaf of Radix Ginseng total saponins, Radix Bupleuri extract and different substrates when 1: 2 the proportioning prepared ginseng bupleurum drop pill in qualitative difference, according to 1: 2 ratio, with stem and leaf of Radix Ginseng total saponins, Radix Bupleuri extract respectively with Polyethylene Glycol
1500, Polyethylene Glycol
2000, Polyethylene Glycol
4000, Polyethylene Glycol
6000, pharmaceutically suitable carrier such as polyoxyethylene stearate 40 esters, betacyclodextrin, poloxamer, carboxymethyl starch sodium, sodium lauryl sulphate, stearic acid, sodium stearate matches, adopt homemade drop pill machine, be prepared according to the step of stipulating in the preparation method, can obtain 11 pharmaceutical compositions experiments that contain stem and leaf of Radix Ginseng total saponins, Radix Bupleuri extract and different substrates, and obtain 11 groups of different experimental results and see Table 2.
Test 3: for observe stem and leaf of Radix Ginseng total saponins, Radix Bupleuri extract and different substrates when 1: 5 the proportioning prepared ginseng bupleurum drop pill in qualitative difference, according to 1: 5 ratio, with stem and leaf of Radix Ginseng total saponins, Radix Bupleuri extract respectively with Polyethylene Glycol
1500, Polyethylene Glycol
2000, Polyethylene Glycol
4000, Polyethylene Glycol
6000, pharmaceutically suitable carrier such as polyoxyethylene stearate 40 esters, betacyclodextrin, poloxamer, carboxymethyl starch sodium, sodium lauryl sulphate, stearic acid, sodium stearate matches, adopt homemade drop pill machine, be prepared according to the step of stipulating in the preparation method, can obtain 11 pharmaceutical compositions experiments that contain stem and leaf of Radix Ginseng total saponins, Radix Bupleuri extract and different substrates, and obtain 11 groups of different experimental results and see Table 3.
Second group: the test of mixed-matrix
1. the Radix Bupleuri extract that contains saikoside---the Radix Bupleuri extract that contains saikoside that obtains by [preparation method] 1;
2. stem and leaf of Radix Ginseng total saponins---commercially available finished product;
3. substrate:
3.1 Polyethylene Glycol
1500---English name Macrogol
1500
3.2 Polyethylene Glycol
2000---English name Macrogol
2000
3.3 Polyethylene Glycol
4000---English name Macrogol
4000
3.4 Polyethylene Glycol
6000---English name Macrogol
6000
3.5 polyoxyethylene stearate 40 esters---English name Polyoxyl (40) Stearate
Molecular formula is with C
17H
35COO (CH
2CH
2O)
nH represents that n is about 40
3.6 betacyclodextrin---English name Betacyclodextrin, molecular formula C
6H
10O
5, this product is that ring dextrin glucosyl transferase acts on 7 glucoses that starch generates with α-1, the bonded cyclic oligosaccharide of 4-glycosidic bond
4. proportioning---with g or kg is unit, by weight, and stem and leaf of Radix Ginseng total saponins: Radix Bupleuri extract=2.6: 2.3; Medicinal mixture: substrate=1: 1～1: 5;
5. be prepared according to [preparation method] 4～7 again, promptly can make the ginseng bupleurum drop pill of various different sizes.
[result of the test]
Test 4: in order to observe the mass discrepancy of stem and leaf of Radix Ginseng total saponins, Radix Bupleuri extract and mixed-matrix prepared compound drop pills of dahurian rhododendron leaf when 1: 1 the proportioning, with Polyethylene Glycol
2000, Polyethylene Glycol
4000, Polyethylene Glycol
6000, 5 kinds of carriers such as polyoxyethylene stearate 40 esters, betacyclodextrin respectively and Polyethylene Glycol
1500With 1: 1 mixed evenly as mixed-matrix, according to 1: 1 ratio different with the 5 kinds respectively mixing matrix phases of stem and leaf of Radix Ginseng total saponins, Radix Bupleuri extract are mixed again and make evenly, adopt homemade drop pill machine, be prepared according to the step of stipulating in the preparation method, can obtain the experiment of 5 pharmaceutical compositions that drug extract and mixed-matrix constituted, and obtain 5 groups of different experimental results and see Table 4.
Test 5: in order to observe the mass discrepancy of stem and leaf of Radix Ginseng total saponins, Radix Bupleuri extract and mixed-matrix prepared compound drop pills of dahurian rhododendron leaf when 1: 2 the proportioning, with Polyethylene Glycol
2000, Polyethylene Glycol
4000, Polyethylene Glycol
6000, 5 kinds of carriers such as polyoxyethylene stearate 40 esters, betacyclodextrin respectively and Polyethylene Glycol
1500With 1: 1 mixed evenly as mixed-matrix, according to 1: 2 ratio different with the 5 kinds respectively mixing matrix phases of stem and leaf of Radix Ginseng total saponins, Radix Bupleuri extract are mixed again and make evenly, adopt homemade drop pill machine, be prepared according to the step of stipulating in the preparation method, can obtain the experiment of 5 pharmaceutical compositions that drug extract and mixed-matrix constituted, and obtain 5 groups of different experimental results and see Table 5.
Test 6: in order to observe the mass discrepancy of stem and leaf of Radix Ginseng total saponins, Radix Bupleuri extract and mixed-matrix prepared compound drop pills of dahurian rhododendron leaf when 1: 5 the proportioning, with Polyethylene Glycol
2000, Polyethylene Glycol
4000, Polyethylene Glycol
6000, 5 kinds of carriers such as polyoxyethylene stearate 40 esters, betacyclodextrin respectively and Polyethylene Glycol
1500With 1: 1 mixed evenly as mixed-matrix, according to 1: 5 ratio different with the 5 kinds respectively mixing matrix phases of stem and leaf of Radix Ginseng total saponins, Radix Bupleuri extract are mixed again and make evenly, adopt homemade drop pill machine, be prepared according to the step of stipulating in the preparation method, can obtain the experiment of 5 pharmaceutical compositions that drug extract and mixed-matrix constituted, and obtain 5 groups of different experimental results and see Table 6.
Test 7: in order to observe the mass discrepancy of stem and leaf of Radix Ginseng total saponins, Radix Bupleuri extract and mixed-matrix prepared compound drop pills of dahurian rhododendron leaf when 1: 1 the proportioning, with Polyethylene Glycol
2000, Polyethylene Glycol
4000, Polyethylene Glycol
6000, 5 kinds of carriers such as polyoxyethylene stearate 40 esters, betacyclodextrin respectively and Polyethylene Glycol
1500With 1: 5 mixed evenly as mixed-matrix, according to 1: 1 ratio different with the 5 kinds respectively mixing matrix phases of stem and leaf of Radix Ginseng total saponins, Radix Bupleuri extract are mixed again and make evenly, adopt homemade drop pill machine, be prepared according to the step of stipulating in the preparation method, can obtain the experiment of 5 pharmaceutical compositions that drug extract and mixed-matrix constituted, and obtain 5 groups of different experimental results and see Table 7.
Test 8: in order to observe the mass discrepancy of stem and leaf of Radix Ginseng total saponins, Radix Bupleuri extract and mixed-matrix prepared compound drop pills of dahurian rhododendron leaf when 1: 2 the proportioning, with Polyethylene Glycol
2000, Polyethylene Glycol
4000, Polyethylene Glycol
6000, 5 kinds of carriers such as polyoxyethylene stearate 40 esters, betacyclodextrin respectively and Polyethylene Glycol
1500With 1: 5 mixed evenly as mixed-matrix, according to 1: 2 ratio different with the 5 kinds respectively mixing matrix phases of stem and leaf of Radix Ginseng total saponins, Radix Bupleuri extract are mixed again and make evenly, adopt homemade drop pill machine, be prepared according to the step of stipulating in the preparation method, can obtain the experiment of 5 pharmaceutical compositions that drug extract and mixed-matrix constituted, and obtain 5 groups of different experimental results and see Table 8.
Test 9: in order to observe the mass discrepancy of stem and leaf of Radix Ginseng total saponins, Radix Bupleuri extract and mixed-matrix prepared compound drop pills of dahurian rhododendron leaf when 1: 5 the proportioning, with Polyethylene Glycol
2000, Polyethylene Glycol
4000, Polyethylene Glycol
6000, 5 kinds of carriers such as polyoxyethylene stearate 40 esters, betacyclodextrin respectively and Polyethylene Glycol
1500With 1: 5 mixed evenly as mixed-matrix, according to 1: 5 ratio different with the 5 kinds respectively mixing matrix phases of stem and leaf of Radix Ginseng total saponins, Radix Bupleuri extract are mixed again and make evenly, adopt homemade drop pill machine, be prepared according to the step of stipulating in the preparation method, can obtain the experiment of 5 pharmaceutical compositions that drug extract and mixed-matrix constituted, and obtain 5 groups of different experimental results and see Table 9.
Test 10: in order to observe the mass discrepancy of stem and leaf of Radix Ginseng total saponins, Radix Bupleuri extract and mixed-matrix prepared compound drop pills of dahurian rhododendron leaf when 1: 1 the proportioning, with Polyethylene Glycol
2000, Polyethylene Glycol
4000, Polyethylene Glycol
6000, 5 kinds of carriers such as polyoxyethylene stearate 40 esters, betacyclodextrin respectively and Polyethylene Glycol
1500With 1: 10 mixed evenly as mixed-matrix, according to 1: 1 ratio different with the 5 kinds respectively mixing matrix phases of stem and leaf of Radix Ginseng total saponins, Radix Bupleuri extract are mixed again and make evenly, adopt homemade drop pill machine, be prepared according to the step of stipulating in the preparation method, can obtain the experiment of 5 pharmaceutical compositions that drug extract and mixed-matrix constituted, and obtain 5 groups of different experimental results and see Table 10.
Test 11: in order to observe the mass discrepancy of stem and leaf of Radix Ginseng total saponins, Radix Bupleuri extract and mixed-matrix prepared compound drop pills of dahurian rhododendron leaf when 1: 2 the proportioning, with Polyethylene Glycol
2000, Polyethylene Glycol
4000, Polyethylene Glycol
6000, 5 kinds of carriers such as polyoxyethylene stearate 40 esters, betacyclodextrin respectively and Polyethylene Glycol
1500With 1: 10 mixed evenly as mixed-matrix, according to 1: 2 ratio different with the 5 kinds respectively mixing matrix phases of stem and leaf of Radix Ginseng total saponins, Radix Bupleuri extract are mixed again and make evenly, adopt homemade drop pill machine, be prepared according to the step of stipulating in the preparation method, can obtain the experiment of 5 pharmaceutical compositions that drug extract and mixed-matrix constituted, and obtain 5 groups of different experimental results and see Table 11.
Test 12: in order to observe the mass discrepancy of stem and leaf of Radix Ginseng total saponins, Radix Bupleuri extract and mixed-matrix prepared compound drop pills of dahurian rhododendron leaf when 1: 5 the proportioning, with Polyethylene Glycol
2000, Polyethylene Glycol
4000, Polyethylene Glycol
6000, 5 kinds of carriers such as polyoxyethylene stearate 40 esters, betacyclodextrin respectively and Polyethylene Glycol
1500With 1: 10 mixed evenly as mixed-matrix, according to 1: 5 ratio different with the 5 kinds respectively mixing matrix phases of stem and leaf of Radix Ginseng total saponins, Radix Bupleuri extract are mixed again and make evenly, adopt homemade drop pill machine, be prepared according to the step of stipulating in the preparation method, can obtain the experiment of 5 pharmaceutical compositions that drug extract and mixed-matrix constituted, and obtain 5 groups of different experimental results and see Table 12.
The group practices of table 1 stem and leaf of Radix Ginseng total saponins, Radix Bupleuri extract and single-matrix
(stem and leaf of Radix Ginseng total saponins, Radix Bupleuri extract: substrate=1: 1)
| The substrate title | Medicament contg (%) | Rounding rate (%) | Dissolve scattered time limit (minute) | The ball method of double differences different (%) | Hardness |
| Polyethylene Glycol 1500 | 50.0 | 82 | ＜30 | ＞10 | ++ |
| Polyethylene Glycol 2000 | 50.0 | 80 | ＜30 | ＞10 | ++ |
| Polyethylene Glycol 4000 | 50.0 | 78 | ＜30 | ＞10 | ++ |
| Polyethylene Glycol 6000 | 50.0 | 78 | ＜30 | ＞10 | ++ |
| Polyoxyethylene stearate 40 esters | 50.0 | 73 | ＜30 | ＞10 | ++ |
| Betacyclodextrin | 50.0 | 70 | ＜30 | ＞10 | ++ |
| Poloxamer | 50.0 | 80 | ＜30 | ＞10 | ++ |
| Carboxymethyl starch sodium | 50.0 | 75 | ＜30 | ＞10 | ++ |
| Sodium lauryl sulphate | 50.0 | 72 | ＜30 | ＞10 | ++ |
| Stearic acid | 50.0 | 68 | ＞30 | ＞10 | +++ |
| Sodium stearate | 50.0 | 65 | ＞30 | ＞10 | +++ |
The group practices of table 2 stem and leaf of Radix Ginseng total saponins, Radix Bupleuri extract and single-matrix
(stem and leaf of Radix Ginseng total saponins, Radix Bupleuri extract: substrate=1: 2)
| The substrate title | Medicament contg (%) | Rounding rate (%) | Dissolve scattered time limit (minute) | The ball method of double differences different (%) | Hardness |
| Polyethylene Glycol 1500 | 33.3 | 93 | ＜30 | ＜10 | +++ |
| Polyethylene Glycol 2000 | 33.3 | 92 | ＜30 | ＜10 | +++ |
| Polyethylene Glycol 4000 | 33.3 | 90 | ＜30 | ＜10 | +++ |
| Polyethylene Glycol 6000 | 33.3 | 91 | ＜30 | ＜10 | +++ |
| Polyoxyethylene stearate 40 esters | 33.3 | 89 | ＜30 | ＜10 | +++ |
| Betacyclodextrin | 33.3 | 87 | ＜30 | ＜10 | ++ |
| Poloxamer | 33.3 | 90 | ＜30 | ＜10 | +++ |
| Carboxymethyl starch sodium | 33.3 | 82 | ＜30 | ＞10 | ++ |
| Sodium lauryl sulphate | 33.3 | 82 | ＜30 | ＞10 | ++ |
| Stearic acid | 33.3 | 78 | ＞30 | ＞10 | +++ |
| Sodium stearate | 33.3 | 80 | ＞30 | ＞10 | +++ |
The group practices of table 3 stem and leaf of Radix Ginseng total saponins, Radix Bupleuri extract and single-matrix
(stem and leaf of Radix Ginseng total saponins, Radix Bupleuri extract: substrate=1: 5)
| The substrate title | Medicament contg (%) | Rounding rate (%) | Dissolve scattered time limit (minute) | The ball method of double differences different (%) | Hardness |
| Polyethylene Glycol 1500 | 16.7 | 94 | ＜30 | ＜10 | +++ |
| Polyethylene Glycol 2000 | 16.7 | 92 | ＜30 | ＜10 | +++ |
| Polyethylene Glycol 4000 | 16.7 | 91 | ＜30 | ＜10 | +++ |
| Polyethylene Glycol 6000 | 16.7 | 92 | ＜30 | ＜10 | +++ |
| Polyoxyethylene stearate 40 esters | 16.7 | 90 | ＜30 | ＜10 | +++ |
| Betacyclodextrin | 16.7 | 89 | ＜30 | ＜10 | +++ |
| Poloxamer | 16.7 | 91 | ＜30 | ＜10 | +++ |
| Carboxymethyl starch sodium | 16.7 | 85 | ＜30 | ＞10 | +++ |
| Sodium lauryl sulphate | 16.7 | 86 | ＜30 | ＞10 | +++ |
| Stearic acid | 16.7 | 82 | ＜30 | ＞10 | +++ |
| Sodium stearate | 16.7 | 85 | ＜30 | ＞10 | +++ |
The group practices of table 4 stem and leaf of Radix Ginseng total saponins, Radix Bupleuri extract and mixed-matrix
(stem and leaf of Radix Ginseng total saponins, Radix Bupleuri extract: mixed-matrix=1: 1)
| The substrate title | Medicament contg (%) | Rounding rate (%) | Dissolve scattered time limit (minute) | The ball method of double differences different (%) | Hardness |
| Polyethylene Glycol 1500: polyoxyethylene stearate 40 esters=1: 1 | 50 | 85 | ＜30 | ＞10 | ++ |
| Polyethylene Glycol 1500: betacyclodextrin=1: 1 | 50 | 82 | ＜30 | ＞10 | + |
| Polyethylene Glycol 1500: Polyethylene Glycol 2000＝1∶1 | 50 | 82 | ＜30 | ＞10 | ++ |
| Polyethylene Glycol 1500: Polyethylene Glycol 4000＝1∶1 | 50 | 86 | ＜30 | ＞10 | ++ |
| Polyethylene Glycol 1500: Polyethylene Glycol 6000＝1∶1 | 50 | 85 | ＜30 | ＞10 | ++ |
The group practices of table 5 stem and leaf of Radix Ginseng total saponins, Radix Bupleuri extract and mixed-matrix
(stem and leaf of Radix Ginseng total saponins, Radix Bupleuri extract: mixed-matrix=1: 2)
| The substrate title | Medicament contg (%) | Rounding rate (%) | Dissolve scattered time limit (minute) | The ball method of double differences different (%) | Hardness |
| Polyethylene Glycol 1500: polyoxyethylene stearate 40 esters=1: 1 | 33.3 | 90 | ＜30 | ＜10 | +++ |
| Polyethylene Glycol 1500: betacyclodextrin=1: 1 | 33.3 | 88 | ＜30 | ＜10 | ++ |
| Polyethylene Glycol 1500: Polyethylene Glycol 2000＝1∶1 | 33.3 | 89 | ＜30 | ＜10 | ++ |
| Polyethylene Glycol 1500: Polyethylene Glycol 4000＝1∶1 | 33.3 | 94 | ＜30 | ＜10 | +++ |
| Polyethylene Glycol 1500: Polyethylene Glycol 6000＝1∶1 | 33.3 | 93 | ＜30 | ＜10 | +++ |
The group practices of table 6 stem and leaf of Radix Ginseng total saponins, Radix Bupleuri extract and mixed-matrix
(stem and leaf of Radix Ginseng total saponins, Radix Bupleuri extract: mixed-matrix=1: 5)
| The substrate title | Medicament contg (%) | Rounding rate (%) | Dissolve scattered time limit (minute) | The ball method of double differences different (%) | Hardness |
| Polyethylene Glycol 1500: polyoxyethylene stearate 40 esters=1: 1 | 16.7 | 93 | ＜30 | ＜10 | +++ |
| Polyethylene Glycol 1500: betacyclodextrin=1: 1 | 16.7 | 90 | ＜30 | ＜10 | +++ |
| Polyethylene Glycol 1500: Polyethylene Glycol 2000＝1∶1 | 16.7 | 90 | ＜30 | ＜10 | +++ |
| Polyethylene Glycol 1500: Polyethylene Glycol 4000＝1∶1 | 16.7 | 94 | ＜30 | ＜10 | +++ |
| Polyethylene Glycol 1500: Polyethylene Glycol 6000＝1∶1 | 16.7 | 93 | ＜30 | ＜10 | +++ |
The group practices of table 7 stem and leaf of Radix Ginseng total saponins, Radix Bupleuri extract and mixed-matrix
(stem and leaf of Radix Ginseng total saponins, Radix Bupleuri extract: mixed-matrix=1: 1)
| The substrate title | Medicament contg (%) | Rounding rate (%) | Dissolve scattered time limit (minute) | The ball method of double differences different (%) | Hardness |
| Polyethylene Glycol 1500: polyoxyethylene stearate 40 esters=1: 5 | 50 | 84 | ＜30 | ＞10 | ++ |
| Polyethylene Glycol 1500: betacyclodextrin=1: 5 | 50 | 80 | ＜30 | ＞10 | ++ |
| Polyethylene Glycol 1500: Polyethylene Glycol 2000＝1∶5 | 50 | 82 | ＜30 | ＞10 | ++ |
| Polyethylene Glycol 1500: Polyethylene Glycol 4000＝1∶5 | 50 | 85 | ＜30 | ＞10 | ++ |
| Polyethylene Glycol 1500: Polyethylene Glycol 6000＝1∶5 | 50 | 85 | ＜30 | ＞10 | ++ |
The group practices of table 8 stem and leaf of Radix Ginseng total saponins, Radix Bupleuri extract and mixed-matrix
(stem and leaf of Radix Ginseng total saponins, Radix Bupleuri extract: mixed-matrix=1: 2)
| The substrate title | Medicament contg (%) | Rounding rate (%) | Dissolve scattered time limit (minute) | The ball method of double differences different (%) | Hardness |
| Polyethylene Glycol 1500: polyoxyethylene stearate 40 esters=1: 5 | 33.3 | 91 | ＜30 | ＜10 | +++ |
| Polyethylene Glycol 1500: betacyclodextrin=1: 5 | 33.3 | 88 | ＜30 | ＜10 | ++ |
| Polyethylene Glycol 1500: Polyethylene Glycol 2000＝1∶5 | 33.3 | 90 | ＜30 | ＜10 | ++ |
| Polyethylene Glycol 1500: Polyethylene Glycol 4000＝1∶5 | 33.3 | 95 | ＜30 | ＜10 | +++ |
| Polyethylene Glycol 1500: Polyethylene Glycol 6000＝1∶5 | 33.3 | 92 | ＜30 | ＜10 | +++ |
The group practices of table 9 stem and leaf of Radix Ginseng total saponins, Radix Bupleuri extract and mixed-matrix
(stem and leaf of Radix Ginseng total saponins, Radix Bupleuri extract: mixed-matrix=1: 5)
| The substrate title | Medicament contg (%) | Rounding rate (%) | Dissolve scattered time limit (minute) | The ball method of double differences different (%) | Hardness |
| Polyethylene Glycol 1500: polyoxyethylene stearate 40 esters=1: 5 | 16.7 | 90 | ＜30 | ＜10 | +++ |
| Polyethylene Glycol 1500: betacyclodextrin=1: 5 | 16.7 | 89 | ＜30 | ＜10 | +++ |
| Polyethylene Glycol 1500: Polyethylene Glycol 2000＝1∶5 | 16.7 | 90 | ＜30 | ＜10 | +++ |
| Polyethylene Glycol 1500: Polyethylene Glycol 4000＝1∶5 | 16.7 | 94 | ＜30 | ＜10 | +++ |
| Polyethylene Glycol 1500: Polyethylene Glycol 6000＝1∶5 | 16.7 | 93 | ＜30 | ＜10 | +++ |
The group practices of table 10 stem and leaf of Radix Ginseng total saponins, Radix Bupleuri extract and mixed-matrix
(stem and leaf of Radix Ginseng total saponins, Radix Bupleuri extract: mixed-matrix=1: 1)
| The substrate title | Medicament contg (%) | Rounding rate (%) | Dissolve scattered time limit (minute) | The ball method of double differences different (%) | Hardness |
| Polyethylene Glycol 1500: polyoxyethylene stearate 40 esters=1: 10 | 50 | 85 | ＜30 | ＞10 | ++ |
| Polyethylene Glycol 1500: betacyclodextrin=1: 10 | 50 | 82 | ＜30 | ＞10 | ++ |
| Polyethylene Glycol 1500: Polyethylene Glycol 2000＝1∶10 | 50 | 83 | ＜30 | ＞10 | ++ |
| Polyethylene Glycol 1500: Polyethylene Glycol 4000＝1∶10 | 50 | 85 | ＜30 | ＞10 | ++ |
| Polyethylene Glycol 1500: Polyethylene Glycol 6000＝1∶10 | 50 | 86 | ＜30 | ＞10 | ++ |
The group practices of table 11 stem and leaf of Radix Ginseng total saponins, Radix Bupleuri extract and mixed-matrix
(stem and leaf of Radix Ginseng total saponins, Radix Bupleuri extract: mixed-matrix=1: 2)
| The substrate title | Medicament contg (%) | Rounding rate (%) | Dissolve scattered time limit (minute) | The ball method of double differences different (%) | Hardness |
| Polyethylene Glycol 1500: polyoxyethylene stearate 40 esters=1: 10 | 33.3 | 92 | ＜30 | ＜10 | +++ |
| Polyethylene Glycol 1500: betacyclodextrin=1: 10 | 33.3 | 90 | ＜30 | ＜10 | +++ |
| Polyethylene Glycol 1500: Polyethylene Glycol 2000＝1∶10 | 33.3 | 91 | ＜30 | ＜10 | +++ |
| Polyethylene Glycol 1500: Polyethylene Glycol 4000＝1∶10 | 33.3 | 94 | ＜30 | ＜10 | +++ |
| Polyethylene Glycol 1500: Polyethylene Glycol 6000＝1∶10 | 33.3 | 93 | ＜30 | ＜10 | +++ |
The group practices of table 12 stem and leaf of Radix Ginseng total saponins, Radix Bupleuri extract and mixed-matrix
(stem and leaf of Radix Ginseng total saponins, Radix Bupleuri extract: mixed-matrix=1: 5)
| The substrate title | Medicament contg (%) | Rounding rate (%) | Dissolve scattered time limit (minute) | The ball method of double differences different (%) | Hardness |
| Polyethylene Glycol 1500: polyoxyethylene stearate 40 esters=1: 10 | 16.7 | 93 | ＜30 | ＞10 | +++ |
| Polyethylene Glycol 1500: betacyclodextrin=1: 10 | 16.7 | 90 | ＜30 | ＞10 | +++ |
| Polyethylene Glycol 1500: Polyethylene Glycol 2000＝1∶10 | 16.7 | 92 | ＜30 | ＞10 | +++ |
| Polyethylene Glycol 1500: Polyethylene Glycol 4000＝1∶10 | 16.7 | 93 | ＜30 | ＞10 | +++ |
| Polyethylene Glycol 1500: Polyethylene Glycol 6000＝1∶10 | 16.7 | 93 | ＜30 | ＞10 | +++ |
1. can be seen by the result in the table: when the ratio of stem and leaf of Radix Ginseng total saponins, Radix Bupleuri extract and substrate was 1: 1, its rounding rate, the ball method of double differences was different and index such as hardness does not all reach perfect condition, and dissolve scattered time limit influenced not obvious.
2. when the ratio of stem and leaf of Radix Ginseng total saponins, Radix Bupleuri extract and substrate is 1: 3, the rounding rate, the ball method of double differences is different and index such as hardness slightly all begins to enter preferable state.
3. when the ratio of stem and leaf of Radix Ginseng total saponins, Radix Bupleuri extract and substrate is 1: 9, the rounding rate, the ball method of double differences is different and index such as hardness improves not obvious.
4. the general effect of composite interstitial substance is better than single-matrix.
5. the hardness method for expressing in the subordinate list adopts drop pill is placed on the glass plate, press...withes one's finger it, observes its metamorphosis."+" expression flicking promptly is out of shape, " ++ " expression distortion of firmly pressing, and " +++" expression is indeformable by it.
Claims (2)
1. a drop pill for the treatment of hepatopathy is a raw material with stem and leaf of Radix Ginseng total saponins, Radix Bupleuri, is prepared from the pharmaceutically suitable carrier as substrate, it is characterized in that:
(1) Radix Bupleuri is added decocting in water three times, 3 hours for the first time, 2 hours for the second time, 1 hour for the third time, collecting decoction filtered, and filtrate is crossed D
101Macroporous resin column washes with water to the sugar-free reaction, uses 75% ethanol elution, and eluent reclaims ethanol and is condensed into thick paste, and drying under reduced pressure is pulverized, and promptly gets the Radix Bupleuri extract that contains saikoside, and is standby;
(2) described substrate is Polyethylene Glycol
1500And Polyethylene Glycol
4000Or Polyethylene Glycol
6000Or the mixture of polyoxyethylene stearate 40 esters, by weight, stem and leaf of Radix Ginseng total saponins is 2.6: 2.3 with the ratio of described Radix Bupleuri extract; The weight of stem and leaf of Radix Ginseng total saponins and described Radix Bupleuri extract and with the ratio of substrate be 1: 1～1: 5;
(3) according to aforementioned proportion, accurately take by weighing stem and leaf of Radix Ginseng total saponins, Radix Bupleuri extract and substrate, substrate is placed heating while stirring in the heating container, treat complete fusion, put into stem and leaf of Radix Ginseng total saponins, Radix Bupleuri extract again, continue to stir until the fused solution that obtains containing stem and leaf of Radix Ginseng total saponins, Radix Bupleuri extract and substrate and/or emulsion and/or suspension standby;
(4) temperature control system of adjustment drop pill machine makes the water dropper heating of drop pill machine and maintains the temperature at 60 ℃～90 ℃, and the temperature cooling of condensing agent also remains on 40 ℃～-5 ℃;
(5) temperature for the treatment of dropping-pill machine head and condensing agent is stable respectively when reaching described state, to contain the fused solution of stem and leaf of Radix Ginseng total saponins, Radix Bupleuri extract and substrate and/or emulsion and/or suspension places in the water dropper storage vat of drop pill machine, splash into and shrink molding in the condensing agent, promptly.
2. drop pill as claimed in claim 1 is characterized in that: described condensing agent be liquid paraffin or/and methyl-silicone oil or/and vegetable oil.
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| 国家中成药标准汇编（中成药地方标准上升国家标准部分）. 国家药品监督管理局，36. 2002 |
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