CN1788773A - Traditional Chinese medicine preparation for treating liver disease and its preparation process - Google Patents
Traditional Chinese medicine preparation for treating liver disease and its preparation process Download PDFInfo
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Abstract
The present invention discloses Chinese medicine preparations for treating hepatopathy and their preparation process. The Chinese medicine preparations are prepared with giant knotweed, cape jasmine, phellodendron bark, pink reineckea herb, flavescent sophora root and red sage in certain weight proportion and proper amount of supplementary material. Of these preparations, the micro pill has good disintegrating property and high bioavailability and is especially suitable for old patient; the dispersed tablet is easy taken and has fast dispersion in water and high bioavailability; the soft capsule has medicine components sealed inside capsule shell and thus with high stability and high bioavailability; and the dripping pill has fast absorption and high bioavailability.
Description
Technical field:
The present invention relates to a kind of Chinese medicine preparation for the treatment of hepatopathy and preparation method thereof, belong to technical field of Chinese medicine.
Background technology:
Hepatopathy is a kind of commonly encountered diseases, and it is having a strong impact on the healthy of people.And existing drug for disease of liver in the treatment hepatopathy, can have infringement all based on Western medicine to other organs of human body, and especially to suffering from the patient of multiple disease, it is worthless taking the western medicine hepatopathy.For reaching the purpose of treatment, a large amount of research has been done by many inventors and medicine enterprise, and the product of some treatments also is provided; Being called " treatment liver disease drug and preparation technology thereof " as ZL 02134141.9, name is exactly to develop for treating this type of disease.But, find that in the research that continues the product hygroscopicity of preparation is strong, have poor taste, dosage is bigger, takes inconvenience.And the dosage form kind is abundant inadequately, is suitable for crowd's narrow range, and bioavailability, the medicine stability of conventional dosage forms are undesirable, and the problem that especially bioavailability of effective ingredient is not high is badly in need of solving; In view of such circumstances, improve dosage changing form and just become the thing that people are badly in need of solving.
Summary of the invention:
The objective of the invention is to: a kind of Chinese medicine preparation for the treatment of hepatopathy and preparation method thereof is provided; The present invention is directed to prior art, the preparation that provides increases medicine stability, absorbs soon, improves the high effect of bioavailability, and it is extensive to be suitable for the crowd, patient's taking convenience; Also can cover the adverse drug abnormal smells from the patient, to address the above problem.
The present invention is achieved in that and calculates by weight that it is with Rhizoma Polygoni Cuspidati 250g, Fructus Gardeniae 200g, Cortex Phellodendri 200g, Herba Reineckeae Carneae 100g, Rhizoma Belamcandae 100g, Radix Sophorae Flavescentis 200g and Radix Salviae Miltiorrhizae 400g, adds appropriate amount of auxiliary materials again and makes.
Described Chinese medicine preparation is capsule, dispersible tablet, pellet, soft capsule, drop pill, tablet, oral liquid.
Get Rhizoma Polygoni Cuspidati, Fructus Gardeniae, Cortex Phellodendri, Herba Reineckeae Carneae, Rhizoma Belamcandae, Radix Sophorae Flavescentis, Radix Salviae Miltiorrhizae, decoct with water three times, 1.5 hours for the first time, 1 hour for the second time, 1 hour for the third time, merge three times decocting liquid, filter, being concentrated into relative density is the clear paste of 1.22～1.25 (25 ℃), add appropriate amount of auxiliary materials, mixing, drying is made different preparations then respectively.
The capsule of described preparation prepares like this: add cane sugar powder 250g ~ 450g, drying is ground into fine powder, incapsulates, promptly.
The dispersible tablet of described preparation prepares like this: the clear paste drying; Get PPVP5g and lemon yellow mixing, get 3/5PPVP3g and cream powder mix homogeneously.Make binding agent with anhydrous alcohol solution, 40 order system material, granulate, the mixed powder of surplus 2/5PPVP2g of Retained and lemon yellow mixing is added in the granule that makes, tabletting, promptly.
The pellet of described preparation prepares like this: clear paste adds appropriate amount of starch, with 60% ethanol and 2% soybean oil system soft material, the soft material of making micropill mechanism ball, cross 16～20 mesh sieve wet feeds and pushed the 0.8mm sieve aperture, the wet grain of strip cuts off round as a ball, and 50～60 ℃ of drying and mouldings are crossed 16～20 mesh sieves, select ball, promptly.
The soft capsule of described preparation prepares like this: the clear paste drying; Press medication amount: substrate amount=1: 1.2 adding soybean oil, mixing; The prescription of rubber is a gelatin: glycerol: water: titanium dioxide=100g: 45g: 100g: 2g, batchingization adhesive tape part is: weigh batching, in the inputization glue jar, merceration is warming up to 65 ± 5 ℃ gradually after 30 minutes, stirred 4 hours and simultaneously evacuation remove bubble, treat evenly back blowing of sizing material, incapsulate after the filtration in the sizing material bucket of machine; The debugging pellet press, 65 ℃ of gelatin box controls, mould rotating speed 2.0 is rolled in 45 ℃ of sprinkler body temperature controls, rubber thickness 0.8mm, 20～24 ℃ of room temperature controls, relative humidity＜50% pelleting; The dry typing drying of rolling that adopts combined with two steps of pallet, dry 3 hours of the typing of rolling, and 24 ℃ of baking temperatures, dry relative humidity answers＜40%, and drying time is at 24～36 hours, promptly.
The drop pill of described preparation prepares like this: the clear paste drying; Get extract powder 200g, PEG4000 200g and polyoxyethylene monostearate Arlacel-40 10g, mix homogeneously fuses in the water-bath, stir evenly, drip and in dimethicone, to become ball, drip apart from 5cm drip footpath 2.5nm/2nm, mix 80 ℃ of ointment temperature, liquid coolant height 70cm, promptly.
The tablet of described preparation prepares like this: clear paste drying, pulverizing, add microcrystalline Cellulose 40g, and use 80% alcohol granulation, drying, granulate adds magnesium stearate 1g, mixing, tabletting, coating, promptly.
The oral liquid of described preparation prepares like this: clear paste 300ml stirs evenly with sucrose 1000g, sodium benzoate 0.5g, filters, and adds water to ormal weight, promptly.
Among the we, Rhizoma Polygoni Cuspidati, Fructus Gardeniae, Cortex Phellodendri, Herba Reineckeae Carneae, Rhizoma Belamcandae, Radix Sophorae Flavescentis, Radix Salviae Miltiorrhizae compatibility heat-clearing and toxic substances removing, depressed liver-energy dispersing and function of gallbladder promoting, blood circulation promoting and blood stasis dispelling.Be applicable to dampness-heat in the liver and gallbladder, the anxious slow motion hepatitis of caused by energy stagnation and blood stasis.
Compared with prior art, micropill disintegrative of the present invention is good, and the bioavailability height is particularly suitable for old people patient and takes; Medicine tablet formulation provided by the invention, the mode of taking is more, can swallow, buccal, and it is convenient to use more than granule, should can in 3 minutes, rapid disintegrate shape solve the not high problem of effective ingredient bioavailability by product chance water simultaneously at homodisperse aqueous solution; Soft capsule of the present invention is that drug blockage is formed in soft gel coat, has solved medicine and has met damp and hot problem of unstable; Can also cover poor taste, abnormal smells from the patient, play the effect that increases stability, improves bioavailability; Drop pill of the present invention absorbs soon the bioavailability height.
In the process of development capsule, find that capsule is covered the adverse drug abnormal smells from the patient, be easy to the patient and carry, take.
Find also that in the process of development capsule pharmacopeia regulation dispersible tablet must disintegrate fully in 3 minutes in 19 ℃～21 ℃ water, and suspension ability, bioavailability, dispersed homogeneous degree etc. are also had higher requirement.And the paste-forming rate of extract of the present invention is very high, viscosity is excessive, hygroscopicity is strong excessively, make must write out a prescription to moulding process in the kind of various adjuvants and consumption select to require very strict, deviation is arranged slightly, will cause product defective.The micropill diameter is similar to particle properties less than 2.5mm, the bioavailability height.
When the development soft capsule, maximum difficulty is exactly that the extractum hygroscopicity is strong and mobile poor, and poor plasticity is difficult to molding and molten diffusing slower.Soft capsule disintegrate in gastrointestinal is fast, and after softgel shell broke, medicine disperseed rapidly, so the drug release stripping is fast, produce effects is rapid, the bioavailability height; Semi-transparent soft capsule and better packaging material can protect medicine not to be subjected to the effect of dampness and airborne oxygen, light, thereby improve the stability of labile element; So the stability of soft capsule itself and moulding process directly influence the stability of product, be the technology of ten minutes crux.
In the process of development drop pill, find, substrate polyethylene glycols commonly used is that esterification forms, it is the surface-active water-soluble base of a kind of tool, dissolubility to insoluble drug is not good, the present invention adds Arlacel-40 change polyethylene glycols itself and does not have lipophilic structure and surface-active property, help the absorption of medicine, if but the consumption of Arlacel-40 is too high, and can cause the hygroscopicity of product to strengthen.
Experimental example 1: Study on Forming
(1) dispersible tablet Study on Forming
Dispersible tablet meet water rapidly disintegrate form the water dispersion tablet of uniform sticky suspension, it is poor to have solved former dosage form disintegrative, stripping is shortcoming slowly, and the dispersible tablet that the present invention makes is disintegrate fully in 3 minutes in 19 ℃～21 ℃ water, and suspension ability is good, bioavailability is high, dispersed homogeneous degree
(1) adjuvant screening
| Prescription | PPVP(g) | K30 (％) | Disintegration time (s) | |
| Add | In add | |||
| 1 | 1 | 4 | 1.5 | 65 |
| 2 | 3 | 2 | 1.5 | 48 |
| 3 | 2 | 3 | 1.0 | 67 |
| 4 | 4 | 1 | 1.0 | 75 |
| 5 | 5 | 0 | 0.8 | 55 |
| 6 | 0 | 5 | 0.8 | 39 |
(2) check disintegration
Adopting changes the basket method, and lift disintegration tester, tablet are got the situation of 6 observations by screen cloth.Percent of pass height then disintegrative is good, more pleasant bulk absorption.
| Group | Disintegration (s) | |||||
| 1 | 2 | 3 | 4 | 5 | 6 | |
| 1 batch in tablet of the present invention | 25 | 28 | 30 | 32 | 29 | 26 |
| 2 batches in tablet of the present invention | 25 | 29 | 30 | 34 | 28 | 28 |
| 3 batches in tablet of the present invention | 25 | 28 | 34 | 32 | 28 | 29 |
The result shows, gets PPVP5g and lemon yellow mixing, get 3/5 with the extract powder mix homogeneously, K30 anhydrous alcohol solution with 1.5% is made binding agent, 40 order system material, granulate, and the mixed powder of surplus 2/5PPVP2g of Retained and lemon yellow mixing is added in the granule that makes, tabletting, the dispersible tablet product that obtains is easy to disintegrate.
(2) pellet Study on Forming
The micropill diameter is less than 2.5mm, and class is in particle properties, the bioavailability height, and when development product micropill of the present invention, maximum difficulty is exactly that hygroscopicity is strong and mobile poor, and poor plasticity is difficult to molding.The micropill manufacturing technology and the adjuvant that adopt screening to obtain make product be easy to disintegrate, and the bioavailability height is well-behaved.
(1) supplementary product kind and consumption are selected
Wettability test is got two parts of extract powders, a starch that adds, and mixing is put respectively in the flat weighing bottle of having weighed, and accurate the title, decide, and is to measure its hygroscopic capacity under 75% condition at 25 ℃ of temperature, relative humidity, the results are shown in Table.
| Sample | Pure extract powder | Extract powder+starch | |
| The weighing bottle numbering | 1 | 2 | |
| Weight of material | 1.0020 | 0.9989 | |
| Moisture absorption blanking time percentage (%) | 1h | 1.48 | 1.07 |
| 2h | 4.26 | 2.05 | |
| 3h | 6.19 | 4.14 | |
| 4h | 8.16 | 6.11 | |
| 6h | 10.18 | 7.24 | |
| 8h | 12.13 | 9.68 | |
| 10h | 15.32 | 11.38 | |
| 12h | 18.14 | 12.47 | |
| 24h | 20.59 | 16.45 | |
| 36h | 24.40 | 18.17 | |
| 48h | 35.48 | 22.48 | |
| 72h | 40.10 | 24.90 | |
| 84h | 45.23 | 32.31 | |
| 96h | 46.51 | 32.10 | |
The result shows that it is rationally feasible to adopt starch to make adjuvant.
(2) system soft material
Get extractum fine powder and starch, soybean oil and ethanol and make soft material with wet granulation process in right amount, make it to reach and hold agglomeratingly, that pinches can loose, standby.Research emphasis concentration of alcohol and soybean oil consumption influence pill, see Table during the experiment knot.
Concentration of alcohol is investigated
| Tested number | Concentration of alcohol | System soft material situation |
| 1 | 70％ | Soft material easily bonds |
| 2 | 60％ | Soft material is moderate |
| 3 | 50％ | Soft material viscosity is not enough |
The soybean oil consumption is investigated
| Tested number | The soybean oil consumption | The pill situation |
| 1 | 60% ethanol, 1% soybean oil | Soft material viscosity is not enough, can't pill |
| 2 | 60% ethanol, 2% soybean oil | Soft material is moderate, is fit to pill |
| 3 | 60% ethanol, 3% soybean oil | Soft material easily bonds, the pill difficulty |
The result as seen, it is more satisfactory to adopt 60% ethanol, 2% soybean oil to be that adhesive is granulated, otherwise is difficult to molding.
(3) pill
The soft material that makes is with micropill mechanism ball, and wet feed pushed the 0.8mm sieve aperture, and the wet grain of strip cuts off round as a ball, and 50～60 ℃ of drying and mouldings are crossed 16～20 mesh sieves and selected ball.
(3) soft capsule Study on Forming
Soft capsule disintegrate in gastrointestinal is fast, and after softgel shell broke, medicine disperseed rapidly, so the drug release stripping is fast, produce effects is rapid, the biological utilisation height; Semi-transparent soft capsule can protect medicine not to be subjected to the effect of oxygen, light in dampness and the air with packaging material preferably, thereby improves the stability of labile element; So capsular stability and moulding process are very crucial technology.
(1) supplementary product kind and consumption are selected
1. disperse medium (or claiming substrate) is selected
At fill material and substrate energy mix homogeneously, and under the prerequisite of unobstructed defeated material of energy and pelleting, reduce substrates quantity as far as possible.By test of many times, determine medication amount (g): substrate amount (g)=be advisable at 1: 1.2, experimental result sees Table.
| Medication amount (g): substrate amount (g) | 1∶1 | 1∶1.2 | 1∶1.5 |
| Quality of liquid medicine | Viscosity is big, mobile poor | Viscosity is big, flowability is all good | Differences in viscosity, mobile big |
2. capsule shells prescription screening
According to the form below proportion scale batching, put into the 500ml bottle,suction, 65 ℃ of water-baths are dissolved, automatic stirringization glue, the while evacuation, about vacuum 0.095Mpa, insulation was placed 1 hour behind the operator hour, filtered glue, get a part of glue and measure viscosity and other performance, part glue evenly is paved into skim (smear below earlier one deck liquid paraffin) on iron plate, be positioned over to observe the rubber performance next day and judge again, with the investigation result of each index by good to poorly using " +++" successively, " ++ ", "+", "-" expression the results are shown in Table.
Rubber batching The selection result
| Batching (gelatin: glycerol: unit water): g | Viscosity (Mpas) | Flexibility | Elasticity | Toughness | Characteristics | Overall merit |
| 1.100∶35∶100 | 3.62 | - | -- | + | Crisp, hard | Difference |
| 2.100∶45∶100 | 3.32 | + | ++ | +++ | Tough, good film-forming property | Fine |
| 3.100∶55∶100 | 3.59 | + | ++ | + | Good springiness | Generally |
| 4.100∶45∶80 | 3.72 | ++ | ++ | + | Good springiness, viscosity is big | Fine |
| 5.100∶45∶120 | 3.11 | +++ | + | -- | Too soft | Difference |
Through above screening, overall merit is considered the characteristics of fill material, selects prescription 2, i.e. gelatin 100g: glycerol 45g: water 100g
3. opacifier is selected
The transparent adhesive tape softgel shell easily causes instability, so need to add a certain amount of opacifier.Select titanium dioxide (titanium dioxide) to make opacifier through investigation and can reach effective shaded effect, and steady quality, not with rubber cement and implant generation chemical change.Its consumption is through investigating with gelatin: glycerol: water: titanium dioxide=100g: 45g: 100g: 2g is advisable, and little to the rubber quality influence, the results are shown in Table.
The opacifier consumption is selected
| Usage ratio (g of unit) gelatin: glycerol: water: titanium dioxide | The rubber transparency | Rubber cement viscosity (Mpas) | Overall merit |
| 100∶45∶100∶0.5 | Translucent | 3.01 | Consumption is not enough |
| 100∶45∶100∶1 | Translucent | 3.10 | Consumption is not enough |
| 100∶45∶100∶2 | Translucent | 3.36 | Good |
| 100∶45∶100∶3 | Translucent | 3.52 | Viscosity is bigger |
Quality is more stable after adding opacifier in the capsule formula.
(2) molding technological condition is investigated
1. the extractum grinding particle size is investigated
Extractum is pulverized, crossed 60 orders, 80 orders, 100 orders, 120 mesh sieves respectively, press extractum: substrate=adding in 1: 1.2 is even through the colloid mill mill, observes the mixing situation, and fruiting period sees Table.
The extractum grinding particle size is investigated
| Granularity (order) | 60 | 80 | 100 | 120 |
| The mixing situation | Can not mixing, high speed centrifugation (10000/min) 30min layering | The energy mixing, high speed centrifugation (10000/min) 30min layering | The energy mixing, 30min is not stratified for high speed centrifugation (10000/min) | The energy mixing, 30min is not stratified for high speed centrifugation (10000/min) |
As seen from the above table, extractum was pulverized 80 mesh sieves, and just therefore the energy mixing, selects extractum to pulverize 80 mesh sieves.
2. fill material mixes
Laboratory is got extractum and was pulverized 80 mesh sieves, presses extractum: substrate=add soybean oil at 1: 1.2, use the colloid mill mixing, and evacuation removes bubble, and is standby.
3. batchingization glue is investigated
By aforementioned preferred prescription is gelatin: glycerol: water: titanium dioxide=100g: 45g: 100g: the 2g weigh batching, and with different temperatures glue.The results are shown in Table.
Changing the glue temperature investigates
| Temperature (℃) | Change the glue time (H) | The rubber quality |
| 50 | 6 | Good |
| 60 | 5 | Good |
| 70 | 5 | Good |
| 80 | 5 | Harder |
| 90 | 4 | Rubber has bubble, and is hard |
By last table prompting, it is the most suitable with 60～70 ℃ to change the glue temperature.So batchingization adhesive tape part is: weigh batching, in the inputization glue jar.Merceration was warming up to 65 ± 5 ℃ in 30 minutes gradually, stir 5 when turbid and simultaneously evacuation remove bubble, treat evenly back blowing of sizing material, incapsulate after the filtration in the sizing material bucket of machine.
4. pelleting: the sizing material bucket and the spice bucket of room temperature of insulation are delivered to the capsule machine top, be connected, debug pellet press with machine, 65 ℃ of gelatin box temperature controls, mould rotating speed 2.0 is rolled in 45 ℃ of sprinkler body temperature controls, rubber thickness 0.8mm, 20～24 ℃ of indoor temperatures, relative humidity＜50%.Treat that it is to survey loading amount once every half an hour in the pelleting process that ball content loading amount is regulated in pellet press debugging back.
5. dry
Typing is dry: in being sent to rotating cage, rotating cage is blown a cold wind over while rotating through the soft capsule of pellet press extrusions, rotates the drying about 2 of finalizing the design when turbid.
Tray dried: the soft gelatin capsule of cold air drying is contained in clean rustless steel charging tray splendid attire in rotating cage, moves to about 22 ℃ of temperature, and airing is 30 hours in the hothouse of relative humidity below 50%, and constantly stirs.Survey capsule moisture and be dry suiting below 10%.
Dry lime light: drying adopts rolling to finalize the design and combines with two steps of tray dried, and rolling typing drying is advisable when investigation is turbid with two, and overlong time is then rough; Baking temperature is advisable about investigating with 22 ℃, and it is long that it's low drying time is past temperature, though increase in temperature can shorten drying time, easily produces Testudinis to capsule surface and splits; Dry relative humidity should be lower than 50% through investigating, otherwise is difficult for dry; Got final product below 10% with control moisture drying time about 24～36 hours.
(4) drop pill moulding process
(1) screening of substrate
The fusion situation of substrate and principal agent relatively
| The prescription number | 1 | 2 | 3 | 4 | 5 | 6 | 7 | 8 |
| Medication amount (g) | 10 | 10 | 10 | 10 | 10 | 10 | 10 | 10 |
| Macrogol 4000 (g) | 30 | 20 | 20 | 20 | 10 | 10 | ----- | ----- |
| Polyethylene glycol 6000 (g) | ----- | ----- | ----- | 20 | 30 | 35 | 40 | 45 |
| Arlacel-40 | ----- | ----- | 10 | 10 | ----- | ----- | 10 | ----- |
| The fusion situation | Principal agent can merge with substrate, but that system does not have is mobile | Principal agent can merge with substrate, but system is better mobile | Principal agent can merge with substrate, but the system flowability is fine | Principal agent can merge with substrate, but the system flowability is fine | Principal agent can merge relatively poor with substrate | Principal agent can merge with substrate, but that system does not have is mobile | Principal agent can merge with substrate, but the system flowability is relatively poor | Principal agent can merge with substrate, but system is better mobile |
| The drop pill outward appearance | ---- | Roundness is poor, hangover | Smooth, roundness is good | Smooth, roundness is good | ---- | Roundness is poor, hangover | ---- | Roundness is poor slightly, and hangover is arranged slightly |
| Drop pill hardness | ---- | Hardness is little | Hardness is better | Hardness is better | ---- | ---- | Hardness is better | Hardness is better |
| The ball method of double differences is different | ---- | 20％ | 8.0％ | 12.5％ | ---- | ---- | 20％ | 20％ |
| Dissolve scattered time limit min) | ---- | 7～8 | 4～5 | 9～10 | ---- | ---- | 6～8 | 6～8 |
The result shows, the drop pill stripping that composite interstitial substance makes is very fast, because the esterification of polyethylene glycols substrate forms, be the surface-active water-soluble base of a kind of tool (fusing point is 46～51 ℃), Arlacel-40 has changed polyethylene glycols itself and has not had lipophilic structure and surface-active character, improve the dissolubility of insoluble drug, help the absorption of medicine show.
(3) drip apart from, drip the selection of speed, temperature
Drip distance, drip selection fast, temperature: external diameter was fixed as 4.1,6.1mm in the interior external diameter of drip was fixing.Evaluation index: the heavy qualification rate of ball is by 2000 editions weight differential requirements of the Pharmacopoeia of the People's Republic of China: meet ± 7.5% within.
| Group | Temperature (℃) | Drip apart from (cm) | Liquid coolant height (cm) | The heavy qualification rate (%) of ball |
| 1 | 90 | 4 | 50 | 78.3 |
| 2 | 90 | 5 | 60 | 86.4 |
| 3 | 90 | 8 | 70 | 82.0 |
| 4 | 80 | 4 | 60 | 91.3 |
| 5 | 80 | 5 | 70 | 95.2 |
| 6 | 80 | 8 | 50 | 90.0 |
| 7 | 70 | 4 | 70 | 91.7 |
| 8 | 70 | 5 | 50 | 89.1 |
| 9 | 70 | 8 | 60 | 85.2 |
The result shows, the optimum condition of preparation drop pill of the present invention: drip to become ball in dimethicone, drip apart from 5cm, drip footpath 2.5mm/2mm mixes 80 ℃ of ointment temperature, liquid coolant height 70cm.
(5) bioavailability relatively
The SD rat, body weight 250～280g, male and female half and half, fasting overnight (can't help water), next day gastric infusion, dosage is 3.8g/Kg.15min after the administration before the electron donating group medicine, 30min, 50min, 80min, 2h, 3h, 4h, and 8h heart blood sampling, each blood sample point is with 6 rats.Blood sample is put the anticoagulant heparin pipe, 3000r/min, and centrifugal 5min, separated plasma is put 30 ℃ and is saved to analysis.High performance liquid chromatogram liquid chromatography instrument is by the M510 pump, the U6K injector, and M490 variable-wavelenght detector and 810 chromatographic data treating stations are formed (WATER, the U.S.).Analytical column is μ Bondpaka (0.45mm * 25cm); Mobile phase is that 0.02mol/L sodium dihydrogen phosphate-acetonitrile (88: 12) is mobile phase, detecting wavelength is that jasminoidin extracts in the 240nm. blood, add 10ml methanol, interior mark 50 μ L, test tube do 30 ° tiltedly in horizontal direction jolting device, 15min is extracted in jolting, centrifugal (3000r/min) 10min, aqueous phase discarded, the accurate 4ml organic facies of drawing is in a clean tube, at 37 ℃ of water-baths, N
2Dry up under the air-flow, residue dissolves the sample introduction analytical attack again with 200 μ L mobile phases.
Rat plasma jasminoidin concentration change (N=6)
| Time/h | Blood plasma jasminoidin concentration/(mgL -1) | ||||
| Dispersible tablet of the present invention | Drop pill of the present invention | Micropill of the present invention | Soft capsule of the present invention | GANFU KELI | |
| 0 | ------- | ------- | ------- | ------- | ------- |
| 0.25 | 1.69±0.41 | 1.61±0.15 | 1.69±0.30 | 1.72±0.21 | 0.69±0.21 |
| 0.50 | 3.52±1.21 | 3.55±0.47 | 3.69±1.21 | 3.37±1.08 | 1.01±0.21 |
| 0.85 | 2.42±0.26 | 2.41±0.65 | 2.32±0.24 | 2.50±0.31 | 1.96±0.41 |
| 1.35 | 1.62±0.54 | 1.70±0.51 | 1.66±0.51 | 1.74±0.35 | 1.37±0.31 |
| 2.00 | 1.32±0.14 | 1.88±0.41 | 1.39±0.30 | 1.38±0.28 | 1.09±0.21 |
| 3.00 | 1.09±0.36 | 1.23±0.25 | 1.69±0.41 | 1.03±0.19 | 0.79±0.11 |
| 4.00 | 0.83±0.28 | 0.79±0.11 | 0.79±0.25 | 0.80±0.11 | 0.69±0.21 |
| 6.00 | 0.47±0.11 | 0.48±0.11 | 0.43±0.21 | 0.46±0.25 | 0.29±0.11 |
| 8.00 | 0.23±0.11 | 0.21±0.21 | 0.30±0.11 | 0.25±0.23 | 0.14±0.12 |
The result shows that the bioavailability of product of the present invention is greater than granule.
(6) antiinflammatory action (influence of xylol induced mice auricle edema)
Experimental technique: face with preceding that dispersible tablet of the present invention, micropill, soft capsule are mixed with the 0.10g/ml suspension with 0.5% hydroxy methocel (CMC-Na) is standby, animal is used healthy Kunming mouse, body weight 20 grams.Mice is divided into 7 groups (matched group normal saline) at random, irritate the long-pending 20ml/kg of being of body of stomach, in two weeks of continuous irrigation stomach, once a day, the last administration is only used microsyringe 0.05ml/ after 30 minutes, dimethylbenzene is applied to mouse right ear, put to death mice after 15 minutes, cut two ears, dash with the 8mm diameter steel and lay round auricle in left and right sides auricle same area respectively along the auricle baseline, the torsion Libra claims two ear weight in wet bases, with two auricle weight differences as the swelling level index.Inhibitory rate of intumesce equals the difference of average swelling degree of matched group and the average swelling degree of administration group and takes advantage of 100% again divided by the average swelling degree of matched group.
| Group | Dosage (g/Kg) | Animal (only) | Average swelling degree (mg) | Suppression ratio (%) |
| Matched group | 20ml/Kg | 8 | 23.31±2.43 | |
| The hydrocortisone group | 0.04 | 8 | 7.03±2.31 | 70.21 |
| The GANFU KELI group | 2.0 | 8 | 16.23±1.31 | 30.13 |
| Dispersible tablet group of the present invention | 2.0 | 8 | 14.34±4.51 | 32.12 |
| Micropill group of the present invention | 2.0 | 8 | 13.48±2.31 | 33.12 |
| Soft capsule group of the present invention | 2.0 | 8 | 13.25±2.38 | 33.25 |
Fruiting period shows that preparation of the present invention has good antiinflammatory do effect, is better than GANFU KELI.
The micropill stability test
3 batches of this product were placed under room temperature 1 year, respectively 0 month, 3 months, 6 months, 9 months, 12 months, carry out character, limit test of microbe, investigate character, the microbial check result shows that every index has no significant change.
The stability of Oral test
3 batches of this product, under room temperature, placed 1 year, respectively 0 month, 3 months, 6 months, 9 months, 12 months, carry out character, ph value and limit test of microbe, investigate character, the variation of ph value, microbial check result and show that every index has no significant change.
Concrete embodiment:
Embodiments of the invention 1: Rhizoma Polygoni Cuspidati 250g, Fructus Gardeniae 200g, Cortex Phellodendri 200g, Herba Reineckeae Carneae 100g, Rhizoma Belamcandae 100g, Radix Sophorae Flavescentis 200g and Radix Salviae Miltiorrhizae 400g decoct with water three times, 1.5 hours for the first time, 1 hour for the second time, 1 hour for the third time, merge three times decocting liquid, filter, being concentrated into relative density is the clear paste of 1.22～1.25 (25 ℃), adds cane sugar powder 250g ~ 450g drying, is ground into fine powder, incapsulate, promptly get capsule.
Embodiments of the invention 2: Rhizoma Polygoni Cuspidati 250g, Fructus Gardeniae 200g, Cortex Phellodendri 200g, Herba Reineckeae Carneae 100g, Rhizoma Belamcandae 100g, Radix Sophorae Flavescentis 200g and Radix Salviae Miltiorrhizae 400g decoct with water three times, 1.5 hours for the first time, 1 hour for the second time, 1 hour for the third time, merge three times decocting liquid, filter, being concentrated into relative density is the clear paste of 1.22～1.25 (25 ℃), drying; Get PPVP5g and lemon yellow mixing, get 3/5PPVP3g and cream powder mix homogeneously.Make binding agent with anhydrous alcohol solution, 40 order system material, granulate, the mixed powder of surplus 2/5PPVP2g of Retained and lemon yellow mixing is added in the granule that makes, and tabletting promptly gets dispersible tablet.
Embodiments of the invention 3: Rhizoma Polygoni Cuspidati 250g, Fructus Gardeniae 200g, Cortex Phellodendri 200g, Herba Reineckeae Carneae 100g, Rhizoma Belamcandae 100g, Radix Sophorae Flavescentis 200g and Radix Salviae Miltiorrhizae 400g decoct with water three times, 1.5 hours for the first time, 1 hour for the second time, 1 hour for the third time, merge three times decocting liquid, filter, being concentrated into relative density is the clear paste of 1.22～1.25 (25 ℃), add appropriate amount of starch, with 60% ethanol and 2% soybean oil system soft material, the soft material of making is crossed 16～20 mesh sieves with micropill mechanism ball, wet feed pushed the 0.8mm sieve aperture, the wet grain of strip cuts off round as a ball, and 50～60 ℃ of drying and mouldings are crossed 16～20 mesh sieves, select ball, promptly get pellet.
Embodiments of the invention 4: Rhizoma Polygoni Cuspidati 250g, Fructus Gardeniae 200g, Cortex Phellodendri 200g, Herba Reineckeae Carneae 100g, Rhizoma Belamcandae 100g, Radix Sophorae Flavescentis 200g and Radix Salviae Miltiorrhizae 400g decoct with water three times, 1.5 hours for the first time, 1 hour for the second time, 1 hour for the third time, merge three times decocting liquid, filter, being concentrated into relative density is the clear paste of 1.22～1.25 (25 ℃), drying; Press medication amount: substrate amount=1: 1.2 adding soybean oil, mixing; The prescription of rubber is a gelatin: glycerol: water: titanium dioxide=100g: 45g: 100g: 2g, batchingization adhesive tape part is: weigh batching, in the inputization glue jar, merceration is warming up to 65 ± 5 ℃ gradually after 30 minutes, stirred 4 hours and simultaneously evacuation remove bubble, treat evenly back blowing of sizing material, incapsulate after the filtration in the sizing material bucket of machine; The debugging pellet press, 65 ℃ of gelatin box controls, mould rotating speed 2.0 is rolled in 45 ℃ of sprinkler body temperature controls, rubber thickness 0.8mm, 20～24 ℃ of room temperature controls, relative humidity＜50% pelleting; The dry typing drying of rolling that adopts combined with two steps of pallet, dry 3 hours of the typing of rolling, and 24 ℃ of baking temperatures, dry relative humidity answers＜40%, and promptly got soft capsule at 24～36 hours drying time.
Embodiments of the invention 5: Rhizoma Polygoni Cuspidati 250g, Fructus Gardeniae 200g, Cortex Phellodendri 200g, Herba Reineckeae Carneae 100g, Rhizoma Belamcandae 100g, Radix Sophorae Flavescentis 200g and Radix Salviae Miltiorrhizae 400g decoct with water three times, 1.5 hours for the first time, 1 hour for the second time, 1 hour for the third time, merge three times decocting liquid, filter, being concentrated into relative density is the clear paste of 1.22～1.25 (25 ℃), drying; Get extract powder 200g, two parts of PEG4000200g and polyoxyethylene monostearate Arlacel-40 10g portion, mix homogeneously fuses in the water-bath, stir evenly, drip and in dimethicone, to become ball, drip apart from 5cm drip footpath 2.5nm/2nm, mix 80 ℃ of ointment temperature, liquid coolant height 70cm promptly gets drop pill.
Embodiments of the invention 6: Rhizoma Polygoni Cuspidati 250g, Fructus Gardeniae 200g, Cortex Phellodendri 200g, Herba Reineckeae Carneae 100g, Rhizoma Belamcandae 100g, Radix Sophorae Flavescentis 200g and Radix Salviae Miltiorrhizae 400g decoct with water three times, 1.5 hours for the first time, 1 hour for the second time, 1 hour for the third time, merge three times decocting liquid, filter, being concentrated into relative density is the clear paste of 1.22～1.25 (25 ℃), drying; Pulverize, add microcrystalline Cellulose 40g, use 80% alcohol granulation, drying, granulate adds magnesium stearate 1g, mixing, tabletting, coating promptly gets tablet.
Embodiments of the invention 7: Rhizoma Polygoni Cuspidati 250g, Fructus Gardeniae 200g, Cortex Phellodendri 200g, Herba Reineckeae Carneae 100g, Rhizoma Belamcandae 100g, Radix Sophorae Flavescentis 200g and Radix Salviae Miltiorrhizae 400g decoct with water three times, 1.5 hours for the first time, 1 hour for the second time, 1 hour for the third time, merge three times decocting liquid, filter, being concentrated into relative density is the clear paste of 1.22～1.25 (25 ℃), clear paste 300ml adds water to ormal weight with sucrose 1000g, sodium benzoate 0.5g, promptly gets oral liquid.
Claims (10)
1. Chinese medicine preparation for the treatment of hepatopathy is characterized in that: calculate by weight, it is with Rhizoma Polygoni Cuspidati 250g, Fructus Gardeniae 200g, Cortex Phellodendri 200g, Herba Reineckeae Carneae 100g, Rhizoma Belamcandae 100g, Radix Sophorae Flavescentis 200g and Radix Salviae Miltiorrhizae 400g, adds appropriate amount of auxiliary materials again and makes.
2. according to the Chinese medicine preparation of the described treatment hepatopathy of claim 1, it is characterized in that: described Chinese medicine preparation comprises capsule, dispersible tablet, pellet, soft capsule, drop pill, tablet, oral liquid.
3. the preparation method of the Chinese medicine preparation of treatment hepatopathy as claimed in claim 1 or 2 is characterized in that: get Rhizoma Polygoni Cuspidati, Fructus Gardeniae, Cortex Phellodendri, Herba Reineckeae Carneae, Rhizoma Belamcandae, Radix Sophorae Flavescentis, Radix Salviae Miltiorrhizae, decoct with water three times, 1.5 hours for the first time, 1 hour for the second time, 1 hour for the third time, merge three times decocting liquid, filter, being concentrated into relative density is the clear paste of 1.22～1.25 (25 ℃), adds appropriate amount of auxiliary materials, mixing, drying is made different preparations then respectively.
4. according to the preparation method of the Chinese medicine preparation of the described treatment hepatopathy of claim 3, it is characterized in that: the capsule of described preparation prepares like this: add cane sugar powder 250g ~ 450g, drying is ground into fine powder, incapsulates, promptly.
5. according to the preparation method of the Chinese medicine preparation of the described treatment hepatopathy of claim 3, it is characterized in that: the dispersible tablet of described preparation prepares like this: the clear paste drying; Get PPVP5g and lemon yellow mixing, get 3/5PPVP3g and cream powder mix homogeneously.Make binding agent with anhydrous alcohol solution, 40 order system material, granulate, the mixed powder of residue 2/5PPVP2g and lemon yellow mixing is added in the granule that makes, tabletting, promptly.
6. according to the preparation method of the Chinese medicine preparation of the described treatment hepatopathy of claim 3, it is characterized in that: the pellet of described preparation prepares like this: clear paste adds appropriate amount of starch, with 60% ethanol and 2% soybean oil system soft material, the soft material of making is crossed 16～20 mesh sieve wet feeds and was pushed the 0.8mm sieve aperture with micropill mechanism ball, and the wet grain of strip cuts off round as a ball, 50～60 ℃ of drying and mouldings, cross 16～20 mesh sieves, select ball, promptly.
7. according to the preparation method of the described treatment hepatopathy of claim 3, it is characterized in that: the soft capsule of described preparation prepares like this: the clear paste drying; Press medication amount: substrate amount=1: 1.2 adding soybean oil, mixing; The prescription of rubber is a gelatin: glycerol: water: titanium dioxide=100g: 45g: 100g: 2g, batchingization adhesive tape part is: weigh batching, in the inputization glue jar, merceration is warming up to 65 ± 5 ℃ gradually after 30 minutes, stirred 4 hours and simultaneously evacuation remove bubble, treat evenly back blowing of sizing material, incapsulate after the filtration in the sizing material bucket of machine; The debugging pellet press, 65 ℃ of gelatin box controls, mould rotating speed 2.0 is rolled in 45 ℃ of sprinkler body temperature controls, rubber thickness 0.8mm, 20～24 ℃ of room temperature controls, relative humidity＜50% pelleting; The dry typing drying of rolling that adopts combined with two steps of pallet, dry 3 hours of the typing of rolling, and 24 ℃ of baking temperatures, dry relative humidity answers＜40%, and drying time is at 24～36 hours, promptly.
8. according to the preparation method of the Chinese medicine preparation of the described treatment hepatopathy of claim 3, it is characterized in that: the drop pill of described preparation prepares like this: the clear paste drying; Get extract powder 200g, PEG4000200g and polyoxyethylene monostearate Arlacel-40 10g, mix homogeneously fuses in the water-bath, stir evenly, drip and in dimethicone, to become ball, drip apart from 5cm drip footpath 2.5nm/2nm, mix 80 ℃ of ointment temperature, liquid coolant height 70cm, promptly.
9. according to the preparation method of the Chinese medicine preparation of the described treatment hepatopathy of claim 3, it is characterized in that: the tablet of described preparation prepares like this: clear paste drying, pulverizing, add microcrystalline Cellulose 40g, and use 80% alcohol granulation, drying, granulate adds magnesium stearate 1g, mixing, tabletting, coating, promptly.
10. according to the preparation method of the Chinese medicine preparation of the described treatment hepatopathy of claim 3, it is characterized in that: the oral liquid of described preparation prepares like this: clear paste 300ml stirs evenly with sucrose 1000g, sodium benzoate 0.5g, filters, and adds water to ormal weight, promptly.
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| CN 200510200648 CN1788773A (en) | 2005-10-26 | 2005-10-26 | Traditional Chinese medicine preparation for treating liver disease and its preparation process |
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| CN 200510200648 CN1788773A (en) | 2005-10-26 | 2005-10-26 | Traditional Chinese medicine preparation for treating liver disease and its preparation process |
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Cited By (1)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN100353978C (en) * | 2006-07-04 | 2007-12-12 | 刘海刚 | Synergistic medicinal composition containing tiopronin and Chinese medicine extract |
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Cited By (1)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN100353978C (en) * | 2006-07-04 | 2007-12-12 | 刘海刚 | Synergistic medicinal composition containing tiopronin and Chinese medicine extract |
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